KINBREX - Celecoxcib 200mg

COMPOSITION:

Each hard gelatin capsule contains :

Celecoxib 200 mg.

Excipients q.s.

Empty gelatin Capsules contains approved colours.

PHARMACOLOGICAL CLASSIFICATION:

A 3.1 Antirheumatics (anti-inflammatory agents)

Celecoxib 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, oedema and pain.

Celecoxib acts as an anti-inflammatory, analgesic and antipyretic

agent by blocking the production of inflammatory

prostanoids via COX-2 inhibition.

Pharmacodynamic properties

PHARMACOLOGICAL ACTION:

When  given under fasting conditions celecoxib is absorbed reaching peak  plasma concentrations after approximately 2-3hours. Celecoxib exhibits  linear and dose proportional pharmacokinetics over the therapeutic dose  range. Plasmaprotein binding, which is concentration independent, is  about 97% at therapeutic plasma concentrations and the drug is  notpreferentially 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%.

Pharmacokinetic properties

Celecoxib is metabolised 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. Pharmacological activity resides in the parent drug.

The main metabolites found in the circulation have no

detectable COX-1 or COX-2 inhibitory activity 

Elimination of celecoxib is mostly by hepatic metabolism with

less than 1 % of the dose excreted unchanged in urine. After

multiple dosing elimination half life is 8-12 hours and the rate of

clearance is about 500ml/min. With multiple dosing steady

state plasma concentrations are reached before day 5. The

intersubject variability on the main pharmacokinetic

parameters (AUC, Cmax, elimination half-life) is about 30%.