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Chỉ định và Liều dùng
Oral
Adjunct to levodopa treatment in Parkinson's disease Adult: 200 mg w/ each levodopa/dopa decarboxylase inhibitor dose. Max: 200 mg 10 times daily (2,000 mg daily). Gradually reduce levodopa dose by approx 10-30% or increase dosing interval w/in the 1st few wk of starting treatment.
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Suy gan
Contraindicated.
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Cách dùng
May be taken with or without food.
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Chống chỉ định
Phaeochromocytoma, history of neuroleptic malignant syndrome and/or non-traumatic rhabdomyolysis. Hepatic impairment. Concomitant use w/ non-selective MAOIs.
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Thận trọng
Patient w/ biliary obstruction, ischaemic heart disease. Avoid abrupt withdrawal. Pregnancy and lactation.
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Tác dụng không mong muốn
Abdominal pain, nausea, vomiting, diarrhoea, constipation, colitis, dry mouth, dyskinesia, dizziness, nightmares, insomnia, hallucinations, confusion, fatigue, increased sweating, behavioural disturbances; urine, skin, hair, beard and nail discolourations; cholestatic hepatitis, rhabdomyolysis. Rarely, agitation, urticaria, erythematous or maculopapular rash, anorexia, wt decrease, increased liver enzymes.
Potentially Fatal: Neuroleptic malignant syndrome (NMS)-like syndrome (w/ abrupt reduction or withdrawal). |
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Thông tin tư vấn bệnh nhân
This drug may cause reddish-brown discolouration of urine. When given w/ levodopa, may cause dizziness and symptomatic orthostatism, if affected, do not drive or operate machinery.
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Chỉ số theo dõi
Monitor BP, hepatic function, mental status and impulse control disorders, daytime sleepiness, serum Fe, wt loss; signs/symptoms of Parkinson's disease, neuroleptic malignant syndrome (if abrupt withdrawal is required); regular dermatologic examination.
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Quá liều
Symptoms: Decreased activity, confusion, somnolence, hypotonia, urticaria, skin discolouration. Management: Symptomatic treatment.
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Tương tác
May interfere w/ metabolism of other drugs metabolised by COMT (e.g. rimiterole). May aggravate levodopa-induced orthostatic hypotension. Risk of dopaminergic effects w/ dopamine agonists (e.g. bromocriptine), selegiline, amantadine. May form chelates w/ Fe in the GI tract. Additive sedative effects w/ other CNS depressants.
Potentially Fatal: Concomitant use w/ non-selective MAOIs (e.g. phenelzine) may result in inhibition of principal pathways in the metabolism of catecholamines. |
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Tương tác với thức ăn
May potentiate the sedative effect of alcohol.
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Tác dụng
Description:
Mechanism of Action: Entacapone decreases the metabolic loss of levodopa to 3-O-methyldopa (3-OMD) through inhibition of COMT enzyme leading to an increased levodopa concentration, thus, extending the duration and effect in the brain. Pharmacokinetics: Absorption: Rapidly absorbed from the GI tract. Bioavailability: 29-46%. Time to peak plasma concentration: Approx 1 hr. Distribution: Plasma protein binding: Approx 98% (primarily to albumin). Metabolism: Undergoes extensive first-pass metabolism; isomerisation to the cis-isomer, followed by direct glucuronidation of the parent and cis-isomer. Excretion: Mainly via faeces (10%); urine (approx 10-20%, as glucuronide conjugates). Elimination half-life: Approx 1.6-3.4 hr. |
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Đặc tính
 Source: National Center for Biotechnology Information. PubChem Database. Entacapone, CID=5281081, https://pubchem.ncbi.nlm.nih.gov/compound/Entacapone (accessed on Jan. 21, 2020) |
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Bảo quản
Store at 25°C.
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Phân loại MIMS
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Phân loại ATC
N04BX02 - entacapone ; Belongs to the class of other dopaminergic agents used in the management of Parkinson's disease.
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Tài liệu tham khảo
Anon. Entacapone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/11/2015. Buckingham R (ed). Entacapone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/11/2015. Comtan Tablet, Film Coated (Novartis Pharmaceuticals Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 27/11/2015. McEvoy GK, Snow EK, Miller J et al (eds). Entacapone. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 27/11/2015.
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