Celecoxib


Other name

DB00482

International/Other brands

Act Celecoxib

Groups

Approved

Structure

Prescription products

NameDosageStrengthRouteLabeller
Accel-celecoxibCapsule200 mgOralAccel Pharma Inc
Accel-celecoxibCapsule100 mgOralAccel Pharma Inc
Act CelecoxibCapsule200 mgOralActavis Pharma Company
Act CelecoxibCapsule100 mgOralActavis Pharma Company
Ag-celecoxibCapsule200 mgOralAngita Pharma Inc.
Ag-celecoxibCapsule100 mgOralAngita Pharma Inc.
Auro-celecoxibCapsule200 mgOralAuro Pharma Inc
Auro-celecoxibCapsule100 mgOralAuro Pharma Inc
Bio-celecoxibCapsule200 mgOralBiomed Pharma
Bio-celecoxibCapsule100 mgOralBiomed Pharma

Target

-

Description

Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis. It is marketed by Pfizer under the brand name Celebrex. In some countries, it is branded Celebra. Celecoxib is available by prescription in capsule form.

Indications

For relief and management of osteoarthritis (OA), rheumatoid arthritis (RA), juvenile rheumatoid arthritis (JRA), ankylosing spondylitis, acute pain, primary dysmenorrhea and oral adjunct to usual care for patients with familial adenomatous polyposis

Other indications

-

Mechaism of action

-

Absorption

Well absorbed in the gastrointestinal tract. When a single dose of 200 mg is given to healthy subjects, peak plasma levels occur 3 hours after an oral dose. The peak plasma level is 705 ng/mL. Absolute bioavailability studies have not been conducted. When multiple doses are given, steady-state is reached on or before Day 5. When taken with a high fat meal, peak plasma levels are delayed for about 1 to 2 hours with an increase in total absorption (AUC) of 10% to 20%.

Metabolism

Hepatic. Celecoxib metabolism is primarily mediated via cytochrome P450 2C9. Three metabolites, a primary alcohol, the corresponding carboxylic acid and its glucuronide conjugate, have been identified in human plasma. CYP3A4 is also involved in the hydroxylation of celecoxib but to a lesser extent. These metabolites are inactive as COX-1 or COX-2 inhibitors.

Toxicity

Symptoms of overdose include breathing difficulties, coma, drowsiness, gastrointestinal bleeding, high blood pressure, kidney failure, nausea, sluggishness, stomach pain, and vomiting.