Celebrex Indication:

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

Celebrex Mechanism Of Action:

The mechanism of action of celecoxib is believed to be due to inhibition of prostaglandin synthesis. Unlike most NSAIDs, which inhibit both types of cyclooxygenases (COX-1 and COX-2), celecoxib is a selective noncompetitive inhibitor of cyclooxygenase-2 (COX-2) enzyme. It binds with its polar sulfonamide side chain to a hydrophilic side pocket region close to the active COX-2 binding site. Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane.

Celebrex Drug Interactions:

Anisindione Increases the anticoagulant effect
Dicumarol Increases the anticoagulant effect
Fluconazole Fluconazole increases the effect of celecoxib
Lithium The COX-2 inhibitor increases serum levels of lithium
Acenocoumarol Increases the anticoagulant effect
Rifampin Decreased levels/effect of the NSAID
Warfarin Increases the anticoagulant effect

Celebrex Food Interactions:

Take without regard to meals.
Taking this product with a high-fat meal will delay the Cmax, but total absorption will be increased by 10 to 20%.

Celebrex Generic Name:

Synonyms:

  • Celocoxib

Drug Type:

Small Molecule; Approved; Investigational

Absorption:

Well absorbed in the gastrointestinal tract. 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%.

Toxicity (Overdose):

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

Protein Binding:

97%, primarily to albumin and, to a lesser extent, a1-acid glycoprotein.

Biotransformation:

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. These metabolites are inactive as COX-1 or COX-2 inhibitors.

Half Life:

Approximately 11 hours.

Dosage Forms of Celebrex:

Capsule Oral

Chemical IUPAC Name:

4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide

Organisms Affected:

Humans and other mammals

Celebrex to general, pharmacology

General, pharmacology..
Pain Relief