Nabumetone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Pain and inflammation
Adult: In patients w/ osteoarthritis and rheumatoid arthritis: 1,000 mg once daily at bedtime, an additional 500-1,000 mg may be given in the morning if necessary. Max: 2,000 mg daily in 1-2 divided doses. Patients <50 kg: <1 g daily.
Elderly: Max: 1 g daily.
Renal Impairment
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.
Hepatic Impairment
Severe: Contraindicated.
Cách dùng
May be taken with or without food. May be taken w/ meals to reduce GI distress.
Chống chỉ định
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.
Thận trọng
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.
Phản ứng phụ
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 (Avoid during 3rd trimester or near delivery.)
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, blurred vision, and confusion, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor BP, LFT, renal function, serum K level, CBC, 1st sign of rash, signs and symptoms of GI bleeding.
Quá liều
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.
Tương tác
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).
Food Interaction
Increased risk of GI bleeding w/ alcohol.
Lab Interference
May lead to false +ve aldosterone/renin ratio.
Tác dụng
Description: 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).
Đặc tính

Chemical Structure Image
Nabumetone

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

Bảo quản
Store between 20-25°C. Protect from light.
Phân loại ATC
M01AX01 - nabumetone ; Belongs to the class of other non-steroidal antiinflammatory and antirheumatic products.
References
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.

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