How NSAIDs Work
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Questions and Answers

What is one of the effects of prostaglandin E2 in the stomach?

  • Increasing the production of protective mucus (correct)
  • Increasing the secretion of acid
  • Decreasing the production of protective mucus
  • Reducing uterine contractions

    • What is the main difference between irreversible and reversible COX inhibitors?

  • Their mechanism of action
  • Their effectiveness in treating pain
  • Their ability to inhibit COX-1 and COX-2
  • Their duration of action (correct)

    • How does aspirin work as an antiplatelet medication?

  • By irreversibly inhibiting COX-1 (correct)
  • By increasing thromboxane A2 production
  • By reversibly inhibiting COX-1
  • By inhibiting COX-2

    • What is the effect of aspirin on bleeding time?

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

    What is the anti-inflammatory effect of salicylate?

    <p>Inhibiting COX-2</p> Signup and view all the answers

    What is the dose-dependent effect of aspirin?

    <p>Antiplatelet effect at low doses</p> Signup and view all the answers

    What is the difference between non-selective COX inhibitors and selective COX-2 inhibitors?

    <p>Their ability to inhibit COX-1</p> Signup and view all the answers

    What is the effect of non-selective COX inhibitors on aspirin's antiplatelet effect?

    <p>It decreases the antiplatelet effect</p> Signup and view all the answers

    What is the indication for indomethacin in neonates and premature infants?

    <p>Closure of patent ductus arteriosus</p> Signup and view all the answers

    What is the main difference between celecoxib and other NSAIDs?

    <p>Its lack of antiplatelet effect</p> Signup and view all the answers

    What is the mechanism of action of NSAIDs?

    <p>Inhibition of COX enzymes</p> Signup and view all the answers

    Which COX inhibitor is selective for COX-2?

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

    What is the primary difference between reversible and irreversible COX inhibitors?

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

    What is the indication for aspirin that is not shared with other NSAIDs?

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

    What is the side effect of NSAIDs that is most severe in the aspirin coop?

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

    What is the condition associated with Samter’s triad?

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

    What is the medication that is used to close patent ductus arteriosus?

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

    What is the side effect of aspirin that is represented by a young man wearing headphones?

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

    What is the medication that is represented by a bulletproof vest?

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

    What is the indication for NSAIDs that is not shared with aspirin?

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

    What is the primary function of NSAIDs in the body?

    <p>To decrease the production of prostaglandins</p> Signup and view all the answers

    What is the source of arachidonic acid in the body?

    <p>Membrane phospholipids broken down by phospholipase A2</p> Signup and view all the answers

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

    <p>COX-1 is constitutive, while COX-2 is inducible</p> Signup and view all the answers

    What is the effect of prostaglandins on nociceptors?

    <p>They decrease the threshold for activation</p> Signup and view all the answers

    What is the role of cyclooxygenase in the body?

    <p>It converts arachidonic acid into prostaglandins</p> Signup and view all the answers

    What is the outcome of increased prostaglandin production in the body?

    <p>Increased vasodilation and pain</p> Signup and view all the answers

    What is the advantage of combining aspirin with a selective COX-2 inhibitor?

    <p>It does not decrease the antiplatelet effect of aspirin.</p> Signup and view all the answers

    What is the effect of COX-1 inhibition in the stomach?

    <p>It decreases the concentration of cytoprotective prostaglandins.</p> Signup and view all the answers

    Why do NSAIDs inhibit COX-2 in the kidneys?

    <p>To decrease the level of prostaglandins that dilate the renal artery.</p> Signup and view all the answers

    What is the effect of low doses of aspirin taken right before bedtime?

    <p>It lowers blood pressure.</p> Signup and view all the answers

    What is the-term for the combination of asthma, nasal polyps, and NSAID hypersensitivity?

    <p>Samter's triad</p> Signup and view all the answers

    Why should aspirin not be given to children with viral infections to reduce fever?

    <p>It can lead to Reye's syndrome.</p> Signup and view all the answers

    What is the effect of high doses of salicylate on the body?

    <p>It inhibits oxidative phosphorylation.</p> Signup and view all the answers

    What is the treatment for aspirin overdose?

    <p>Administration of activated charcoal and alkalization of urine.</p> Signup and view all the answers

    What is the term for the condition characterized by liver damage and progressive encephalopathy?

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

    What is the term for the NSAID-induced condition characterized by chronic nephritis or renal papillary necrosis?

    <p>Analgesic nephropathy</p> Signup and view all the answers

    What is the primary function of phospholipase A2 in the context of inflammation?

    <p>To take membrane phospholipids and produce arachidonic acid</p> Signup and view all the answers

    What is the effect of prostaglandin E2 on nociceptors?

    <p>It increases their sensitivity to stimuli</p> Signup and view all the answers

    Which of the following is NOT a characteristic of COX-1?

    <p>It is triggered by immune cells and vascular endothelial cells</p> Signup and view all the answers

    What is the effect of NSAIDs on prostaglandins?

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

    What is the source of arachidonic acid in the body?

    <p>It is produced from membrane phospholipids</p> Signup and view all the answers

    What is the effect of cyclooxygenase on arachidonic acid?

    <p>It converts arachidonic acid into prostaglandins</p> Signup and view all the answers

    What is the primary effect of aspirin on platelet function?

    <p>Decrease in thromboxane A2 production</p> Signup and view all the answers

    Which of the following NSAIDs is available in parenteral form?

    <p>Ketorolac, ibuprofen, and indomethacin</p> Signup and view all the answers

    What is the primary indication for celecoxib?

    <p>Treatment of pain and inflammation</p> Signup and view all the answers

    What is the effect of aspirin on bleeding time?

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

    Which of the following is a characteristic of irreversible COX inhibitors?

    <p>Irreversible inhibition of COX-1 and COX-2</p> Signup and view all the answers

    What is the primary mechanism of action of NSAIDs?

    <p>Inhibition of COX-1 and COX-2</p> Signup and view all the answers

    Which of the following NSAIDs is used to treat severe acute pain?

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

    What is the effect of low doses of aspirin on platelet function?

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

    What is the primary difference between aspirin and non-aspirin NSAIDs?

    <p>Aspirin is irreversible, while non-aspirin NSAIDs are reversible</p> Signup and view all the answers

    Which of the following is a characteristic of selective COX-2 inhibitors?

    <p>Lack of antiplatelet effect</p> Signup and view all the answers

    What is the primary mechanism of action of NSAIDs in treating pain, inflammation, and fever?

    <p>Inhibition of COX enzymes</p> Signup and view all the answers

    Which of the following medications is NOT used to treat gout?

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

    What is the primary difference between the effects of aspirin and reversible COX inhibitors on the stomach?

    <p>Aspirin causes more severe bleeding</p> Signup and view all the answers

    Which of the following medications is used to treat pain, inflammation, and fever, but not gout?

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

    What is the primary effect of COX-2 inhibition in the kidneys?

    <p>Increased blood pressure</p> Signup and view all the answers

    Which of the following is a common side effect of NSAIDs that is most severe with aspirin?

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

    What is the primary indication for ketorolac?

    <p>Post-surgical pain relief</p> Signup and view all the answers

    Which of the following is NOT a side effect of aspirin overdose?

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

    What is the primary difference between the effects of COX-1 and COX-2 inhibition?

    <p>COX-1 inhibition affects the stomach</p> Signup and view all the answers

    Which of the following medications is used to treat a specific condition in neonates and premature infants?

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

    What is the reason why selective COX-2 inhibitors cause the least gastrointestinal side effects?

    <p>They don't affect COX-1 in the stomach</p> Signup and view all the answers

    What is the mechanism by which low doses of aspirin taken right before bedtime can lower blood pressure?

    <p>The mechanism is still being studied</p> Signup and view all the answers

    What is the result of chronic abuse of NSAIDs in individuals with underlying heart, liver, or kidney disease?

    <p>It can lead to analgesic nephropathy</p> Signup and view all the answers

    What is the reason why people with nasal polyps and asthma are more likely to experience NSAID hypersensitivity?

    <p>They are more likely to have Samter's triad</p> Signup and view all the answers

    What is the effect of high doses of salicylate on the body's energy production?

    <p>It inhibits oxidative phosphorylation</p> Signup and view all the answers

    What is the treatment for aspirin overdose that helps facilitate salicylate excretion?

    <p>Alkalization of urine by sodium bicarbonate</p> Signup and view all the answers

    What is the difference between the effects of aspirin and other NSAIDs on the renin-angiotensin-aldosterone system?

    <p>Aspirin increases blood pressure, while other NSAIDs decrease it</p> Signup and view all the answers

    What is the outcome of increased lactic acid production in the body due to salicylate overdose?

    <p>It leads to metabolic acidosis</p> Signup and view all the answers

    What is the reason why aspirin should not be given to children with viral infections to reduce fever?

    <p>It can lead to Reye's syndrome</p> Signup and view all the answers

    What is the effect of salicylate on the blood-brain barrier at high doses?

    <p>It shifts towards its non-ionized form, salicylic acid, and crosses the blood-brain barrier</p> Signup and view all the answers

    Which of the following effects of prostaglandin E2 is NOT mentioned in the text?

    <p>Increasing the production of acid in the stomach</p> Signup and view all the answers

    What is the primary mechanism of action of acetaminophen?

    <p>Reversibly inhibiting COX in the central nervous system</p> Signup and view all the answers

    What is the main reason why acetaminophen is preferred over aspirin in certain individuals?

    <p>It does not affect COX in platelets and the stomach</p> Signup and view all the answers

    What is the toxic metabolite produced by the metabolism of acetaminophen?

    <p>N-acetyl-p-benzoquinone imine</p> Signup and view all the answers

    What is the primary treatment for acetaminophen toxicity?

    <p>Administration of N-acetylcysteine</p> Signup and view all the answers

    What is the condition that can occur in children after a viral infection and is associated with the use of aspirin?

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

    What is the main difference between the effects of acetaminophen and NSAIDs?

    <p>Acetaminophen does not inhibit COX peripherally</p> Signup and view all the answers

    What is the role of glutathione in the metabolism of acetaminophen?

    <p>It inactivates the toxic metabolite produced by acetaminophen</p> Signup and view all the answers

    What is the primary indication for acetaminophen in children?

    <p>Fever and mild to moderate pain</p> Signup and view all the answers

    What is the common characteristic of individuals who are more susceptible to acetaminophen toxicity?

    <p>They have a lower glutathione level</p> Signup and view all the answers

    What is the primary effect of prostaglandin E2 on the body?

    <p>It increases the sensitivity of nociceptors to pain</p> Signup and view all the answers

    What is the role of cyclooxygenase in the production of prostaglandins?

    <p>It converts arachidonic acid to prostaglandin E2</p> Signup and view all the answers

    What is the primary effect of acetaminophen on prostaglandin production?

    <p>It decreases the production of prostaglandin E2</p> Signup and view all the answers

    What is the mechanism by which COX-2 is induced during inflammation?

    <p>It is induced by immune cells and vascular endothelial cells</p> Signup and view all the answers

    What is the primary effect of prostaglandin E2 on blood vessels?

    <p>It causes vasodilation</p> Signup and view all the answers

    What is the primary source of arachidonic acid in the body?

    <p>It is produced by phospholipase A2</p> Signup and view all the answers

    Study Notes

    Prostaglandins and Inflammation

    • Prostaglandin E2 causes uterine contractions, decreases acid secretion, and increases protective mucus production in the stomach.
    • Prostaglandins are involved in inflammation, pain, and fever.

    NSAIDs and COX Enzymes

    • NSAIDs work by inhibiting cyclooxygenase (COX) enzymes.
    • COX enzymes have two isoforms: COX-1 and COX-2.
    • COX-1 is a constitutive enzyme, always active, while COX-2 is inducible and triggered by immune cells and vascular endothelial cells during inflammation.

    Aspirin (Irreversible COX Inhibitor)

    • Works by irreversibly inhibiting both COX-1 and COX-2.
    • Taken orally, with most absorption in the ileum.
    • Irreversibly inhibits COX-1 in platelets, decreasing thromboxane A2 production, making it useful as an antiplatelet medication.
    • Effects persist until new platelets are produced that can synthesize COX-1 enzymes.
    • Increases bleeding time without affecting PT or PTT.
    • Metabolized in the liver to salicylate, which has anti-inflammatory properties.
    • Used to treat headaches, musculoskeletal pain, osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.
    • Effects are dose-dependent: low doses (under 300 mg/day) work as an antiplatelet medication, medium doses (300-2400 mg/day) work as an antipyretic and analgesic, and high doses (over 2400 mg/day) work as an anti-inflammatory medication.

    Non-Selective COX Inhibitors (Reversible)

    • Include ibuprofen, naproxen, ketorolac, indomethacin, sulindac, and meloxicam.
    • Reversibly inhibit both COX-1 and COX-2.
    • Can be taken orally or parenterally (ketorolac, ibuprofen, and indomethacin).
    • Have antiplatelet effects, but are transient due to reversible inhibition.
    • Inhibit COX-2, reducing inflammation, pain, and fever.
    • Used to treat pain, inflammation, and fever, as well as gout, patent ductus arteriosus, and acute pain after surgery.

    Selective COX-2 Inhibitors

    • Include celecoxib.
    • Reversibly inhibit COX-2, reducing inflammation, pain, and fever.
    • Lack antiplatelet effects.
    • Used to treat pain, inflammation, and fever.

    Side Effects and Precautions

    • NSAIDs can cause gastrointestinal problems (gastritis, ulcers, bleeding) by blocking COX-1.
    • NSAIDs can cause kidney damage and hypertension by inhibiting COX-2.
    • Hypersensitivity reactions can occur, including Stevens-Johnson Syndrome, toxic epidermal necrolysis, and anaphylaxis.
    • Cross-hypersensitivity can occur between NSAIDs.
    • Individuals with nasal polyps and asthma are more likely to experience NSAID hypersensitivity (Samter's triad).
    • Aspirin overdose can be fatal, causing tinnitus, deafness, headache, vomiting, respiratory alkalosis, and metabolic acidosis.
    • Treatment of aspirin overdose includes activated charcoal, urinary alkalization, ventilatory support, and management of acid-base imbalance.### Prostaglandin E2 and NSAIDs
    • Prostaglandin E2 causes uterine contractions, decreases acid secretion, and increases protective mucus production in the stomach
    • NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) inhibit cyclooxygenase, decreasing prostaglandin production, and are used to treat inflammation, pain, and fever

    Classification of NSAIDs

    • Irreversible COX inhibitors: aspirin (acetylsalicylic acid)
    • Reversible COX inhibitors:
      • Non-selective COX inhibitors: ibuprofen, naproxen, ketorolac, indomethacin, sulindac, meloxicam
      • Selective COX-2 inhibitors: celecoxib

    Aspirin (Acetylsalicylic Acid)

    • Irreversibly inhibits COX-1 and COX-2
    • Taken orally, absorbed in the ileum
    • Decreases thromboxane A2 production in platelets, making it an antiplatelet medication
    • Effect persists until new platelets are produced
    • Metabolized into salicylate in the liver, which has anti-inflammatory properties
    • Used to treat headaches, musculoskeletal pain, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis
    • Dose-dependent effects:
      • Low doses (<300 mg/day): antiplatelet medication
      • Medium doses (300-2400 mg/day): antipyretic and analgesic
      • High doses (>2400 mg/day): anti-inflammatory medication

    Non-Selective COX Inhibitors

    • Reversibly inhibit COX-1 and COX-2
    • Include ibuprofen, naproxen, ketorolac, indomethacin, sulindac, meloxicam
    • Available in oral and parenteral forms (except sulindac and meloxicam)
    • Antiplatelet effect is transient and competes with aspirin's effect
    • Used to treat pain, inflammation, and fever, including gout, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis
    • Indomethacin also used to close patent ductus arteriosus in neonates and premature infants
    • Ketorolac used to treat severe acute pain, usually after surgery

    Selective COX-2 Inhibitors

    • Celecoxib
    • Reversibly inhibits COX-2, reducing inflammation, pain, and fever
    • Lacks antiplatelet effect
    • Used to treat pain, inflammation, and fever, including osteoarthritis, rheumatoid arthritis, ankylosing spondylitis

    Side Effects of NSAIDs

    • Gastritis and gastric ulcers (most severe with aspirin)
    • Kidney damage and hypertension
    • Cross-hypersensitivity between NSAIDs

    Acetaminophen

    • Reversibly inhibits COX in the central nervous system
    • Used to treat fever and mild to moderate pain
    • Not an NSAID due to lack of peripheral COX inhibition
    • Indications: fever, myalgia, headache
    • Preferred in individuals with bleeding disorders, peptic ulcers, or allergies to aspirin
    • First-line therapy for children with fever or pain (due to risk of Reye's syndrome with aspirin)
    • Metabolized by hepatocytes in the liver
    • Can cause liver toxicity due to NAPQI production
    • Treatment: administration of N-acetylcysteine (NAC)

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    Description

    Learn how Non-steroidal anti-inflammatory drugs (NSAIDs) reduce inflammation, relieve pain, and lower fever by decreasing the production of prostaglandins. Understand the body's response to harmful stimuli and how NSAIDs interact with it.

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