Nabumetone
Nabumetone
Relafen
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Summary
Common uses
Osteoarthritis0, Rheumatoid arthritis0, Acute musculoskeletal pain0
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)[1]
Bioavailability
~38% (oral; non-acidic prodrug improves GI tolerability over many other NSAIDs)[1]
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
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[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Relafen (nabumetone), GSK, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019583s045lbl.pdf