Nabumetone

Non-steroidal anti-inflammatory drug (NSAID), Acetic acid derivative

Nabumetone

Relafen

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Summary

Classes

Non-steroidal anti-inflammatory drug (NSAID), Acetic acid derivative

Pharmacy

Starting dose

1000 mg PO once daily; 500-2000 mg/d in single or divided doses

Preparations

500, 750 mg tablets

US FDA Max

2000 mg/d

Pharmacology

Routes

Oral

Onset

Analgesia within hours; anti-inflammatory effect over days

Duration

24 hours

Half-life

~24 hours (6-methoxy-2-naphthylacetic acid, the active metabolite)

Bioavailability

~38% (oral; non-acidic prodrug improves GI tolerability over many other NSAIDs)

Pregnancy

Avoid after 20 weeks (NSAID-class FDA 2020 advisory on fetal renal injury and oligohydramnios with second/third-trimester use).^{[citation needed]}

Legal status

Rx-only in US. Carries the NSAID-class Boxed Warning for cardiovascular thrombotic events and serious GI bleeding

Purported mechanism

Nabumetone is a non-acidic prodrug hepatically converted to 6-methoxy-2-naphthylacetic acid (6-MNA), a non-selective cyclooxygenase (COX-1/COX-2) inhibitor; the non-acidic parent and prolonged half-life of the active metabolite contribute to relatively favorable GI tolerability for chronic use compared with diclofenac or ibuprofen.▲0▼ Like all NSAIDs, raises CV thrombotic risk modestly (FDA 2014/2015 advisory) and produces GI, renal, hypertensive, and platelet-inhibitory effects characteristic of the class.