Nabumetone

Oral
Pain and inflammation

CrCl (mL/min)	Dosage
<30	Initially, 500 mg once daily. Max: 1,000 mg daily.
30-49	Initially, 750 mg once daily. Max: 1,500 mg daily.

Severe: Contraindicated.

May be taken with or without food. May be taken w/ meals to reduce GI distress.

Hypersensitivity. History of asthma, urticaria, or allergic reaction w/ aspirin or other NSAIDS. Active or history of recurrent GI bleeding, ulceration, or perforation. Recent MI, severe heart failure. Coronary artery bypass graft (CABG) surgery. Pregnancy and lactation. Concomitant use w/ other NSAIDs.

Patient w/ HTN, oedema, CHF, ischaemic heart disease, peripheral arterial disease, coagulation disorders, risk factors for CV disease; history of GI disease (e.g. ulcerative colitis, Crohn’s disease). Moderate to severe renal impairment. Elderly.

Significant: HTN, drowsiness, dizziness, blurred vision, confusion, decreased platelet adhesion and aggregation, prolonged bleeding time, fluid retention, oedema, cardiac failure, anaemia, elevated transaminases, abnormal LFT, hyperkalaemia, photosensitivity reaction, renal papillary necrosis and renal injury (long-term use).
Nervous: Headache, drowsiness, asthenia, fatigue, insomnia, nervousness, somnolence, paraesthesia, anxiety.
GI: Diarrhoea, dyspepsia, abdominal pain, constipation, flatulence, nausea, occult blood in stools, gastritis, stomatitis, vomiting, xerostomia, haematemesis.
Resp: Dyspnoea, resp disorder, epistaxis.
Musculoskeletal: Myopathy.
Ophthalmologic: Eye disorder.
Otic: Tinnitus, ear disorder.
Dermatologic: Pruritus, rash, diaphoresis, urticaria.
Potentially Fatal: Anaphylactoid reactions, CV thrombotic events (e.g. MI, stroke); GI bleeding, ulceration, or perforation; bronchospasm; serious skin reactions (e.g. exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrosis. Rarely, severe blood dyscrasias (e.g. agranulocytosis, thrombocytopenia, aplastic anaemia); severe hepatic reactions (e.g. fulminant hepatitis, liver necrosis, jaundice, hepatic failure).

PO: C, Z (NSAIDs caused foetal ductus arteriosus premature closure, foetal renal impairment and persistent pulmonary hypertension. Avoid near term, else use lowest dose for shortest time.)

This drug may cause dizziness, blurred vision, and confusion, if affected, do not drive or operate machinery.

Monitor BP, LFT, renal function, serum K level, CBC, 1st sign of rash, signs and symptoms of GI bleeding.

Symptoms: Headache, nausea, vomiting, epigastric pain, GI bleeding, diarrhoea, disorientation, excitation, coma, drowsiness, tinnitus, convulsions. Acute renal failure, liver damage. Management: Symptomatic and supportive treatment. Consider admin of activated charcoal. Perform gastric lavage immediately following large ingestion. Convulsions can be treated w/ IV diazepam. Ensure good urine output.

Increased risk of GI bleeding w/ corticosteroids, anticoagulants (e.g. warfarin), SSRIs, antiplatelets (e.g. clopidogrel). May induce hyperkalaemia w/ ACE-inhibitors. May decrease elimination of lithium, methotrexate. Increased risk of nephrotoxicity w/ ciclosporin, tacrolimus. Increased risk of haematological toxicity w/ zidovudine.
Potentially Fatal: Increased GI complications w/ other NSAIDs (e.g. aspirin).

Increased risk of GI bleeding w/ alcohol.

May lead to false +ve aldosterone/renin ratio.

Description:
Mechanism of Action: Nabumetone is a naphthylalkanone derivative, non-active prodrug which is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid (6-MNA) which is structurally similar to naproxen. 6-MNA reversibly inhibits cyclooxygenase-1 and 2 enzymes resulting in inhibition of prostaglandin synthesis.
Onset: Several days.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Bioavailability: Approx 35 % (6-MNA). Time to peak plasma concentration: Approx 3 hr (6-MNA).
Distribution: Diffuses into synovial fluid. Crosses placenta and enters breast milk. Volume of distribution 7.5 L (6-MNA). Plasma protein binding: >99% (6-MNA).
Metabolism: Undergoes rapid and extensive first-pass metabolism in the liver into active metabolite, 6-methoxy-2-naphthylacetic acid (6-MNA), and some inactive metabolites; further metabolised via O-methylation and conjugation.
Excretion: Via urine (approx 80% as inactive or conjugated metabolites, <1% as unchanged 6-MNA; faeces (9%). Elimination half-life: Approx 24 hr (6-MNA).

Source: National Center for Biotechnology Information. PubChem Database. Nabumetone, CID=4409, https://pubchem.ncbi.nlm.nih.gov/compound/Nabumetone (accessed on Jan. 22, 2020)

Store between 20-25°C. Protect from light.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AX01 - nabumetone ; Belongs to the class of other non-steroidal antiinflammatory and antirheumatic products.

Anon. Nabumetone. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 22/08/2017.

Anon. Nabumetone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 22/08/2017.

Buckingham R (ed). Nabumetone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 22/08/2017.

Joint Formulary Committee. Nabumetone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 22/08/2017.

Nabumetone Tablet (Eon Labs, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 22/08/2017.