Nabumetone

Nabumetone structure: in Kenya

Mode of Action:

Nabumetone 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.

Drug Label Information | Brands:

NABUMETONE INDICATIONS

Nabumetone is indicated:

  • For relief of the signs and symptoms of rheumatoid arthritis.
  • For relief of the signs and symptoms of osteoarthritis.

CONTRAINDICATIONS:

  • 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 allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients
  • In the setting of coronary artery bypass graft (CABG) surgery

ADVERSE DRUG REACTIONS:

Blood and lymphatic system disorders

Very Rare: Thrombocytopenia,

Not known: Neutropenia, agranulocytosis, aplastic anaemia, leucopenia and haemolytic anaemia

Immune system disorders

Very rare: Anaphylaxis, anaphylactoid reaction

Psychiatric disorders

Uncommon: Confusion, nervousness, insomnia

Not known: Depression, hallucinations

Nervous system disorders

Uncommon: Somnolence, dizziness, headache, paresthesia, anxiety

Not known: Aseptic meningitis (especially in patients with existing autoimmune disorders such as systemic lupus erythematosus, mixed connective tissue disease, with symptoms such as stiff neck, headache, nausea, vomiting, fever or disorientation , vertigo, drowsiness

Eye disorders

Uncommon: Abnormal vision, eye disorders

Not known: Optic neuritis

Ear and labyrinth disorders

Common: Tinnitus, ear disorder

Vascular disorders

Common: Increases in blood pressure

Respiratory, thoracic and mediastinal disorders

Uncommon: Dyspnoea, respiratory disorder, epistaxis

Very rare: Interstitial pneumonitis

Not known: Asthma, aggravated asthma, bronchospasm

Gastrointestinal disorders

Common: Diarrhoea, constipation, dyspepsia, gastritis, nausea, abdominal pain, flatulence

Uncommon: Duodenal ulcer, GI bleeding, gastric ulcer, GI disorder, melaena, vomiting, stomatitis, dry mouth

Very rare: Pancreatitis

Gastrointestinal: The most commonly observed adverse events are gastrointestinal in nature. Peptic ulcers, perforation or GI bleeding, sometimes fatal, particularly in the elderly, may occur  Nausea vomiting, diarrhoea, flatulence, constipation, dyspepsia, abdominal pain, melaena, haematemesis, ulcerative stomatitis, exacerbation of colitis and Crohn’s disease have been reported following administration. Less frequently, gastritis has been reported.

Hepatobiliary disorders

Very rare: Hepatic failure, jaundice

Skin and subcutaneous tissue disorders

Common: Rash, pruritus

Uncommon: Photosensitivity, urticaria, sweating

Very rare: Bullous reactions including toxic epidermal necrolysis, Stevens Johnson syndrome, erythema multiforme, angioedema, pseudoporphyria, alopecia

Not known: Purpura

Musculoskeletal and connective tissue disorders

Uncommon: Myopathy

Renal and urinary disorders

Uncommon: Urinary tract disorder

Very rare: Renal failure, nephrotic syndrome

Not known: Interstitial nephritis

Reproductive system and breast disorders

Very rare: Menorrhagia

General disorders and administration site conditions

Common: Oedema

Uncommon: Asthenia, fatigue

Not known: Malaise

Investigations

Uncommon: Elevated liver function tests

Hypersensitivity reactions have been reported following treatment with NSAIDs. These may consist of (a) non-specific allergic reactions and anaphylaxis (b) respiratory tract reactivity comprising asthma, aggravated asthma, bronchospasm or dyspnoea, or (c) assorted skin disorders, including rashes of various type, pruritus, urticaria, purpura, angioedema and, more rarely exfoliative and bullous dermatoses (including epidermal necroylsis and erythema multiforme).

Other adverse reactions reported include:

Neurological and special senses: Optic neuritis, reports of aseptic meningitis (especially in patients with existing auto-immune disorders, such as systemic lupus erythematosus, mixed connective tissue disease), with symptoms such as a stiff neck, headache, nausea, vomiting, fever or disorientation, depression, confusion, hallucinations, tinnitus, vertigo, dizziness, malaise, fatigue and drowsiness.

Renal: Nephrotoxicity in various forms, including interstitial nephritis,

Oedema, hypertension and cardiac failure have been reported in association with NSAID treatment.

Clinical trial and epidemiological data suggest that use of some NSAIDs (particularly at high doses and in long term treatment) may be associated with an increased risk of arterial thrombotic events (for example myocardial infarction, stroke and death)

In clinical trials, increases in doses above 1 g did not lead to an increase in the incidence of side effects. However, the lowest effective dose should always be used.

DRUG INTERACTIONS

ACE-inhibitors

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.

Aspirin

When nabumetone is administered with aspirin, its protein binding is reduced, although the clearance of free nabumetone is not altered. The clinical significance of this interaction is not known; however, as with other NSAIDs, concomitant administration of nabumetone and aspirin is not generally recommended because of the potential of increased adverse effects.

Diuretics

Clinical studies, as well as post-marketing observations, have shown that nabumetone can reduce the natriuretic effect of furosemide and thiazides in some patients. This response has been attributed to inhibition of renal prostaglandin synthesis. During concomitant therapy with NSAIDs, the patient should be observed closely for signs of renal failure, as well as to assure diuretic efficacy.

Lithium

NSAIDs have produced an elevation of plasma lithium levels and a reduction in renal lithium clearance. The mean minimum lithium concentration increased 15% and the renal clearance was decreased by approximately 20%. These effects have been attributed to inhibition of renal prostaglandin synthesis by the NSAID. Thus, when NSAIDs and lithium are administered concurrently, subjects should be observed carefully for signs of lithium toxicity.

Methotrexate

NSAIDs have been reported to competitively inhibit methotrexate accumulation in rabbit kidney slices. This may indicate that they could enhance the toxicity of methotrexate. Caution should be used when NSAIDs are administered concomitantly with methotrexate.

Warfarin

The effects of warfarin and NSAIDs on GI bleeding are synergistic, such that users of both drugs together have a risk of serious GI bleeding higher than users of either drug alone.


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