Non-steroidal anti-inflammatory and anti-rheumatic
Mode of Action
|Celecoxib, an NSAID, is a selective cyclooxygenase-2 (COX-2) inhibitor primarily responsible for inhibition of prostaglandin synthesis. It exhibits anti-inflammatory, analgesic and antipyretic activities. Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract. High fat meal may delay absorption time. Time to peak plasma concentration: Approx 2-3 hours. Distribution: Extensively distributed in tissues and present in breastmilk. Volume of distribution: Approx 400 L. Plasma protein binding: Approx 97%, mainly to albumin. Metabolism: Metabolised in the liver by CYP2C9 to form inactive metabolites such as a primary alcohol, corresponding carboxylic acid and its glucuronide conjugate. Excretion: Via urine (27% as metabolites, <3% as unchanged drug), faeces (approx 57% as metabolites, <3% as unchanged drug). Elimination half-life: Approx 11 hours.|
Treatment of RA including juvenile idiopathic arthritis, OA & ankylosing spondylitis. Adjunctive treatment of adenomatous colorectal polyps. Management of acute pain & dysmenorrhea.
OA 200 mg daily as a single dose or in 2 divided doses. If necessary, may be increased to 200 mg bid.
RA 100-200 mg bid.
Ankylosing spondylitis Initially 200 mg daily as a single dose or in 2 divided doses. Pain & dysmenorrhea Initially 400 mg followed by 200 mg if necessary on the 1st day & 200 mg bid thereafter.
History of CVA, MI, CABG, uncontrolled HTN, CHF NYHA II-IV.
History of ischemic heart disease, peripheral arterial disease, cerebrovascular disease; risk factors for CV disease eg, HTN, hyperlipidemia & DM.
CYP2C9 inhibitors & inducers; drugs metabolized by CYP2C9 & CYP2D6. Fluconazole.