Anti-Inflammatory Drugs: NSAIDs and Glucocorticoids
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Questions and Answers

Which of the following are examples of Salicylates (A type of NSAIDs)? Choose all that apply.

  • Aspirin, Diflunisal (correct)
  • Ketoprofen, Flurbiprofen
  • Naproxen, Etodolac (correct)
  • Ibuprofen, Keterolac

    • Glucocorticoids have relatively little effect on humoral immunity. (True/False)

    True

    What is a common adverse effect of NSAIDs?

  • Respiratory problems
  • Induction of asthma (correct)
  • Immune system suppression
  • Muscle cramps

    • What is the effect of NSAIDs on platelet function?

    <p>Inhibit platelet aggregation</p> Signup and view all the answers

    What is the risk associated with the use of NSAIDs in patients with pre-existing heart failure?

    <p>Worsening of heart failure</p> Signup and view all the answers

    Why should patients taking aspirin for cardioprotection avoid concomitant NSAID use?

    <p>To prevent the reduction of aspirin's antiplatelet effects</p> Signup and view all the answers

    What is the effect of NSAIDs on renal blood flow?

    <p>Decrease in PGE2 and PGI2 production</p> Signup and view all the answers

    What is the effect of NSAIDs on the kidneys?

    <p>Decrease renal prostaglandins</p> Signup and view all the answers

    Which patients are at high risk for NSAID-induced edema?

    <p>Patients with a history of heart failure or kidney disease</p> Signup and view all the answers

    What is a potential interaction between NSAIDs and warfarin?

    <p>Increased risk of bleeding</p> Signup and view all the answers

    What is the cardiovascular effect of agents with high COX-2 selectivity?

    <p>Increased risk of cardiovascular events</p> Signup and view all the answers

    What is a gastrointestinal adverse effect of NSAIDs?

    <p>Gastrointestinal bleeding and ulceration</p> Signup and view all the answers

    Why should NSAIDs be used with caution in patients with asthma?

    <p>NSAIDs may exacerbate asthma by shifting towards leukotriene production</p> Signup and view all the answers

    What is a cardiovascular risk associated with NSAIDs?

    <p>All of the above</p> Signup and view all the answers

    What is a common central nervous system adverse event associated with NSAIDs?

    <p>All of the above</p> Signup and view all the answers

    What is the mechanism of action of spironolactone?

    <p>Antagonism of the mineralocorticoid receptor</p> Signup and view all the answers

    Which NSAID may be the LEAST likely to be harmful in patients with cardiovascular disease?

    <p>Naproxen</p> Signup and view all the answers

    What is the therapeutic use of ketoconazole?

    <p>Treatment of Cushing syndrome</p> Signup and view all the answers

    What is a common adverse effect of spironolactone?

    <p>All of the above</p> Signup and view all the answers

    What is the effect of NSAIDs on sodium and water retention?

    <p>Decreased excretion of sodium and water</p> Signup and view all the answers

    Why are NSAIDs contraindicated in patients with established cardiovascular disease?

    <p>Due to the increased risk of cardiovascular events</p> Signup and view all the answers

    What is the effect of aspirin on TXA2 production?

    <p>Decreases TXA2 production</p> Signup and view all the answers

    What is a potential renal effect of NSAIDs?

    <p>Salt and water retention</p> Signup and view all the answers

    Why do NSAIDs pose a bleeding risk?

    <p>They inhibit platelet aggregation</p> Signup and view all the answers

    What is the effect of NSAIDs on prostaglandins in the stomach and small intestine?

    <p>Decrease the production of prostacyclin (PGI2) and PGE2</p> Signup and view all the answers

    Why should NSAIDs be taken with food or fluids?

    <p>To diminish GI upset</p> Signup and view all the answers

    How do NSAIDs affect the cardiovascular system?

    <p>They increase cardiovascular risk</p> Signup and view all the answers

    What is a potential interaction between NSAIDs and other medications?

    <p>Increased risk of bleeding with warfarin</p> Signup and view all the answers

    What is the effect of aspirin on platelet aggregation?

    <p>Reduces platelet aggregation</p> Signup and view all the answers

    Why do glucocorticoids have a broad anti-inflammatory effect?

    <p>They suppress the activation of nuclear factor-κB</p> Signup and view all the answers

    Why is aspirin often withheld for at least 1 week prior to surgery?

    <p>To reduce the risk of bleeding</p> Signup and view all the answers

    What is a potential effect of chronic glucocorticoid use?

    <p>Adrenal insufficiency</p> Signup and view all the answers

    How do NSAIDs affect platelet function?

    <p>They inhibit platelet aggregation</p> Signup and view all the answers

    Why are proton pump inhibitors or misoprostol often used concomitantly with NSAIDs?

    <p>To reduce the risk of GI bleeding and ulceration</p> Signup and view all the answers

    What is a potential effect of NSAIDs on the kidneys?

    <p>Decreased kidney function</p> Signup and view all the answers

    What is the effect of NSAIDs with higher relative selectivity for COX-1 on GI events?

    <p>Increases the risk of GI events</p> Signup and view all the answers

    Why do NSAIDs pose a cardiovascular risk?

    <p>They inhibit the production of prostaglandins</p> Signup and view all the answers

    Why do NSAIDs other than aspirin not have a significant antiplatelet effect?

    <p>Because they are reversible inhibitors of COX-1</p> Signup and view all the answers

    Ibuprofen, naproxen, fenoprofen, ketoprofen and flurbiprofen are examples of

    <p>Propionic acid derivatives</p> Signup and view all the answers

    Aspirin and diflunisal are examples of

    <p>salicylates</p> Signup and view all the answers

    Etodolac is a

    <p>indole and indene derivative</p> Signup and view all the answers

    Keterolac is a

    <p>Pyrrole derivative</p> Signup and view all the answers

    Which is associated with aspirin

    <p>all of the above</p> Signup and view all the answers

    Study Notes

    Anti-inflammatory drugs

    • Anti-inflammatory drugs include NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) and Glucocorticoids.

    NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)

    • Types of NSAIDs:
      • Salicylates: Aspirin, Diflunisal
      • Propionic acid derivatives: Ibuprofen, Naproxen, Fenoprofen, Ketoprofen, Flurbiprofen
      • Indole and indene derivatives: Etodolac
      • Pyrrole derivatives: Ketorolac

    Mechanism of Glucocorticoids

    • Glucocorticoids have broad anti-inflammatory effects on multiple components of cellular immunity but relatively little effect on humoral immunity.
    • Glucocorticoids bind to receptors inside cells and regulate the transcription of numerous other genes.
    • Glucocorticoids curtail activation of nuclear factor-κB, suppress formation of proinflammatory cytokines such as IL-1 and IL-6, inhibit T cells from making IL-2 and proliferating, and inhibit the activation of cytotoxic T lymphocytes.
    • Glucocorticoids also inhibit the activation of neutrophils and monocytes.

    Aspirin

    • Aspirin is a weak organic acid that irreversibly acetylates and inactivates cyclooxygenase.
    • Aspirin inhibits cyclooxygenase, which diminishes the formation of prostaglandins and modulates aspects of inflammation mediated by prostaglandins.
    • Aspirin does not arrest the progression of the disease or induce remission.

    Adverse effects of NSAIDs

    • Gastrointestinal effects:
      • Increased risk of bleeding
      • Ulceration
    • Increased risk of bleeding (antiplatelet effect):
      • Prolonged bleeding time
      • Aspirin should be withheld for at least 1 week prior to surgery
    • Renal effects:
      • Retention of sodium and water
      • Edema
      • Decreased renal blood flow
    • Cardiac effects:
      • Increased risk for cardiovascular events
      • MI and stroke
      • Cardiovascular protective effect due to reduced production of TXA2
    • Other adverse effects:
      • Asthma exacerbations
      • Central nervous system (CNS) adverse events
      • Headache, tinnitus, and dizziness
      • Hypersensitivity reactions

    Inhibitors of endogenous steroids (Adrenocorticoids) secretion or function

    • Ketoconazole:
      • Strongly inhibits all gonadal and adrenal steroid hormone synthesis
      • Used in the treatment of patients with Cushing syndrome when surgical management is not an option
    • Spironolactone:
      • Competes for the mineralocorticoid receptor
      • Inhibits sodium reabsorption in the kidney
      • Effective for the management of hyperaldosteronism, resistant hypertension, and hepatic cirrhosis
      • Used with other standard therapies for treatment of heart failure with reduced ejection fraction
      • Used in the management of hirsutism in women, probably due to antiandrogen activity on the hair follicle
      • Adverse effects: hyperkalemia, gynecomastia, menstrual irregularities, and skin rashes
    • Eplerenone:
      • Selectively binds to the mineralocorticoid receptor
      • Acts as a selective aldosterone antagonist
      • Has a lower affinity for the androgen receptor
      • Lessens the potential for gynecomastia and irregular menstrual bleeding associated with spironolactone
      • Approved for the treatment of hypertension and for heart failure with reduced ejection fraction after an acute myocardial infarction

    NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)

    • Patients taking aspirin for cardioprotection should avoid concomitant NSAID use or take aspirin at least 30 minutes prior to the NSAID.
    • NSAIDs prevent the synthesis of PGE2 and PGI2, prostaglandins responsible for maintaining renal blood flow, which can result in retention of sodium and water, leading to edema.
    • Patients with a history of heart failure or kidney disease are at high risk for these effects, which can mitigate the beneficial effects of antihypertensive medications.
    • NSAIDs can lead to acute kidney injury in susceptible patients.

    Cardiac Effects

    • Aspirin, with high COX-1 selectivity at low doses, has a cardiovascular protective effect due to reduced TXA2 production.
    • Agents with higher relative COX-2 selectivity have been associated with an increased risk for cardiovascular events, possibly by decreasing PGI2 production mediated by COX-2.
    • All NSAIDs except aspirin carry a boxed warning regarding the increased risk for cardiovascular events, including MI and stroke.
    • Use of NSAIDs other than aspirin is discouraged in patients with established cardiovascular disease.
    • Naproxen may be the least likely to be harmful in patients with cardiovascular disease.

    Other Adverse Effects

    • NSAIDs inhibit cyclooxygenases, which can cause a shift toward leukotriene production and increase the risk of asthma exacerbations.
    • Central nervous system (CNS) adverse events, such as headache, tinnitus, and dizziness, may occur.

    Pharmacokinetics

    • NSAIDs are inhibitors of cyclooxygenases and, therefore, inhibit the synthesis of prostaglandins but not of leukotrienes.

    Inhibitors of Endogenous Steroids (Adrenocorticoids) Secretion or Function

    • Ketoconazole: an antifungal agent that strongly inhibits all gonadal and adrenal steroid hormone synthesis, used in the treatment of Cushing syndrome.
    • Spironolactone: an antihypertensive drug that competes for the mineralocorticoid receptor, inhibiting sodium reabsorption in the kidney, and also antagonizes aldosterone and testosterone synthesis.
    • Eplerenone: a selective aldosterone antagonist that binds to the mineralocorticoid receptor, approved for the treatment of hypertension and heart failure with reduced ejection fraction after an acute myocardial infarction.

    Adverse Effects of Aspirin

    • Gastrointestinal: the most common adverse effects of NSAIDs, ranging from dyspepsia to bleeding.
    • Increased risk of bleeding (antiplatelet effect): aspirin inhibits COX-1–mediated formation of TXA2 and reduces platelet aggregation for the lifetime of the platelet.

    Glucocorticoids

    • Mechanism: glucocorticoids bind to receptors inside cells and regulate the transcription of numerous other genes, curtailing activation of nuclear factor-κB, suppressing formation of proinflammatory cytokines, and inhibiting T cells and neutrophils.
    • Chronic adverse effects: glucocorticoids have broad anti-inflammatory effects on multiple components of cellular immunity but relatively little effect on humoral immunity.

    Selected Drug-Drug Interactions: Glucocorticoids

    • No specific interactions mentioned in the text.

    NSAIDs

    • Classification:
      • Salicylates: Aspirin, Diflunisal
      • Propionic acid derivatives: Ibuprofen, naproxen, fenoprofen, ketoprofen, flurbiprofen
      • Indole and indene derivatives: Etodolac
      • Pyrrole derivatives: Keterolac

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