Drug reference

Nabumetone

NSAID · Anti-inflammatory, Analgesic

NSAIDAnti-inflammatory, Analgesic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Avoid during third trimester (risk of premature closure of fetal ductus arteriosus and persistent pulmonary hypertension of the newborn); onset of labour may be delayed and duration may be increased.

FDA category + note

Top interactionssee all 12 →

AminoglycosideSevereTextbookKDT 7e · p746
AminoglycosidesSevereTextbookKDT 7e
AnticoagulantsSevereTextbookKDT 7e
CorticosteroidsSevereTextbookKDT 7e

Mechanism

Nabumetone is a traditional nonsteroidal anti-inflammatory drug (tNSAID) that acts as a competitive, reversible, active site inhibitor of both cyclooxygenase (COX) enzymes, COX-1 and COX-2. This inhibition leads to a reduction in prostaglandin synthesis, such as PGE2, thereby mitigating pain and inflammation.

Indications

Pain and inflammation in osteoarthritis and rheumatoid arthritisRheumatoid arthritisOsteoarthritissoft tissue injury

Dosing

Adult: For pain and inflammation in osteoarthritis and rheumatoid arthritis: 1 g once daily, dose to be taken at night. For severe and persistent symptoms: 0.5–1 g, dose to be taken in the morning and 1 g, dose to be taken at night.
Renal adjustment: Avoid if possible or use with caution. Avoid if eGFR less than 25 mL/minute/1.73 m2.
Hepatic adjustment: Manufacturer advises caution in mild to moderate impairment; avoid in severe impairment.
Geriatric: 0.5–1 g daily
Max dose: 2 g daily

Pharmacokinetics

Onset

Peak plasma concentration (Cp) ~3 h

Half-life

longer than 10 hours

Protein binding

99%

Metabolism

First-pass effects during conversion of prodrug to active metabolite; conjugates.

Contraindications

Active gastro-intestinal bleeding
Active gastro-intestinal ulceration
History of gastro-intestinal bleeding related to previous NSAID therapy
History of gastro-intestinal perforation related to previous NSAID therapy
History of recurrent gastro-intestinal haemorrhage (two or more distinct episodes)
History of recurrent gastro-intestinal ulceration (two or more distinct episodes)
Severe heart failure
Third trimester of pregnancy (risk of premature closure of fetal ductus arteriosus and persistent pulmonary hypertension of the newborn)

Side effects

Common

ConstipationDiarrhoeaEar disorderGastrointestinal discomfortGastrointestinal disordersNauseaLess fecal blood loss during short-term therapyAdverse effects (13%): GI upset, abdominal painCrampy lower abdominal pain (12%)Diarrhea (14%)Rash (3%–9%)Headache (3%–9%)Dizziness (3%–9%)HeartburnTinnitusPruritus (3%–9%)abdominal cramps

Pregnancy & lactation

Pregnancy

Avoid during third trimester (risk of premature closure of fetal ductus arteriosus and persistent pulmonary hypertension of the newborn); onset of labour may be delayed and duration may be increased.

Lactation

Use with caution during breast-feeding. Present in milk in animal studies—manufacturer advises avoid.

Drug interactions

Aminoglycoside

Severe

Textbook

Increased risk of nephrotoxicity.

Avoid concurrent use.

Source: KDT 7e · p746

Aminoglycosides

Severe

Textbook

Increased aminoglycoside levels and potential toxicity.

Monitor aminoglycoside levels and renal function; adjust dosage as needed.

Source: KDT 7e

Anticoagulants

Severe

Textbook

Increased risk of gastrointestinal bleed.

Monitor for bleeding; consider alternative analgesics or gastroprotective agents.

Source: KDT 7e

Corticosteroids

Severe

Textbook

Increased risk of gastrointestinal bleed.

Monitor for bleeding; consider gastroprotective agents.

Source: KDT 7e

Dapoxetine

Severe

Textbook

Increased risk of gastrointestinal bleed.

Monitor for bleeding; consider gastroprotective agents or alternative analgesics.

Source: KDT 7e

Enalaprilat

Severe

Textbook

Reduced effectiveness of ACE inhibitors. Marked hyperkalemia, potentially leading to cardiac arrhythmia.

Use with caution, especially in the elderly and in patients with hypertension, diabetes mellitus, or ischemic heart disease.

Source: G&G 14e · p836

Escitalopram + Clonazepam

Severe

Textbook

Increased risk of gastrointestinal bleed.

Monitor for bleeding; consider gastroprotective agents or alternative analgesics.

Source: KDT 7e

Glucocorticoids

Severe

Textbook

Increased risk of gastritis, ulcer formation, and gastrointestinal bleeding. Glucocorticoids can also mask the symptoms of serious gastrointestinal disease, increasing the risk of perforated sigmoid diverticular abscesses.

Not explicitly stated, but implies caution and awareness of increased risk.

Source: G&G 14e · p1013

Quinolones

Severe

Textbook

Enhanced neurological adverse effects.

Use with caution, especially in patients with a history of epilepsy.

Source: G&G 14e · p1144

Acalabrutinib

Severe

Database

Drug interaction classified as: synergy