nabumetone

Absorption: Nabumetone (a prodrug) is 80% absorbed after oral administration; 35% is rapidly converted to 6-methoxy-2-naphthylacetic acid (6-MNA), which is the active drug.

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: 6-MNA is metabolized by the liver to inactive compounds.

Half-Life: 24 hr (↑ in severe renal impairment).

Time/Action Profile ⬆ ⬇

(analgesia/anti-inflammatory effects)

ROUTE	ONSET	PEAK	DURATION
PO	1–2 days	few days–2 wk	12–24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Use with other NSAIDs, including aspirin; cross-sensitivity may occur;
Active GI bleeding or ulcer disease;
Perioperative pain from coronary artery bypass graft surgery;
OB: Avoid use after 30 wk gestation;
Lactation: Lactation.

Use Cautiously in:

Severe renal impairment;
Severe hepatic impairment;
Cardiovascular disease or risk factors for cardiovascular disease (may ↑ risk of serious cardiovascular thrombotic events, MI, and stroke, especially with prolonged use or use of higher doses);
History of ulcer disease;
OB: Use at or after 20 wk gestation may cause fetal or neonatal renal impairment; if treatment is necessary between 20 wk and 30 wk gestation, limit use to the lowest effective dose and shortest duration possible;
Pedi: Safety and effectiveness not established in children;
Geri: Appears on Beers list. risk GI bleeding or peptic ulcer disease in older adults. Avoid chronic use unless other alternatives are not effective and the patient can take a gastroprotective agent; avoid short-term use in combination with oral or parenteral corticosteroids, anticoagulants, or antiplatelet agents unless other alternatives are not effective and the patient can take a gastroprotective agent.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema, HF, hypertension, MI, vasculitis

Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), EXFOLIATIVE DERMATITIS, ↑sweating, photosensitivity, pruritus, rash, STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS

EENT: abnormal vision, tinnitus

GI: abdominal pain, diarrhea, anorexia, constipation, dry mouth, dyspepsia, flatulence, gastritis, gastroenteritis, GI BLEEDING, ↑liver enzymes, nausea, stomatitis, vomiting

GU: albuminuria, azotemia, interstitial nephritis

Hemat: prolonged bleeding time

Metab: ↑appetite, weight gain

Neuro: agitation, anxiety, confusion, depression, dizziness, drowsiness, fatigue, headache, insomnia, malaise, paresthesia, STROKE, tremor, weakness

Resp: dyspnea, hypersensitivity pneumonitis

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

↑adverse GI effects with aspirin, other NSAIDs, potassium supplements, corticosteroids, or alcohol.
Chronic use with acetaminophen may ↑ risk of adverse renal reactions.
May ↓ effectiveness of diuretics or antihypertensives.
May ↑ hypoglycemic effects of insulins or oral hypoglycemic agents.
↑risk of toxicity from methotrexate.
↑risk of bleeding with cefotetan, valproic acid, anticoagulants, clopidogrel, eptifibatide, tirofiban, or thrombolytics.
↑risk of adverse hematologic reactions with antineoplastics or radiation therapy.
Concurrent use with cyclosporine may ↑ risk of renal toxicity.

Route/Dosage ⬆ ⬇

PO (Adults ): 1000 mg/day as a single dose or divided dose twice daily; may be ↑ up to 2000 mg/day; use lowest effective dose during chronic therapy.

Availability ⬆ ⬇

(Generic available)

Tablets: 500 mg; 750 mg; 1000 mg

Assessment ⬆ ⬇

Patients who have asthma, aspirin-induced allergy, and nasal polyps are at increased risk for developing hypersensitivity reactions. Monitor for rhinitis, asthma, and urticaria.
Assess pain and range of motion before and periodically throughout therapy.
Monitor for signs and symptoms of DRESS (fever, rash, lymphadenopathy, facial swelling) periodically during therapy. Discontinue therapy if symptoms occur.

Lab Test Considerations:

Evaluate BUN, serum creatinine, CBC, and liver function periodically in patients receiving prolonged therapy.
- Serum potassium, BUN, serum creatinine, alkaline phosphatase, LDH, AST, and ALT tests may show ↑ levels. Blood glucose, hemoglobin, and hematocrit concentrations; leukocyte and platelet counts; and CCr may be ↓.
- May cause prolonged bleeding time.

Implementation ⬆ ⬇

Administration in higher-than-recommended doses does not provide increased effectiveness but may cause increased side effects. Use lowest effective dose for the shortest duration possible to minimize cardiac risks.
PO: Administer with meals or antacids to decrease GI irritation and increase absorption.

Patient/Family Teaching ⬆ ⬇

Advise patient to take this medication with a full glass of water and to remain in an upright position for 15–30 min after administration.
Instruct patient to take medication as directed. Take missed doses as soon as remembered but not if almost time for the next dose. Do not double dose.
May cause drowsiness, dizziness, or visual disturbances. Advise patient to avoid driving or other activities requiring alertness until response to the medication is known.
Advise patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
Caution patient to avoid the concurrent use of alcohol, aspirin, acetaminophen, or other OTC medications without consulting health care professional.
Advise patient to inform health care professional of medication regimen before treatment or surgery.
Advise patient to consult health care professional if rash, itching, visual disturbances, tinnitus, weight gain, edema, black stools, persistent headache, or influenza-like syndrome (chills, fever, muscle aches, pain) occurs.
Rep: May cause fetal harm. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Advise women to avoid nabumetone in the 3rd trimester of pregnancy (after 29 wk), may cause premature closure of the fetal ductus arteriosus. Use of nabumetone after 20 wk may cause fetal renal dysfunction leading to oligohydramnios. May cause reversible infertility in women attempting to conceive; may consider discontinuing nabumetone.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇