Rofecoxib is a nonsteroidal anti-inflammatory drug (NSAID) that has now been withdrawn over safety concerns. It was marketed by Merck & Co. to treat osteoarthritis, acute pain conditions, and dysmenorrhea.

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: 12.5-25 mg/d.

Condition: Analgesia

Dose: Adults: 25-50 mg/d. Maximum: 5 days..

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, hypersensitivity to rofecoxib.

Warnings / Precautions

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

> Rofecoxib 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).

Clinically Important Drug Interactions

> Drugs that increase effects/toxicity of rofecoxib: rifampin, other P450 inhibitors, aspirin.

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

> Rofecoxib increases effects/toxicity of methotrexate, warfarin, lithium.

> Rofecoxib decreases effects/toxicity of furosemide, thiazide diuretics

Adverse Reactions

> Common: None.

> Serious: GI bleeding, arrhythmias, allergic reactions.

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 dyspepsia, changes in stool, abdominal pain, or swelling of ankles.

Further Useful Info

> In limited studies, rofecoxib is as effective as other NSAIDs in osteoarthritis and has 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 NSAIDs or other COX-2 inhibitors. Future uses of Cox-2 inhibitors may include chemoprevention of colonic neoplasms.

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