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Pharmacology of Drug -Nimesulide |
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Mechanism of Action |
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This Non Steroidal Anti Inflammatory Drug reduces prostaglandin synthesis by the inhibition of cyclo oxygenase enzyme2 selectively. This is a weaker inhibition .So it produces weaker analgesic property. Its potent anti-inflammatory activity is due to its action on various stages of inflammation. This leads to the inhibition of super oxide anion formation invitro by activated neutrophil, inhibition of histamine release from tissue mast cells and basophiles. Additionally it also prevents platelet activating factor synthesis and metalloproteinase synthesis thus prevents the breakdown of osteoarthritic human cartilage. It also prevent tumor necrosis factor alpha and thus reduce the formation of cytokines. This drug can activate glucocorticoid receptors in the body. |
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Pharmaco Kinetics |
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Absorption-Completely absorbed after oral administration. Distribution-Widely distributed in the body and extensively bind to the plasma proteins i.e.99%. Metabolism-It is metabolized in liver to its metabolites.4-hydroxyl derivative is its one active metabolite. Excretion - Excreted via urine and bile. |
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Onset Of Action |
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30 to 60 minutes |
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Half Life |
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Its plasma half life is long-nearly 2days |
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Duration Of Action |
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8-10 hours |
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Adverse Effects |
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1. Nausea 2. Vomiting 3. Diarrhea 4. Heart burn 5. Epigastric pain 6. Pruritis 7. Skin rash 8. Headache 9. Dizziness 10.Somnolence |
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ContraIndications |
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1. Hypersensitivity to this drug 2. Active peptic ulcer 3. Hepatic impairment |
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Special Precautions |
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1. Renal impairment 2. Heart failure 3. Alcohol abuse 4. Colitis 5. Crohns disease 6. Diverticulitis 7. Gastric ulcer 8. Diabetis mellitus 9. Hemarrhoids 10. Hepatic failure 11. Rectal irritation or bleeding |
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Pregnancy |
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Contraindicated |
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Breast Feeding |
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Contraindicated |
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Old Age |
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Use with caution |
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Children |
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Use with caution |
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Interactions |
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Fenofibrate, Salicyclic acid, Valproic acid and Tolbutamide: These drugs displace nimesulide from the plasma binding sites. Methotrexate and Frusemide: These drugs may be displaced from plasma proteins by nimesulide. Warfarin: Exercise caution since efficacy may be increased. Theophylline: Efficacy of slow release theophylline preparations reduced. |
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Indications |
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1. Painful inflammatory conditions associated with - Musculoskeletal system, Dysmenorrhea, Thrombophlebitis, Gout 2. Dental pain 3. ENT infection 4. Osteoarthritis 5. Rheumatoid arthritis 6. Gynecological disorder 7. Low back pain 8. Post operative pain 9. Fever |
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Dosage |
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Oral- Adults - 100 mg two times daily. Children - 5mg/kg/day divided in 2 or 3 doses. |
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Schedule |
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H |
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Storage |
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Store in cool, dark, dry place |
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Over Dose |
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Empty the stomach if necessary. Symptomatic treatment should be given |
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