1. what are the functions of prostaglandins in the body
    • 1. inflammation
    • - erythema, edema, hyperalgesia
    • - do not evoke inflammation by themselves; they potentiate proinflammatory mediators
    • - involved in perio Dz
    • 2. pain
    • - lower threshold of C fiber nocireceptors
    • 3. fever
    • - increase PGE2 synthesis in hypothalamus, leading to raised body temp and decreased heat loss
  2. general role of NSAIDS
    inhibit the functions of prostaglandins by inhibiting cyclooxygenases

    *anti-inflammatory, analgesic, antipyretic*
  3. NSAID pharmacokinetics

    metabolized by P450 enzymes in liver and excreted in urine
  4. NSAID uses
    • analgesic for mild to moderate pain
    • - not for pain of visceral orgin

    • anti-inflammatory
    • - arthritis, general pain from any joint Dz

    • antipyretic
    • - never in kids less than 20 y/o with a viral illness (risk of Reye's Syndrome)

    • cancer prevention
    • - aspirin use has been assoc. w/ decreased risk of colon, stomach, and esophageal cancer
  5. NSAID side effects
    • GI
    • - nausea, diarrhea, ulcers

    • renal
    • - salt and water retention, edema

    • CNS
    • - headache, vertigo, dizziness

    • vascular
    • - inhibits platelet aggregation (elevated risk of bleeding and bruising)
  6. aspirin (acetylsalicylic acid) mode of action
    irreversibly inhibits cyclooxygenase (COX inhibitor)
  7. aspirin uses
    mild to moderate pain not of visceral orgin

    reduces elevated body temp (no effect on regular temp)

    • anti-platelet activity by decreasing thromboxane A2
    • - prolonged bleeding time
    • - stop use 1 week before surgery

    lower dose decreases risk of TIA, MI, etc due to platelet activity
  8. aspirin side effects
    • salicylism
    • - mild intoxication, headache, tinnitus, confusion

    • salicylate poisoning
    • - large dose can be fatal, esp in children
    • - Tx by giving large dose of fluid to induce diuresis and alkalanize the urine
  9. indomethacin uses
    closure of ductus arteriosus

    often more effective to Tx osteoarthritis, ankylosing spondylitis, etc when tolerated
  10. indomethacin side effects
    headaches, aplastic anemia, diarrhea, ulcers, etc

    15-30% of pts stop Rx due to side effects

    not for use in pt w/ renal or peptic ulcer Dz
  11. ketorolac (Toradol) uses
    • potent analgesic
    • moderately anti-inflammatory

    • often given post-operatively
    • equally effective as Demerol
    • short-term substitute for opioids
  12. ibuprofen (Advil, Motrin, etc)
    rapidly absorbed

    half life of 2 hrs

    often better tolerated than aspirin, but still has GI effects
  13. most commonly used NSAID in US
  14. second most used NSAID in US
  15. naproxen (Aleve)
    similar to ibuprofen, but longer half life (14 hours)
  16. NSAID contraindications
    aspirin allergy, renal or kidney problems, etc
  17. celecoxib (Celebrex) uses

    Tx osteoarthritis

    Tx rheumatoid arthritis
  18. celecoxib (Celebrex) mech of action
    selective COX-2 inhibitor
  19. celecoxib (Celebrex) pharmacology
    no effect on bleeding time or platelet function

    lower ulcer rate than non-selective NSAIDS

    COX-2 is constitutive to the kidney, so effects are similar to those of other NSAIDS

    HTN and edema have also been reported
  20. acetominophen uses
    substitute for aspirin



    NOT anti-inflammatory

    no GI problems often seen with NSAIDS
  21. acetominophen side effects
    liver damage at high doses
  22. Tx for acetominophen overdose
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