Immune System Drugs
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Questions and Answers

First-generation NSAIDs inhibit which of the following?

  • COX-1 (correct)
  • COX-3
  • COX-2 (correct)
  • COX-5
  • Aspirin is a nonselective inhibitor of which enzyme?

  • Cyclooxygenase (correct)
  • Prostaglandin synthase
  • Thromboxane synthase
  • Lipoxygenase
  • Which of the following is a therapeutic use of aspirin?

  • Promotion of platelet aggregation
  • Reduction of blood clotting
  • Prevention of thrombotic disorders (correct)
  • Inhibition of inflammation (correct)
  • Which of the following is an adverse effect associated with aspirin use?

    <p>Gastrointestinal bleeding (C)</p> Signup and view all the answers

    Which of the following drug interactions is associated with aspirin?

    <p>Increased effects of Warfarin (D)</p> Signup and view all the answers

    What is the primary action of cyclooxygenase (COX) inhibitors?

    <p>Inhibiting the conversion of arachidonic acid into prostanoids (B)</p> Signup and view all the answers

    Which adverse effect is specifically associated with the inhibition of COX-1?

    <p>Gastric ulceration (A)</p> Signup and view all the answers

    What is a beneficial effect linked to the inhibition of COX-1?

    <p>Protection against myocardial infarction and stroke (C)</p> Signup and view all the answers

    What is a primary beneficial effect associated with inhibiting COX-2?

    <p>Suppression of inflammation (B)</p> Signup and view all the answers

    Which of the following drugs is classified as a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory properties?

    <p>Celecoxib (C)</p> Signup and view all the answers

    Which of the following is a potential consequence of Cyclosporine?

    <p>Increased levels of nephrotoxic agents (B)</p> Signup and view all the answers

    A patient taking Cyclosporine is advised to avoid which of the following?

    <p>Grapefruit Juice (D)</p> Signup and view all the answers

    Which of the options is an example of a drug WITHOUT anti-inflammatory properties?

    <p>Acetaminophen (B)</p> Signup and view all the answers

    During periods of significant physiological stress, such as surgery or severe infection, what is the primary role of glucocorticoids released by the adrenal glands?

    <p>To help maintain blood pressure and blood glucose levels. (D)</p> Signup and view all the answers

    What are the potential consequences of insufficient glucocorticoid release during severe stress?

    <p>Hypotension and hypoglycemia. (B)</p> Signup and view all the answers

    In the context of glucocorticoid drug effects, how does the dosage typically influence the therapeutic outcome?

    <p>Low doses primarily modulate glucose metabolism in adrenocortical insufficiency, while high doses suppress inflammation. (B)</p> Signup and view all the answers

    Which of the following is a common adverse effect associated with prolonged use of high-dose glucocorticoids?

    <p>Thinning of the skin. (D)</p> Signup and view all the answers

    How do glucocorticoids influence water and electrolyte balance in the body?

    <p>They promote retention of sodium and water while increasing urinary excretion of potassium, potentially leading to hypernatremia, hypokalemia, and edema. (D)</p> Signup and view all the answers

    What is the primary mechanism by which glucocorticoids elevate blood glucose levels?

    <p>By promoting the storage of glucose in the form of glycogen. (B)</p> Signup and view all the answers

    Which of the following best describes the effect of glucocorticoids on bone?

    <p>They decrease the protein matrix of bone, potentially leading to osteoporosis. (D)</p> Signup and view all the answers

    With reference to mineralocorticoid activity, how do most glucocorticoid drugs compare to endogenous mineralocorticoids like aldosterone?

    <p>They possess significantly lower mineralocorticoid activity. (B)</p> Signup and view all the answers

    Which of the following statements BEST characterizes the mechanism by which first-generation NSAIDs alleviate mild to moderate pain?

    <p>They primarily work by reducing inflammation at the site of injury, which subsequently diminishes the activation of pain pathways. (B)</p> Signup and view all the answers

    Aspirin is known to protect against thrombotic disorders through the suppression of platelet aggregation. By what specific mechanism does aspirin achieve this effect?

    <p>Aspirin irreversibly acetylates cyclooxygenase-1 (COX-1) in platelets, preventing the formation of thromboxane A2, a potent platelet aggregator. (B)</p> Signup and view all the answers

    Which of the following BEST describes the underlying mechanism that links aspirin use to the prevention of Alzheimer’s disease?

    <p>Aspirin reduces neuroinflammation by inhibiting COX-2 in the brain, which leads to decreased amyloid plaque formation and improved cognitive function. (D)</p> Signup and view all the answers

    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?

    <p>Aspirin increases the breakdown of fibrin clots and impairs platelet aggregation, resulting in an increased risk of bleeding during delivery and potentially causing anemia. (A)</p> Signup and view all the answers

    Why is the concurrent use of aspirin and glucocorticoids particularly risky regarding gastrointestinal (GI) effects?

    <p>Glucocorticoids impair the mucosal defense mechanisms in the stomach, and aspirin further reduces prostaglandin synthesis, both contributing to an elevated risk of GI bleeding. (C)</p> Signup and view all the answers

    Which of the following medications is known to have drug interactions that affect cyclosporine levels?

    <p>Sandimmune (C)</p> Signup and view all the answers

    Which of the following dietary substances is specifically noted for its potential to interact with Cyclosporine, altering drug metabolism and effectiveness?

    <p>Grapefruit Juice (D)</p> Signup and view all the answers

    What is the primary mechanism by which Cyclooxygenase (COX) inhibitors exert their effects?

    <p>Inhibiting the conversion of arachidonic acid into prostanoids. (C)</p> Signup and view all the answers

    Inhibition of COX-1 is associated with gastric ulceration, bleeding, and renal impairment, but also offers which beneficial effect?

    <p>Protection against myocardial infarction and stroke. (A)</p> Signup and view all the answers

    Which of the following best describes the primary effect of inhibiting COX-2?

    <p>Suppression of inflammation, alleviation of pain, and reduction of fever. (D)</p> Signup and view all the answers

    Which medication is classified as a cyclooxygenase inhibitor that lacks anti-inflammatory properties?

    <p>Acetaminophen (D)</p> Signup and view all the answers

    What is the rationale behind avoiding nephrotoxic drugs when a patient is taking cyclosporine?

    <p>To minimize the combined risk of kidney damage (C)</p> Signup and view all the answers

    Repaglinide's interaction with cyclosporine can potentially lead to what specific outcome?

    <p>Elevated repaglinide levels, increasing the risk of hypoglycemia (D)</p> Signup and view all the answers

    What is a potential consequence of administering excessive glucocorticoids during periods of significant physiological stress?

    <p>Exacerbated hyperglycemia, potentially leading to insulin resistance. (B)</p> Signup and view all the answers

    Which of the following electrolyte imbalances is least likely to be associated with the administration of glucocorticoid drugs?

    <p>Hyperkalemia (B)</p> Signup and view all the answers

    How do glucocorticoids impact protein metabolism in the body, particularly concerning muscle mass and bone matrix?

    <p>Reduce muscle mass and decrease the protein matrix of bone, impacting both structural integrity and growth. (D)</p> Signup and view all the answers

    How does severe glucocorticoid insufficiency manifest during conditions of significant physiological stress, and what are its potential consequences?

    <p>Hypotension and hypoglycemia, possibly leading to circulatory failure and death. (A)</p> Signup and view all the answers

    In the context of nonendocrine disorders, how do glucocorticoids influence renal function and electrolyte balance, and what is the underlying mechanism?

    <p>By promoting sodium and water retention while increasing urinary excretion of potassium. (D)</p> Signup and view all the answers

    What describes the relationship between glucocorticoids and mineralocorticoid activity?

    <p>Most glucocorticoid drugs have very low mineralocorticoid activity, minimizing sodium and water retention. (A)</p> Signup and view all the answers

    Which of the following best describes the effects of high-dose glucocorticoid therapy on the distribution of body fat?

    <p>Lipolysis and redistribution of fat, leading to characteristic features like 'potbelly,' 'moon face,' and 'buffalo hump'. (B)</p> Signup and view all the answers

    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?

    <p>Recommending a high-protein diet with weight-bearing exercise to mitigate muscle wasting and bone density loss. (A)</p> Signup and view all the answers

    Flashcards

    Glucocorticoids

    Hormones secreted by adrenal glands during stress to maintain blood pressure and glucose levels.

    Physiologic stress

    Conditions like surgery, trauma, infection prompting glucocorticoid release.

    Adrenal glands

    Glands that secrete glucocorticoids and epinephrine in response to stress.

    Insufficient glucocorticoids

    Lack of hormone leads to hypotension and hypoglycemia.

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    Glucocorticoid drugs

    Corticosteroids resembling adrenal cortex steroids, used to modulate glucose and inflammation.

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    Adverse effects of glucocorticoids

    Include high blood glucose, muscle mass reduction, skin thinning, and fat redistribution.

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    Mineralocorticoid activity

    Influences on sodium retention, potassium excretion, causing fluid imbalance.

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    Hypernatremia and hypokalemia

    Elevated sodium levels and low potassium levels caused by glucocorticoid action.

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    Cyclosporine interactions

    Drugs that can affect cyclosporine levels in the body.

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    Nephrotoxic drugs

    Drugs that can harm the kidneys, especially when combined with cyclosporine.

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    Grapefruit juice effect

    Grapefruit juice can increase cyclosporine levels, leading to toxicity.

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    COX Inhibition

    Blocking cyclooxygenase enzymes reduces pain, inflammation, and fever.

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    First-Generation NSAIDs

    Inhibit COX-1 and COX-2, treating inflammatory disorders and alleviating pain.

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    COX-1 effects

    Inhibition can lead to gastric ulceration and bleeding, but also heart protection.

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    COX-2 benefits

    Inhibition is mainly beneficial for reducing inflammation and pain.

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    Aspirin uses

    Analgesic, antipyretic, antiinflammatory, and prevents platelet aggregation.

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    NSAIDs classification

    Nonsteroidal anti-inflammatory drugs used for pain relief, such as ibuprofen.

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    Adverse effects of Aspirin

    May cause GI issues, bleeding, renal impairment, and tinnitus.

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    Acetaminophen use

    Drug that relieves pain and fever but lacks antiinflammatory properties.

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    Drug interactions with Aspirin

    Can interact with anticoagulants, glucocorticoids, and alcohol.

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    Reye’s syndrome

    Serious condition linked to Aspirin use in children, causing liver damage.

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    Aspirin

    A nonselective COX inhibitor used as an analgesic, antipyretic, and antiinflammatory agent.

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    Aspirin Adverse Effects

    Includes gastrointestinal issues, bleeding, renal impairment, and tinnitus.

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    Aspirin Drug Interactions

    Aspirin can interact with anticoagulants, glucocorticoids, alcohol, and ibuprofen.

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    Cyclooxygenase Inhibitors

    Drugs that suppress inflammation, relieve pain, and reduce fever.

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    Adverse effects of COX Inhibitors

    Potential side effects include gastric ulceration, bleeding, and renal impairment.

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    COX-1 vs COX-2

    COX-1 inhibition can cause harmful effects; COX-2 inhibition provides benefits.

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    NSAIDs

    Nonsteroidal anti-inflammatory drugs relieve pain and inflammation.

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    Cyclooxygenase mechanism

    Inhibition of COX enzymes reduces prostanoids from arachidonic acid.

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    Grapefruit juice interaction

    Grapefruit juice can increase cyclosporine levels, risking toxicity.

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    Glucocorticoid secretion

    Release of glucocorticoids and epinephrine by adrenal glands during stress.

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    Effects of glucocorticoids during stress

    Help maintain blood pressure and glucose levels during stress.

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    Consequences of glucocorticoid deficiency

    Insufficient glucocorticoids can lead to hypotension and hypoglycemia.

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    Glucocorticoids and electrolyte balance

    They can promote sodium retention and potassium excretion, mimicking aldosterone.

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    Hypernatremia

    Elevated sodium levels commonly caused by glucocorticoids.

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    Hypokalemia

    Low potassium levels that may result from glucocorticoid action.

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    Corticosteroids vs. glucocorticoids

    Corticosteroids encompass glucocorticoids, which mimic adrenal cortex steroids.

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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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