Pharmacology: Pharmacodynamics: Mechanism of Action: Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic, and antipyretic activities. The mechanism of action of celecoxib is believed to be due to the inhibition of prostaglandin synthesis, primarily via the inhibition of cyclo-oxygenase-2 and the therapeutic concentrations in humans. Celecoxib does not inhibit the cyclo-oxygenase-1 isoenzyme. Pharmacokinetics: Absorption: Peak plasma levels of celecoxib occur approximately 3 hours after an oral dose. Under fasting conditions, both peak plasma levels (Cmax) and area under the curve (AUC) are roughly dose proportional up to 200 mg twice a day; at higher doses, there are less than proportional increases in Cmax and AUC.
Indications/Uses
It is used for the treatment of rheumatoid arthritis and osteoarthritis. Used in the treatment of Familial adenomatous polyposis (FAP) as adjunct.
Dosage/Direction for Use
For OSTEOARTHRITIS the recommended dose is 200 mg daily given by mouth as a single dose or in 2 divided doses.
FOR RHEUMATOID ARTHRITIS the dose is 100 to 200 mg given twice daily. In elderly patients and those of Afro-Carribbean origin treatment should be initiated at the lowest recommended dose.
In the treatment of PAIN and DYSMENORRHEA, an initial dose of 400 mg followed by an additional dose of 200 mg, if necessary, is recommended on the first day, thereafter the dose is 200 mg twice daily.
Treatment for FAP is 40 mg twice daily.
Doses for Osteoarthritis or Rheumatoid Arthritis may be given with or without meals. But for Familial Adenomatous Polyposis, it should be taken with meals.
Or as prescribed by physician.
Contraindications
It is contraindicated in patients with severe heart failure, inflammatory bowel disease and renal impairment associated with a creatinine clearance of less than 30 mL per minute.
It is also contraindicated in patients with asthma and urticaria.
Contraindicated in patients with previous or active ulceration, nervousness, somnolence. Absolute Contraindications: Not to be given to those patients who have history of: Stroke, cerebrovascular accident, CVA; Heart Attack, myocardial infarction; Coronary artery bypass graft: CABG; Uncontrolled Hypertension; Congestive heart failure (CHF), NVHA II-V.
Special Precautions
Celecoxib should not be used in patients with severe hepatic impairment. Therapy should be withdrawn if signs and symptoms of hepatic toxicity develops. Celecoxib should not be given to patients with a history of hypersensitivity to sulfonamides.
Celecoxib should not be used in patients with liver dysfunction, impaired renal function, dehydration, anemia, pre-existing asthma and pregnant.
The metabolism of celecoxib is mediated mainly by the cytochrome P450 isoenzyme CYP2C9. Concomitant administration of other drugs that inhibit or are metabolised by this isoenzyme may result in changes in the plasma concentration of celecoxib; co-administration of fluconazole has resulted in increased in plasma concentration of celecoxib. Celecoxib is an inhibitor of the isoenzyme CYP2D6 and the potential therefore exist for an effect on drugs metabolised by this enzyme.
Storage
Store at a temperature not exceeding 30°C. Protect from light.
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