Celecoxib is 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide and is a diaryl-substituted pyrazole.
Nonsteroidal anti-inflammatory drug.
Pharmacology: The mechanism of action of celecoxib is due to inhibition of prostaglandin synthesis, primarily via inhibition of cyclooxygenase-2 (COX-2) and at therapeutic concentrations in humans, celecoxib does not inhibit the cyclooxygenase-1 (COX-1) isoenzyme.
Pharmacokinetics: Absorption: Peak plasma levels of celecoxib occur approximately 3 hrs after an oral dose. Both peak plasma levels and area under the curve are roughly dose proportional across the clinical dose range of 100-200 mg.
Distribution: In healthy subjects, celecoxib is highly protein-bound within the clinical dose range.
Metabolism: Celecoxib metabolism is primarily mediated via cytochrome P-450 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 -2 inhibitors.
Excretion: Celecoxib is eliminated predominantly by hepatic metabolism with little unchanged drug recovered in the urine and feces.
Relief of signs and symptoms of osteoarthritis and rheumatoid arthritis in adults.
The lowest dose of celecoxib should be sought for each patient.
Recommended Oral Dose: Osteoarthritis: 200 mg/day administered as a single dose or as 100 mg twice a day.
Rheumatoid Arthritis: 100-200 mg twice a day.
Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur.
Patients should be managed by symptomatic and supportive care following an NSAID overdose. There are no specific antidotes.
Emesis and/or activated charcoal and/or osmotic cathartic may be indicated in patients seen within 4 hrs of ingestion with symptoms following overdose.
Hypersensitivity to celecoxib and who have demonstrated allergic-type reactions to sulfonamides.
Patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDS. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients.
General: Celecoxib cannot be expected to substitute for corticosteroids or to treat corticosteroid insufficiency. Abrupt discontinuation of corticosteroids may lead to exacerbation of corticosteroid-responsive illness.
Gastrointestinal Effects: Risk of gastrointestinal ulceration, bleeding and perforation. Serious gastrointestinal toxicity eg, bleeding, ulceration and perforation of the stomach, small or large intestines, can occur at any time, with or without warning symptoms, in patients treated with NSAIDs. Minor upper gastrointestinal problems eg, dyspepsia, are common and may also occur at any time during NSAID therapy.
Use in pregnancy: In late pregnancy, celecoxib should be avoided because it may cause premature closure of the ductus arteriosus.
Use in lactation: Celecoxib is excreted in the milk of lactating rats at concentrations similar to those in plasma. It is not known whether celecoxib is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from celecoxib, a decision should be made whether to discontinue nursing or to discontinue celecoxib, taking into account the importance of celecoxib to the mother.
Use in pregnancy: In late pregnancy, celecoxib should be avoided because it may cause premature closure of the ductus arteriosus.
Use in lactation: Celecoxib is excreted in the milk of lactating rats at concentrations similar to those in plasma. It is not known whether celecoxib is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from celecoxib, a decision should be made whether to discontinue nursing or to discontinue celecoxib, taking into account the importance of celecoxib to the mother.
Gastrointestinal: Abdominal pain, diarrhea, dyspepsia, flatulence and nausea.
Body as a Whole: Back pain, peripheral edema and injury.
Central and Peripheral Nervous System: Dizziness and headache.
Psychiatric: Insomnia.
Respiratory: Pharyngitis, rhinitis, sinusitis and upper respiratory tract infections.
Skin: Rash.
General: Celecoxib metabolism is predominantly mediated via cytochrome P-450 2C9 in the liver. Co-administration of celecoxib with drugs that are known to inhibit 2C9 should be done with caution.
ACE Inhibitors: Reports suggest that NSAIDs may diminish the antihypertensive effect of angiotensin-converting enzyme (ACE) inhibitors.
Furosemide: NSAIDs can reduce the natriuretic effect of furosemide and thiazides in some patients.
Aspirin: Concomitant administration of aspirin with celecoxib may result in an increased rate of gastrointestinal ulceration or other complications.
Fluconazole: Concomitant administration of fluconazole at 200 mg once daily resulted in a 2-fold increase in celecoxib plasma concentration.
Store in a cool, dry place.
M01AH01 - celecoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.
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