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Presentation On Non-Steroidal Anti-Inflammatory Drugs

Presentation On Non-Steroidal Anti-Inflammatory Drugs. Presented by: Mahwish Nasir. CELECOXIB DRUG CATEGORY : Coxib(cox-2-inhibitor). Next Drug. KETOROLAC TROMETHAMINE Nonselective Cox inhibitor DRUG CATEGORY : NSAID. Previous Drug.

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Presentation On Non-Steroidal Anti-Inflammatory Drugs

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  1. Presentation On Non-Steroidal Anti-Inflammatory Drugs Presented by: Mahwish Nasir

  2. CELECOXIB DRUG CATEGORY : Coxib(cox-2-inhibitor) Next Drug

  3. KETOROLAC TROMETHAMINE • Nonselective Cox inhibitor • DRUG CATEGORY : NSAID Previous Drug

  4. Celecoxib

  5. Main Menu Celecoxib DRUG DESCRIPTION: Celecoxib is chemically designated as 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzene sulfonamide and is a diaryl-substituted pyrazole. It has the following chemical structure: MECHANISM OF ACTION: • Celecoxib is a highly selective COX-2inhibitor , about 10 – 20 times more selective for COX -2 than for COX-1 . • COX-2 selective inhibitors , were developed in an attempt to inhibit prostacyclin synthesis. • It is done by COX-2 ISO enzyme Induced at sites of inflammation without affecting the action of the constitutively active “house keeping” COX-1 ISO enzyme found in the GI tract, kidneys, and platelets. • COX-2 inhibitors have analgesic, anti-pyretic, and anti-inflammatory effects similar to those of non-selective NSAIDs. Next

  6. Main Menu Celecoxib INDICATIONS: • Rheumatoid arthritis • Osteoarthritis DOSAGE: • Osteoarthritis (adults): 200mg capsule once daily or in two divided doses. • Increase to 200mg twice daily if necessary. Maximum 400mg daily. CHILDREN: not recommended. • Rheumatoid arthritis (adults): 200 to 400mg daily. • CHILDERN: not recommended. Next

  7. Main Menu Celecoxib PHARMACOLOGY: • Pharmacokinetics: • HALF-LIFE(hours): 11 • URINARY EXCRETION: 27% • Pharmacodynamics: • The Coxib continue to be investigated to determine whether their effects on prostacyclin production could lead to a prothrombotic state. • It causes no more edema or renal effects than other members of NSAIDs group. Next

  8. Main Menu Celecoxib CONTRA-INDICATION: • History of hypersensitivity to sulphonamides orNSAIDs. • Active peptic ulceration or GI bleeding. • Severe renal or hepatic impairment. • Severe congestive heart failure. • Safe-use during pregnancy or lactation is not advisable. • Precautions: • Risk of hypovolaemia in elderly patient ( > 65 yrs). • Left ventricular dysfunction. Next

  9. Main Menu Celecoxib INTERACTIONS: • Diuretics • Anti-hypertensive • ACE inhibitors • Anti-coagulants • Lithium • Cyclosporine • Rifampicin • Barbiturates • Fluconazole • Methotrexate Next

  10. Main Menu Celecoxib SIDE-EFFECTS: • Fluid retention • GI upset • Dizziness • Insomnia • Skin rash Next

  11. Main Menu Celecoxib AVAILABLE BRANDS AND PRICES: • CELART(Hilton) Price: • Caps 100mg:10’s: 97.75 • Caps 200mg:10’s: 148.75 • CELBEXX (Getz-pharma) Price: • Caps: 100mg: 20’s :102.00 • Caps: 200mg: 20’s: 170.00

  12. KETOROLAC TROMETHAMINE

  13. Main Menu KETOROLAC TROMETHAMINE Mechanism of action: • It is an NSAID promoted for systemic use. • It inhibits prostaglandin biosynthesis. DRUG DESCRIPTION: Ketorolac is potent analgesic but only a moderately effective anti-inflammatory drug. It is one of the few NSAIDs approved for Perenteral administration. Next

  14. Main Menu KETOROLAC TROMETHAMINE • Indications: • Short -term management of moderate to severe post- operative pain. • Available dosage forms: Oral: • 10mg tablets Perenteral: • 10-30mg per ml for IM or Iv injection. Ophthalmic: • 0.5 % solution. Continue

  15. Main Menu KETOROLAC TROMETHAMINE • Dosage regimen: Adults: • Initially 10mg by IM or bolus IV daily for upto2 days. • Maximum 90mg daily for up to 2 days. Elderly: • Initially 10mg by IM or bolus Iv injection then 10-30mg every 4-6 hours. • Maximum 60mg daily for 2 days. Children: • Under 16 yrs, not recommended. Next

  16. Main Menu KETOROLAC TROMETHAMINE Contra-indication: • Peptic ulcer • GI or cerebrovascular bleeding • Coagulation disorders • Asthma • Renal impairment • Hypovolaemia during dehydration Pregnancy & Lactation: • Safe use during pregnancy and lactation is not advisable. ( NOTE: unless expected benefit outweighs potential risk.) Next

  17. Main Menu KETOROLAC TROMETHAMINE PHARMACOLOGY: Pharmacokinetics: • HALF-LIFE(hours): 4-10 • URINARY EXCRETION: 58% Pharmacodynamics: • The drug does appear to have significant analgesic efficacy and has been used successfully to replace morphine in some situations involving mild to moderate post surgical pain. • When used with an opioid, it may decrease the opioid requirement by 25 to 50%. Precautions: • Homeostasis • Allergic disease • Cardiac dysfunction Next

  18. Main Menu KETOROLAC TROMETHAMINE Interaction: • Anticoagulants • Lithium • Frusemide • Oxypentifylline • NSAIDs • Methotrexate Next

  19. Main Menu KETOROLAC TROMETHAMINE Side effects: • Abnormal liver function tests • Acute renal failure • Bronchospasm • Anaphylaxis • Pain at injection site • Ulcers • Wound hemorrhage • GI disturbances • Dizziness Next

  20. Main Menu KETOROLAC TROMETHAMINE AVAILABLE BRANDS AND PRICES: • TORADOL(Roche) Price: • Inj 30mg :5×1ml : 455.50 • TORAPAN (Duopharma) Price: • Inj 30mg :10×1ml : 589.68. References

  21. Main Menu REFRENCES: • Katzung • Pharma guide • Goodman Gilman

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