First Generation NSAIDs: Mechanism and Adverse Effects
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What is the primary outcome of COX-1 and COX-2 inhibition by First Generation NSAIDs?

  • Reduced pain and fever (correct)
  • Prostaglandin synthesis
  • Enhanced bronchospasm
  • Increased platelet aggregation

    • Which of the following adverse effects is NOT associated with Propionic Acid Derivatives?

  • Gingival hyperplasia
  • Hepatotoxicity
  • Myocardial damage (correct)
  • Hemoptysis

    • What is the primary mechanism of action of acetaminophen?

  • Inhibition of COX-1 and COX-2
  • Inhibition of prostaglandin synthesis
  • Stimulation of platelet aggregation
  • Relief of pain and fever (correct)

    • Which of the following NSAIDs is classified as a Second Generation NSAID?

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

    What is the primary advantage of Second Generation NSAIDs over First Generation NSAIDs?

    <p>Fewer gastrointestinal adverse effects</p> Signup and view all the answers

    Which of the following medications is classified as a Propionic Acid Derivative NSAID?

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

    What is the primary mechanism of action of acetaminophen in relieving pain and fever?

    <p>Decreasing prostaglandins in the CNS to relieve fever and pain</p> Signup and view all the answers

    Which of the following is a contraindication for aspirin use?

    <p>Allergy to sulfonamides</p> Signup and view all the answers

    What is the primary therapeutic use of aspirin in low doses?

    <p>Decreasing platelet aggregation to prevent MI and stroke</p> Signup and view all the answers

    Which of the following medications is considered safer for individuals with sensitive stomachs?

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

    What is the primary adverse effect of acetaminophen overdose?

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

    What is the primary mechanism of action of NSAIDs in reducing inflammation?

    <p>Inhibiting the synthesis of prostaglandins by blocking COX enzymes</p> Signup and view all the answers

    What is a common adverse effect of NSAIDs, particularly in the stomach?

    <p>GI bleeding</p> Signup and view all the answers

    Which of the following is NOT a characteristic of third-generation H1 receptor antagonists?

    <p>More anti-cholinergic effects</p> Signup and view all the answers

    What is the primary indication for acetaminophen?

    <p>Pain and fever reduction</p> Signup and view all the answers

    Which enzyme is responsible for producing prostaglandins, and is inhibited by NSAIDs?

    <p>Cyclooxygenase (COX)</p> Signup and view all the answers

    What is a potential contraindication for the use of NSAIDs?

    <p>Renal impairment</p> Signup and view all the answers

    Which of the following is a potential therapeutic benefit of COX-2 inhibition in NSAIDs?

    <p>Reduced risk of myocardial infarction</p> Signup and view all the answers

    What is the primary mechanism by which acetaminophen exerts its analgesic effect?

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

    Which of the following is a characteristic of Third Generation H1 Receptor Antagonists?

    <p>Reduced sedation and drowsiness</p> Signup and view all the answers

    What is the primary adverse effect of acetaminophen overdose?

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

    Which of the following NSAIDs is likely to have the most significant anti-inflammatory effects?

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

    Which of the following is a common adverse effect of NSAIDs, particularly in the kidney?

    <p>Renal blood flow reduction</p> Signup and view all the answers

    What is the primary reason why acetaminophen is preferred over aspirin in pediatric patients?

    <p>Because it is less likely to cause Reye's syndrome</p> Signup and view all the answers

    Which of the following is a characteristic of ibuprofen that is not shared with acetaminophen?

    <p>It has anti-inflammatory effects</p> Signup and view all the answers

    What is the primary mechanism by which aspirin and ibuprofen reduce the risk of myocardial infarction and stroke?

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

    Which of the following is a potential adverse effect of long-term use of NSAIDs?

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

    What is the primary mechanism by which acetaminophen reduces fever?

    <p>By inhibiting the production of prostaglandins in the CNS</p> Signup and view all the answers

    Which of the following is a characteristic of aspirin that is not shared with ibuprofen?

    <p>It is more effective in reducing platelet aggregation</p> Signup and view all the answers

    What is the primary mechanism of pain relief for propionic acid derivatives, such as ibuprofen?

    <p>Inhibition of COX-2, leading to reduced prostaglandin synthesis</p> Signup and view all the answers

    What is the primary concern with high-dose acetaminophen use?

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

    What is the primary advantage of COX-2 inhibitors, such as celecoxib, over non-selective NSAIDs?

    <p>Reduced risk of gastrointestinal adverse effects</p> Signup and view all the answers

    What is the primary mechanism of anti-inflammatory action for aspirin?

    <p>Inhibition of COX-2, leading to reduced prostaglandin synthesis</p> Signup and view all the answers

    What is a potential complication of NSAID use in patients with pre-existing kidney disease?

    <p>Nephrotoxicity and elevated BUN and creatinine</p> Signup and view all the answers

    Study Notes

    Nonsteroidal Anti-inflammatory Drugs (NSAIDs)

    • Inhibit the synthesis of prostaglandins, which respond to the inflammatory response
    • COX (cyclooxygenase) enzymes, which produce prostaglandins, are inhibited by NSAIDs
    • COX enzymes occur in various areas, including:
      • Tissue injury, where they promote inflammation and sensitize to painful stimuli
      • Stomach, where they protect gastric mucosa
      • Platelets, where they stimulate aggregation
      • Blood vessels, where they cause vasodilation
      • Kidney, where they maintain renal blood flow
      • Brain, where they mediate fever and pain perception

    First Generation NSAIDs (inhibit both COX1 and COX2)

    • Salicylates:
      • Prototype: aspirin
      • Relieve pain, antipyretic, and suppress platelet aggregation
    • Propionic Acid Derivatives:
      • Prototype: ibuprofen
      • Inhibit prostaglandin synthesis
      • Adverse effects:
        • Dry mouth
        • Gingival hyperplasia
        • Dyspepsia
        • Heartburn
        • Nausea
        • Epigastric pain
        • Constipation
        • GI ulceration
        • Nephrotoxicity
        • Elevated BUN and creatinine
        • Dyspnea
        • Bronchospasm
        • Hemoptysis
      • Others include naproxen and ketorolac (injectable drug often used for pain)

    Non-NSAID

    • Prototype: acetaminophen
    • Non-narcotic analgesic
    • Relieves pain and fever
    • Large number of prescription and OTC meds
    • Adverse effects:
      • Hepatotoxicity
      • Renal failure
      • Myocardial damage if high doses

    Second Generation NSAIDs (inhibit only COX-2)

    • Prototype: celecoxib
    • Referred to as coxibs
    • Expensive
    • Seems to be less bleeding, especially initially, but maybe not for long term
    • Contraindicated if allergic to sulfonamides, NSAIDs, or aspirin

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    Description

    Test your knowledge on the first generation of NSAIDs, including salicylates and propionic acid derivatives, their mechanisms of action, and their numerous adverse effects. Learn about the prototypes of these medications, such as aspirin and ibuprofen, and their impact on the body.

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