Rofecoxib

Oral
Osteoarthritis

Oral
Pain relief

Oral
Rheumatoid arthritis

Max: 12.5 mg/day.

Hypersensitivity. Severe renal impairment.

Hepatic dysfunction, pregnancy and lactation. History of ulcer disease or GI bleeding. Elderly or debilitated patients. Prolonged treatment, smoking and alcoholism may increase risk of GI bleeding. Ischaemic heart disease.

Mouth ulcers, chest pain, weight gain, atopic eczema, muscle cramps, diarrhoea, headache, nausea; upper respiratory tract infection, hypertension, ischaemia, dyspepsia, epigastric discomfort, heart burn, nausea, sinusitis, back pain, headache, bronchitis, urinary tract infections.
Potentially Fatal: Renal failure; nephrotoxicity; MI.

PO: C, Z (NSAIDs caused foetal ductus arteriosus premature closure, foetal renal impairment and persistent pulmonary hypertension. Avoid near term, else use lowest dose for shortest time.)

General supportive measures and clinical monitoring should be used.

Increases plasma concentrations of methotrexate and lithium. Increased nephrotoxicity when used with thiazide, loop diuretics and ACE inhibitors. May reduce efficacy of loop diuretics.

High fat meals may delay time to reach peak plasma concentrations.

Description: Rofecoxib selectively inhibits cyclooxygenase-2 (COX-2) enzyme that is involved in the synthesis of prostaglandins. It has no significant inhibitory action on cyclooxygenase-1 (COX-1) enzymes.
Onset: 45 min.
Duration: >24 hr.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract (oral); peak plasma concentrations after 2 hr.
Distribution: Protein-binding: 85%.
Metabolism: Extensively hepatic by reduction to cis- and trans-dihydrorofecoxib.
Excretion: Urine and faeces; 17 hr (elimination T_1/2 at steady state).

Store at 25°C.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)