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Questions and Answers
First-generation NSAIDs inhibit which of the following?
First-generation NSAIDs inhibit which of the following?
Aspirin is a nonselective inhibitor of which enzyme?
Aspirin is a nonselective inhibitor of which enzyme?
Which of the following is a therapeutic use of aspirin?
Which of the following is a therapeutic use of aspirin?
Which of the following is an adverse effect associated with aspirin use?
Which of the following is an adverse effect associated with aspirin use?
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Which of the following drug interactions is associated with aspirin?
Which of the following drug interactions is associated with aspirin?
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What is the primary action of cyclooxygenase (COX) inhibitors?
What is the primary action of cyclooxygenase (COX) inhibitors?
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Which adverse effect is specifically associated with the inhibition of COX-1?
Which adverse effect is specifically associated with the inhibition of COX-1?
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What is a beneficial effect linked to the inhibition of COX-1?
What is a beneficial effect linked to the inhibition of COX-1?
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What is a primary beneficial effect associated with inhibiting COX-2?
What is a primary beneficial effect associated with inhibiting COX-2?
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Which of the following drugs is classified as a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory properties?
Which of the following drugs is classified as a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory properties?
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Which of the following is a potential consequence of Cyclosporine?
Which of the following is a potential consequence of Cyclosporine?
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A patient taking Cyclosporine is advised to avoid which of the following?
A patient taking Cyclosporine is advised to avoid which of the following?
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Which of the options is an example of a drug WITHOUT anti-inflammatory properties?
Which of the options is an example of a drug WITHOUT anti-inflammatory properties?
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During periods of significant physiological stress, such as surgery or severe infection, what is the primary role of glucocorticoids released by the adrenal glands?
During periods of significant physiological stress, such as surgery or severe infection, what is the primary role of glucocorticoids released by the adrenal glands?
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What are the potential consequences of insufficient glucocorticoid release during severe stress?
What are the potential consequences of insufficient glucocorticoid release during severe stress?
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In the context of glucocorticoid drug effects, how does the dosage typically influence the therapeutic outcome?
In the context of glucocorticoid drug effects, how does the dosage typically influence the therapeutic outcome?
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Which of the following is a common adverse effect associated with prolonged use of high-dose glucocorticoids?
Which of the following is a common adverse effect associated with prolonged use of high-dose glucocorticoids?
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How do glucocorticoids influence water and electrolyte balance in the body?
How do glucocorticoids influence water and electrolyte balance in the body?
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What is the primary mechanism by which glucocorticoids elevate blood glucose levels?
What is the primary mechanism by which glucocorticoids elevate blood glucose levels?
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Which of the following best describes the effect of glucocorticoids on bone?
Which of the following best describes the effect of glucocorticoids on bone?
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With reference to mineralocorticoid activity, how do most glucocorticoid drugs compare to endogenous mineralocorticoids like aldosterone?
With reference to mineralocorticoid activity, how do most glucocorticoid drugs compare to endogenous mineralocorticoids like aldosterone?
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Which of the following statements BEST characterizes the mechanism by which first-generation NSAIDs alleviate mild to moderate pain?
Which of the following statements BEST characterizes the mechanism by which first-generation NSAIDs alleviate mild to moderate pain?
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Aspirin is known to protect against thrombotic disorders through the suppression of platelet aggregation. By what specific mechanism does aspirin achieve this effect?
Aspirin is known to protect against thrombotic disorders through the suppression of platelet aggregation. By what specific mechanism does aspirin achieve this effect?
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Which of the following BEST describes the underlying mechanism that links aspirin use to the prevention of Alzheimer’s disease?
Which of the following BEST describes the underlying mechanism that links aspirin use to the prevention of Alzheimer’s disease?
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Which of the following statements accurately describes the mechanism through which aspirin use during pregnancy can lead to adverse outcomes, such as anemia or postpartum hemorrhage?
Which of the following statements accurately describes the mechanism through which aspirin use during pregnancy can lead to adverse outcomes, such as anemia or postpartum hemorrhage?
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Why is the concurrent use of aspirin and glucocorticoids particularly risky regarding gastrointestinal (GI) effects?
Why is the concurrent use of aspirin and glucocorticoids particularly risky regarding gastrointestinal (GI) effects?
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Which of the following medications is known to have drug interactions that affect cyclosporine levels?
Which of the following medications is known to have drug interactions that affect cyclosporine levels?
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Which of the following dietary substances is specifically noted for its potential to interact with Cyclosporine, altering drug metabolism and effectiveness?
Which of the following dietary substances is specifically noted for its potential to interact with Cyclosporine, altering drug metabolism and effectiveness?
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What is the primary mechanism by which Cyclooxygenase (COX) inhibitors exert their effects?
What is the primary mechanism by which Cyclooxygenase (COX) inhibitors exert their effects?
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Inhibition of COX-1 is associated with gastric ulceration, bleeding, and renal impairment, but also offers which beneficial effect?
Inhibition of COX-1 is associated with gastric ulceration, bleeding, and renal impairment, but also offers which beneficial effect?
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Which of the following best describes the primary effect of inhibiting COX-2?
Which of the following best describes the primary effect of inhibiting COX-2?
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Which medication is classified as a cyclooxygenase inhibitor that lacks anti-inflammatory properties?
Which medication is classified as a cyclooxygenase inhibitor that lacks anti-inflammatory properties?
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What is the rationale behind avoiding nephrotoxic drugs when a patient is taking cyclosporine?
What is the rationale behind avoiding nephrotoxic drugs when a patient is taking cyclosporine?
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Repaglinide's interaction with cyclosporine can potentially lead to what specific outcome?
Repaglinide's interaction with cyclosporine can potentially lead to what specific outcome?
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What is a potential consequence of administering excessive glucocorticoids during periods of significant physiological stress?
What is a potential consequence of administering excessive glucocorticoids during periods of significant physiological stress?
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Which of the following electrolyte imbalances is least likely to be associated with the administration of glucocorticoid drugs?
Which of the following electrolyte imbalances is least likely to be associated with the administration of glucocorticoid drugs?
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How do glucocorticoids impact protein metabolism in the body, particularly concerning muscle mass and bone matrix?
How do glucocorticoids impact protein metabolism in the body, particularly concerning muscle mass and bone matrix?
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How does severe glucocorticoid insufficiency manifest during conditions of significant physiological stress, and what are its potential consequences?
How does severe glucocorticoid insufficiency manifest during conditions of significant physiological stress, and what are its potential consequences?
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In the context of nonendocrine disorders, how do glucocorticoids influence renal function and electrolyte balance, and what is the underlying mechanism?
In the context of nonendocrine disorders, how do glucocorticoids influence renal function and electrolyte balance, and what is the underlying mechanism?
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What describes the relationship between glucocorticoids and mineralocorticoid activity?
What describes the relationship between glucocorticoids and mineralocorticoid activity?
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Which of the following best describes the effects of high-dose glucocorticoid therapy on the distribution of body fat?
Which of the following best describes the effects of high-dose glucocorticoid therapy on the distribution of body fat?
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Given the various adverse effects, and considering a patient is on long-term, high-dose glucocorticoid therapy, which intervention would be MOST BENEFICIAL to counteract one of its effects?
Given the various adverse effects, and considering a patient is on long-term, high-dose glucocorticoid therapy, which intervention would be MOST BENEFICIAL to counteract one of its effects?
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Flashcards
Glucocorticoids
Glucocorticoids
Hormones secreted by adrenal glands during stress to maintain blood pressure and glucose levels.
Physiologic stress
Physiologic stress
Conditions like surgery, trauma, infection prompting glucocorticoid release.
Adrenal glands
Adrenal glands
Glands that secrete glucocorticoids and epinephrine in response to stress.
Insufficient glucocorticoids
Insufficient glucocorticoids
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Glucocorticoid drugs
Glucocorticoid drugs
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Adverse effects of glucocorticoids
Adverse effects of glucocorticoids
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Mineralocorticoid activity
Mineralocorticoid activity
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Hypernatremia and hypokalemia
Hypernatremia and hypokalemia
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Cyclosporine interactions
Cyclosporine interactions
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Nephrotoxic drugs
Nephrotoxic drugs
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Grapefruit juice effect
Grapefruit juice effect
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COX Inhibition
COX Inhibition
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First-Generation NSAIDs
First-Generation NSAIDs
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COX-1 effects
COX-1 effects
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COX-2 benefits
COX-2 benefits
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Aspirin uses
Aspirin uses
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NSAIDs classification
NSAIDs classification
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Adverse effects of Aspirin
Adverse effects of Aspirin
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Acetaminophen use
Acetaminophen use
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Drug interactions with Aspirin
Drug interactions with Aspirin
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Reye’s syndrome
Reye’s syndrome
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Aspirin
Aspirin
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Aspirin Adverse Effects
Aspirin Adverse Effects
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Aspirin Drug Interactions
Aspirin Drug Interactions
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Cyclooxygenase Inhibitors
Cyclooxygenase Inhibitors
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Adverse effects of COX Inhibitors
Adverse effects of COX Inhibitors
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COX-1 vs COX-2
COX-1 vs COX-2
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NSAIDs
NSAIDs
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Cyclooxygenase mechanism
Cyclooxygenase mechanism
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Grapefruit juice interaction
Grapefruit juice interaction
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Glucocorticoid secretion
Glucocorticoid secretion
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Effects of glucocorticoids during stress
Effects of glucocorticoids during stress
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Consequences of glucocorticoid deficiency
Consequences of glucocorticoid deficiency
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Glucocorticoids and electrolyte balance
Glucocorticoids and electrolyte balance
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Hypernatremia
Hypernatremia
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Hypokalemia
Hypokalemia
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Corticosteroids vs. glucocorticoids
Corticosteroids vs. glucocorticoids
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Study Notes
Immune System Drugs
- Immunosuppressants inhibit the immune response.
- Uses include organ rejection prevention and autoimmune disease treatment.
- Immunosuppressants increase the risk of infection and neoplasms.
Calcineurin Inhibitors
- Principal use: Preventing organ rejection in transplant recipients.
- Cyclosporine, tacrolimus, and pimecrolimus are the most effective immunosuppressants available.
- These drugs share a similar mechanism, inhibiting calcineurin, which suppresses interleukin (IL-2) production.
- IL-2 is needed for T-cell proliferation.
- Cyclosporine was developed first and is more commonly used than tacrolimus.
Cyclosporine [Sandimmune]
- Mechanism: Suppresses the production of IL-2, interferon gamma, and other cytokines.
- Therapeutic uses: Drug of choice for organ rejection (kidney, liver, heart) in allogenic transplants and some autoimmune diseases.
- Pharmacokinetics: (details not provided).
Cyclosporine [Sandimmune] Adverse Effects
- Nephrotoxicity
- Infection
- Hepatotoxicity
- Lymphoma
- Hypertension
- Tremor
- Hirsutism
- Leukopenia, gingival hyperplasia, gynecomastia, sinusitis, and hyperkalemia
- Anaphylactic reactions
Cyclosporine [Sandimmune] Drug and Food Interactions
- Drugs that decrease cyclosporine levels
- Drugs that increase cyclosporine levels (nephrotoxic drugs, grapefruit juice, repaglinide)
Cyclooxygenase Inhibitors
- Uses: Suppress inflammation, relieve pain and reduce fever.
- Adverse effects include gastric ulceration, bleeding, and renal impairment.
Cyclooxygenase Inhibitors: Mechanism of Action
- Inhibit cyclooxygenase (COX), the enzyme that converts arachidonic acid into prostanoids.
- Inhibition of COX-1 is linked to gastric ulceration, bleeding, and renal impairment.
Cyclooxygenase Inhibitors: Inhibition of COX-1: Beneficial effects
- Protection against myocardial infarction (MI) and stroke.
Cyclooxygenase Inhibitors: Inhibition of COX-2: Beneficial effects
- Suppression of inflammation
- Alleviation of pain and reduction of fever
- Protection against colorectal cancer
Classification of Cyclooxygenase Inhibitors
- Drugs with anti-inflammatory properties: Nonsteroidal anti-inflammatory drugs (NSAIDs), including aspirin, celecoxib, ibuprofen, and naproxen.
- Drugs without anti-inflammatory properties: Acetaminophen.
First-Generation NSAIDs
- Inhibit COX-1 and COX-2.
- Used to treat inflammatory disorders such as rheumatoid arthritis, osteoarthritis, and bursitis.
- Alleviate mild to moderate pain.
- Suppress fever.
- Relieve dysmenorrhea.
- May cause serious harm.
Aspirin
- Nonselective inhibitor of cyclooxygenase.
- Therapeutic uses: Analgesic, antipyretic, anti-inflammatory, suppression of platelet aggregation, protecting in thrombotic disorders, dysmenorrhea, cancer prevention, and prevention of Alzheimer's disease.
- Adverse effects: Gastrointestinal (GI) effects (bleeding), renal impairment, Salicylism (tinnitus, sweating, headache, and dizziness), Reye's syndrome, pregnancy-related issues (anemia, postpartum hemorrhage, prolonged labor), hypersensitivity reaction.
- Drug interactions: Anticoagulants (warfarin and heparin), glucocorticoids, alcohol, ibuprofen, ACE inhibitors and ARBs, and acute poisoning can cause respiratory depression, hyperthermia, dehydration, and acidosis (treatment is largely supportive).
Ibuprofen [Advil, Motrin]
- Inhibits cyclooxygenase, having anti-inflammatory, analgesic, and antipyretic actions.
- Indications: Fever, mild to moderate pain, and arthritis.
- Generally well tolerated.
- Low incidence of adverse effects.
- SAFETY ALERT: Associated with increased risk of GI bleeding that can cause hospitalization or death.
Acetaminophen [Tylenol]
- Analgesic and antipyretic, but does not have anti-inflammatory or antirheumatic actions.
- Not associated with Reye's syndrome.
- Inhibits prostaglandin synthesis in the central nervous system.
Acetaminophen [Tylenol] Adverse Effects
- Rare adverse effects at normal doses.
- Serious risks associated with overdose: Stevens-Johnson syndrome (SJS), acute generalized exanthematous pustulosis (AGEP), toxic epidermal necrolysis (TEN), hepatotoxicity, hepatic necrosis with overdose or liver failure.
- Symptoms of overdose include nausea, vomiting, diarrhea, sweating, and abdominal pain.
- Treatment for overdose includes acetylcysteine (Mucomyst).
Acetaminophen [Tylenol] Drug Interactions
- Alcohol
- Warfarin
- Vaccines
Glucocorticoid Physiology
- Effects during stress (e.g., surgery, infection, trauma, hypovolemia): Adrenal glands secrete large quantities of glucocorticoids and epinephrine.
- Hormones help maintain blood pressure and blood glucose levels.
- Insufficient release of glucocorticoids: Hypotension and hypoglycemia occur.
- Very severe stress: Glucocorticoid insufficiency can result in circulatory failure and death.
Glucocorticoid Drugs
- Also known as corticosteroids, nearly identical to steroids produced by the adrenal cortex.
- Physiologic effects (low doses): Modulation of glucose metabolism in adrenocortical insufficiency.
- Pharmacologic effects (high doses): Suppression of inflammation.
Glucocorticoid Drugs Adverse Effects
- Elevates blood glucose.
- Promotes glucose storage as glycogen.
- Reduces muscle mass.
- Decreases bone protein matrix.
- Causes skin thinning.
- Lipolysis, redistribution of fat ("potbelly," "moon face," "buffalo hump").
Glucocorticoids in Nonendocrine Disorders
- Effects on water and electrolytes: Can exert actions like aldosterone, promoting sodium and water retention, increasing potassium excretion.
- Most glucocorticoid drugs have low mineralocorticoid activity.
Pharmacology of Glucocorticoids
- Anti-inflammatory and immunosuppressant effects stem from their ability to suppress immune responses and inflammation.
- Therapeutic uses in autoimmune disorders (rheumatoid arthritis, systemic lupus erythematosus, inflammatory bowel disease), and other non-endocrine disorders (allergic conditions, asthma, dermatologic disorders, neoplasms, suppression of allograft rejection, prevention of respiratory distress syndrome in preterm infants).
Pharmacology of Glucocorticoids Adverse Effects
- Adrenal insufficiency with prolonged administration.
- Osteoporosis with prolonged systemic therapy.
- Infection.
- Glucose intolerance (hyperglycemia, glycosuria).
- Myopathy (proximal muscles of arms and legs affected most).
- Peptic ulcer disease (inhibit prostaglandin synthesis, augment gastric acid and pepsin secretion, inhibit cytoprotective mucus, and reduce gastric mucosal blood flow).
Pharmacology of Glucocorticoids Drug Interactions
- Interactions related to potassium loss.
- Nonsteroidal anti-inflammatory drugs.
- Insulin and oral hypoglycemics.
- Vaccines.
Pharmacology of Glucocorticoids Contraindications and Precautions
- Patients with systemic fungal infections
- Those receiving live virus vaccines
- Use with caution in pediatric patients and in pregnancy/breast-feeding.
Glucocorticoid Routes of Administration
- Oral, intravenous (IV), intramuscular (IM), subcutaneous (subQ), and topical.
- Individual glucocorticoids differ in their biologic half-life, mineralocorticoid potency, and glucocorticoid potency.
Glucocorticoid Drugs: Examples
- Hydrocortisone
- Prednisone
- Dexamethasone
Glucocorticoid Dosage
- Dosage is determined empirically (trial and error).
- No immediate threat: Start low and slow.
- Immediate threat: Start high, decrease as possible.
- Long-term use: Smallest effective amount.
- Increase dosage during times of stress.
- Gradual weaning.
- Administer medication before 0900 if possible.
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