Inhibition of COX-2 by celecoxib is time dependent and reversible.
It is readily absorbed orally. Its peak concentration is approximately 3 hours. It is metabolized in the liver by cytochrome P450 (CYP2C9). It is excreted in feces and urine. Its half life is 11 hours, so its dose is adjusted according to once a day.
It may cause abdominal pain, Diarrhea, Dyspepsia and Kidney toxicity may also occur.
It inhibits CYP2D6 and so can elevate levels of ß-blockers, anti-depressants and anti-psychotic drugs.
Fluconozole, fluvastatin and zafirlukast may increase serum level of celecoxib.
It should be avoided in patients;
- with chronic renal insufficiency
- Severe heart disease
- Volume depletion
- Hepatic failure