Celecoxib (Seleco) tablet is a Non steroidal antiinflammatory drug. The chemical name is 4-[5-(4-methyl phenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzene sulfonamide and is a diaryl-substituted pyrazole.
MECHANISM OF ACTION:
Celecoxib (Seleco) is a specific Cyclooxygenase-2 inhibitor (SCI). Cyclooxygenase-2 (COX-2) is induced in response to inflammatory stimuli. This leads to the synthesis and accumulation of inflammatory prostanoids, in particular prostaglandin E2, causing inflammation, edema and pain. Celecoxib (Seleco) acts as an anti-inflammatory analgesic and antipyretic agent by blocking the production of inflammatory prostanoids via COX-2 inhibition. In-vivo and ex-vivo studies show that Celecoxib has a very low affinity for the constitutively expressed cyclooxygenase-1 enzyme (COX-1).
PHARMACOKINETICS:
When given under fasting conditions Celecoxib (Seleco) is absorbed reaching peak plasma concentrations after approximately 2-3 hours. Celecoxib (Seleco) exhibits linear and dose proportional pharmacokinetics over the therapeutic dose range. Plasma protein binding, which is concentration independent, is about 97% at therapeutic plasma concentrations and the drug is not preferentially bound to erythrocytes in the blood. Dosing with food (high-fat meal) delays absorption resulting in a Tmax of about 4 hours and increases bioavailability by about 20%. In the population > 65 years there is a two-fold increase in mean Cmax and AUC for Celecoxib. This is a predominantly weight related rather than age-related change, with celecoxib levels being higher in lower-weight individuals and consequently higher in the elderly population who are generally of lower mean weight than the younger population. Therefore elderly females tend to have slightly higher drug plasma concentrations than elderly males. Celecoxib is metabolized in the liver by hydroxylation, oxidation and some glucuronidation and in vitro and in vivo studies indicate that metabolism is mainly by cytochrome P450 CYP2C9. Elimination of Celecoxib is mostly by hepatic metabolism with less than 1% of the dose excreted unchanged in the urine. After multiple dosing elimination half life is 8-12 hours and the rate of clearance is about 500 ml/min. With multiple dosing, steady state plasma concentrations are reached before day 5. The inter-subject varibility on the main pharmacokinetic parameters (AUC, Cmax and elimination half-life) is about 30%. The mean steady-state volume of distribution is about 500 L/70 kg in young healthy adults after a single 200 mg dose indicating the wide distribution of Celecoxib into the tissues. Preclinical studies indicate that the drug crosses the blood-brain barrier.
INDICATIONS:
Celecoxib (Seleco) is indicated: For relief of the signs and symptoms of osteoarthritis, for relief of the signs and symptoms of rheumatoid arthritis in adults, for the management of acute pain in adults, including dental pain, for the treatment of primary dysmenorrhea.
INSTRUCTIONS:
Store in a cool & dry place below 25ºC.
Protect from light, heat and moisture.
Keep out of reach of children.