Nabumetone is a non-steroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic, and antipyretic properties in pharmacologic studies. As with other non-steroidal anti-inflammatory agents its mode of action is not known; however, the ability to inhibit prostaglandin synthesis may be involved in the anti-inflammatory effect. The parent compound is a prodrug. which undergoes hepatic biotransformation to the active component, 6-methoxy-2-naphthylacetic acid (6MNA), that is a potent inhibitor of prostaglandin synthesis
Reports suggest that NSAIDs may diminish the antihypertensive effect of ACE-inhibitors. This interaction should be given consideration in patients taking NSAIDs concomitantly with ACE-inhibitors.
Nabumetone is contraindicated in patients with known hypersensitivity to nabumetone or its excipients. Nabumetone should not be given to patients who have experienced asthma, urticaria, or allergictype reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients. Nabumetone is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery
Pregnancy Category C. There are no adequate, well-controlled studies in pregnant women. This drug should be used during pregnancy only if dearly needed Because of the known effect of prostaglandin-synthesis-inhibiting drugs on the human fetal cardiovascular system (closure of ductus arteriosus), use of Nabumetone during the third trimester of pregnancy is not recommended Lactation: Nabumetone is not recommended for use in nursing mothers because of the possible adverse effects of prostaglandin-synthesis-inhibiting drugs on neonates
As a class, NSAIDs have been associated with renal papillary necrosis and other abnormal renal pathology during long-term administration to animals. The second form of renal toxicity often associated with NSAIDs is seen in patients with conditions leading to a reduction in renal blood flow or blood volume, where renal prostaglandins have a supportive role in the maintenance of renal perfusion in these patients, administration of an NSAID results in a dose-dependent decrease in prostaglandin synthesis and, secondarily, in a reduction of renal blood flow, which may precipitate overt renal decompensation Patients at greatest risk of this reaction are those with impaired renal function, heart failure, liver dysfunction, those taking diuretics, and the elderly Discontinuation of NSAID therapy is typically followed by recovery to the pretreatment state
Symptoms following acute NSAIDs overdoses are usually limited to lethargy, drowsiness, nausea, and vomiting. and epigastric pain, which is generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression, and coma may occur but are rare. Anaphylactoid reactions have been reported with therapeutic ingestion of NSAIDs and may occur following an overdose. Patients should be managed by symptomatic and supportive care following a NSAID overdose. There are no specific antidotes. Emesis and/or activated charcoal (60 to 100 grams in adults, 1 to 2 g/kg in children). and/or osmotic cathartic may be indicated in patients seen within 4 hours of ingestion with symptoms or following a large overdose (5 to 10 times the usual dose) Forced diuresis, alkalinization of urine, hemodialysis, or hemoperfusion may not be useful due to high protein binding. There have been overdoses of up to 25 grams of Nabumetone reported with no long-term sequelae following standard emergency treatment (ie. activated charcoal gastric lavage, IV H2-blockers, etc).
Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis
