CYNAGRA
CYROX
CECAL
CYFLOX-200
CYFLOX-400
LECOURSE-500
CYPAN
CYPAN-D
NOM
TRACE
GINCER
     
 
 
 
 
 
 
Pharmacology of Drug  -Nimesulide
 
       
  Mechanism of Action

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.
 
  Pharmaco Kinetics
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.
 
  Onset Of Action
30 to 60 minutes
 
  Half Life
Its plasma half life is long-nearly 2days
 
  Duration Of Action
8-10 hours
 
  Adverse Effects
1. Nausea  2. Vomiting  3. Diarrhea  4. Heart burn  5. Epigastric pain  6. Pruritis  7. Skin rash  8. Headache  9. Dizziness  10.Somnolence 
 
  ContraIndications
1. Hypersensitivity to this drug  2. Active peptic ulcer  3. Hepatic impairment
 
  Special Precautions
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
 
  Pregnancy
Contraindicated
 
  Breast Feeding
Contraindicated
 
  Old Age
Use with caution
 
  Children
Use with caution
 
  Interactions
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.
 
  Indications
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
 
  Dosage  
Oral-  Adults - 100 mg two times daily.  Children - 5mg/kg/day divided in 2 or 3 doses.
 
  Schedule  
H
 
  Storage  
Store in cool, dark, dry place
 
  Over Dose  
Empty the stomach if necessary. Symptomatic treatment should be given