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Presentation on Non Steroidal Anti-inflammatory Agents
- 1. ANTI-INFLAMMATORY AGENTS • Drugsthat relieve pain, reduce inflammation and reduce temperature • Blocks the production of Prostaglandins which is responsible for pain and swelling of inflammatory conditions.
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- 3. • Prostaglandins arethe mediators of inflammation. • NSAIDs are irreversible inhibitors of cyclooygenase activity thus they prevent the formation of prostaglandins and reduces the symptoms of inflammation.
- 4. Classification • Salicylates- aspirin,sodium salicylate • Propionic acid derivative (profens)- ibuprofen, naproxen • Indole derivative- indomethacin, sulindac • Pyrrole acetic acid derivative- ketorolac, tolmetin, zomepirac • Anthranilates (fenamates)- diclofenac, mefenamic acid • Oxicam derivative- piroxicam • Phenylpyrazolones- phenylbutazone, antipyrine
- 5. Salicylates • Derivatives of2-hydroxy benzoic acid. • Used as analgesic to relieve pain. • MOA- inhibit cyclooxygenase and reduce levels of PGE2 SAR- • -COOH & -OH replacement decreases activity • Reduction of –COOH to –CONH2, retains analgesic property but devoid of anti-inflammatory activity. Eg Slicylamide • -OH at meta or para to –COOH decreases activity • Halogen on aromatic ring inceases activity as well as toxicity. • Substitution of hydrophobic aryl group at 5th position improves activity. COOH OH SALICYLIC ACID
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- 7. Sodium Salicylate • MOA- •Blocks synthesis of PG by inhibiting cyclooxygenase which converts arachidonic acid to cyclic endoperoxides,precursor of PG • Uses- relieve pain, fever, treatment of gout OH O - Na + O
- 8. ASPIRIN • MOA- • InhibitCOX-1 & COX-2 and decrease formation of PG and thromboxane • Uses- relief pain, inflammation associated with rheumatoid arthritis, osteoarthritis • Side effects- effects of overdose tinitus, hypokalemia, hypoglycemia, hypotention OCOCH 3 OH O
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- 10. PROPIONIC ACID DERIVATIVE(PROFENS) • Contain chiral carbon in the alpha position of acetic acid side chain IBUPROFEN • Non selective Inhhibitor of COX which is used for PG synthesis. • Uses-treatment of rheumatoid arthritis, osteoarthritis, management of desmenorrhea, spondylytis, gout. • Adverse effect- edema, nausea, vomiting, peptic ulcer, GI bleeding COOH CH3 CH3 C H3
- 11. NAPROXEN • MOA • InhibitCOX-1 and COX-2 • Uses-treatment of rheumatoid arthritis, osteoarthritis, management of desmenorrhea, spondylitis, gout. • AE- nephrotoxicity, drowsiness, nausea, vomiting COOH CH3 H3CO
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- 13. SAR • Carboxyl groupis essential for anti-inflammatory activity. • Substitution at R1, C6H4CH2>CH3>H • Presence of indole Nitrogen is not essential, 1- benzylidenylindene analogue is also active. Eg sulindac • 5-methoxy in indomethacin is imp. • Presence of Cl or F at para position of phenyl is imp. For antiinflammatory activity.
- 14. INDOMETHACINE • MOA • InhibitCOX 1 and COX 2 • Inhibit Phospholipase A2 enzyme responsible for releasing arachidonic acid from phospholipids. • Uses • Rheumatoid arthritis, osteoarthritis, spondylitis N H3CO COOH CH3 O Cl INDOMETHACIN
- 15. SULINDAC • MOA • InhibitCOX 1 and COX 2 which leads to inhibition of PG • Uses • Rheumatoid arthritis, osteoarthritis, spondylitis, gout F COOH CH3 S C H3 O SULINDAC
- 16. PYRROLE ACETIC ACIDDERIVATIVE O N OH O KETOROLAC N O H O CH3 C H3 O TOLMETIN ZOMEPIRAC N O H O Cl C H3 O CH3
- 17. TOLMETIN • MOA • InhibitPG Synthesis • Uses • Rheumatoid arthritis, osteoarthritis, spondylitis N O H O CH3 C H3 O TOLMETIN
- 18. ZOMEPIRAC • MOA • DecreasePG Synthesis • Withdrawn from market due to its adverse effect, anaphylactic reactions. ZOMEPIRAC N O H O Cl C H3 O CH3
- 19. KETOROLAC • MOA • InhibitCOX-1 and COX-2 LEADS TO INHIBITION OF PG Synthesis • Uses • Potent NSAID used to treat moderate to severe pain O N OH O KETOROLAC
- 20. OXICAM DERIVATIVE PIROXICAM • NSAIDused to relieve symptoms of painful inflammatory conditions like arthritis • Inhibit COX-1, Prevents production of PG involved in mediation of swelling and pain. N NH O S O O OH
- 21. ANTHRANILATES (FENAMATES) • N-arylsubstituted derivatives of anthranilic acid. • SAR • Position of –COOH is imp. For activity • Replacement of –COOH by tetrazole retains the activity. • Substitution on anthranilic acid ring reduces the activity. • Replacement of –NH , no acticity COOH NH
- 22. DICLOFENAC • Inhibit COX-1and COX-2 • Uses-treatment of rheumatoid arthritis, osteoarthritis • Adverse effect- hepatotoxicity COOH NH Cl Cl
- 23. Mefenamic acid • InhibitCOX-1 and COX-2 • Uses-used for mild to moderate pain and primary dysmenorrhea HOOC NH C H3 CH3
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- 25. PHENYLBYTAZONE • Inactivate PGsynthase through peroxide mediated deactivation • Reduce production of PG. • Use- spondylitis N N O O CH3 PHENYLBUTAZONES
- 26. ANTIPYRINE • Inhibit COX-1AND COX-2 involved in PG synthesis. • Analgesic N N CH3 O C H3 ANTIPYRINE