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Nabumetone

Pronunciation

Pronunciation: nab-UE-me-TONE
Class: NSAID

Trade Names

Nabumetone
- Tablets 500 mg
- Tablets 750 mg

Apo-Nabumetone (Canada)
Gen-Nabumetone (Canada)

Pharmacology

Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.

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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%. 6 MNA 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 Impairment

Terminal t ½ of 6-MNA was increased.

Elderly

Steady-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 Arthritis
Adults

PO 1,000 mg initially; may increase to 1,500 to 2,000 mg daily in 1 to 2 divided doses.

Renal Function Impairment
Adults

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.

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.

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

Warnings

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.


Monitor

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.


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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