No

Nonsteroidal Anti-Inflammatory Agent (NSAID)

Management of osteoarthritis and rheumatoid arthritis

C (D in 3rd trimester)

Hypersensitivity to nabumetone; should not be administered to patients with active peptic ulceration and those with severe hepatic impairment or in patients in whom nabumetone, aspirin, or other NSAIDs have induced asthma, urticaria, or other allergic-type reactions; fatal asthmatic reactions have occurred following NSAID administration

Elderly patients may sometimes require lower doses; patients with impaired renal function may need a dose reduction; use with caution in patients with severe hepatic impairment; dehydration

>10%:

Central nervous system: Dizziness

Dermatologic: Rash

Gastrointestinal: Abdominal cramps, heartburn, indigestion, nausea

1% to 10%:

Central nervous system: Headache, nervousness

Dermatologic: Itching

Endocrine & metabolic: Fluid retention

Gastrointestinal: Vomiting

Otic: Tinnitus

<1%: Congestive heart failure, hypertension, arrhythmia, tachycardia, confusion, hallucinations, aseptic meningitis, mental depression, drowsiness, insomnia, angioedema, urticaria, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, polydipsia, hot flashes, gastritis, GI ulceration, cystitis, polyuria, agranulocytosis, anemia, hemolytic anemia, bone marrow suppression, leukopenia, thrombocytopenia, hepatitis, peripheral neuropathy, toxic amblyopia, blurred vision, conjunctivitis, dry eyes, decreased hearing, acute renal failure, allergic rhinitis, shortness of breath, epistaxis

Symptoms of overdose include apnea, metabolic acidosis, coma, nystagmus, leukocytosis, and renal failure. Management of nonsteroidal anti-inflammatory (NSAID) intoxication is supportive and symptomatic.

Aspirin decreases serum concentrations probably by protein-binding displacement; there is an increased bleeding potential with concomitant warfarin therapy; may increase lithium and methotrexate concentrations by decreasing renal clearance; may decrease diuretic and hypotensive effects of thiazides, loop diuretics, ACE inhibitors, and beta-blockers; may increase nephrotoxicity of cyclosporine

Nabumetone is a nonacidic, nonsteroidal anti-inflammatory drug that is rapidly metabolized after absorption to a major active metabolite, 6-methoxy-2-naphthylacetic acid. As found with previous nonsteroidal anti-inflammatory drugs, nabumetone's active metabolite inhibits the cyclo-oxygenase enzyme which is indirectly responsible for the production of inflammation and pain during arthritis by way of enhancing the production of endoperoxides and prostaglandins E₂ and I₂ (prostacyclin). The active metabolite of nabumetone is felt to be the compound primarily responsible for therapeutic effect. Comparatively, the parent drug is a poor inhibitor of prostaglandin synthesis.

Onset of effect: May require several days to maximum effect

Distribution: Diffusion occurs readily into synovial fluid with peak concentrations in 4-12 hours

Protein binding: >99%

Metabolism: A prodrug being rapidly metabolized to an active metabolite (6-methoxy-2-naphthylacetic acid); extensive first-pass hepatic metabolism

Half-life, elimination: Major metabolite: 24 hours

Time to peak serum concentration: Metabolite: Oral: Within 3-6 hours

Elimination: 80% recovered in urine and 10% in feces, with very little excreted as unchanged compound

Adults: Oral: 1000 mg/day; an additional 500-1000 mg may be needed in some patients to obtain more symptomatic relief; may be administered once or twice daily

Alcohol: May add to irritant action in the stomach, avoid use if possible

Food: Increases the rate but not the extent of oral absorption. Take without regard to meals OR take with food or milk to minimize GI upset.

Dizziness is common; may cause nervousness; may rarely cause insomnia, confusion, depression, or hallucinations

May rarely cause agranulocytosis; use caution with clozapine and carbamazepine; may decrease lithium clearance resulting in an increase in serum lithium levels and potential lithium toxicity; monitor serum lithium levels

No information available to require special precautions

NSAID formulations are known to reversibly decrease platelet aggregation via mechanisms different than observed with aspirin. The dentist should be aware of the potential of abnormal coagulation. Caution should also be exercised in the use of NSAIDs in patients already on anticoagulant therapy with drugs such as warfarin (Coumadin®).

Take this medication exactly as directed; do not increase dose without consulting prescriber. Do not crush tablets or break capsules. Take with food or milk to reduce GI distress. Maintain adequate fluid intake (2-3 L/day of fluids unless instructed to restrict fluid intake). Do not use alcohol, aspirin, or aspirin-containing medication, and all other anti-inflammatory medications without consulting prescriber. You may experience drowsiness, dizziness, nervousness, or headache (use caution when driving or engaging in tasks requiring alertness until response to drug is known); anorexia, nausea, vomiting, or heartburn (frequent small meals, frequent oral care, sucking lozenges, or chewing gum may help); fluid retention (weigh yourself weekly and report unusual (3-5 lb/week) weight gain). GI bleeding, ulceration, or perforation can occur with or without pain; discontinue medication and contact prescriber if persistent abdominal pain or cramping, or blood in stool occurs. Report breathlessness, difficulty breathing, or unusual cough; chest pain, rapid heartbeat, palpitations; unusual bruising/bleeding; blood in urine, stool, mouth, or vomitus; swollen extremities; skin rash or itching; acute fatigue; or changes in hearing or ringing in ears. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Breast-feeding is not recommended.

Advise patient to inform physician if stomach disturbances, blurred vision, or other eye symptoms, rash, weight gain, edema, or passing of dark-colored or tarry stools occurs; concomitant use of alcohol should be avoided if possible since it may add to the irritant action of nabumetone in the stomach; aspirin should be avoided

Tablet: 500 mg, 750 mg

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