4. NSAID

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Pharmacology
Third Year

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4. NSAID

  1. 1. CLASSIFICATION 1. NON SELECTIVE COX INHIBITORS: a. Salycilates: Aspirin b. Ibuprofen c. Indomethacin d. Diclofenac f. Piroxicam g. Mefenamic acid 2. SELECTIVE COX-2 INHIBITORS: Celecoxib, Meloxicam 2. ANALGESIC, ANTIPYRETIC WITH POOR ANTI- INFLAMMATORY ACTION: Paracetamol Non-Steroidal Anti-inflammatory Drugs (NSAIDs)
  2. 2. NSAIDs • Mechanism of Action • Inhibits cyclo-oxygenase enzyme = ↓↓ Prostaglandin synthesis COX-I Most cells in the body COX-II Inflammatory and immune cells COX-III Hypothalamic temperature control center NSAIDs that act on COX-I, COX-II & COX-III, more side effects Selective COX-II NSAIDs, less side effects
  3. 3. NSAIDs Common Pharmacological Effects • Analgesic (CNS and peripheral effect) • Antipyretic (CNS effect) • Anti-inflammatory (except Paracetamol) • Antiplatelet effect: – prevents platelet aggregation. ( Aspirin low dose) Common Adverse Effects • Gastritis and peptic ulceration with bleeding (inhibition of PG + other effects) • Platelet Dysfunction • Acute Renal Failure in susceptible persons • Sodium+ water retention and edema • Analgesic nephropathy
  4. 4. NSAIDs ASPIRIN: Actions & Uses Antiplatelet: Prophylaxis of angina & myocardial infarction (MI) Analgesic : Mild to moderate pain Acute dental pain as in pulpitis, dentoalveolar abscess or post dental surgical procedures. Headache, musculoskeletal pain & arthritic pains Anti-inflammatory: Rheumatic fever, rheumatoid arthritis, Antipyretic : Fever
  5. 5. NSAIDs Adv effects of Aspirin Gastritis, Peptic ulcer & GI bleeding. Reyes’ syndrome in children with viral fever Salicylism:  doses => Tinnitus, vertigo, vomiting &hearing Contraindications: • Bleeding disorders (Hemophilia), • Peptic ulcer, • Children with Viral fever, • Hypersensitivity/bronchial asthma,
  6. 6. NSAIDs INDOMETHACIN – Potent NSAID. Non selective COX-inhibitor, Inhibition of Phospholipase A & C, ↓ PMN migration. Uses; Acute gouty arthritis, ankylosing spondylitis, osteoarthritis, Medical closure of Patent Ductus Arteriosus Uterine relaxant ( tocolytic agent ).
  7. 7. NSAIDs PARACETAMOL • Antipyretic, Analgesic & Weak Anti-inflammatory Uses: Fever, Headache, myalgias, etc. Safe in patients with peptic ulcer, hemophilia, children with viral fever, bronchial asthma Adv effects: Least GI and platelet effects •  dosage = Hepatic damage due to accumulation of a toxic metabolite, N-acetyl-benzoquinone Antidotes: Acetylcysteine & Methionine
  8. 8. NSAIDs SelectiveCOX-2 Inhibitors (COXIBs) • Meloxicam, Celecoxib • More selective inhibition of Cyclooxygenase-II enzyme • Long duration of action – given once or twice daily -- better patient compliance • Least GI effects Adverse effects: • Thrombosis (Risk of myocardial infarction & stroke ) • Nephrotoxicity

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