Brands, Medical Use, Clinical Data
Drug Category
- Anti-Inflammatory Agents, Non-Steroidal
- Antineoplastic Agents
Dosage Forms
- Tablets for oral administration (500 mg or 750 mg)
Brands / Synonyms
Arthaxan; Balmox; Consolan; Dolsinal; Flambate; Listran; Mebutan; Nabumetona; Nabumetone [USAN:BAN:INN:JAN]; Nabumetonum [INN-Latin]; Nabuser; Prodac; Relafen; Relif; Relifen; Relifex; Unimetone
Indications
For acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.
Pharmacology
Nabumetone is a naphthylalkanone. It is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic and antipyretic properties in pharmacologic studies. As with other nonsteroidal 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.
Mechanism of Action
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, most likely through binding to the COX-1 and COX-2 receptors.
Absorption
Well absorbed from the gastrointestinal tract. Coadministration of food increases the rate of absorption and subsequent appearance of 6MNA (the active metabolite) in the plasma but does not affect the extent of conversion of nabumetone into 6MNA.
Toxicity
The one overdose occurred in a 17-year-old female patient who had a history of abdominal pain and was hospitalized for increased abdominal pain following ingestion of 30 nabumetone tablets (15 grams total). Stools were negative for occult blood and there was no fall in serum hemoglobin concentration. The patient had no other symptoms.
Biotrnasformation / Drug Metabolism
Undergoes rapid biotransformation to the principal active metabolite, 6-methoxy-2-naphthylacetic acid (6MNA). Approximately 35% of a 1000 mg oral dose of nabumetone is converted to 6MNA and 50% is converted into unidentified metabolites which are subsequently excreted in the urine.
Contraindications
Nabumetone is contraindicated in patients who have previously exhibited hypersensitivity to it.
Nabumetone is contraindicated in patients in whom nabumetone, aspirin or other NSAIDs induce asthma, urticaria or
other allergic-type reactions. Fatal asthmatic reactions have been reported in such patients receiving NSAIDs.
Drug Interactions
In vitro studies have shown that, because of its affinity for protein, 6MNA may displace other
protein-bound drugs from their binding site. Caution should be exercised when administering nabumetone with warfarin
since interactions have been seen with other NSAIDs.
Concomitant administration of an aluminum-containing antacid had no significant effect in the bioavailability of
6MNA. When administered with food or milk, there is more rapid absorption; however, the total amount of 6MNA in the
plasma is unchanged .
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