Trade Names:Nabumetone- Tablets 500 mg- Tablets 750 mgApo-Nabumetone (Canada)Gen-Nabumetone (Canada)
Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.
Nabumetone is well absorbed from the GI tract. Food increases the rate of absorption and plasma concentration of 6-methoxy-2-naphthylacetic acid (6î“¸MNA). Bioavailability is greater than 80%.
Protein binding is more than 99% (active metabolite), and the Vd is at 0.1 to 0.2 L/kg.
Undergoes rapid biotransformation to main active metabolite 6î“¸MNA approximately 35% and the remaining unidentified metabolites approximately 50%. 6 MNA is metabolized in the liver to inactive metabolites.
80% recovered in urine, 9% in feces. The t ½ of major metabolite is 22.5 to 24 hr, and plasma Cl is 20 to 30 mL/min.
Terminal t ½ of 6î“¸MNA was increased.Elderly
Steady-state concentrations are generally higher.
Relief of symptoms of chronic and acute rheumatoid arthritis and osteoarthritis.
Asthma, urticaria, or allergic-type reaction to aspirin; treatment of perioperative pain in the setting of coronary artery bypass graft; hypersensitivity to any component of the product.
PO 1,000 mg initially; may increase to 1,500 to 2,000 mg daily in 1 to 2 divided doses.Renal Function ImpairmentAdults
PO The max starting dose in moderate to severe renal function impairment is 500 or 750 mg, respectively. After careful monitoring of renal function, the dose may be increased in moderate or severe renal function impairment to a max of 1,000 or 1,500 mg, respectively.
Store in tightly closed, light-resistant container at controlled room temperature (68° to 77°F).
Antihypertensive effects of ACE inhibitors may be reduced.Anticoagulants
May increase effect of anticoagulants. May increase risk of gastric erosion and bleeding.Aspirin
Risk of adverse reactions may be increased.Cyclosporine
Neurotoxicity of both agents may be increased.Lithium
May increase lithium levels.Loop diuretics (eg, furosemide), thiazide diuretics (eg, hydrochlorothiazide)
Natriuretic effect of diuretics may be reduced.Methotrexate
Increased risk of methotrexate toxicity.Salicylates
Additive GI toxicity.
May prolong bleeding time.
Angina, arrhythmia, hypertension, MI, palpitations, syncope, thrombophlebitis (postmarketing).
Dizziness, headache (3% to 9%); fatigue, increased sweating, insomnia, nervousness, somnolence (1% to 3%); nightmares (postmarketing).
Pruritus, rash (3% to 9%); acne, alopecia (postmarketing).
Tinnitus (3% to 9%).
Diarrhea (14%); dyspepsia (13%); abdominal pain (12%); constipation, flatulence, positive stool guaiac (3% to 9%); dry mouth, gastritis, stomatitis, vomiting (1% to 3%); bilirubinuria, duodenitis, eructation, gallstones, gingivitis, glossitis, pancreatitis, rectal bleeding, taste disorder (postmarketing).
Dysuria, hematuria, impotence, renal stones (postmarketing).
Anemia, granulocytopenia, leukopenia (postmarketing).
Elevations of ALT, AST (1%).
Hyperglycemia, hypokalemia, weight loss (postmarketing).
Edema (3% to 9%); chills, fever (postmarketing).
NSAIDs may cause an increased risk of serious CV thrombotic events, MI, and stroke, which can be fatal. This risk may increase with length of therapy. Patients with CV disease or risk factors for CV disease may be at greater risk. NSAIDs cause an increased risk of serious GI adverse events, including inflammation, bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur any time during use and without warning symptoms. Elderly patients are at greater risk of serious GI events.
Closely monitor coagulation parameters in patients with coagulation disorders or who are receiving anticoagulants. Monitor for signs and symptoms of GI ulcerations and bleeding. Check CBC and chemistry profile periodically.
Category C .
Safety and efficacy not established.
Increased risk of adverse reactions.
May occur; use drug with caution in aspirin-sensitive patients because of possible cross-sensitivity.
Lower doses may be necessary in patients with renal function impairment.
Check Hgb or Hct in patients on long-term therapy if there are signs or symptoms of anemia.
Fluid retention and edema may occur; use with caution in patients with fluid retention or heart failure.
Can cause premature closure of the ductus arteriosus in fetus in late pregnancy.
Nabumetone can lead to onset of new hypertension or worsening of preexisting hypertension, which may contribute to an increased incidence of CV events.
Serious, life-threatening skin adverse reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, can occur.
Acute renal failure, coma, drowsiness, epigastric pain, GI bleeding, hypertension, lethargy, nausea, respiratory depression, vomiting.
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