NSAIDs

• Analgesic, antipyretic, and anti-inflammatory effects
• Inhibits cyclooxygenase (COX) which in turn blocks prostaglandin formation.
• Should not be used in patients with asthma as it may produce bronchoconstrictor mediators (leukotrienes)
• Joint concentrations remain constant while serum concentrations vary
• Adverse Effects:
  • GI – Nausea/vomiting, indigestion, ulceration/bleeding, diarrhea
    • Should not be used in patients with IBD due to risk of ulcerations and bleeding
  • Renal – Salt and fluid retention, HTN
    • Due to inhibition of prostaglandin synthesis (a vasodilator)
  • Increased bleeding tendency
  • Not recommended during pregnancy, especially third trimester.
• Drug Interactions:

Arachidonic Acid Pathway

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Prostaglandins

• Inflammatory response
• increases pain sensitivity
• Pyrogenic (induces fever)
• Protect stomach (increase bicarb and mucin levels)
• Stimulates uterine contractions
• Maintain patency of ductus arteriosus

Thromboxanes

• platelet aggregation
• Platelet release
• A vasoconstrictor
• Aspirin
  • Analgesia - 325mg - 1gm qd
  • Antiinflammatory - 3-6gm qd
  • Prolongs bleeding time (irreversibly inhibits cyclooxygenase)
  • increased incident of Reye's syndrome in children when used for febrile viral infections
  • Drug of choice for RA
  • Contraindications:
    • Gout - inhibits excretion of uric acid
    • Asthmatic
    • Coumadin
• Diclofenac (Voltaren)
  • 50mg PO bid/tid
  • Arthrotec - Diclofenac/Misoprostol
    • 50/200, 75/200
    • Combined with 200μ Misoprostol which is a GI protector making safer with patients with sensative stomachs
• Ibuprofen
  • 300-800mg PO qid
  • A minimum of 1,800mg and a maximum dose of 2,400mg qd best for inflammatory conditions
  • Pediatric formulation - 5-10mg/kg PO q6h
• Indomethacin
  • 25-50mg tid
  • Used to treat inflammation caused by gout
• Ketorolac Tromethamine (Toradol)
  • 30mg IV/IM q6h - First IM dose may be 60mg
  • 10mg PO q4-6h
  • indicated for short term (less than 5 days) management of moderate/severe post-op pain when opioid level analgesia is desired
• Naproxen Naprosyn, Aleve
  • 250-500mg PO bid

NSAID's COX-2 Inhibitors

• Rofecoxib (Vioxx)
  • Osteoarthritis 12.5-25mg qd
  • Pain 50mg qd
  • not contraindicated in patients with stomach problems or patients on anticoagulants
• Celecoxib (Celebrex)
  • Osteoarthritis: 200mg PO QD or 100mg PO BID
  • Rheumatoid Arthritis: 100-200mg BID
  • not contraindicated in patients with stomach problems or patients on anticoagulants
  • contraindicated in patients with sulfa allergy