Nabumetone

Indications
 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.
CrCl (ml/min)Dosage Recommendation
30-49Max initial dose: 750 mg once daily. Increase if needed to a max dose of 1.5 g daily.
<30Max initial dose: 500 mg once daily. Increase if needed to a max dose of 1 g daily.
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.
Warnings / 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.
Adverse Reactions
 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.
Overdose Reactions
 Symptoms: Drowsiness, epigastric pain, lethargy, nausea, vomiting. Rarely, acute renal failure, coma, hypertension and respiratory depression. Management: Supportive and symptomatic. 6-MNA is not dialysable.
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).
See Below for More nabumetone Drug Interactions
Food 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.
Mechanism of Actions
 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).
Administration
 May be taken with or without food. (May be taken w/ meals to reduce GI distress.)
Storage Conditions
 Oral: Store at 20-25°C (68-77°F).
ATC Classification
 M01AX01 - nabumetone ; Belongs to the class of other non-steroidal antiinflammatory and antirheumatic products.
Storage
 Oral: Store at 20-25°C (68-77°F).
Available As
  • Nabumetone 500 mg
  • Nabumetone 750 mg

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