Nabumetone information from DrugsUpdate
P - Contraindicated in pregnancy
L - Contraindicated in lactation
Nabumetone is a non-steroidal anti-inflammatory drug (NSAID) of the arylalkanoic acid family (which includes diclofenac). Nabumetone has been developed by Beecham. It is available under numerous brand names, such as Relafen, Relifex and Gambaran.
It is used to treat pain or inflammation caused by arthritis. Nabumetone works by reducing the effects of hormones that cause pain and inflammation.
It has been shown to have a slightly lower risk of gastrointestinal side effects than most other non-selective NSAIDs.
Pharmacodynamics
Pharmacokinetics
Nabumetone is a weak cyclooxygenase (COX) inhibitor and is converted in the liver to 6-methoxy-2-naphthylacetic acid (6-MNA), a potent inhibitor of COX, the enzyme responsible for prostaglandin synthesis. This results in the reduction of prostaglandin levels and alleviation of pain and inflammation.
Absorption
Well absorbed from the GI tract (oral).
Distribution:
Diffuses into synovial fluid; crosses the placenta; enters breast milk. Protein-binding: >99% (6-MNA).
Metabolism
Extensively hepatic; rapidly metabolised to 6-MNA; further metabolism by O-methylation and conjugation.
Excretion:
Via urine (as inactive or conjugated metabolites). Elimination half-life of 6-MNA: 22-27 hr (adult), 25-34 hr (elderly).
Nabumetone Indications / Nabumetone Uses
Information Not Available
Nabumetone Adverse Reactions / Nabumetone Side Effects
Abdominal pain, dyspepsia, diarrhoea, nausea, flatulence, gastritis, vomiting, xerostomia, stomatitis; headache, tinnitus, dizziness; rash, pruritus; constipation; oedema; insomnia, fatigue, nervousness, somnolence; diaphoresis.
Potentially Fatal: Exfoliative dermatitis, Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN). Severe hepatic reactions (e.g. fulminant hepatitis, liver failure). Anaphylactoid reactions.
Precautions
Nabumetone tablets cannot be expected to substitute for corticosteroids or to treat corticosteroid insufficiency. Abrupt discontinuation of corticosteroids may lead to disease exacerbation. Patients on prolonged corticosteroid therapy should have their therapy tapered slowly if a decision is made to discontinue corticosteroids.
The pharmacological activity of Nabumetone tablets in reducing fever and inflammation may diminish the utility of these diagnostic signs in detecting complications of presumed noninfectious, painful conditions.
Special Precautions
Pre-existing CV risk factors or disease; fluid retention, CHF, hypertension. History of GI disease (bleeding or ulcers). Elderly or debilitated patients. Other forms of asthma. Hepatic impairment; closely monitor patients with any abnormal LFT. Renal impairment; rehydrate patient prior to therapy and closely monitor renal function. Withhold for at least 4-6 half-lives prior to surgical or dental procedures.
Other Drug Interactions
Antihypertensive effects of hypotensive agents may be reduced. May increase ciclosporin levels. Increased risk of seizures with fluoroquinolones. May reduce efficacy of diuretics. May diminish the cardioprotective effect of acetylated salicylates. Alcohol may enhance gastric mucosal irritation.
Potentially Fatal: Increased risk of GI ulceration with corticosteroids. May increase lithium levels/toxicity. Severe bone marrow suppression, aplastic anaemia and GI toxicity may occur with methotrexate. Increased risk of bleeding with anticoagulants (e.g. warfarin, heparin, LMWHs) and antiplatelet agents (e.g. ticlopidine, clopidogrel, aspirin, abciximab, dipyridamole, eptifibatide, tirofiban). Absorption may be reduced with colestyramine (and other bile acid sequestrants).
Other Interactions
Bioavailability of 6-MNA is unaffected by food; peak serum concentrations may be increased. Avoid herbs/food with antiplatelet activity e.g. alfalfa, anise, bilberry, grapeseed, green tea, bladderwrack, turmeric, bromelain, cat's claw, celery, ginkgo biloba, coleus, cordyceps, dong quai, evening primrose, feverfew, fenugreek, garlic, ginger, red clover, horse chestnut, ginseng, guggul, horse chestnut seed, horseradish, licorice, prickly ash, reishi, sweet clover, white willow.
Dosage
Oral
Pain and inflammation associated with musculoskeletal and joint disorders
Adult: 1 g as a single dose in the evening, followed by 0.5-1 g in the morning if necessary. Patients <50 kg: Less likely to require >1 g daily.
Elderly: 500 mg daily may be adequate in certain patients. Max: 1 g daily.
Food(before/after)
May be taken with or without food. (May be taken w/ meals to reduce GI distress.)
List of Contraindications
Nabumetone and Pregnancy
Contraindicated in pregnancy.
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
In 3rd trimester or near delivery:
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Nabumetone and Lactation
Contraindicated in lactation
Nabumetone and Children
Safety and efficacy not established
Nabumetone and Geriatic
Increased risk of adverse reactions
Nabumetone and Other Contraindications
Active peptic ulceration; severe hepatic impairment; hypersensitivity; patients in whom other NSAIDs or aspirin are likely to induce asthma, angioedema, pruritus or urticaria. Pregnancy (3rd trimester), lactation. Perioperative pain in the setting of CABG.
Storage
Oral
Store at 20-25°C (68-77°F)
Lab interference
Oral
Store at 20-25°C (68-77°F)
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