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Look Up > Drugs > Nabumetone
Nabumetone
Pronunciation
U.S. Brand Names
Generic Available
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(na BYOO me tone)

U.S. Brand Names
Relafen®

Generic Available

No


Pharmacological Index

Nonsteroidal Anti-Inflammatory Agent (NSAID)


Use

Management of osteoarthritis and rheumatoid arthritis


Pregnancy Risk Factor

C (D in 3rd trimester)


Contraindications

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


Warnings/Precautions

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


Adverse Reactions

>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


Overdosage/Toxicology

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


Drug Interactions

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


Mechanism of Action

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.


Pharmacodynamics/Kinetics

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


Usual Dosage

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


Dietary Considerations

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.


Mental Health: Effects on Mental Status

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


Mental Health: Effects on Psychiatric Treatment

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


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

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®).


Patient Information

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.


Nursing Implications

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


Dosage Forms

Tablet: 500 mg, 750 mg


References

Bernhard GC, "Worldwide Safety Experience With Nabumetone," J Rheumatol, 1992, 19(Suppl 36):48-57.

Brier ME, Sloan RS, and Aronoff GR, "Population Pharmacokinetics of the Active Metabolite of Nabumetone in Renal Dysfunction," Clin Pharmacol Ther, 1995, 57(6):622-7.

Brooks PM and Day RO, "Nonsteroidal Anti-inflammatory Drugs - Differences and Similarities," N Engl J Med, 1991, 324(24):1716-25.

Clinch D, Banerjee AK, Ostick G, "Absence of Abdominal Pain in Elderly Patients With Peptic Ulcer," Age Ageing, 1984, 13:120-3.

Clive DM, Stoff JS, "Renal Syndromes Associated With Nonsteroidal Anti-inflammatory Drugs," N Engl J Med, 1984, 310(9):563-72.

Court H and Volans GN, "Poisoning After Overdose With Nonsteroidal Anti-inflammatory Drugs," Adverse Drug React Acute Poisoning Rev, 1984, 3(1):1-21.

Graham DY, "Prevention of Gastroduodenal Injury Induced by Chronic Nonsteroidal Anti-inflammatory Drug Therapy," Gastroenterology, 1989, 96(2 Pt 2 Suppl):675-81.

Gurwitz JH, Avorn J, Ross-Degnan D, et al, "Nonsteroidal Anti-Inflammatory Drug-Associated Azotemia in the Very Old," JAMA, 1990, 264(4):471-5.

Hawkey CJ, Karrasch JA, Szczepanski L, et al, "Omeprazole Compared With Misoprostrol for Ulcers Associated With Nonsteroidal Anti-inflammatory Drugs," N Engl J Med, 1998, 338(11):727-34.

Hoppmann RA, Peden JG, and Ober SK, "Central Nervous System Side Effects of Nonsteroidal Anti-inflammatory Drugs. Aseptic Meningitis, Psychosis, and Cognitive Dysfunction," Arch Intern Med, 1991, 151(7):1309-13.

Hyneck ML, "An Overview of the Clinical Pharmacokinetics of Nabumetone," J Rheumatol, 1992, 19(Suppl 36):20-4.

Jackson RE, Mitchell FN, and Brindley DA, "Safety Evaluation of Nabumetone in United States Clinical Trials," Am J Med, 1987, 83(4B):115-20.

Jenner PN, "A 12-Month Postmarketing Surveillance Study of Nabumetone: A Preliminary Report," Drugs, 1990, 40(Suppl 5):80-6.

Pounder R, "Silent Peptic Ulceration: Deadly Silence or Golden Silence?" Gastroenterology, 1989, 96:(2 Pt 2 Suppl)626-31.

Smolinske SC, Hall AH, Vandenberg SA, et al, "Toxic Effects of Nonsteroid Anti-inflammatory Drugs in Overdose. An Overview of Recent Evidence on Clinical Effects and Dose-Response Relationships," Drug Saf, 1990, 5(4):252-74.

Vale JA and Meredith TJ, "Acute Poisoning Due to Nonsteroidal Anti-inflammatory Drugs," Med Toxicol, 1986, 1(1):12-31.

Verbeeck RK, "Pharmacokinetic Drug Interactions With Nonsteroidal Anti-inflammatory Drugs," Clin Pharmacokinet, 1990, 19(1):44-66.

Yeomans ND, Tulassay Z, Juhasz L, et al, "A Comparison of Omeprazole With Ranitidine for Ulcers Associated With Nonsteroidal Anti-inflammatory Drugs," N Engl J Med, 1998, 338(11):719-26.


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