Pharmacology of NSAIDs and Coxibs
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Questions and Answers

Which of the following is a consequence of long-term use of COX-2 selective NSAIDs?

  • Increased production of mucus in the stomach
  • Increased risk of gastrointestinal toxicity (correct)
  • Improved efficacy of diuretics
  • Decreased risk of thromboembolic events
  • What is the primary mechanism by which aspirin produces antiplatelet effects?

  • Inhibition of PGI2 in platelets
  • Inhibition of COX-1 in platelets (correct)
  • Stimulation of prostacyclin in endothelium
  • Inhibition of COX-2 in endothelium
  • What is the primary mechanism by which NSAIDs cause gastrointestinal effects?

  • Increased production of thromboxane A2
  • Inhibition of COX-1 leading to decreased prostaglandin production (correct)
  • Inhibition of COX-2 leading to increased prostaglandin production
  • Direct gastric irritation
  • Which of the following is a contraindication for the use of NSAIDs?

    <p>Peptic ulcer disease</p> Signup and view all the answers

    What is the primary mechanism by which NSAIDs cause renal effects?

    <p>Inhibition of local prostaglandins leading to decreased renal blood flow</p> Signup and view all the answers

    Which of the following is a drug interaction associated with NSAIDs?

    <p>Decreased effect of diuretics</p> Signup and view all the answers

    Which of the following is a unique property of aspirin compared to other NSAIDs?

    <p>Irreversible inhibition of COX-1</p> Signup and view all the answers

    What is the primary indication for the use of low-dose aspirin?

    <p>Secondary prophylaxis of MI and unstable angina</p> Signup and view all the answers

    What is the major concern of using aspirin in children and teens for treating viral acute febrile illness?

    <p>Increased risk of Reye's syndrome</p> Signup and view all the answers

    What is the impact of chronic and high-dose intake of aspirin on the kidneys?

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

    Which of the following drugs is known to increase the activity of warfarin?

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

    What is the major difference between the effects of aspirin and ibuprofen on the gastrointestinal system?

    <p>Ibuprofen is better tolerated and has a lower risk of gastrointestinal ADRs</p> Signup and view all the answers

    What is the contraindication of aspirin during pregnancy?

    <p>Closure of patent ductus arteriosus (PDA) in babies</p> Signup and view all the answers

    What is the effect of non-selective COX inhibitors on platelet function?

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

    Which of the following drugs does not interact with oral anticoagulants and oral antidiabetic agents?

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

    What is the main mechanism by which NSAIDs mediate their effects?

    <p>Inhibiting the enzyme cyclooxygenase (COX)</p> Signup and view all the answers

    What is the major risk of paracetamol poisoning?

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

    What is the role of COX-1 in the body?

    <p>It is constitutively expressed in the body and plays a role in maintaining gastrointestinal mucosa lining, kidney function, and platelet aggregation</p> Signup and view all the answers

    Which of the following NSAIDs is classified as a nonselective COX inhibitor with high efficacy and analgesic activity?

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

    What is the effect of NSAIDs on gastrointestinal mucosa?

    <p>They decrease the production of prostaglandins, which can lead to gastrointestinal ulceration</p> Signup and view all the answers

    What is the main difference between COX-1 and COX-2?

    <p>COX-1 is constitutively expressed in the body, while COX-2 is inducibly expressed during an inflammatory response</p> Signup and view all the answers

    Which of the following NSAIDs is contraindicated in patients with kidney disease?

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

    What is the effect of NSAIDs on platelet aggregation?

    <p>They inhibit platelet aggregation, mainly through the inhibition of COX-1</p> Signup and view all the answers

    What is the anti-inflammatory mechanism of NSAIDs?

    <p>Inhibition of prostaglandin synthesis at the site of inflammation</p> Signup and view all the answers

    Study Notes

    NSAIDs Overview

    • NSAIDs have four major actions: anti-inflammatory, analgesic, antipyretic, and antiplatelet
    • Main mechanism of action is inhibiting enzyme COX, which is required to convert arachidonic acid into thromboxanes, prostaglandins, and prostacyclins
    • COX-1 is constitutively expressed in the body and plays a role in maintaining gastrointestinal mucosa lining, kidney function, and platelet aggregation
    • COX-2 is not constitutively expressed in the body and is instead inducibly expressed during an inflammatory response

    Non-Selective COX Inhibitors

    • Examples: Ibuprofen, Aspirin, Indomethacin, Piroxicam, Diclofenac, Naproxen, Ketoprofen, Mefenamic acid
    • Irreversible inhibition of platelets with Aspirin
    • Efficacy varies among non-selective COX inhibitors
    • Ibuprofen is equipotent to Aspirin and has a moderate efficacy
    • Aspirin is an irreversible inhibitor of COX with a moderate efficacy

    Selective COX2 Inhibitors

    • Examples: Celecoxib, Etoricoxib
    • Moderate efficacy

    Actions of NSAIDs

    Anti-Inflammatory Action

    • Main mechanism of action: ↓ prostaglandins synthesis at site of inflammation
    • Other mechanisms of action: free radical scavenging, inhibition of lipooxygenase pathway

    Analgesic Action

    • ↓ pain
    • Used for analgesia and anti-inflammatory action in conditions such as toothache, headache, backache, joint sprains, dysmenorrhea, and mild postoperative pain

    Antipyretic Action

    • ↓ body temperature in fever
    • Paracetamol is preferred as an antipyretic

    Antiplatelet Action

    • Inhibits COX-1, mainly with Aspirin
    • Used for antiplatelet action in low doses for secondary prophylaxis of MI and unstable angina or transient ischaemic attacks

    Adverse Drug Reactions (ADRs)

    • GIT: nausea, vomiting, dyspepsia, gastric erosion, hematemesis
    • Renal: salt and water retention, edema, analgesic nephropathy
    • CVS: closure of patent ductus arteriosus, CCF, MI, stroke
    • Psychiatric reactions: excitement with indomethacin
    • Hepatotoxicity: with large doses of paracetamol
    • Hypersensitivity: skin rash, precipitation of asthma

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    Description

    This quiz covers the mechanisms of action of NSAIDs and Coxibs, including their effects on platelet aggregation, thromboembolic events, and gastrointestinal effects. It also touches on their adverse drug reactions.

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