Celecoxib is a COX-2 selective nonsteroidal anti-inflammatory drug (NSAID). It is used to treat the pain and inflammation of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute pain in adults, painful menstruation, and juvenile rheumatoid arthritis in people two years or older.

Molecular Structure


Class of Drug

Antiinflammatory, analgesic, COX-2 inhibitor

Mechanism of Action

Selective inhibitor of COX-2, the enzyme required for synthesis of prostaglandins and other products of the arachidonic acid cascade.

Indications / Dosage / Route

Routes of Administration: Oral only.

Condition: Osteoarthritis

Dose: Adults: 100 mg b.i.d. or 200 mg as single dose.

Condition: Rheumatoid arthritis

Dose: Adults: 100-200 mg b.i.d.

Adjustment of Dosage

Kidney disease: None. Potentially toxic to kidney

Liver disease: Reduce dosage. Monitor carefully.

Elderly: Use lowest recommended dose.

Pediatric: Safety and efficacy have not been determined in chil­dren <18 years.

Food and Drug Interactions

Food: May be taken with or without food.

Pregnancy: Category C. Category D in third trimester and near delivery.

Lactation: No data available. Best to avoid.

Contraindications: Severe liver disease, history of allergic reaction to aspirin or other NSAIDs.

Warnings / Precautions

> Use with caution in patients with the following conditions: active gastric ulcer, history of ulcer disease or GI bleeding, active asthma, hypertension, fluid retention, chronic kidney or liver disease.

> Celecoxib can cause significant GI bleeding despite being a specific COX-2 inhibitor.

> Potentially toxic to kidneys, particularly when prostaglandins maintain renal blood flow (renal and heptatic insufficiency), CHF.

> Avoid in patients with kidney or severe hepatic dysfunction.

Clinically Important Drug Interactions

> Drugs that increase effects/toxicity of celecoxib: rifampin, aspirin, fluconazole, inhibitors of cytochrome P450 2C9.

> Drugs that decrease effects/toxicity of celecoxib: antacids.

> Celecoxib increases effects/toxicity of following drugs: methotrexate, warfarin, lithium.

> Celecoxib decreases effects/toxicity of following drugs: fureosemide, thiazide diuretics, ACE inhibitors.

Adverse Reactions

> Common: Headache.

> Serious: GI bleeding, hypertension, angina, hypersensitivity reactions, hepatitis, nephrotoxicity, anemia, neuropathy.

Parameters to Monitor

> Improvement in pain and inflammation

> Signs and symptoms of salt and water retention.

> Signs and symptoms of GI toxicity.

> Signs and symptoms of renal toxicity.

Advice to Patient

> Report to treating physician if you experience any of the following symptoms: dyspepsia, changes in stool, abdominal pain, swelling of ankles.

Further Useful Info

> Celecoxib is as effective as other NSAIDs in osteoarthritis and is associated with a lower incidence of GI toxicity than the older drugs. However, the incidence of long-term GI effects has not been determined as compared with older NSAIDs or other COX-2 inhibitors.

> Celecoxib was recently approved as chemoprophylaxsis for adenoma development in patients with familial adenomatous polyposis. Dosage for this indication is 400 mg b.i.d.

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