Nabumetone
Pronouncation: (nab-UE-me-TONE)Class: NSAID
Trade Names:
Nabumetone
- Tablets 500 mg
- Tablets 750 mg
Gen-Nabumetone (Canada)
Rhoxal-nabumetone (Canada)
Pharmacology
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Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.
Pharmacokinetics
Absorption
Nabumetone is well absorbed from the GI tract. Food increases the rate of absorption and plasma concentration of 6-methoxy-2-naphthylacetic acid (6MNA). Bioavailability is greater than 80%.
Distribution
Protein binding is more than 99% (active metabolite), and the Vd is at 0.1 to 0.2 L/kg.
Metabolism
Undergoes rapid biotransformation to main active metabolite 6MNA approximately 35% and the remaining unidentified metabolites approximately 50%. 6ߙMNA is metabolized in the liver to inactive metabolites.
Elimination
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.
Special Populations
Renal Function ImpairmentTerminal t ½ of 6MNA was increased.
ElderlySteady-state concentrations are generally higher.
Indications and Usage
Relief of symptoms of chronic and acute rheumatoid arthritis and osteoarthritis.
Contraindications
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.
Dosage and Administration
Osteoarthritis/Rheumatoid ArthritisAdults
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.
General Advice
- Administer with full glass of water, without regard to meals. Administer with food if GI upset occurs.
Storage/Stability
Store in tightly closed, light-resistant container at controlled room temperature (68° to 77°F).
Drug Interactions
ACE inhibitors (eg, captopril)Antihypertensive effects of ACE inhibitors may be reduced.
AnticoagulantsMay increase effect of anticoagulants. May increase risk of gastric erosion and bleeding.
AspirinRisk of adverse reactions may be increased.
CyclosporineNeurotoxicity of both agents may be increased.
LithiumMay increase lithium levels.
Loop diuretics (eg, furosemide), thiazide diuretics (eg, hydrochlorothiazide)Natriuretic effect of diuretics may be reduced.
MethotrexateIncreased risk of methotrexate toxicity.
SalicylatesAdditive GI toxicity.
Laboratory Test Interactions
May prolong bleeding time.
Adverse Reactions
Cardiovascular
Angina, arrhythmia, hypertension, MI, palpitations, syncope, thrombophlebitis (postmarketing).
CNS
Dizziness, headache (3% to 9%); fatigue, increased sweating, insomnia, nervousness, somnolence (1% to 3%); nightmares (postmarketing).
Dermatologic
Pruritus, rash (3% to 9%); acne, alopecia (postmarketing).
EENT
Tinnitus (3% to 9%).
GI
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).
Genitourinary
Dysuria, hematuria, impotence, renal stones (postmarketing).
Hematologic-Lymphatic
Anemia, granulocytopenia, leukopenia (postmarketing).
Hepatic
Elevations of ALT, AST (1%).
Metabolic-Nutritional
Hyperglycemia, hypokalemia, weight loss (postmarketing).
Miscellaneous
Edema (3% to 9%); chills, fever (postmarketing).
Precautions
WarningsNSAIDs 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. |
MonitorClosely 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. |
Pregnancy
Category C .
Lactation
Undetermined.
Children
Safety and efficacy not established.
Elderly
Increased risk of adverse reactions.
Hypersensitivity
May occur; use drug with caution in aspirin-sensitive patients because of possible cross-sensitivity.
Renal Function
Lower doses may be necessary in patients with renal function impairment.
Anemia
Check Hgb or Hct in patients on long-term therapy if there are signs or symptoms of anemia.
CHF and edema
Fluid retention and edema may occur; use with caution in patients with fluid retention or heart failure.
Ductus arteriosus
Can cause premature closure of the ductus arteriosus in fetus in late pregnancy.
Hypertension
Nabumetone can lead to onset of new hypertension or worsening of preexisting hypertension, which may contribute to an increased incidence of CV events.
Skin reactions
Serious, life-threatening skin adverse reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, can occur.
Overdosage
Symptoms
Acute renal failure, coma, drowsiness, epigastric pain, GI bleeding, hypertension, lethargy, nausea, respiratory depression, vomiting.
Patient Information
- Remind patient to take medication with full glass of water, either with or without food.
- Explain that therapeutic effects may take up to 1 mo to be noted.
- Instruct patients to report the following symptoms to health care provider: chest pain, dyspepsia, epigastric pain, hematemesis, melena, shortness of breath, slurring of speech, weakness, unexplained weight gain, or edema.
- Advise patient to seek immediate medical attention if difficulty breathing, swelling of the face or throat, nausea, fatigue, lethargy, pruritus, jaundice, right upper quadrant tenderness, flu-like symptoms, skin rash, blisters, fever, or other signs of hypersensitivity such as itching occur.
- Caution patient to avoid intake of alcoholic beverages and to avoid smoking.
- Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.
- Caution patient to avoid exposure to sunlight and to use sunscreen or wear protective clothing to avoid photosensitivity reaction.
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More Nabumetone resources:
Nabumetone - Includes detailed dosage instructions.
Rheumatoid Arthritis, Frozen Shoulder, Osteoarthritis
