The course will provide an overview of pharmacology, raise awareness and understanding of the various aspects of pharmacology, and increase the participant’s knowledge base.
CEUFast, Inc. is accredited as a provider of nursing continuing professional development by the American Nurses Credentialing Center's Commission on Accreditation. ANCC Provider number #P0274.
The course will provide an overview of pharmacology, raise awareness and understanding of the various aspects of pharmacology, and increase the participant’s knowledge base.
After completing this continuing education course, the participants will be able to meet the following objectives:
Nurses have a significant role in medication safety. The median error rate is estimated to be 8–25% during medication administration (MacDowell et al., 2021). Medication errors are estimated to occur in approximately 6.5 per 100 hospital admissions (Tariq et al., 2024). By actively engaging in quality nursing care, nurses play a crucial part in preventing medication errors and promoting safe medication practices in healthcare settings.
Nurses play a crucial role in medication administration, ensuring that patients receive the right medication, in the right dosage, through the right route, and at the right time while monitoring for any adverse effects to promote patient safety and well-being. Research has found low drug administration guideline adherence (Rohde & Domm, 2018). Study results have shown that at least one of the ten drug rights was regularly violated. Most of these errors are preventable, and according to the Institute of Medicine report, The Future of Nursing, nurses are pivotal in reducing drug errors (Flynn et al., 2012).
Older adults, children, and pregnant women have physiologic differences that must be considered when administering drugs.
Due to physiological changes, particularly in hepatic metabolism and renal elimination, dosing in older adults can be challenging. Older adults may experience an increase in side effects or toxicity more easily. Awareness of side effects in older adults is particularly important as they are often on more than one drug. Care should be taken when combining drugs.
In pediatric patients, dosing medications requires careful consideration due to weight, age, developmental stage, and pharmacokinetic differences compared to adults. Here are some key aspects of dosing in pediatric patients:
In summary, dosing medications in pediatric patients requires careful assessment, calculation, and consideration of various factors to ensure safe and effective treatment. Nurses play a vital role in this process, from accurate dosing calculations to patient education and monitoring for adverse effects. Collaboration with other healthcare professionals and adherence to established guidelines are essential for pediatric medication safety.
Pregnant women present another population where careful consideration must be taken when administering drugs. The effect of the drug on the fetus may be detrimental. An understanding of how the fetus develops during pregnancy must be considered. The risks of not treating a disorder must be contemplated, as well.
Pharmacodynamics is what a drug does to the body, whereas pharmacokinetics is what the body does to the drug. Pharmacodynamics includes receptor binding, chemical interactions, and post-receptor effects. Pharmacokinetics includes the terms absorption, distribution, excretion, and metabolism. The pharmacokinetics determines the onset of the drug in addition to its duration and intensity of the effect. Clinical pharmacokinetics is when pharmacokinetic principles are applied to the appropriate and effective therapeutic management of drugs in patients (Open Resources for Nursing et al., 2023a).
A common acronym used to remember key principles in pharmacokinetics is ADME, which describes the four main aspects of pharmacokinetics.
The Pharmacokinetics Process
The Cmax is the maximum drug concentration and will help predict the therapeutic benefit and the most likely time side effects are seen (Kreutzer et al., 2011). The time that the maximum concentration is reached is called the Tmax. At this point, the drug concentration starts to go down (gets eliminated), and the amount of time the drug goes down 50% is known as the half-life (Open Resources for Nursing et al., 2023a).
Absorption is how the drug enters the body. In intravenous administration, drugs are absorbed across a tissue membrane to enter the bloodstream. Absorption depends on how the drug is administered. Oral drugs are typically swallowed and absorbed through the small intestine. Then, they enter the portal venous system, pass through the liver, and move through the cardiopulmonary and arterial systems.
Parenteral administration involves giving a drug that avoids the gastrointestinal tract. Parenteral administration includes a transdermal application, injection, and inhalation. These drugs avoid first-pass metabolism, including potential alterations from stomach acid, food, or gut wall interference.
Drugs that are given through the intravenous route tend to reach a high Cmax in a shorter period when compared to orally taken drugs. The half-life is the same for the drug, no matter the route of administration.
The volume of distribution (Vd) is another concept commonly discussed under distribution but is beyond a basic pharmacology introduction. In general, the volume of distribution describes how extensively the drug is dispersed to the rest of the body compared to the plasma. The amount of the drug in the body is divided by the plasma concentration to determine the Vd (Mansoor & Mahabadi, 2023).
Metabolism is how the drug is chemically changed to be excreted. Drugs must be water-soluble enough to be excreted in the stool or urine. Metabolism occurs mainly in the liver, kidney, gut wall, and skin (Open Resources for Nursing et al., 2023a).
In the liver, drugs are metabolized by cytochrome P450 enzymes. Many different cytochrome P450 enzymes metabolize drugs. It is estimated that there are 50 cytochrome P450 enzymes, but ten are responsible for metabolizing 90% of the drugs (Lynch & Price, 2007). The metabolism of drugs occurs in either phase I or phase II. Phase I metabolism involves chemically altering the drug to allow it to go through phase II metabolism or to be excreted. There are multiple methods by which phase I metabolism may occur, including oxidation, reduction, or hydrolysis. Oxidation is the most common reaction. It mainly involves the cytochrome P450 family of membrane-bound enzymes in the liver. Most products of the drugs that go through phase I metabolism become pharmacologically inactive, but some drug metabolites retain some of the original drug activity.
Phase II drug metabolism is the second stage of drug metabolism, following Phase I metabolism (Open Resources for Nursing et al., 2023a). Phase II metabolism involves conjugating the drug or its metabolites with endogenous molecules to make them more water-soluble and easier to eliminate from the body. This process typically results in forming larger, polar molecules that are less likely to be reabsorbed by the kidneys and more readily excreted in urine or bile.
Excretion is how the drug leaves the body.
Urinary excretion typically occurs for water-soluble drugs that have a low molecular weight. The urinary system also excretes drugs that are made water-soluble by liver metabolism.
Larger molecular weight drugs prefer to leave the body through fecal excretion. These drugs include those that are not absorbed and those that are metabolized in the liver. If the drug is still significantly lipid-soluble, it may be reabsorbed and enter the portal vein in enterohepatic circulation.
Pharmacodynamics includes how the drug works in the body, including the intensity of its effects, its adverse effects, and its time course. Receptors on different body organs bind to drugs to give a therapeutic effect. For example, a drug that acts on a receptor in the cardiac tissue may increase the heart's contraction force. Generally, the drug’s intensity is determined by the concentration of the drug at the receptor, the density of the receptors on the cell’s surface, how the signal is transmitted into the cell, and factors that affect the protein production of a drug’s effect.
With continued use, some individuals develop tolerance, and the drug becomes less effective. Tolerance may occur because of increased drug metabolism. A typical example of drug tolerance is the chronic use of opiates. The chronic use of opiates leads to less effect with a given dose, requiring a patient to need an escalating dose to get the same pain relief.
Understanding pharmacokinetics improves the prescriber’s ability to prescribe safely and effectively. It will help the prescriber understand the proper dose, frequency, and dosing route. Understanding pharmacokinetics helps the prescriber know how to prescribe to ensure the effective drug concentrations reach the target tissue for adequate time to treat the condition.
Some key points to understand from pharmacokinetics:
Preventive healthcare is meant to reduce death and disability and maintain health in the targeted population. Its primary goal is to implement cost-effective measures to help most of the population. The goals look to the individual and the community at large. The major goals of prevention are to:
Preventive healthcare is critical to ongoing healthcare and can significantly reduce morbidity and mortality. Preventive healthcare can occur in the setting of an annual physical exam or during a “sick visit.” There are four main types of clinical prevention: chemoprevention, immunizations, behavioral counseling, and screening.
Drugs and therapeutic devices (products that help people deal with physical illness, such as hearing aids, mobility devices, or pacemakers) can potentially prevent disease, prevent its complications, and help individuals maintain health. Three types of preventive healthcare exist: primary, secondary, and tertiary (AbdulRaheem, 2023).
Primary preventive healthcare prevents disease by eliminating its causes. Examples of primary prevention include immunizations, bariatric surgery, and smoking cessation.
Secondary prevention involves finding the disease early before symptoms have occurred and implementing interventions to stop its progression. This prevention involves doing a screening test to detect the problem and then implementing interventions. Examples are screening for human immunodeficiency virus (HIV) in asymptomatic people and routine Pap smears.
Tertiary prevention looks to stop deterioration after a disease process is identified. Examples include giving a statin to a patient after a heart attack. It is another term for disease treatment.
There can be some confusion around these terms, with some overlap occurring. For example, a patient can undergo a colonoscopy to remove a polyp, which is classified as primary prevention. The colonoscopy can also find early colon cancer that is not causing any symptoms, which would be classified as secondary prevention. The colonoscopy could also be done on a patient treated for colon cancer to look for recurrence, which would be classified as tertiary prevention.
Chemoprevention is done when drugs are used to prevent disease. While there are many examples of chemoprevention, some have excellent benefits. Some examples include:
Preventive care is important in those with established chronic diseases. CVD, which includes heart disease and stroke, is the leading cause of death. Risk factors such as high blood pressure, high cholesterol, smoking, obesity, and diabetes significantly contribute to the prevalence of these conditions. Between these two diseases, 934,500 Americans die annually. Heart disease and stroke cost the healthcare system 251 billion dollars annually, leading to 156 billion dollars in lost job productivity (Centers for Disease Control [CDC], 2024).
Cancer is the second leading cause of death and accounts for 600,000 deaths annually, with an estimated healthcare cost of 240 billion dollars by 2030. Diabetes affects 38 million Americans, with a total estimated cost of 413 billion dollars of lost productivity and medical expenses. The overall cost of arthritis is estimated at 600 billion dollars (CDC, 2024).
The utilization of drugs and therapeutic devices are primary weapons used to combat known medical diseases. With proper use of drugs, risk factors for many chronic diseases may help ensure that these conditions are controlled to reduce the risk of morbidity and mortality.
The goal of using drugs and therapeutic devices to prevent disease looks to modify factors that can lead to the disease or slow its progression. The goal of prevention is to extend the disease-free lifespan. This prevention works best on many chronic diseases that progress over the years.
Examples of this include managing risk factors for heart disease. In the overwhelming majority of cases, heart disease develops over the years and is preceded by years of unmanaged risk factors. Identifying the risk factors for heart disease and managing them will increase the time until clinical disease manifests. Many lifestyle interventions, including regular exercise, a healthy diet, and smoking cessation, can be implemented.
While these interventions can significantly reduce the risk of heart disease, drugs and therapeutic devices can also significantly maintain health and prevent disease progression. These interventions include using blood pressure drugs to maintain good blood pressure, lipid-lowering agents to keep cholesterol levels in the optimal range, and daily aspirin therapy, which may be beneficial in reducing risk in some patients. Also, the influenza vaccine reduces major cardiovascular events (Behrouzi et al., 2022).
Another example of drug use and therapeutic devices to maintain health is a patient with heart failure (HF). Several drugs improve morbidity, mortality, and quality of life in HF patients. A variety of drug classes are used in the management of HF. Some work by off-loading fluid, while others are involved in adjusting the body's hormonal balance to improve cardiac function (angiotensin-converting enzyme inhibitors, angiotensin receptor blockers, angiotensin receptor neprilysin inhibitor, sodium-glucose co-transporter 2 (SGLT2) inhibitors, beta-blockers, and spironolactone). The treatment of HF often requires the use of multiple drugs.
The next section will look at some major classes of drugs and provide a basic overview of pharmacology. It will provide a practical look at the use of selected drugs.
Antibiotics are a diverse group of medications that fight infection (Patel et al., 2023a). They are classified by action as bacteriostatic or bactericidal. Bacteriostatic action inhibits growth and bactericidal kills bacteria. These actions are accomplished through various mechanisms, including inhibiting cell wall synthesis, altering cell permeability, prohibiting cell protein synthesis, changing nucleic acid metabolism of the cell, blocking metabolic steps of the cell, and blocking DNA synthesis.
Common classes of antibiotics include:
The effectiveness of an antibiotic can be altered by how it is taken. Antibiotics should be taken at regular intervals to maintain appropriate concentrations. Some antibiotics must be taken on an empty stomach, while others are best taken with a meal. Most should be taken with a full glass of water, and some should not be taken with dairy products or close to when dairy products are consumed.
It is good practice to culture the suspected bacteria before administering the drug (Patel et al., 2023a). Typically, the infection is treated empirically, and once the culture returns, the antibiotic may be changed to ensure that the antibiotic will eradicate the organism. It is also essential to assess the severity of the illness. This assessment will determine how aggressively and how long to treat.
Allergic reactions to antibiotics can vary in severity from mild rashes to life-threatening anaphylaxis. The most common antibiotics associated with allergic reactions include penicillins (such as amoxicillin and ampicillin), cephalosporins (like cephalexin), and sulfonamides (such as trimethoprim-sulfamethoxazole). Symptoms of an allergic reaction to antibiotics may include skin rashes, itching, hives, swelling of the face or throat, difficulty breathing, wheezing, or, in severe cases, anaphylaxis characterized by a rapid drop in blood pressure and difficulty breathing.
A significant complication of antibiotic therapy is infection. Many antibiotics can disrupt the natural balance of bacteria in the body, which can occur due to the antibiotic killing off beneficial bacteria. Common antibiotic-induced infections include yeast infections and Clostridium difficile (C. difficile) infections. When antibiotics disrupt the natural balance of microorganisms in the vagina, it leads to overgrowth of yeast, particularly Candida species, which can result in symptoms such as itching, burning, and abnormal discharge. Yeast infections are generally less serious than C. difficile infections but can cause significant discomfort. Treatment usually involves antifungal medications, such as creams, suppositories, or oral tablets.
Adverse effects are different from allergic reactions. They are often considered the expected side effects of the drugs. Common adverse effects of antibiotics are nausea, vomiting, and diarrhea. Some antibiotics have very specific and severe adverse effects and contraindications. Nurses should familiarize themselves with the antibiotics’ adverse effects and contraindications.
Nursing consideration and patient education:
Nebulized medications are a cornerstone in treating respiratory conditions, delivering medication directly to the lungs for rapid effect. As a nurse, understanding the types, administration techniques, and safety considerations of nebulized therapies is essential for effective patient care (Barjaktarevic & Milstone, 2020).
Common Nebulized Medications
Administration Techniques
Safety Considerations
Documentation
Administering nebulized medications requires careful preparation, patient education, and monitoring to ensure safe and effective treatment. By following best practices and maintaining a patient-centered approach, nurses can significantly enhance the management of respiratory conditions.
Antivirals treat and manage viral infections, including influenza, HIV, hepatitis, herpes simplex, and herpes zoster. There are several classes of antivirals, each working at a different stage of the viral life cycle. The exact mechanism of action is different for each disease and particular virus. Antiviral drugs’ most common side effects are diarrhea, nausea, vomiting, dizziness, sleep issues, and headaches. However, each type of antiviral classification has additional side effects and serious reactions.
Protease Inhibitors (PIs) block the activity of an enzyme called protease, which HIV uses to produce infectious viral particles. Examples include ritonavir, atazanavir, and darunavir. Integrase Strand Transfer Inhibitors (INSTIs) inhibit the action of integrase, an enzyme HIV uses to insert its genetic material into the deoxyribonucleic acid (DNA) of the host cell. Examples include raltegravir, dolutegravir, and bictegravir. Entry inhibitors prevent HIV from entering human cells. There are two types: fusion inhibitors, which block HIV from fusing with the host cell, and CCR5 antagonists, which block a co-receptor on the host cell that HIV uses to enter. Examples include enfuvirtide (fusion inhibitor) and maraviroc (CCR5 antagonist) (Kemnic & Gulick, 2022).
Post-attachment inhibitors are an innovative class of antiretroviral drugs specifically designed to treat HIV infection. They function by interfering with the virus’s ability to fuse with the host cell after it has attached to the CD4 receptor on the surface of T-cells. Post-attachment inhibitors target the CD4 receptors on T-cells. After HIV attaches to the CD4 receptor, these inhibitors bind to the receptor, preventing the virus from completing the fusion process necessary to enter the cell. By binding to the CD4 receptor, the inhibitors prevent the conformational changes required for the virus’s envelope protein (gp120) to interact effectively with the co-receptors (CCR5 or CXCR4) on the T-cell, thereby blocking the fusion process.
Ibalizumab-uiyk (Trogarzo®) and fostemsavir (Rukobia®) are agents available in this class. While not a first-line option, it offers a treatment option for patients with limited choices due to resistance to other medications. It is generally well-tolerated with manageable side effects.
Ritonavir and cobicistat are essential components of modern HIV therapy, primarily used to enhance the effectiveness of other antiretroviral drugs by increasing their plasma concentrations. Their use allows for more effective viral suppression with potentially lower doses of active antiretroviral drugs, reducing side effects and improving patient adherence to treatment regimens.
Combination therapy is the standard treatment approach for HIV/acquired immunodeficiency syndrome (AIDS). It involves using a combination of drugs from different classes to target the virus at multiple points in its life cycle. The specific combination of drugs used may vary depending on factors such as the individual’s viral load, drug resistance profile, potential side effects, and other medical considerations (Kemnic & Gulick, 2022).
This approach has several key benefits:
HIV replicates and creates copies that are different from their parent strain. Because of this, many mutations are made. More drug-associated resistant mutations may occur in those who take less potent ART therapy, which less effectively suppresses viral replications. Those who develop resistance – as evidenced by viral load rising despite compliance with therapy – need to have drug resistance testing.
Abacavir (ABC) | Ziagen® |
Lamivudine (3TC) | Epivir® |
Didanosine (ddI) | Videx® Videx® EC |
Zidovudine (ZDV, AZT) | Retrovir® |
Emtricitabine (FTC) | Emtriva® |
Tenofovir disoproxil fumarate (TDF) | Viread®* |
Rilpivirine (RPV) | Edurant® |
Doravirine (DOR) | Pifeltro® |
Delavirdine (DLV) | Rescriptor |
Efavirenz (EFV) | Sustiva® |
Nevirapine (NVP) | Viramune® |
Fosamprenavir (FPV) | Lexiva® |
Ritonavir (RTV) | Norvir® |
Darunavir (DRV) | Prezista® |
Lopinavir/ritonavir (LPV/r) | Kaletra® |
Atazanavir (ATV) | Reyataz® |
Integrase inhibitors:
|
CCR5 antagonist:
|
Fusion inhibitor:
|
Post-attachment inhibitors:
|
Pharmacokinetic enhancers:
|
Efavirenz + Emtricitabine + Tenofovir disoproxil fumarate |
Bictegravir + Emtricitabine + Tenofovir alafenamide |
Darunavir + Cobicistat + Emtricitabine + Tenofovir alafenamide |
Rilpivirine + Emtricitabine + Tenofovir |
Doravirine + Lamivudine + tenofovir disoproxil fumarate |
Dolutegravir + Lamivudine |
Zidovudine + Lamivudine |
Emtricitabine + Tenofovir disoproxil fumarate |
Dolutegravir + Rilpivirine |
Lamivudine + Abacavir |
Abacavir + Dolutegravir + Lamivudine |
Emtricitabine + Tenofovir disoproxil fumarate + rilpivirine |
Emtricitabine + Tenofovir alafenamide |
Elvitegravir + Cobicistat + Emtricitabine + Tenofovir alafenamide |
Elvitegravir + Cobicistat + Emtricitabine + Tenofovir disoproxil fumarate |
(Kemnic & Gulick, 2022; NIH, 2024) |
HIV drugs have many side effects. Many drugs lead to nausea, vomiting, and diarrhea. The NRTIs are associated with hepatotoxicity and must be used watchfully in patients with liver insufficiency. NRTIs can be associated with peripheral neuropathy, lactic acidosis, pancreatitis, and lipodystrophy (Kemnic & Gulick, 2022).
PIs are associated with nausea, vomiting, diarrhea, elevated liver enzymes, dyslipidemia, hyperglycemia, and lipodystrophy. Approximately 2 in 3 patients on PI's have triglyceride levels higher than 240 mg/dL, and many have triglycerides over 500 mg/dL (Dubé et al., 2013). Atazanavir and darunavir are the least likely to cause dyslipidemia. PI's have multiple drug-to-drug interactions as the CYP450 system metabolizes them (Kemnic & Gulick, 2022).
Herpes simplex virus (HSV) is a virus that causes herpes. There are two types, 1 and 2. Type 1 HSV typically causes cold sores but can also cause genital herpes. Type 2 HSV is the most common cause of genital herpes (sexually transmitted) but can also cause sores around the mouth.
Treatment of HSV is with antiviral drugs. Drugs, including – acyclovir (Zovirax®), famciclovir (Famvir®), and valacyclovir (Valtrex®) – are used to lessen symptoms and reduce outbreaks. There are generally two ways to take the drug: suppressive and episodic. Suppressive therapy entails taking drugs every day to suppress outbreaks. Episodic therapy is taking medicine at the first symptom (typically a burning or tingling sensation in the area where there will be a breakout).
Episodic therapy:
Suppressive therapy:
Antivirals | Side Effects |
---|---|
Acyclovir | Malaise, gastrointestinal (GI) upset, thrombocytosis, rash, pain |
Famciclovir | Headache, fatigue, dizziness, somnolence, GI upset, pruritis |
Valacyclovir | GI upset, headache, dizziness, depression, dysmenorrhea, arthralgia |
(Samuel et al., 2022) |
Influenza, commonly known as the flu, is a highly contagious viral infection primarily affecting the respiratory system. It is caused by influenza viruses, primarily types A and B, which belong to the Orthomyxoviridae family. Influenza viruses are known for their ability to mutate rapidly, leading to seasonal outbreaks and occasional pandemics (Boktor & Hafner, 2023).
There are two main classes of influenza antiviral medications: neuraminidase inhibitors and cap-dependent endonuclease inhibitors. The neuraminidase inhibitors include drugs such as oseltamivir (Tamiflu®), zanamivir (Relenza®), and peramivir (Rapivab®). These medications work by blocking the action of the neuraminidase enzyme, which is essential for releasing newly formed influenza viruses from infected cells. By inhibiting neuraminidase, these drugs help reduce the spread of the virus within the body and alleviate symptoms. They are typically effective against both influenza A and B viruses.
The cap-dependent endonuclease inhibitor has only one medication in its class – Baloxavir marboxil (Xofluza®). It works by inhibiting the cap-dependent endonuclease enzyme, which is necessary for viral replication. By targeting this enzyme, baloxavir interferes with the ability of the influenza virus to replicate and spread within the body. These antiviral medications are most effective when taken early in the course of illness, ideally within the first 48 hours of symptom onset. They can help reduce the severity and duration of symptoms and the risk of complications associated with influenza (Fukao et al., 2022).
Antivirals for Influenza | Side effects |
---|---|
Oseltamivir (Tamiflu®) – oral | Dizziness, fatigue, headache, insomnia, epistaxis, conjunctivitis, GI upset, cough, lymphedema, and dermatitis in children. |
Zanamivir (Relenza®) – inhaled | Hives, difficulty breathing, and swelling of the face, lips, tongue, or throat are potentially life-threatening. Other side effects include headache, dizziness, GI upset, joint pain, chills, fever, stuffy nose, sneezing, and sore throat. |
Peramivir (Rapivab®) -intravenous | Severe reactions include abnormal liver function tests, decreased neutrophils, erythema multiform, and Stevens-Johnson Syndrome. Other side effects include GI upset, high blood pressure, increased glucose, and rash. |
Baloxavir marboxil (Xofluza®) – oral | Diarrhea, bronchitis, nausea, runny nose, headache |
(Świerczyńska et al., 2022) |
Nursing Considerations and Patient Education
Antiseizure medications, also known as antiepileptic drugs (AEDs), work by influencing the electrical activity in the brain to prevent or reduce the occurrence of seizures. The exact mechanisms of action vary depending on the specific medication, but there are several common ways in which these drugs work (Springer & Nappe, 2023):
Seizure drugs have been around since phenobarbital was first used as an anti-epileptic in 1912. Compared to older drugs (phenytoin, carbamazepine, valproate, and phenobarbital), the newer drugs are easier to use as they typically do not require serum monitoring and have fewer drug-to-drug interactions, have more simple dosing and fewer side effects.
Carbamazepine (Tegretol®) inactivates sodium channels and inhibits the creation of rapid action potentials (Maan et al., 2023). It can treat generalized and focal seizures and other illnesses such as trigeminal neuralgia and bipolar disease. It is effective for a wide range of seizure disorders in both adults and children. This drug has many drug-to-drug interactions. Levels should be closely monitored to ensure appropriate levels are present.
Side effects include nausea, vomiting, rash, itch, diarrhea, dizziness, vision change, lethargy, headache, and fluid retention. Also, lower testosterone levels and increased rates of sexual dysfunction may be seen. Hyponatremia may be seen, and it is recommended to measure the level at the start of therapy and when therapeutic levels are reached. Serious side effects include liver failure, Stevens-Johnson syndrome/toxic epidermal necrolysis, agranulocytosis, aplastic anemia, pancreatitis, and lupus syndrome.
Lacosamide (Vimpat®, Motpoly XR®) inactivates voltage-dependent sodium channels, stabilizing the neuronal membrane (Subbarao et al., 2023). It is approved as monotherapy or add-on therapy for focal-onset seizures and as an adjunctive treatment for primary generalized tonic-clonic seizures. Its recommended starting dose is 50-100 mg twice daily (for the immediate-release formulation) to a maximum of 400 mg daily.
Side effects include dizziness, ataxia, vertigo, nausea, headache, diplopia, and poor coordination. Syncope has been reported in a small percentage of patients with diabetic neuropathy and those receiving doses of more than 400 mg daily. Serious side effects include neutropenia, multiorgan hypersensitivity, and atrioventricular block.
Lamotrigine (Lamictal®) has multiple mechanisms of action, including inactivating the voltage-dependent sodium channels (Betchel et al., 2023). It may also affect neurons that synthesize aspartate and glutamate. It is approved for focal-onset seizures and adjunctive therapy for generalized tonic-clonic seizures and Lennox-Gastaut syndrome (LGS). It is often considered an alternative to valproate with fewer side effects.
Pregnancy and oral contraceptives can affect serum levels. This drug interacts with many other seizure drugs, including valproate, phenytoin, and carbamazepine. The typical starting dose is 25 mg every day and is slowly increased. The maximum dose depends on the patient’s other drugs, including valproate, carbamazepine, phenytoin, rifampin, and some protease inhibitors.
Side effects include nausea, rash, headache, dizziness, fatigue, sleepiness, and diplopia. The rash is common and most likely to occur in those who have the dose increased too quickly. Serious side effects include Stevens-Johnson syndrome/toxic epidermal necrolysis, multiorgan hypersensitivity, and aseptic meningitis.
Levetiracetam (Keppra®, Roweepra®) is a commonly used drug with a unique mechanism of action primarily involving the binding to synaptic vesicle protein SV2A, which modulates neurotransmitter release. This binding reduces neuronal excitability and helps prevent seizures. Additional mechanisms include the modulation of calcium channels and enhancement of GABAergic inhibitory transmission. It is a drug with broad-spectrum antiseizure properties. Drug interactions are minimal with levetiracetam, as it is independent of the CYP system.
Dosing starts at 250-500 mg twice a day and is often very effective at reducing seizures after the first day. It may be titrated to 3000 mg daily as a maximum dose. An intravenous form is available, but it is no more bioavailable than oral. Levels of the drugs do not need to be routinely monitored but may be monitored in renal insufficiency, pregnancy, those who are critically ill, or to monitor for adherence (Kumar et al., 2023).
Side effects include somnolence, dizziness, agitation, irritability, fatigue, behavioral change, and upper respiratory tract infection. These side effects are more common during the initial phase of therapy. Serious side effects include Stevens-Johnson syndrome/toxic epidermal necrolysis, pancytopenia, and psychosis.
Oxcarbazepine (Trileptal®) is similar to carbamazepine and blocks voltage-sensitive sodium channels and affects high-voltage calcium channels (Preuss et al., 2023). In adults, it is indicated for monotherapy or adjunctive therapy in the treatment of focal seizures. It has fewer drug-to-drug interactions when compared to carbamazepine.
Side effects include dizziness, vertigo, fatigue, rash, ataxia, diplopia, sedation, nausea, headache, and hyponatremia. Serious side effects include Stevens-Johnson syndrome/toxic epidermal necrolysis, multiorgan hypersensitivity, agranulocytosis, and pancytopenia.
Carbamazepine and oxcarbazepine are two seizure drugs likely to cause hyponatremia. It is more likely to be seen in older adults, those on diuretics, those with high serum levels of the seizure drug, and those on polytherapy for seizures. Baseline sodium levels should be checked, and then once levels are therapeutic, sodium levels should be rechecked. The sodium levels should be checked if the patient develops any indication of hyponatremia, such as headaches, lethargy, or confusion. |
Phenobarbital works on the GABA receptor to extend the GABA effect (Subbarao et al., 2023). It is the oldest anti-epileptic and is indicated for generalized and focal seizures. It is metabolized in the liver and should be used cautiously in those with hepatic impairment. It is a schedule IV controlled substance in intravenous, intramuscular, and oral forms. This drug has abuse potential and can lead to hypotension, respiratory depression, and coma. It is dosed at 1-5 mg/kg/day, and blood levels should be monitored.
Side effects include nausea, rash, mood changes, sedation, tolerance, dependence, and reduced concentration. Chronic use may be associated with frozen shoulder, bone problems, Dupuytren’s contractures, and plantar fibromatosis. Serious side effects include liver failure, agranulocytosis, and Stevens-Johnson syndrome/toxic epidermal necrolysis.
Phenytoin (Dilantin®) blocks the sodium channels, thereby reducing synaptic transmission. It is another older drug that was first used in the 1930s. It can be used for those with generalized and focal seizures and status epilepticus (Gupta & Tripp, 2023).
Phenytoin interacts with many drugs, which can affect phenytoin levels. Phenytoin is available as an oral agent and an intravenous agent. The maintenance dose is typically 300-400 mg daily in 2-3 divided doses. The loading dose may be 15 mg/kg in three divided doses. Target doses should control seizures without significant side effects, which generally correlates with a serum concentration between 10-20 mcg/mL. Caution must be used with dosing as small changes in dose may cause significant changes in drug levels.
Pregabalin (Lyrica®) is similar to gabapentin. It binds to the alpha-2-delta subunit of the calcium channel and affects glutamate, substance P, and noradrenaline. It is used as an adjunctive treatment for focal seizures (Subbarao et al., 2023). It does not have significant interactions with other drugs used to manage seizures, and overall, very few drug interactions. It is dosed 150 mg daily in 2 to 3 divided doses, which may increase to 600 mg daily.
Side effects include ataxia, dizziness, sedation, weight gain, vision change, tremor, impaired concentration, peripheral edema, and dry mouth. It may also cause euphoria and is classified as a Schedule V controlled substance. Serious side effects include angioedema, hypersensitivity reactions, and rhabdomyolysis.
Topiramate (Topamax®) exerts its therapeutic effects through multiple mechanisms, including inhibiting voltage-gated sodium channels, enhancing GABAergic activity, antagonizing AMPA/glutamate receptors, and inhibiting carbonic anhydrase. These actions collectively contribute to its efficacy in controlling seizures, preventing migraines, and potentially treating other conditions. Topiramate helps stabilize brain activity and prevent abnormal electrical discharges by reducing neuronal excitability and enhancing inhibitory neurotransmission. It is indicated for monotherapy for primary generalized tonic-clonic and focal-onset seizures. It may also be used for adjunctive therapy for Lennox-Gastaut syndrome.
Side effects include weight loss, fatigue, dizziness, cognitive impairment, sedation, paresthesia, depression, kidney stones, reduced appetite, nervousness, mood disturbance, and tremor. Serious side effects include hyperthermia, acute myopia, glaucoma, and kidney stones.
Valproate (Depakote®) is a versatile medication used primarily for epilepsy, bipolar disorder, and migraine prophylaxis. Its mechanism of action involves enhancing GABAergic activity, inhibiting voltage-gated sodium and T-type calcium channels, and modulating excitatory neurotransmission. It is metabolized in the liver, and the dose may need to be decreased in those with hepatic insufficiency. It is also bound to protein, so those with low albumin in the blood may have elevated levels despite a low serum value. Dosing is between 10 and 15 mg/kg and may increase weekly. Serum levels should be checked about one to two weeks after starting the drug.
Side effects include tremors, hair loss, nausea, vomiting, dizziness, easy bruising, weight gain, and an increase in alanine aminotransferase levels. In rare situations, it may cause elevated ammonia levels, leading to encephalopathy, acute liver injury, or pancreatitis. It can also cause thrombocytopenia and elevations in thyroid-stimulating hormone levels. It has a high rate of teratogenicity when compared to other anti-seizure drugs. Serious side effects include liver failure, agranulocytosis, Stevens-Johnson syndrome/toxic epidermal necrolysis, aplastic anemia, and pancreatitis.
Zonisamide (Zonegran®) blocks the sodium and calcium channels and is indicated for generalized and focal seizures. It is mainly metabolized in the liver. It interacts with multiple other anti-seizure drugs. Its mechanism of action includes the inhibition of sodium and T-type calcium channels, modulation of neurotransmitter release, and weak carbonic anhydrase inhibition (Subbarao et al., 2023).
Common side effects include fatigue, dizziness, somnolence, mental status changes, ataxia, anorexia, weight loss, nausea, kidney stones, concentration problems, and depression. Serious side effects include Stevens-Johnson syndrome/toxic epidermal necrolysis, aplastic anemia, agranulocytosis, nephrolithiasis, acute myopia, glaucoma, hyperammonemia, and encephalopathy.
Patient Education
Nursing Considerations
Generic Name | Brand Name | Mechanism of Action | Common Uses | Notable Side Effects |
---|---|---|---|---|
Carbamazepine | Tegretol® | Blocks voltage-gated sodium channels | Focal seizures, generalized tonic-clonic seizures, bipolar disease, trigeminal neuralgia | Dizziness, drowsiness, nausea, risk of Stevens-Johnson syndrome |
Lamotrigine | Lamictal® | Inhibits voltage-gated sodium channels, reduces glutamate release | Focal seizures, generalized seizures, bipolar disorder | Rash (including Stevens-Johnson syndrome), headache, nausea |
Levetiracetam | Keppra® | Modulates synaptic vesicle protein SV2A | Focal seizures, generalized seizures | Drowsiness, dizziness, behavioral changes |
Valproate | Depakote® | Increases GABA levels, inhibits sodium and calcium channels | Focal seizures, generalized seizures, bipolar disorder, migraine prophylaxis | Weight gain, hair loss, liver toxicity, teratogenicity |
Topiramate | Topamax® | Blocks sodium channels, enhances GABA, antagonizes glutamate receptors | Focal seizures, generalized seizures, migraine prophylaxis | Weight loss, cognitive effects, kidney stones, metabolic acidosis |
Phenytoin | Dilantin® | Blocks voltage-gated sodium channels | Focal seizures, generalized tonic-clonic seizures | Gingival hyperplasia, hirsutism, bone density loss, ataxia |
Gabapentin | Neurontin® | Modulates calcium channels, increases GABA synthesis | Focal seizures, neuropathic pain | Drowsiness, dizziness, peripheral edema |
Oxcarbazepine | Trileptal® | Blocks voltage-gated sodium channels, modulates calcium channels | Focal seizures | Hyponatremia, dizziness, fatigue |
Lacosamide | Vimpat® | Enhances slow inactivation of sodium channels | Focal seizures, adjunctive therapy for primary generalized tonic-clonic seizures | Dizziness, headache, nausea |
Zonisamide | Zonegran® | Inhibits sodium and T-type calcium channels, modulates GABA and glutamate | Focal seizures, generalized seizures | Drowsiness, dizziness, kidney stones, weight loss |
Drugs are frequently used to treat depression and anxiety. The major classes of drugs include selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors (MAOIs), tricyclic antidepressants (TCAs) and other agents.
SSRIs are first-line agents for depression and work by increasing the amount of the neurotransmitter serotonin in the brain. They are first-line treatment options primarily because of their safety profile, efficacy, and limited drug-to-drug interactions.
Fluoxetine (Prozac®) is dosed at 20 mg in the morning and may increase to 80 mg daily. Each titration must occur after a few weeks on the drug. It is not indicated for those less than eight years old. Fluoxetine has a long half-life and is less likely to lead to withdrawal symptoms if abruptly discontinued. A weekly formulation is available that is dosed at 90 mg once a week (Coryell, 2023).
Fluoxetine can increase warfarin, phenytoin, carbamazepine, TCAs, and benzodiazepines. It may lower the therapeutic effect of codeine. It may cause serotonin syndrome when combined with other SSRIs and other antidepressants.
Sertraline (Zoloft®) is started at 25-50 mg orally daily, and the dose can be increased gradually to a maximum of 200 mg daily. It is not indicated for those less than six years old. Common side effects include dizziness, fatigue, headache, insomnia, somnolence, diarrhea, nausea, tremor, and diaphoresis. It may interact with warfarin, cimetidine, digoxin, and diazepam. It is indicated for major depressive disorder, premenstrual dysphoric disorder, panic disorder, posttraumatic stress disorder (PTSD), obsessive-compulsive disorder (OCD), and social anxiety disorder.
Paroxetine (Paxil®) has a short half-life and may lead to discontinuation syndrome when the drug is stopped or there are missed doses. It has the most potent anticholinergic effects of any of the SSRIs. For major depression, the standard form is dosed at 10 mg per day to a maximum of 50 mg orally per day, and the extended-release form (Paxil CR) is dosed at 12.5 mg once a day to a maximum of 62.5 mg orally every day. Paroxetine is indicated for major depressive disorder, panic disorder, OCD, social anxiety disorder, generalized anxiety disorder, PTSD, and premenstrual dysphoric disorder. Side effects include somnolence, insomnia, dizziness, headache, nausea, xerostomia, constipation, diarrhea, weakness, tremors, and diaphoresis (Coryell, 2023).
Citalopram (Celexa®) is indicated for depression and is dosed at 20 mg once a day, and the dose can be increased to 40 mg once a day after one week. It interacts with macrolide antibiotics, cimetidine, azole antifungal, omeprazole, and carbamazepine. Side effects include sleep disturbance, xerostomia, nausea, and diaphoresis.
Escitalopram (Lexapro®) is dosed at 10 mg daily and may increase to 20 mg after one week. It has few interactions but may interact with other SSRIs, cimetidine, and alcohol. The FDA warns that both citalopram (more than 40 mg/day) and escitalopram (more than 20 mg/day) can potentially prolong the QT interval and may be fatal. They should be used cautiously in those with underlying heart disease and those prone to becoming hypokalemic (Coryell, 2023).
SNRIs are newer drugs to treat depression and anxiety. Drugs in this class include venlafaxine (Effexor®), duloxetine (Cymbalta®, Drizalma®, Irenka®), desvenlafaxine (Khedezla®, Pristiq®), milnacipran (Savella®), and levomilnacipran (Fetzima®).
Venlafaxine comes in an extended-release form and is dosed 37.5 to 75 mg a day and maybe titrated up to 225 mg daily. It may interact with other antidepressants, cimetidine, diuretics, and alcohol. It should not be used in those with severe uncontrolled hypertension. At doses less than 150 mg daily, it mainly affects serotonin levels, but higher doses affect dopamine and norepinephrine levels. Discontinuation syndrome is high with this drug, and when the medication is stopped, it must be tapered slowly.
Desvenlafaxine is dosed at 50 mg daily for adults. It may be titrated up to 400 mg once a day, but positive effects are not proven with higher doses (as reported by the manufacturer). Common side effects include nausea, headache, dizziness, dry mouth, insomnia, fatigue, and bowel disturbance. It may interact with other SSRIs or blood thinners.
Milnacipran is dosed at 12.5 mg daily on the first day and titrated upwards to a maximum of 200 mg daily, divided every 12 hours (Gupta et al., 2021). It should be used cautiously in those with moderate to severe renal and hepatic impairment. Those who take it may suffer from nausea, headache, dizziness, sleep disturbance, and constipation.
Levomilnacipran is started at 20 mg once a day and increased to 40 mg once a day (Coryell, 2023). The maximum dose is 120 mg a day. Doses should be reduced in those with moderate and severe renal insufficiency. Common side effects include nausea but may also be associated with sexual dysfunction, constipation, urinary hesitancy, and elevated heart rate.
Duloxetine is dosed at 20 mg twice a day to start and may be increased to 30 mg twice daily or 60 mg once a day in the adult. The maximum dose is 120 mg a day. It may interact with ciprofloxacin, SSRIs, TCAs, antiarrhythmic agents, and anticoagulants. Common adverse effects include nausea, headache, dry mouth, dizziness, sleep disturbance, and fatigue.
Duloxetine has multiple indications. It is approved for treating depression in addition to diabetic peripheral neuropathy, chronic musculoskeletal pain, fibromyalgia, and generalized anxiety disorder. This drug is often used by those with depression in addition to one of these co-morbid conditions.
Other antidepressants include bupropion (Wellbutrin SR®, Wellbutrin XL®), mirtazapine (Remeron®), vortioxetine (Brintellix®), vilazodone (Viibryd®) and trazodone. Generally, this group has low toxicity in overdose and may have an advantage over the SSRIs by causing less sexual dysfunction and gastrointestinal distress.
Nursing Considerations
Antipsychotics can be classified as typical (first-generation) or atypical (second-generation). Antipsychotic drugs are used to manage schizophrenia, bipolar disease, and some cases of depression.
Typical antipsychotics (first-generation agents) have existed since the 1950s and include haloperidol (Haldol®), thioridazine (Mellaril®), molindone (Moban®), fluphenazine (Prolixin®), and perphenazine (Trilafon®). First-generation antipsychotics are effective at treating hallucinations and delusions and lower the risk of recurrent psychosis. Atypical (second-generation) antipsychotics not only treat hallucinations and delusions (positive symptoms) but also negative symptoms of schizophrenia, such as ambivalence and withdrawal.
Atypical antipsychotics have existed since the late 1980s. These drugs are less likely to lead to neurological side effects, which results in better compliance. This class of drugs is associated with other side effects such as weight gain, diabetes, and elevated cholesterol.
First-generation antipsychotics | Second-generation antipsychotics |
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|
|
(Meissner, 2024) |
Recognizing and treating side effects is a key component of pharmacotherapy with antipsychotics. Those afflicted with too many side effects will discontinue therapy and likely relapse.
The first-generation antipsychotic drugs, known as typical antipsychotics, generally have more neurological side effects than second-generation antipsychotics (Chokhawala & Stevens, 2023). High-potency drugs have more side effects. High-potency first-generation antipsychotics have a high risk of extrapyramidal side effects and a medium risk of sedation. Low-potency first-generation drugs have a lower risk of extrapyramidal side effects and a high risk of sedation and anticholinergic effects.
Extrapyramidal side effects include Parkinsonism, tardive dyskinesia, dystonia, and akathisia.
The atypical antipsychotic drugs have less risk of neurological side effects but are not without risk. These agents may cause weight gain, diabetes, and abnormal cholesterol levels. Antipsychotics may cause weight gain and diabetes, but weight gain and diabetes may be reversed when the drug is stopped.
Nursing Considerations
Cholinesterase inhibitors and N-methyl-D-aspartate (NMDA) receptor antagonists are the two classes of older drugs used to manage Alzheimer’s disease (Jones, 2011). Patients with Alzheimer’s disease have a reduced amount of acetylcholine with resultant reduced cortical cholinergic function. Cholinesterase inhibitors enhance the cholinergic transmission in the synaptic cleft by inhibiting the enzyme cholinesterase.
Donepezil, galantamine, and rivastigmine are three currently available cholinesterase inhibitors. Patients show variable responses to cholinesterase inhibitors, with some patients having profound benefits and others demonstrating minimal to no benefit. Therefore, nurses should assess the efficacy of these drugs on all patients. Patients who do not have a good clinical benefit from one drug may benefit from another drug in the same class.
Common side effects of cholinesterase inhibitors include headaches, dizziness, diarrhea, nausea, anorexia, muscle cramps, and nightmares. Side effects may be minimized by slow titration.
Donepezil (Aricept®) is started at 5 mg every night for four weeks and then titrated up to 10 mg every night. It is well tolerated and available as a pill and an orally disintegrating tablet. Donepezil is also available as a weekly patch. It is approved for mild, moderate, and severe dementia.
Donepezil also comes as a 23 mg dose, approved for those with moderate to severe Alzheimer’s disease who have been on donepezil 10 mg for at least three months. The 23 mg per day dose is no more effective than the 10 mg dose, but the 10 mg dose is more effective than the 5 mg dose (Birks, 2018). Side effects and withdrawal rates are more pronounced in those taking higher doses. Common side effects of donepezil include nausea, vomiting, and diarrhea. Bradycardia can arise and may slow the heart rate to a point associated with syncope (Huang, 2023).
Rivastigmine (Exelon®) is approved for mild to moderate dementia and Parkinson’s disease dementia. Common side effects include headache, nausea, vomiting, anorexia, and weight loss. Rivastigmine should be taken with food to reduce GI side effects. Rivastigmine also comes in a patch form associated with less nausea and vomiting. The patch is available in three doses: 4.6 mg/24 hours, 9.5 mg/24 hours, and 13.3 mg/24 hours.
Galantamine (Razadyne®) is used in mild to moderate Alzheimer’s dementia. It is dosed twice daily in the standard form and once daily in the extended-release form. Side effects include anorexia, weight loss, nausea, vomiting, and diarrhea.
Memantine (Namenda®) is the only NMDA receptor antagonist and is approved for moderate-to-severe dementia. Side effects include dizziness, confusion, headache, cough, and constipation. Like cholinesterase inhibitors, the side effects are minimized when the dose is titrated.
Memantine may aid in treating dementia partly through its ability to help control behavior issues, as it has been shown to manage agitation and aggression (Ford & Almeida, 2017). Combining memantine and a cholinesterase inhibitor may have extra benefits when combined (Huang, 2023).
Two newer drugs to treat Alzheimer’s disease, called anti-amyloid antibody agents, target amyloid plaques, which are thought to play a central role in Alzheimer’s disease. Both are given through intravenous infusion. Aducanumab (Aduhelm®) was approved by the FDA in 2021, and it is intended for early Alzheimer’s disease and works by reducing amyloid plaques in the brain. Aducanumab is designed to target and reduce amyloid-beta plaques, which are abnormal protein deposits in the brain associated with Alzheimer’s disease. These plaques are thought to contribute to the neurodegenerative process seen in Alzheimer’s. By binding to aggregated forms of amyloid-beta, Aducanumab promotes their clearance from the brain through microglial-mediated phagocytosis.
Lecanemab (Leqembi®) was approved by the FDA in 2023, and it also targets amyloid plaques and is intended for early stages of the disease. Lecanemab is designed to target and reduce soluble amyloid-beta protofibrils, which are considered toxic intermediates in forming amyloid plaques. Lecanemab facilitates their clearance from the brain by binding to these protofibrils, potentially altering the disease’s progression.
Attention deficit hyperactivity disorder (ADHD) results in many problems for children and adolescents. They have problems with impulse control, paying attention, and being overactive. In addition to the symptoms above, those with ADHD tend to forget or lose things, talk excessively, take unnecessary risks, have trouble taking turns, daydream excessively, fidget, and do not get along well with others. While many people will have features of ADHD from time to time, those with ADHD have severe symptoms that cause difficulty in their lives.
ADHD is a condition of distractibility and inattention. It may or may not be associated with hyperactivity. It is the most common neuropsychiatric disorder in childhood and adolescence, and many of these cases persist into adulthood (CDC, n.d.). The pathology of ADHD is unknown, but it is theorized that certain brain parts are linked to attention lack in neural transmission. ADHD is present in 3-7 percent of school-aged children and is more common in boys than in girls, but the inattentive type is more common in girls. Those with ADHD are at increased risk of having substance abuse problems. In adults, its prevalence is estimated at 6.76% (Song et al., 2021).
While the exact etiology is unknown, it is known that genetics plays a significant role. Other potential causes include low birth weight, alcohol and tobacco use during pregnancy, brain injury, exposure to lead, and premature delivery (CDC, n.d.).
There are three types of ADHD:
The inattention type must have at least six symptoms (at least five symptoms if an adolescent is 17 years old or older) of inattention persisting for at least six months to the point that it is maladaptive and inconsistent with the developmental level (American Psychological Association [APA], 2013). These include difficulty maintaining attention in play or tasks, forgetful in daily activities, avoiding tasks/strongly disliking tasks that require mental effort, being easily distracted, losing items necessary for tasks or activities, not seeming to listen, having difficulty organizing tasks and activities, failing to pay close attention to details or makes careless mistakes and does not follow through on instructions.
The hyperactive/impulsive type must have at least six of the following symptoms (at least five if an adolescent is 17 years old or older) for at least six months to the point that it is maladaptive and inconsistent with the developmental level (APA, 2013). These include hyperactivity with difficulty playing or engaging in leisure activities quietly; fidgeting with feet and hands or squirming in the seat; running around, climbing excessively when it is inappropriate; impulsive with blurting out answers to questions before the question being asked; difficulty waiting in line or waiting for their turn in a group situation; and leaving the seat when the individual is expected to remain sitting.
Other features include being present before the age of 12; symptoms present in two or more situations (e.g., work, home, or school); these symptoms cause significant distress or impairment in academic, occupational, or social functioning; and another mental illness does not better explain symptoms (APA, 2013).
The first-line treatment in children aged 4-5 should include parent training in behavioral management and behavioral classroom interventions. Methylphenidate can be used if behavior interventions do not provide significant clinical improvement and the child still has significant problems (Wolraich et al., 2019).
Considering current medical data, children aged 4-5 should only be given drugs when they have moderate to severe disease. No drugs are FDA-approved to treat ADHD in the child below 6, but the American Academy of Pediatrics recommends using stimulants if needed in those 4-5 years old. The criteria for moderate-to-severe disease include symptoms at least nine months, symptoms not controlled by behavioral therapy, and symptoms seen in the home and other settings (Wolraich et al., 2019).
There are concerns regarding drug treatment in the preschool child, including a lack of data on long-term effects. Research suggests that methylphenidate is metabolized slower in those under six years old, and therefore, the dose should be started low and titrated slowly (Wolraich et al., 2019). Other than methylphenidate, no drug has adequate research backing on safety and effectiveness in those under six years old (Wolraich et al., 2019).
In children between 6-12 years old, the use of stimulants has shown good effectiveness. Non-stimulant drugs that are effective but not as effective as stimulants include atomoxetine, extended-release guanfacine, and extended-release clonidine (Nazarova et al., 2022).
Combining treatment modalities work best for those between 6-18 years old. Drugs should be FDA-approved. The school should be included in the treatment plan. Schools often implement an individualized education program as part of the plan to manage ADHD (Wolraich et al., 2019).
For those 12 to 18, using FDA-approved drugs for ADHD is strongly recommended in combination with behavioral interventions (Wolraich et al., 2019). When the drug is used, the prescriber needs to adjust the drug dose to manage symptoms while minimizing side effects optimally. In adolescents, the patient should be involved in the decision to use the drug. A list of FDA-approved drugs for ADHD is available here.
Treatment with stimulants for ADHD constitutes the best first-line treatment (Nazarova et al., 2022). Stimulants have similar effectiveness but different dosing, duration of action, and side effects. The dose should be started low and titrated upwards while monitoring for symptoms.
Stimulants come in an immediate-release formulation, typically dosed every 4-6 hours, and longer-acting formulations, typically dosed once daily. Dosing should not be done close to bedtime, as this may lead to sleep impairment. Common side effects of stimulants include insomnia, headaches, depression, irritability, weight loss, and poor appetite. There is also concern that they may lead to substance abuse, but recent studies have shown no link between stimulant therapy and future substance abuse (Volkow & Swanson, 2008).
Multiple formulations of stimulants exist for managing ADHD (See tables below). Short-acting stimulants have a longer history of safety and a lot of data efficacy, but they must be taken multiple times daily. The long-acting stimulants are only dosed once a day but are more expensive and have side effects that last into the evening.
Methylphenidate is available as a transdermal patch, Daytrana®, which is placed on for 9 hours and off for 15 hours daily. The patch should be applied two hours before the effect is needed, and the patch may be removed when the effects are no longer needed. The effect lasts about 2-3 hours after the patch is removed.
Stimulants are sometimes abused. They can be used to stay awake or improve cognitive performance. They may also be used to get high. Some individuals will crush the tablets and snort or inject them.
Methylphenidate
Methylphenidate is a Schedule II stimulant approved for ADHD in those six and older (Farzam et al., 2023). Methylphenidate has multiple interactions; always check all other drugs before prescribing methylphenidate. Compliance is an issue; therefore, long-acting (once-a-day) drugs are better at improving compliance. This drug’s exact mechanism of action is unknown, but it may work by stimulating the central nervous system (CNS), stimulating the cerebral cortex, and blocking the reuptake of norepinephrine and dopamine.
Methylphenidate comes in multiple formulations (see table below for dosing). The medication, particularly the short-acting formulation, has the potential to be chronically abused and should be used carefully in those with a history of drug dependence. Methylphenidate is contraindicated in those with glaucoma, hypersensitivity to the drug; marked agitation, anxiety, or tension; those with a family history of Tourette syndrome or motor tics; and within two weeks of taking an MAOI. It should be used carefully in those with hypertension, bipolar disease, psychosis, and seizures. Potential side effects include headaches, nausea, seizures, increased blood pressure, increased heart rate, arrhythmias, anxiety, angina, fatigue, anger, irritability, rash, constipation, cough, blurred vision, and priapism.
Dexmethylphenidate
Dexmethylphenidate is dosed as an immediate and an extended-release formulation. This drug acts as a stimulant and blocks the reuptake of dopamine and norepinephrine. The immediate-release tablet is dosed with 2.5 mg twice daily and increased weekly by 2.5 to 5 mg increments with a maximum dose of 20 mg daily. The extended-release formulation is dosed with 5-10 mg daily and increased to 30 mg in children and 40 mg in adults.
Common side effects of dexmethylphenidate include headache, insomnia, abdominal pain, anxiety, and restlessness. Other side effects include poor appetite, dizziness, nausea, sore throat, irritability, dyspepsia, blurred vision, and priapism. This drug is contraindicated in those with hypersensitivity to dexmethylphenidate, those with Tourette syndrome, motor tics, significant agitation, glaucoma, or anxiety. It should not be used within 14 days of taking an MAOI. It should be used carefully in those with a history of drug dependence, bipolar disease, hypertension, or any structural cardiac abnormalities.
Non-Stimulant Drugs
Non-stimulant drugs that are effective for ADHD but not as effective as stimulants include atomoxetine (Strattera®), extended-release guanfacine (Intuniv®), and extended-release clonidine (Kapvay®) (Wolraich et al., 2019).
Atomoxetine is a second-line agent for ADHD and has a delayed onset of therapeutic action. It is a norepinephrine reuptake inhibitor. It may take up to four weeks before effectiveness is noted. When switching from stimulants to atomoxetine, both drugs are given to allow atomoxetine time to demonstrate effectiveness. It is approved for children and adults and is often used by those with a history of substance abuse. Atomoxetine is well tolerated; side effects may include slight heart rate/blood pressure increases. Other common side effects include headache, drowsiness, insomnia, sweating, dry mouth, anorexia, abdominal pain, nausea, constipation, and erectile dysfunction.
Extended-release guanfacine and extended-release clonidine are classified as alpha-2-adrenergic agonists. They are used in children when using stimulants or when atomoxetine is not effective, has significant side effects, or co-morbid conditions exist. Guanfacine or clonidine is sometimes used with stimulants as adjunctive therapy (Wolraich et al., 2019).
Research has shown effectiveness in non-stimulant options, but the effectiveness is not as robust as those with stimulants (Roh & Kim, 2021). Non-stimulants are not approved for adults. The effectiveness of clonidine may be due to its sedating effects, reducing agitation.
Common side effects of guanfacine include drowsiness, fatigue, dizziness, headache, abdominal pain, and anorexia. Common side effects of clonidine include drowsiness, fatigue, dizziness, headache, dry mouth, abdominal pain, rash, and low blood pressure.
Drugs | Starting Dose | Titration | Usual dosage |
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Methylphenidate | |||
Short-Acting (Ritalin®, Methylin®) | 5 mg two times a day before breakfast and lunch | Increased 5 or 10 mg weekly | 40 to 60 mg per day divided two or three times |
Long-Acting | |||
Metadate® CD and Quillivant® XR | 10 or 20 mg each morning | Increase 10 or 20 mg weekly | 40 to 60 mg once each morning |
Ritalin® LA | 10 or 20 mg each morning | Increase 10 mg weekly | 40 to 60 mg once per morning |
Concerta® | 18 or 36 mg per morning | Increase 18 mg weekly | 54 to 72 mg each morning |
Dexmethylphenidate | |||
Focalin® | 2.5 mg two times a day | Increase 2.5-5 mg weekly | 10-20 mg a day |
Focalin® XR | 10 mg each morning | Increase 10 mg weekly | 20-40 mg a day |
Dextroamphetamine and amphetamine (mixed salts) | |||
Short-acting – Adderall® | 10 mg one time a day | Increase 5-10 mg weekly | 5 to 60 mg a day in 1 to 3 divided doses |
Long-acting – Adderall® XR | 20 mg each morning | Increase 10 mg weekly | 5 to 60 mg each morning |
Other | |||
Lisdexamfetamine (Vyvanse®) | 30 mg each morning | Increase 10-20 mg weekly | 30 to 70 mg each morning |
Drugs | Starting Dose | Titration | Maximum Dose |
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Methylphenidate | |||
Short-acting (Ritalin®, Methylin®) | 2.5 to 5 mg before breakfast and lunch if less than 25 kg – 2.5 mg per day | Increase 5-10 mg weekly | 60 mg |
Long-acting | |||
Metadate® CD and QuilliVant® XR | 20 mg per morning | Increase 10-20 mg weekly | 60 mg |
Ritalin® LA | 10 or 20 mg each morning | Increase 10 mg weekly | 60 mg |
Daytrana® transdermal patch (on for 9 hours and off for 15 hours each day Apply patch two hours before needed onset) | 10 mg once daily | Increase the next transdermal dose each week | 30 mg |
Concerta® | 18 mg per morning | Increase 18 mg each week |
|
Dexmethylphenidate | |||
Focalin® | 2.5 mg two times each day (at least 4 hours apart) | Increase 2.5 to 5 per week | 20 mg |
Focalin® XR | 5 mg per morning | Increase 5 mg per week | 30 mg |
Dextroamphetamine | |||
Short-acting | 2.5-5 mg one or two times a day | Increase 2.5-5 mg each week | 40 mg |
Long-acting Dexedrine® Spansule | 5 mg once or twice a day | Increase 5 mg each week | 40 mg |
Dextroamphetamine and amphetamine (mixed salts) | |||
Short-acting – Adderall® | 2.5 – 5 mg one or two times a day | Increase by 2.5 – 5 mg each week | 40 mg |
Long-acting – Adderall® XR | 5-10 mg each morning | Increase 5-10 mg weekly, may be increased by 20 mg in those over 13 years old | 20-30 mg |
Other | |||
Lisdexamfetamine -Vyvanse® | 20-30 mg | Increase 10 or 20 mg each week | 70 mg |
Drug | Starting dose | Titrations | Usual Dose |
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Non-Stimulant Drugs for Adults for ADHD | |||
Strattera® (atomoxetine) | 40 mg once a day | Increased after at least three days to 80 mg once daily or divided twice a day |
|
Non-Stimulant Drugs for Pediatrics for ADHD | |||
Intuniv® (guanfacine, extended-release) |
|
| Target dose-based effect vs. adverse effects |
Strattera® (atomoxetine) | Greater than 6 years and ≤ 70 kg: 0.5 mg/kg once/day |
| Target dose-based effect vs. adverse effects |
Kapvay® (clonidine, extended-release) |
|
|
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(Northwell Health System, n.d.) |
Sam is an eight-year-old male who is in second grade. He has no known medical or surgical history. His parents are generally healthy, but his mother was diagnosed with ADHD as a child and depression and anxiety as an adult. His parents describe him as a “normal” child who spends time with friends, playing video games, and playing soccer. He enjoys social events and is often invited to friends’ houses for playdates.
Sam interacts well with his friends but is easily influenced by others. He has made some poor decisions when with friends, such as staying out too late and vandalizing some property in the neighborhood. Sam gets upset when he does not receive the attention that he wants.
He does fair academically and gets mostly C’s. At the last teacher conference, the teacher reported that he sometimes engages in attention-seeking behavior and has difficulty maintaining attention. Also, she said that he often interrupts other students when answering questions in class. His teacher also reports that he does not listen to instructions but interacts with his peers well.
When Sam is interviewed, he admits to having difficulty focusing on “boring things” but can focus well when it interests him, like video games. He admits that school is boring and reports that he has a difficult time focusing at school. He reports poor sleep, both in falling asleep and waking up in the middle of the night with difficulty getting back to sleep.
Sam’s parents report that he is a very active child and only sits still when playing video games. He often needs to be reminded to stay on task. At home, his parents report that he has problems following instructions. His parents also report that he is very emotional, getting upset and crying easily. Other behavioral concerns include lying, arguing, and aggression.
Sam is diagnosed with ADHD of the hyperactive/impulsive type. He is treated with a combination of drug and behavioral treatments. The consultant psychologist manages the behavioral treatments in combination with the school psychologist. Strategies implemented include counseling, behavioral parent training, and behavioral classroom management.
The drug of choice in a patient over six is a stimulant that is the most effective. While stimulants have similar efficacy, choosing the most appropriate one depends on the side effect profile and the duration of action. Starting the lowest dose and increasing slowly while assessing the effectiveness and adverse effects is recommended.
Sam’s physician chose dexmethylphenidate extended-release because he felt that dosing was optimal once a day. Dexmethylphenidate extended-release was started at 10 mg each morning with reevaluation in one week; at this point, the dose was increased to 20 mg. The next week’s symptoms were reasonably well controlled with minimal side effects (he reported some appetite reduction and an occasional mild headache). Over the next year, he was assessed regularly by a school psychologist, an outside psychologist, and his primary care provider. His symptoms improved significantly, and his grades improved to all A’s and B’s with fewer behavior problems.
Globally, approximately one billion individuals have hypertension, which makes up about 25% of the adult population (World Health Organization [WHO], 2023). Drugs are used when lifestyle modifications do not control blood pressure. Multiple drug classes are available to control blood pressure. Each medicine has a unique mechanism of action, and individuals will respond differently to different drug classes.
Four classes of medicine are recommended as initial therapy for hypertension:
Diuretics are equivalent to other antihypertensive drugs as a first-line drug in treating high blood pressure (ALLHAT, 2002). Diuretics help the body excrete excess fluid and lower peripheral vascular resistance. Classes of diuretics commonly used to treat hypertension include loop diuretics, thiazide diuretics, and potassium-sparing diuretics. Each type works at a different site within the kidney. Although these drugs are widely used and cost-effective, care should be taken with special populations such as older adults. Diuretics are particularly helpful in those with diabetes, congestive heart failure, at high risk for CVD, and in preventing a second stroke.
Common interactions include:
Thiazide diuretics, hydrochlorothiazide, chlorthalidone, and indapamide are commonly used as first-line blood pressure drugs. They are effective at managing blood pressure in those with normal renal function.
Loop diuretics, including – furosemide (Lasix®), torsemide (Demadex®), and bumetanide (Bumex®) – are more useful in those with renal dysfunction, do not respond to thiazide diuretics or those who need a drug that more robustly off-loads fluid.
Aldosterone antagonists are also used in those with chronic heart failure. The two major drugs in this class are (Spironolactone®) and eplerenone (Inspra®).
Potassium-sparing diuretics are often combined with other diuretics to offset the hypokalemic effects of those drugs. Triamterene (Dyazide®) is a common drug in this class.
Thiazide diuretics are recommended as first-line drugs in uncomplicated hypertension and part of the combination in controlling those with blood pressure more than 20/10 mm Hg over the goal (Chobanian et al., 2003). Diuretics should also be considered in those with a history of stroke, heart disease, heart failure, and diabetes.
Thiazide diuretics are more effective than CCBs in those with heart failure and angina and better than ACE-I in CVD and stroke, but no overall mortality benefit was shown (ALLHAT, 2002).
Class of Diuretic | Site of Action | Examples | Notes |
---|---|---|---|
Loop | Ascending limb of the loop or Henle | Furosemide, bumetanide, Torsemide | Most powerful |
Thiazide and thiazide-like | Distal convoluted tubule | Bendroflumethiazide, indapamide, metolazone, chlortalidone | Preferred for hypertension |
Potassium-sparing | Collecting tubules; blocks the loss of potassium | Spironolactone, Eplerenone, Amiloride, Triamterene | Some inhibit aldosterone: slower acting but effects last longer |
(Arumugham & Shahin, 2023) |
Nursing Considerations
ACE-Is include agents such as quinapril (Accupril®), captopril (Capoten®), benazepril (Lotensin®), and ramipril (Altace®). Angiotensin II is a hormone that constricts blood vessels and raises blood pressure. ACE-Is prevent the conversion of angiotensin I to angiotensin II and, in so doing, drop blood pressure. Angiotensin II also elevates blood pressure by contributing to water and sodium retention (Alcocer et al., 2023).
ACE-Is can be used as a first-line agent, particularly in patients with heart failure, diabetes, proteinuria, peripheral vascular disease, cerebral vascular disease, and diabetic nephropathy. Common side effects include hypotension (especially in those on diuretics or those who are dehydrated), dizziness, dry hacking cough, hyperkalemia, headache, and nausea. Infrequently, angioedema happens, but this can be severe, so monitor patients carefully during the first few doses. ACE-Is can worsen kidney function, so blood urea nitrogen (BUN), creatinine, and potassium levels should be monitored while on ACE-Is.
ARBs include the drugs candesartan (Atacand®), losartan (Cozaar®), and valsartan (Diovan®). They work by dilating blood vessels and lowering blood pressure.
Hyperkalemia, dizziness, headache, fatigue, and angioedema are side effects associated with ARBs. This drug has similar indications and works through a similar mechanism to ACE-Is and is often substituted in those who cannot tolerate ACE-Is secondary to a dry hacking cough (Alcocer et al., 2023).
Nursing Considerations with ACE-Is and ARBs:
CCBs result in vasodilation and lower blood pressure. Non-dihydropyridine and dihydropyridines are two broad categories that make up CCBs. Verapamil (Calan®) and diltiazem (Cardizem®) are the primary non-dihydropyridines. Amlodipine (Norvasc®), felodipine (Plendil®), nicardipine (Cardene®), and nifedipine (Procardia®) are examples of dihydropyridines. The non-dihydropyridines have negative chronotropic and ionotropic actions and should be used with extreme caution in those with heart failure or those on beta-blockers. The dihydropyridines may result in vasodilatation and may lead to reflex tachycardia.
Common side effects of this class include low blood pressure, edema, constipation, headache, dizziness, fatigue, nausea, and heart rate changes.
CCBs have multiple drug interactions. Interactions can occur with beta-blockers since they both interfere with the AV node, resulting in bradycardia, heart block, and asystole. Verapamil and diltiazem inhibit the metabolism of statins (especially simvastatin and atorvastatin), thereby increasing the risk of statin-induced myopathy and rhabdomyolysis. Many CCBs (especially dihydropyridines) are metabolized by the cytochrome P450 3A4 (CYP3A4) enzyme and, when given with inhibitors (e.g., ketoconazole, erythromycin, grapefruit juice), may result in increased levels of CCBs, leading to enhanced effects and side effects. When given with inducers (e.g., rifampin, carbamazepine), there may be decreased levels of CCBs, reducing their efficacy.
Nursing Considerations
Beta-blockers regulate blood pressure by affecting the heart’s response to epinephrine and norepinephrine, reducing heart rate and cardiac output, and lowering blood pressure (Khalil & Zeltser, 2023). Also, beta-blockers lower renin release and tend to be most effective in lowering blood pressure in those with elevated renin levels, especially younger individuals.
Adverse reactions include bradycardia, angina, syncope, heart failure, arrhythmias, fluid retention, peripheral edema, nausea, vomiting, diarrhea, and difficulty breathing due to bronchiole constriction.
Beta-blockers are often used in those with hypertension and co-morbid conditions such as heart failure, diabetes, tachyarrhythmia, coronary heart disease, or migraine. Beta-blockers may mask hypoglycemia, so use caution with beta-blockers in those with diabetes who are on agents that lower blood sugar (e.g., insulin). Beta-blockers can potentially worsen depression, peripheral vascular disease, asthma, and chronic obstructive pulmonary disease.
Commonly used beta-blockers include atenolol (Tenormin®), metoprolol (Lopressor®), nadolol (Corgard®), and propranolol (Inderal®).
It is important to note that several drugs interact with beta-blockers:
Nursing Considerations
Other drugs available to manage blood pressure include (Khalil & Zeltser, 2023):
Antianginal drugs are medications used to treat angina pectoris, a symptom of ischemic heart disease characterized by chest pain due to reduced blood flow to the heart muscle (Rousan & Thadani, 2019). These drugs improve the balance between oxygen supply and demand in the myocardium, alleviate symptoms, and prevent angina attacks. They reduce systolic, diastolic, and mean arterial blood pressures and improve coronary circulation at therapeutic doses.
Nitrates relax and dilate blood vessels, primarily veins, reducing preload and myocardial oxygen demand. They also dilate coronary arteries, increasing blood flow to the heart muscle and are typically used for acute angina as they have a rapid onset. Side effects are headaches, dizziness, orthostatic hypotension, flushing, and palpitations. Drugs in this class are isosorbide dinitrate, isosorbide mononitrate, and nitroglycerin. Nitrates are given sublingually, as a patch, as a pill, or as an aerosol.
Beta-adrenergic blockers are used for the long-term prevention of angina. These include atenolol, metoprolol, nadolol, and propranolol. These drugs reduce oxygen demand as they cause a decrease in heart rate and reduce the contraction force.
CCBs include amlodipine, diltiazem, nifedipine, and verapamil. These drugs block calcium ions from entering the cell membrane and smooth muscle cells, causing peripheral and coronary artery dilation. This drug decreases the contraction force of the heart and decreases afterload, increasing the oxygen supply.
Nursing Considerations and Patient Education:
Antiarrhythmic drugs treat disturbances in normal heart rhythms by altering the conductivity and automaticity of the cells (Barton et al., 2020). All cardiac cells can generate excitatory impulses, affecting the heart’s contractility and cardiac output. Careful monitoring must be observed as these drugs can worsen conditions in the heart. There are four classes of antiarrhythmics. The desired endpoint of this therapy includes eliminating the dysrhythmias, controlling the heart rate, and preventing the dysrhythmias from returning. Monitoring EKGs and the heart rate are integral to the therapy.
Common adverse effects are syncope, vision change, dizziness, drowsiness, hypotension, nausea, vomiting, diarrhea, respiratory depression, hair loss, rash, and bone marrow suppression. Symptoms of overdosage are hypokalemia, seizures, and tachydysrhythmias.
This class includes quinidine, disopyramide phosphate (Norpace®), and procainamide hydrochloride (Pronestyl®). These drugs are quickly absorbed and metabolized. There are extended-release versions to prolong their effects. Quinidine does cross the blood-brain barrier. All are metabolized by the liver and excreted through the kidneys. Class 1A antiarrhythmics block sodium and potassium channels, thereby slowing the depolarization and prolonging the repolarization phases of the cardiac action potential. These effects stabilize the cardiac electrical activity but require careful monitoring due to the risk of inducing other arrhythmias.
This class of drugs includes mexiletine (Mexitil®) and lidocaine, which primarily target sodium channels in ischemic or depolarized cardiac tissues, slightly shortening the action potential and refractory period. They have minimal impact on the QT interval, making them safer with a lower risk of proarrhythmic effects like torsades de pointes. This characteristic makes them particularly useful in managing ventricular arrhythmias, especially in the context of ischemic heart disease. Side effects seen with this class of drugs are drowsiness, light-headedness, hypotension, and bradycardia. Side effects particular to mexiletine are AV block, confusion, ataxia, double vision, nausea, vomiting, and tremors. Lidocaine can cause seizures as well as respiratory and cardiac arrest (Barton et al., 2020).
Class 1C antiarrhythmics are used to treat severe, resistant ventricular arrhythmias. Drugs include flecainide acetate (Tambocor®) and propafenone (Rythmol®). These medications are potent sodium channel blockers for managing atrial and ventricular arrhythmias. They significantly slow conduction through the heart without notably affecting repolarization, making them effective but also carrying a risk of proarrhythmia, especially in patients with structural heart disease. Careful patient selection and monitoring are essential when using these drugs. Side effects include the development of new arrhythmias, aggravation of current arrhythmia, palpitations, shortness of breath, chest pain, heart failure, and cardiac arrest (Barton et al., 2020).
Class II antiarrhythmics are beta-adrenergic blockers. These drugs block beta-adrenergic receptors in the conduction system of the heart. This drug slows the firing of the SA Node and the AV Node, which decreases conductivity. These drugs also reduce the strength of the contractions, so less force is needed with each beat, and therefore, less oxygen is required. Class II drugs are used for atrial flutter, atrial fibrillation, and paroxysmal atrial tachycardia. Drugs include propranolol, metoprolol, and atenolol. Side effects include arrhythmia, bradycardia, heart failure, hypotension, GI reactions, bronchoconstriction, and fatigue (Barton et al., 2020).
Class III drugs treat atrial and ventricular arrhythmias. Class III antiarrhythmics primarily block the potassium channels responsible for phase 3 repolarization in the cardiac action potential. By inhibiting these potassium channels, these drugs slow down the efflux of potassium ions out of the cardiac cells. This prolongs the duration of the action potential (the time during which the cell is electrically active) and extends the refractory period (when the cell cannot be re-excited). This drug delays repolarization and increases action potential time in the effective refractory period.
Drugs in this class are amiodarone (Cordarone®), sotalol (Betapace®), and ibutilide (Corvert®). These drugs are particularly useful in patients with atrial fibrillation, atrial flutter, and ventricular arrhythmias. Still, they should be used with caution in those with underlying structural heart disease or a predisposition to prolonged QT interval. Side effects include aggravation of current arrhythmia, hypotension, bradycardia, nausea, and anorexia. Amiodarone can cause pulmonary toxicity, thyroid dysfunction (hypothyroidism or hyperthyroidism), liver toxicity, skin discoloration, corneal deposits, and photosensitivity (Barton et al., 2020).
Class IV drugs are CCBs used to treat supraventricular arrhythmias. These drugs block calcium ions in cardiac and smooth muscle cells, decreasing contractility. This drug decreases oxygen requirements and dilates coronary arteries and arterioles. Examples of Class IV drugs are verapamil and diltiazem (Barton et al., 2020).
Nursing Considerations and Patient Education:
Cardiac glycosides (digoxin) treat heart failure and some arrhythmias. Digoxin works by inhibiting the Na+/K+-ATPase pump, increasing intracellular calcium levels, and enhancing cardiac contractility. Its effects on the autonomic nervous system help slow the heart rate and improve rhythm control. These actions make it useful in treating heart failure and certain arrhythmias, though careful monitoring is necessary to avoid toxicity.
In heart failure, digoxin (Lanoxin®) has been shown to improve symptoms but does not improve survival (David & Shetty, 2023). It works by increasing the strength of heart muscle contractions. It was once a mainstay of treatment for heart failure, but it is used less frequently today. Digoxin can be used in those with systolic heart failure and atrial fibrillation.
In atrial fibrillation and flutter, digoxin can lower ventricular rate when an elevated atrial rate causes it. Digoxin activates vagal efferent nerves, which diminishes the conduction of electrical impulses in the AV node, thereby blocking some impulses. Also, it increases the refractory period in the AV node. Recent evidence suggests that digoxin is associated with an increased mortality rate in individuals with atrial fibrillation, with higher levels more likely to be associated with mortality (Lopes et al., 2018).
Digoxin has a long half-life (40 hours) and takes multiple days to reach a steady state. Digoxin has a narrow therapeutic index with a recommended serum level between 0.8 to 2 ng/mL.
Adverse side effects of cardiac glycosides include dysrhythmias (AV block, atrial tachycardia), anorexia, nausea, vomiting, electrolyte disturbances, bradycardia, and headache. Dysrhythmias are more common when the dose is above the therapeutic window.
Common drug interactions include quinidine, non-steroidal anti-inflammatory agents, CCBs, amiodarone, diuretics, and beta-blockers.
Nursing Consideration and Patient Education
In the United States, heartburn affects approximately 7% of the population daily, and up to 25-40% experience symptomatic gastroesophageal reflux disease (GERD). Heartburn causes a burning sensation that starts in the stomach or lower chest and rises to the throat and neck (Salisbury & Terrell, 2023).
When lifestyle modifications do not sufficiently manage the disease, drugs are used. Using drugs does not mean that lifestyle interventions are stopped when the drug is added – they are used together.
The first-line treatment for GERD is antacids, which are bought over the counter. Common brands include Alka-Seltzer, Maalox, Mylanta, Pepto-Bismol, and Rolaids. Antacids neutralize the acid in the stomach and provide fast, short-term relief. Antacids can be taken as needed or after each meal and bedtime to control stomach acid.
The main side effects of antacids are diarrhea or constipation. Magnesium-based antacids – such as Maalox and Mylanta – cause diarrhea, while aluminum or calcium-containing antacids – such as Rolaids and Tums – lead to constipation. Some antacids are mixed with alginic acid (Gaviscon). Adding alginic acid to an antacid is more effective than an antacid alone but is more expensive. A stronger drug is needed if lifestyle changes and antacids do not help symptoms.
Antacids may interact with other drugs. Some interactions to be aware of include ACE-Is, beta-blockers, levodopa, oral anticoagulants, some antibiotics (quinolones), some anti-diabetic agents, and anticonvulsants (Salisbury & Terrell, 2023).
The next drug to treat GERD controls acid production in the stomach. The drugs cimetidine (Tagamet®), famotidine (Pepcid®), and [prescription only] nizatidine (Axid®) are in a class of drugs called histamine two receptor antagonists (H2RA). Drugs in this class provide similar efficacy to each other. H2RAs block histamine from binding to the histamine two receptors on the parietal cell, leading to a decreased amount of acid production. Long-term use is not recommended because tolerance can develop. H2RA's have a slower onset of action than antacids but works longer. As opposed to antacids, H2RA's can potentially stop heartburn before it starts.
PPIs have increased efficacy in treating GERD compared to H2RA's, with individual PPIs being equally effective. The PPIs provide a slower onset of relief when compared to the H2RA's. It may take 1-4 days to notice complete relief with PPIs. PPIs have multiple indications. Treatment of GERD or GERD symptoms is a common indication in all PPIs. Other indications of PPIs include treatment of duodenal and gastric ulcers, treatment of erosive esophagitis, and treatment of Zollinger-Ellison syndrome.
Selected drug interactions for PPIs include some HIV drugs, bisphosphonates, cefuroxime (reduces absorption), clopidogrel (diminishes anti-platelet effect), citalopram, iron (decreases absorption), methotrexate (increases serum concentration) and phenytoin.
Less commonly, metoclopramide (Reglan®) is used to treat GERD. Metoclopramide increases the speed at which food goes through the digestive tract, but this drug has many side effects that limit its usefulness.
Acetaminophen is a very common over-the-counter drug used in the management of pain. It was previously recommended as a primary agent in managing hip and knee osteoarthritis. Recently, many trials found it only slightly better than placebo with minimal clinically important differences (Pradelli et al., 2021).
Acetaminophen is dosed 325 to 650 mg every four hours or 500-1000 mg every 6 hours, not exceeding 3000 to 3250 mg daily. In the pediatric population, acetaminophen is dosed at 10-15 mg/kg/dose every 4-6 hours with a maximum of 75 mg/kg/day, but no more than 3000-4000 mg a day. The dose should be reduced in those with hepatic insufficiency or alcohol abuse. Absolute contraindication to acetaminophen is liver failure, while relative contraindications include chronic alcohol abuse or hepatic insufficiency. Those on a statin cholesterol drug may need a lower dose of acetaminophen.
NSAIDs manage acute and chronic painful and inflammatory conditions. Short-to-moderate acting agents, including ibuprofen or naproxen, are the preferred agents in this class. NSAIDs are used for anti-inflammatory, analgesic, and antipyretic effects.
There are over 20 different types of NSAIDs, and individual patients have different responses to different NSAIDs. NSAIDs work by inhibiting the cyclooxygenase (COX) enzyme. NSAIDs inhibit two major isoforms of the enzyme (COX-1 and COX-2). Many genes affect COX-1 and COX-2 metabolism, which may explain some variations in response to the drug.
Most NSAIDs are equally effective, but if one agent is ineffective, it may be reasonable to try a different NSAID, as there is individual variation in response to different drugs.
Absolute contraindications to NSAIDs include an active peptic ulcer, chronic kidney disease, or heart failure. Relative contraindications include a history of peptic ulcer disease, Helicobacter pylori infection, hypertension, or concomitant use of selective serotonin receptor inhibitors or corticosteroids (Wongrakpanich et al., 2018).
Side effects of NSAIDs include gastrointestinal bleeding, renal insults, adverse cardiovascular effects, headaches, constipation, and mental status changes. Gastrointestinal effects may include gastric ulceration and dyspepsia. Taking the drug with food or antacids may reduce the risk of dyspepsia. Those at high risk of gastric ulceration – older age, on corticosteroids, bleeding problems, or a history of gastric ulceration – should likely not use NSAIDs. The use of a PPI reduces the risk of gastric ulceration with the use of NSAIDs.
The use of misoprostol or PPIs may be considered with NSAIDs to reduce the risk of gastrointestinal ulceration. It may be reasonable to use a COX-2 inhibitor in those at high risk for gastrointestinal bleeding. A COX-2 agent and a PPI can be considered in very high-risk patients. In some cases, checking for and eradicating Helicobacter pylori in those when it is present reduces the risk of NSAID-induced gastrointestinal injury.
NSAIDs have the potential to cause nephrotoxicity. NSAIDs inhibit prostaglandin synthesis, which leads to vasoconstriction of the afferent arteriole in the kidney. This vasoconstriction results in a reduction in the glomerular filtration rate. NSAIDs should be used cautiously in those with renal impairment.
NSAIDs may interfere with the antiplatelet activity of aspirin therapy. Chronic NSAID use should be avoided in those on chronic aspirin therapy. They should also be avoided in those with thrombocytopenia (low platelet count). Patients receiving warfarin or heparin should not receive NSAIDs (Wongrakpanich et al., 2018).
Ibuprofen
Naproxen
Diclofenac
Celecoxib
Meloxicam
Indomethacin
Ketorolac
Aspirin
NSAIDs have many interactions. Common interactions include:
The dose of the given NSAID should be started at the lowest effective dose but may be titrated up to the maximal anti-inflammatory range. When the patient has a history of an inadequate response to an NSAID, the healthcare provider should determine if an adequate dose was tried.
Nursing Considerations and Patient Education:
NSAIDs are laced with risks, and some patients are unable to tolerate NSAIDs due to side effects and co-morbid conditions. The risk associated with NSAIDs is one reason many clinicians choose an opioid to manage pain. Opioid therapy effectively manages many chronic conditions, including osteoarthritis, low back pain, neuropathic pain, and postherpetic neuralgia. Nury et al. (2022) evaluated the effectiveness and safety of strong opioids in managing chronic noncancer pain (CNCP) and chronic low back pain (CLBP) and suggested that strong opioids provide modest pain relief and functional improvement in patients with CNCP and CLBP. However, the degree of pain reduction and improvement in function was relatively small, suggesting that while opioids can be effective, the overall benefit may be limited for many patients.
The above study (Nury et al., 2022) highlighted significant safety concerns associated with long-term opioid use. These include a higher risk of adverse effects such as constipation, nausea, dizziness, and increased risk of dependence and overdose. The study emphasized the importance of balancing the potential benefits with these risks. There was limited evidence that opioid use substantially improves the quality of life for patients, which underscores the need for careful consideration when prescribing opioids, particularly for long-term use. The study suggests that non-opioid treatments should be considered and optimized before initiating opioid therapy.
When opioids are used for chronic pain, treatment is typically started with a short-acting drug, and the drug is titrated upwards to control pain while side effects are monitored. After determining the dose of the drug required to provide adequate pain relief with minimal side effects, the drug can be converted to a sustained release form and administered once or twice a day. When a long-acting drug is used, a breakthrough drug can be given.
Opioid naïve | Those who have not had opioids in the last 30 days. |
Opioid tolerant | Someone who has taken 60 mg daily of oral morphine, 30 mg daily of oral oxycodone, or equianalgesic dosages of other opioids for at minimum one week. |
(University of Florida Health, 2012) |
While there are many opioids, morphine is considered by many as a standard comparator for other drugs. Morphine can be given orally, rectally, intravenously, subcutaneously, or intramuscularly (Murphy et al., 2023).
Morphine is used for moderate to severe acute pain and chronic severe pain. It comes in multiple formulations. There is an oral and rectal formulation for acute pain, and it is dosed at 5-30 mg every 4 hours. It is available as a tablet, suppository, and parenteral solution. Morphine also comes in longer-acting formulations, including Kadian® and MS Contin®.
Morphine should not be used in those with a hypersensitivity to morphine, those with toxin-mediated diarrheal disease, and those with severe/acute asthma, paralytic ileus, or severe respiratory depression. The extended-release form should not be used in those with GI obstruction.
The extended-release forms of morphine are not interchangeable. Changing from one drug to another should be done only by those experienced in how to do this. Extreme caution should be used when using a highly concentrated solution so overdoses do not occur.
Given fentanyl’s high potency, careful consideration and close monitoring are essential to ensure safe and effective pain management (Ramos-Matos et al., 2023). Fentanyl is administered through various forms, including intravenous injections, transdermal patches, buccal tablets, sublingual tablets, and lozenges/troches. The transdermal patch is used in opioid-tolerant patients with moderate to severe pain and is often started at 25 mcg per hour and changed every 72 hours.
Fentanyl can be used for multiple reasons, including procedural sedation, general anesthesia, as an adjunct to general and regional anesthesia, and chronic pain management. The transdermal patch is for around-the-clock pain management in those with severe chronic pain. Fentanyl can also be used for cancer pain.
As with most opioids, contraindications include hypersensitivity, toxin-mediated diarrheal disease, and paralytic ileus. It should not be used for those who have severe respiratory disease. The patch form should not be exposed to external heat, as this may increase the absorption of the drug. Also, patients with a fever may notice an increase in the absorption of the drug. The patch should only be applied to intact skin; it contains aluminum and must be removed before an MRI.
Fentanyl has a high potential for abuse and is frequently implicated in overdose deaths due to its potency and availability. It is often mixed with other drugs, leading to unintentional overdoses (Ramos-Matos et al., 2023).
Oxycodone is a schedule II-controlled substance and is available in multiple forms (Sadiq et al., 2024). Immediate release is dosed 5-15 mg every 4-6 hours (lower range for opioid-I patients). The controlled-release tablet is indicated for those requiring around-the-clock pain control. It is dosed with 10 mg every 12 hours to start and titrated carefully. There is also an extended-release capsule (Xtampza® ER), starting at 9 mg every 12 hours. It also comes as an oral concentrate and oral solution. Oxycodone is often combined with other analgesic agents such as acetaminophen, aspirin, and ibuprofen.
Those with a creatinine clearance of less than 60 mL/min should have the dose adjusted as serum concentration of oxycodone will increase in renal insufficiency. Those with hepatic impairment should have doses reduced. The starting dose should be lowered one-third to one-half and slowly titrated.
Oxycodone is contraindicated in those with paralytic ileus, significant respiratory depression, hypercarbia, acute or severe bronchial asthma, and GI obstruction. Caution should be used in those with biliary tract impairment, such as acute pancreatitis, as it may constrict the sphincter of Oddi. It may lead to an elevation of intracranial pressure (ICP) and should be used carefully for those with intracranial lesions, elevated ICP, or a head injury.
Hydrocodone, classified as a Schedule II Controlled Substance in October 2014, is available as a combination pill with a non-narcotic analgesic and by itself in an extended-release form (Cofano et al., 2024). The combination pill has a short-acting version of hydrocodone and is dosed with 2.5 to 10 mg of hydrocodone every 4-6 hours as needed for moderate to severe pain.
Hydrocodone extended-release (Zohydro® ER, Hysingla® ER) is typically dosed at 10 mg every 12 hours in patients. It is used for severe pain requiring around-the-clock dosing of hydrocodone. The dose may be increased every 3-7 days in 10 mg increments. Hysingla® ER is dosed 20 mg once daily while increasing the dose of 10-20 mg every three to five days.
Those with severe hepatic impairment should start at the lowest dose and titrate slowly while monitoring for side effects. Caution should be used with renal impairment as plasma concentration may rise. Contraindications to hydrocodone include paralytic ileus, severe asthma, severe respiratory depression, and hypercarbia.
As of August 18, 2014, the DEA placed tramadol into Schedule IV of the Controlled Substance Act. It is indicated for acute and chronic pain. For those who do not need a rapid onset of pain relief and are affected by side effects, it may be dosed at 25 mg/day and titrated up every three days to 50-100 mg every 4-6 hours to a maximum of 400 mg a day.
Tramadol also comes in an extended-release form, dosed 100 mg once a day, and may be titrated by 100 mg every five days to a maximum dose of 300 mg daily. When prescribing tramadol to older adults, use the lower end of the dosage range and titrate slowly. In those over 75 years old, 300 mg a day should not be exceeded, and utilize extreme caution with the extended-release form.
In those with a creatinine clearance of less than 30 mL/min, only the immediate-release formulation should be used with 25-100 mg split every 12 hours (maximum 200 mg a day). In those with severe liver impairment, the immediate release form should be given at a maximum of 50 mg every 12 hours (Subedi et al., 2019).
Patients may experience withdrawal symptoms from tramadol, including nausea, diarrhea, anxiety, pain, sweating, tremors, and rigors. Extended use of tramadol may lead to dependence, and these drugs should be tapered slowly to reduce the risk of withdrawal symptoms.
Tramadol has been shown to increase the risk of seizures. This risk is increased in those who take serotonin reuptake inhibitors, tricyclic antidepressants, neuroleptics, other opioids, or other drugs that lower the seizure threshold.
Oxymorphone is a potent opioid analgesic used for the management of moderate to severe pain. It is available in immediate-release and extended-release formulations. The dosing of oxymorphone must be individualized based on factors such as the patient’s previous opioid exposure, the severity of pain, and the patient’s overall medical condition.
The initial dose for opioid-naïve patients with immediate-release oxymorphone is 5 to 10 mg every 4 to 6 hours as needed for pain. It is recommended to start at the lower end of the dosing range to minimize the risk of side effects. The initial dose with extended-release oxymorphone is typically 5 mg every 12 hours. It is important to start at a low dose to reduce the risk of respiratory depression and other side effects. Dose adjustments can be made every 3 to 7 days based on the patient’s response and tolerability. Increases should be made cautiously, usually by 25% to 50% of the current dose. Oxymorphone should be taken on an empty stomach, at least 1 hour before or 2 hours after eating, as food can significantly increase the absorption of the drug, leading to higher plasma concentrations and an increased risk of side effects.
The oral form of hydromorphone comes in immediate and extended-release forms. The initial dose for opioid-naïve patients is 1 to 2 mg orally every 4 to 6 hours as needed for pain. Starting at the lower end of the dosing range is recommended to minimize the risk of side effects. The initial dose for the extended-release formulation is generally 8 mg orally every 24 hours. As with immediate-release formulations, starting at a low dose helps reduce the risk of respiratory depression and other side effects. Adjust doses every 3 to 4 days based on the patient’s response and tolerability, usually by 25% to 50%. Consistent administration with regard to meals is recommended to avoid variations in drug absorption. Hydromorphone can be taken with or without food.
Methadone is a synthetic opioid often used for pain management, especially in cases of chronic pain where other pain relievers have been ineffective. Due to its unique pharmacokinetics and pharmacodynamics, methadone dosing for pain requires careful consideration and should be done under the guidance of a healthcare professional experienced in its use. Methadone has a highly variable half-life (ranging from 8 to 59 hours) and can accumulate in the body, making dosing complex. Dosing must be individualized based on factors such as age, liver function, concomitant medications, and opioid tolerance.
The oral dose is started in the opioid-naïve patient at 2.5 mg every 8-12 hours. Methadone is a high-risk drug that may lead to overdose. Dose adjustments should be made gradually, often no more frequently than every 5-7 days, to allow methadone to reach steady-state levels in the body. Methadone may also prolong the QT interval, leading to cardiac arrhythmias, especially at doses higher than 120 mg daily. Methadone should be used for severe pain that has not been responsive to other agents and only by clinicians with specific training in using methadone. Methadone is also used in detoxification and opioid use disorder.
Tapentadol (Nucynta®, Nucynta® ER) is used for acute moderate to severe pain and starts at 50-100 mg every four to six hours for the immediate-release formulation. The starting dose for the extended-release tablet is 50 mg every 12 hours. For chronic pain, it is typically dosed 100-250 mg two times a day as needed. This drug is not recommended for those with severe liver or renal insufficiency. It is also indicated for diabetic peripheral neuropathy.
Nursing Considerations and Patient Education
Ms. L is a 52-year-old female with a history of bilateral knee pain; she currently rates the pain as 8/10 in her right knee and 5/10 in her left knee. She takes meloxicam 7.5 mg daily and uses 1000 mg of acetaminophen three times a day for breakthrough pain. She has been using this treatment for the past six months, but over the last month, she has not been getting adequate relief from her pain, has stopped exercising, and is having trouble getting her pants on due to the pain.
The pain is attributed to osteoarthritis and has progressively worsened over the last 1-2 years. She has a past medical history of hypertension, dyslipidemia, depression, obesity, and osteoarthritis. She has a past surgical history of a hysterectomy approximately five years ago. She is currently on simvastatin, lisinopril, meloxicam, acetaminophen, and aspirin. She has no known allergies.
She has no history of alcohol, drug, or substance abuse. She has a strong family network, including a supportive husband of 25 years and two sons who live within twenty miles of her home. She has a history of depression but is currently not depressed.
The physical exam is significant for obesity (BMI of 34). She has crepitus in both her knees and cannot extend the right knee due to pain. An X-ray demonstrates moderate arthritic changes in both knees. The patient is unwilling to consider the surgery on her knees.
The prescriber offers tramadol immediate-release 25 mg in the morning, which is titrated every three days in 25 mg increments as distinct doses to 100 mg/day (25 mg four times daily). Pain control was still inadequate, and the dose was then increased from 25 mg every three days to 50 mg every 6 hours.
Pain control was significantly improved, and the patient was given tramadol extended-release 200 mg daily. The patient was able to function and exercise. Her quality of life was much improved.
Urinary incontinence (UI) refers to the involuntary leakage of urine. It can range in severity from occasional leakage when coughing or sneezing (stress incontinence) to sudden, strong urges to urinate that result in leakage before reaching the toilet (urge incontinence) or a combination of both. If no improvement in UI is noted after three months of lifestyle and behavioral therapy, pharmacotherapy may be considered (Leslie et al., 2024).
In those with urgency, frequency, and nocturia, options include anticholinergics, antispasmodics (anticholinergic and antispasmodic agents are classified as antimuscarinic agents), and tricyclic antidepressants. Stress incontinence is managed with alpha agonists, estrogen, and tricyclic antidepressants. Switching agents within the class may be tried before disregarding the class of drugs.
Drugs are ideally combined with a pelvic exercise routine. When one drug does not work, combination therapy (e.g., oxybutynin and imipramine) may be tried. A drug trial should be at least 4-6 weeks at the maximum tolerated dose. Side effects may be minimized with extended-release forms and slow titration.
Urgency and mixed incontinence are managed with antimuscarinic agents. Antimuscarinic agents increase bladder capacity and reduce urgency as they block the release of acetylcholine when the bladder is filling. Antimuscarinics reduce involuntary bladder contractions by affecting afferent signaling and blocking the muscarinic cholinergic receptors on the detrusor muscle cell wall. Antimuscarinic agents are generally effective in reducing symptoms of overactive bladder and improving the quality of life for individuals with UI. Still, their use should be carefully considered in light of potential adverse effects and individual patient characteristics.
Drug | Dose | Notes |
---|---|---|
Antimuscarinic Agents | ||
Oxybutynin (Ditropan® XL, Gelnique®, Oxytrol®) | Oral: Immediate release: 2.5 – 5 mg, 2-3 times a day; the maximum dose is 5 mg, four times daily. Extended-release: Start 5-10 mg once a day, and increase the dose by 5 mg weekly to a maximum of 30 mg daily. Transdermal: Apply one 3.9 mg/day patch twice weekly. | The label does not discuss dosage adjustments for renal or liver impairment, so it should be used cautiously in renal and liver insufficiency. |
Darifenacin (Enablex®) | Start at 7.5 mg once daily. If the response is not sufficient, the dosage may be increased to 15 mg once daily for two weeks | Interactions: azole antifungals, erythromycin, isoniazid, protease inhibitors – with these drugs do not exceed 7.5 mg/day. With moderate liver failure, do not exceed 7.5 mg /day; no adjustment with renal insufficiency. |
Fesoterodine (Toviaz®) | Start at 4 mg once daily, may be increased to 8 mg once daily | Interactions: ketoconazole, itraconazole, clarithromycin – with these drugs or with a creatinine clearance of less than 30 mL/minute, use a maximum of 4 mg/day. |
Solifenacin (VESIcare®) | Start oral dosing at 5 mg once a day; may increase to 10 mg a day | When the creatinine clearance is less than 30 mL/minute, the maximum dose is 5 mg/day. |
Tolterodine (Detrol®, Detrol® LA) | Immediate-release tablet: 1-2 mg twice daily Extended-release capsule: 2-4 mg once daily | Dosing adjustment in patients concurrently taking strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir): 1 mg twice daily for immediate release and 2 mg once a day for extended-release Immediate release tablet: creatinine clearance 10-30 mL/minute): 1 mg twice a day; Extended-release capsule: creatinine clearance 10-30 mL/minute: 2 mg once daily creatinine clearance <10 mL/minute: Not recommended Caution with hepatic impairment |
Trospium (Sanctura®, Sanctura® XR) | Immediate-release: 20 mg twice a day Extended-release: 60 mg once a day | In those over 75 years old, a dose of 20 mg once a day with immediate release may be appropriate. Creatinine clearance less than 30 mL/min uses 20 mg of immediate-release once a day at bedtime. |
Other | ||
Mirabegron(Myrbetriq®) | It is indicated for overactive bladder with urge incontinence, urgency, and urinary frequency, and is dosed at 25 mg once a day. The dose may be increased to 50 mg per day. | This drug is classified as a Beta3 agonist. The drug is not recommended for end-stage renal disease and severe hepatic impairment. For those with creatinine clearance between 15-29 mL/min and moderate hepatic impairment, the dose should not exceed 25 mg a day. |
(Rovner & Wein, 2006) |
For individuals who do not respond to treatment after 4-6 weeks at the maximum tolerable dose, switching to another antimuscarinic agent may be considered. Also, the use of mirabegron may be tried.
Those at risk for urinary retention should have their post-void residual checked while on an antimuscarinic agent.
While no drug in the United States is approved for stress incontinence, many drugs are used. Duloxetine is a serotonin and norepinephrine reuptake inhibitor approved for depression but occasionally used for urinary stress incontinence as it stimulates pudendal motor neurons’ alpha-adrenergic and 5-hydroxytryptamine-2 receptors. While duloxetine can help women with stress incontinence, some believe the harms outweigh the benefits (Maund et al., 2017). Common side effects include nausea, dry mouth, and headache. It should not be used in those with chronic liver disease. Topical estrogen treats stress incontinence in those with vaginal atrophy, while oral estrogens may increase UI.
Anticoagulants prevent blood clots, treating and preventing thromboembolic disorders. They include Vitamin K antagonists (e.g., warfarin), direct oral anticoagulants (DOACs) like factor Xa inhibitors (apixaban, rivaroxaban) and direct thrombin inhibitors (dabigatran), and heparins (unfractionated and low molecular weight). Used for conditions like atrial fibrillation, deep vein thrombosis (DVT), and pulmonary embolism (PE), they reduce stroke risk and manage acute coronary syndromes. DOACs are favored for ease of use, requiring no regular monitoring. Risks include bleeding and interactions, managed with specific reversal agents, and careful monitoring in select scenarios (Heestermans et al., 2022).
Anticoagulant drugs’ most common side effect is an increased risk of bleeding. Renal excretion must be considered as these drugs are excreted mostly in the urine. Anticoagulants are used for the following conditions:
Before administering an anticoagulant, coagulation test values are often checked; the tests vary per drug. Below is a chart depicting the most common coagulation tests for the drug prescribed. Note that each facility or laboratory may vary.
Warfarin inhibits vitamin K synthesis, impacting Factors II, VII, IX, and X. At a therapeutic level, warfarin inhibits the ability of the liver to produce vitamin K, which creates a therapeutic effect (Patel et al., 2023b). Although therapeutic ranges may be achieved in 1-2 hours, the full effect is not achieved for 4-5 days until Factor II is depleted. It is important to draw the international normalized ratio (INR) on time and before administering the drug. The INR is one way to determine the dose of the drug, and it is checked regularly until the therapeutic range is achieved. The INR should be monitored closely after starting or changing the dose or a new drug is added.
Warfarin has a black box warning as it can cause major bleeding. Bleeding is more likely to occur during the start of the treatment. It is important to monitor INR carefully and complete a full patient assessment. Warfarin also interacts with several other drugs and foods. Check all drugs for interactions, assess the patient’s diet, and ask about any herbals or vitamins taken.
Use | International Normalization Ratio (INR) Therapeutic Range |
---|---|
Venous thrombosis Pulmonary embolism Prevention of systemic embolism Bioprosthetic valves Acute MI Atrial Fibrillation | 2.0-3.0 |
Mechanical mitral valve and some mechanical aortic valves | 2.5-3.5 |
Warfarin may impact other laboratory tests. | |
---|---|
ALT, AST | Increase |
INR, PT, PTT | Increase |
Theophylline | False decrease |
(Patel et al., 2023b) |
Be sure to assess alcohol intake and vegetable intake, especially vegetables high in vitamin K, such as kale, parsley, collards, spinach, turnip greens, mustard greens, and collard greens.
Heparin is a vital anticoagulant used to prevent and treat thromboembolic disorders by inhibiting clotting factors, particularly thrombin and factor Xa. It comes in two main forms: Unfractionated Heparin (UFH) and Low Molecular Weight Heparins (LMWHs), such as enoxaparin and dalteparin (Qiu et al., 2021).
UFH is administered intravenously or subcutaneously and requires frequent monitoring via activated partial thromboplastin time (aPTT) tests to ensure therapeutic levels. It is used for immediate anticoagulation in conditions like acute coronary syndromes, DVT, PE, and during certain surgeries.
LMWHs, administered subcutaneously, have more predictable pharmacokinetics and usually do not require regular monitoring. They are used for the treatment and prevention of DVT and PE, management of acute coronary syndromes, and as bridging therapy during transitions to or from oral anticoagulants.
Heparin is also employed in dialysis to prevent clotting in the dialysis circuit and as perioperative anticoagulation, particularly in surgeries involving cardiopulmonary bypass or vascular surgery.
Heparin’s rapid action and reversibility make it invaluable in various clinical settings, though its use requires careful monitoring to balance efficacy and safety.
Here is a simplified chart on monitoring heparin.
Parameter | Unfractionated Heparin (UFH) | Low Molecular Weight Heparin (LMWH) |
---|---|---|
Administration | IV or Subcutaneous (SQ) | Subcutaneous (SQ) |
Initial Dose | IV bolus followed by continuous infusion | Weight-based dosing (e.g., enoxaparin 1 mg/kg) |
Monitoring Test | aPTT | Anti-Xa levels (in specific populations) |
Target Range | 1.5-2.5 times the normal aPTT or lab-specific target | 0.5-1.0 IU/mL (therapeutic); 0.2-0.4 IU/mL (prophylactic) |
Frequency of Monitoring |
| Generally not required for most patients Anti-Xa levels in:
|
Adjustments | Based on aPTT results:
| Based on Anti-Xa levels, if monitored |
Risk Factors |
|
|
Reversal Agent | Protamine sulfate | Protamine sulfate (partially effective) |
Considerations for Heparin
Patient Teaching for Heparin
DOACs are a class of medications used to prevent and treat DVTs and PEs and are used in atrial fibrillation.
Common DOACs include:
The mechanism of action is different when compared to warfarin. Apixaban, rivaroxaban, and edoxaban inhibit Factor Xa, preventing the conversion of prothrombin to thrombin. Dabigatran is a direct thrombin inhibitor that inhibits thrombin, preventing the conversion of fibrinogen to fibrin.
Nursing Considerations
Assessment
Administration
Patient Education
Monitoring and Follow-Up
Management of Bleeding
Special Considerations
John Doe is a 55-year-old male with a medical history of hypertension, diabetes, obesity, and a recent knee surgery (3 weeks ago). He currently takes metformin and lisinopril and presented to the emergency department with complaints of swelling, pain, and redness in his left calf, which had worsened over the past two days. John reported no chest pain or shortness of breath.
Assessment and Diagnosis
Treatment Plan
Given the confirmed diagnosis of DVT and his recent surgery, the decision was made to start treatment with a DOAC. Rivaroxaban was chosen for its once-daily dosing and efficacy in treating DVT.
Nursing Care Plan
Education and Counseling
Monitoring and Follow-Up
Diet and Interactions
Outcome and Follow-Up
Reflection and Learning Points
Diabetic pharmacology is a crucial aspect of nursing care for patients with diabetes mellitus, a chronic condition characterized by high blood glucose levels due to insulin resistance, inadequate insulin production, or both. Nurses play a vital role in managing diabetes through medication administration, patient education, monitoring for complications, and promoting adherence to treatment plans.
Sulfonylureas are a class of oral hypoglycemic agents used to manage Type 2 Diabetes Mellitus (T2DM). These drugs function primarily by stimulating the pancreas to release more insulin. They achieve this by binding to and closing the ATP-sensitive potassium channels on pancreatic beta cells, depolarizing the cell membrane and triggering insulin secretion.
Common sulfonylureas include glipizide, glyburide, and glimepiride. These medications are typically used when lifestyle changes and first-line medications, such as metformin, are insufficient in controlling blood glucose levels.
Sulfonylureas effectively lower blood glucose levels and HbA1c by 1-2% (Feingold, 2022). They are usually administered once or twice daily before meals. Their glucose-lowering effects make them a valuable option, especially in patients with relatively preserved pancreatic beta cell function early in the disease course.
The advantages of sulfonylureas include:
Despite their benefits, sulfonylureas have several drawbacks:
Nursing Considerations
Rosiglitazone (Avandia®) and pioglitazone (Actos®) are the two thiazolidinediones (TZDs). TZDs activate peroxisome proliferator-activated receptor-gamma (PPAR-γ) in adipose tissue, muscle, and the liver. This activation increases insulin sensitivity in peripheral tissues, enhances glucose uptake by muscles and adipose tissue, and reduces hepatic glucose production. TZDs lower the HbA1C by 0.4 to 1.4 points when used alone (Feingold, 2022).
These agents have been shown to lower triglyceride levels but may increase LDL cholesterol. They can potentially cause hepatotoxicity, and liver monitoring should occur while on these drugs. Individuals with symptomatic heart failure or New York Heart Association Class III or IV heart failure should not use this class. Other side effects include fluid retention, weight gain, headache, sinusitis, muscle aches, and elevated liver enzymes.
Due to side effects, lack of efficacy, and negative cardiovascular effects, this drug is relegated to a second or third-line agent.
Metformin is an oral antihyperglycemic agent commonly used to manage T2DM. It belongs to the biguanide class of medications and is known for its effectiveness in lowering blood glucose levels without causing significant hypoglycemia (Weinberg Sibony et al., 2023).
Metformin primarily works by decreasing hepatic glucose production, increasing insulin sensitivity in peripheral tissues, particularly muscles, enhancing glucose uptake and utilization by cells, and slightly reducing intestinal glucose absorption.
Metformin and lifestyle changes are recommended for the initial diabetes treatment, assuming no contraindications exist. Metformin significantly improves blood sugar control, has a low risk of hypoglycemia, lacks the side effect of weight gain, and is inexpensive. Metformin lowers HbA1C by 1-2 percentage points and lowers the risk of death and diabetes-related endpoints (Feingold, 2022).
Side effects of metformin include gastrointestinal upset, diarrhea, and weight loss.
Also, metformin should not be used in those with hemodynamic instability, heart failure, liver disease, or alcohol abuse. Those who are to have radiography with an intravenous iodinated contrast agent should have their metformin held. Those who are to have surgery that compromises circulation should have the metformin held until normal circulation and renal blood flow are established.
Acarbose (Precose®) and miglitol (Glyset®) are alpha-glucosidase inhibitors. They block the breakdown of sugar in the stomach, reducing the amount that gets into the blood. The result is a smaller rise in blood glucose after a meal. When regularly used, alpha-glucosidase inhibitors lower HbA1C by 0.5 to 0.8 percent (Feingold, 2022). These drugs should be given 30 minutes before a meal. Common side effects include bloating, gas, and abdominal pain. Alpha-glucosidase inhibitors have fallen out of favor because they are not as effective as other agents, have more side effects, and are expensive.
Meglitinides lower blood sugar by stimulating the pancreas to release insulin. They are short-acting medicines and are taken 30 minutes before eating. Meglitinides are effective at lowering blood sugars after a meal, and when used regularly, they lower HbA1C by 1.0 to 1.5 percent (Feingold, 2022). The drugs in this class include repaglinide (Prandin®) and nateglinide (Starlix®). The side effects include hypoglycemia, weight gain, back pain, flu symptoms, and dizziness.
The liver metabolizes repaglinide; the kidney metabolizes nateglinide. Nateglinide is more likely to result in hypoglycemia in those with chronic renal insufficiency. These drugs are sometimes used in those who cannot tolerate sulfonylureas.
Dipeptidyl peptidase 4 (DPP-4) inhibitors are a class of oral medications used primarily to treat type 2 diabetes. They function by blocking the enzyme DPP-4, which is responsible for the breakdown of incretin hormones. Incretin hormones, such as glucagon-like peptide-1 (GLP-1), play a key role in regulating blood glucose levels by stimulating insulin release and inhibiting glucagon secretion. By preventing the degradation of these hormones, DPP-4 inhibitors help to increase their levels, thereby enhancing their glucose-lowering effects.
Drugs in this class include Saxagliptin, Linagliptin, Alogliptin, and Sitagliptin. They are often combined with other antidiabetic drugs like metformin, sulfonylureas, or insulin for improved glucose control. DPP-4 inhibitors offer a valuable option for managing type 2 diabetes, particularly for patients who may benefit from an oral medication with a low risk of hypoglycemia and no significant impact on weight.
DPP-4 inhibitors are newer drugs, and expense can be a limiting factor in their use.
Common side effects are usually mild, including upper respiratory tract infections, headaches, and gastrointestinal issues. Rare but serious adverse effects may include pancreatitis and severe joint pain. Nurses should monitor patients for signs of pancreatitis (severe abdominal pain) and allergic reactions. Regular blood glucose monitoring is essential to assess the efficacy of the medication. Renal function should be evaluated periodically, as dosing adjustments may be necessary for patients with renal impairment (Weinberg Sibony et al., 2023).
GLP-1 is a hormone involved in regulating glucose metabolism. It is an incretin, a gastrointestinal hormone critical in maintaining blood sugar levels. GLP-1 is secreted by the L-cells in the intestines in response to food intake (Weinberg Sibony et al., 2023).
Some common GLP-1 receptor agonists include:
GLP-1 receptor agonists are primarily used to treat T2DM. They effectively lower blood glucose levels and have additional benefits, including weight loss and potential cardiovascular benefits. Some agents have shown reduced major adverse cardiovascular events in high-risk patients (liraglutide and semaglutide).
Common side effects of GLP-1 receptor agonists include gastrointestinal issues (nausea, vomiting, diarrhea) and hypoglycemia (usually when combined with other glucose-lowering agents like sulfonylureas or insulin). Rare but serious side effects include pancreatitis.
Sodium-glucose co-transporter 2 (SGLT2) inhibitors are a class of oral medications used to manage T2DM. These medications include canagliflozin, dapagliflozin, empagliflozin, and ertugliflozin. SGLT2 inhibitors help lower blood glucose levels by promoting glucose excretion through the urine (Weinberg Sibony et al., 2023).
SGLT2 inhibitors block the SGLT2 protein in the kidneys, which is responsible for reabsorbing glucose back into the bloodstream. By inhibiting this protein, SGLT2 inhibitors prevent glucose reabsorption and increase its excretion in the urine, lowering blood glucose levels.
SGLT2 inhibitors are typically taken once daily, usually in the morning, with or without food. The specific dose varies depending on the particular drug and patient factors such as renal function.
Common side effects include urinary tract infections, genital mycotic infections, increased urination, and dehydration. Rare but serious side effects may include ketoacidosis, acute kidney injury, and an increased risk of lower limb amputations (notably with canagliflozin).
Nursing Considerations:
Patient Education:
Understanding insulin is crucial for nurses who care for patients with diabetes, as insulin plays a central role in managing blood sugar levels. Insulin is a hormone produced by the beta cells of the pancreas. Its primary function is to regulate glucose metabolism by facilitating glucose uptake from the bloodstream into cells, which are used for energy production or stored for future use. Insulin is often added to one of the above medicines to enhance blood glucose control. Insulin has the most potential to lower HbA1C but is associated with the highest risk of hypoglycemia (Donnor & Sarkar, 2023).
Types of Insulin:
Administration:
Nursing Considerations:
Complications and Adverse Effects:
Type Insulin | Onset | Peak | Duration |
---|---|---|---|
Lispro, aspart, glulisine 15 minutes before a meal or immediately after | 3-15 mins | 0.5-1.5 hrs | 2 – 4 hrs |
Regular 30-60 min before meals | 0.5 –1 hr | 2-4 hrs | 5-8 hrs |
NPH | 1-2 hrs | 4-12 hrs | Approx. 12 hrs |
Insulin glargine | 2 hrs | None | 24 or more hrs |
Insulin detemir | 2 hrs | 6-24 hrs | |
Insulin degludec | 2 hrs | None | Up to 41 hrs |
(University of Calirfornia, San Franciso, n.d.) |
Nurses are critical in storing and handling medications correctly to maintain efficacy and safety. Here are some key medications that should not be exposed to light and other special considerations nurses should be aware of:
Medications Sensitive to Light
General Special Storage and Handling Considerations
Practical Tips
By following these guidelines, healthcare providers can help maintain the integrity and effectiveness of medications, ensuring patient safety and therapeutic efficacy. Always consult with a pharmacist or refer to the medication's prescribing information for detailed storage requirements.
Commonly Used Equivalents for Drug Calculations
Accurate drug calculations are essential for safe medication administration. Here are commonly used equivalents that healthcare providers should be familiar with (Open Resources for Nursing et al., 2023b):
Metric System
Household Measures
Conversions Between Metric and Household Systems
International Units (IU)
Practical Applications
Example Calculations
The Institute of Medicine (2000) report “To Err is Human: Building a Safer Health Care System” revealed the seriousness of these errors and found that most were preventable. Dosing errors are the most common form of drug errors. Other errors occur during ordering and administration, including the wrong dose, prescription, allergy, time, route, or missed dose. Although several reasons have been found for the errors, communication is a common thread.
Another area of concern is that of handoffs or transitions. As continuity of care is disrupted, the risk for error is higher. This continuity can happen with changes in providers, such as shift change or when the patient is moved to a different facility or unit. Communication is, again, a key component. The Joint Commission National Patient Safety Goals require a standardized handoff procedure that discusses patient information (The Joint Commission, 2024).
Nurses find themselves as the last link in the chain of medication management. Nurses are habitually blamed for drug errors when, in fact, there are multiple people and tasks involved in drug errors, and nurses discover most drug errors. Studies reveal several factors in drug errors that can lead to adverse reactions and sentinel events. Causes identified specific to nursing care are unsafe practices, misidentification of the patient or drug, lack of knowledge, violation of policy and procedures, calculation errors, faulty checking procedures, equipment deficits, and not following drug directions (Ciapponi et al., 2021).
The use of technology in drug administration has been somewhat successful in reducing drug errors. Barcoding drugs for administration, computerized order entry, education, and electronic drug distribution systems have been helpful to providers in catching and reducing drug errors.
Techniques to reduce drug errors may include the following:
Among Medicare patients, four drugs, antidiabetic drugs, oral anticoagulants, antiplatelet drugs, and opioids, account for over half of emergency room visits for adverse drug events (Agency for Healthcare Research and Quality, 2019).
The Institute for Safe Drug Practices reports the drugs considered Look-Alike-Sound-Alike as well as high-risk drugs. The list is extensive and should be reviewed periodically. The Institute recommends that the review include storage and dispensing procedures to help decrease sentinel events involving drug errors (Institutional high-alert meds). The entire list can be found here.
Computerized Medication Ordering, also known as Computerized Physician Order Entry (CPOE), is a system that allows healthcare providers to enter medication orders and other treatment instructions electronically rather than using paper charts. CPOE systems are integrated with Electronic Health Records (EHRs) and other healthcare information systems, enhancing the accuracy and efficiency of the medication ordering process and improving patient safety.
CPOE has multiple benefits (Korb-Savoldelli et al., 2018 & Wimmer et al., 2023).
Reduction in Medication Errors
Improved Efficiency
Enhanced Communication and Documentation
Improved Patient Safety
Ms. Smith is a 72-year-old woman with a history of chronic obstructive pulmonary disease, coronary artery disease, hypertension, hyperlipidemia, chronic renal insufficiency, and depression. She was admitted to a post-operative unit after receiving a total hip arthroplasty after a femoral neck fracture from a fall. When she awoke from surgery, she complained of hip pain.
She has an order for IV morphine 2 to 4 mg every 2 to 4 hours as needed. When the nurse did the initial assessment, the patient reported pain as 10/10. She reviewed the order, and the nurse drew up 3 mg of hydromorphone instead of morphine. After giving the drug, she left the room and came back 20 minutes later and found the patient cyanotic and not breathing. A code was called, and aggressive measures were undertaken, including intubation and ventilation. An assessment of brain activity revealed no brain activity, and the family decided to take the patient off life support. The patient died after twenty minutes off the ventilator.
A lawsuit was filed, and the verdict was found against the hospital for 3 million dollars.
Why did the patient die?
The nurse gave the incorrect drug; consequently, the patient received a higher medication dose than expected. Three milligrams of hydromorphone is approximately equivalent to 12-21 mg of morphine. For practical purposes, healthcare providers often use a middle value or the lower end of the range to ensure patient safety, so a typical conversion might consider 3 mg of hydromorphone roughly equivalent to around 15 mg of morphine. In an opiate naïve patient, this led to respiratory arrest.
What lessons can be gleaned from the above study?
This course provided an overview of pharmacology. Starting with the basic duties of the healthcare provider, discussing pharmacokinetics and how to use drugs, then discussing basic pharmacology of multiple drug classes, and finishing with drug administration and drug errors. This course aims to improve the healthcare provider's knowledge of administering drugs safely and effectively.
CEUFast, Inc. is committed to furthering diversity, equity, and inclusion (DEI). While reflecting on this course content, CEUFast, Inc. would like you to consider your individual perspective and question your own biases. Remember, implicit bias is a form of bias that impacts our practice as healthcare professionals. Implicit bias occurs when we have automatic prejudices, judgments, and/or a general attitude towards a person or a group of people based on associated stereotypes we have formed over time. These automatic thoughts occur without our conscious knowledge and without our intentional desire to discriminate. The concern with implicit bias is that this can impact our actions and decisions with our workplace leadership, colleagues, and even our patients. While it is our universal goal to treat everyone equally, our implicit biases can influence our interactions, assessments, communication, prioritization, and decision-making concerning patients, which can ultimately adversely impact health outcomes. It is important to keep this in mind in order to intentionally work to self-identify our own risk areas where our implicit biases might influence our behaviors. Together, we can cease perpetuating stereotypes and remind each other to remain mindful to help avoid reacting according to biases that are contrary to our conscious beliefs and values.