Perampanel


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Generalised tonic-clonic seizures, Partial seizures
Adult: As adjunctive therapy: Initially, 2 mg once daily at bedtime, adjusted in increments of 2 mg at intervals of at least 2 wk, according to response. Maintenance: 4-8 mg daily. Max: 12 mg daily.
Child: ≥12 yr Same as adult dose. 
Special Patient Group
Patients taking concomitant CYP3A inducing antiepileptics: Titrate at intervals of at least 1 wk.
Renal Impairment
Moderate to severe: Contraindicated.
Hepatic Impairment
Mild to moderate: Max: 8 mg daily. Severe: Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Severe hepatic and moderate to severe renal impairment.
Thận trọng
Patient w/ history of psychiatric or behavioural problems and substance abuse, and those at risk of falls. Patients taking concomitant CYP3A inducing antiepileptics. Mild to moderate hepatic impairment. Childn. Pregnancy and lactation.
Phản ứng phụ
Significant: Dizziness, somnolence, fatigue, gait disturbance (e.g. balance disorder, ataxia, abnormal coordination).
Nervous: Drowsiness, dysarthria, vertigo, anxiety, confusion, paraesthesia, fall.
GI: Increased/decreased appetite, nausea, vomiting.
Endocrine: Wt gain.
Musculoskeletal: Back pain.
Ophthalmologic: Diplopia, blurred vision.
Dermatologic: Rash.
Potentially Fatal: Serious neuropsychiatric events (e.g. aggression, irritability, anger, hostility, homicidal and suicidal ideation).
Thông tin tư vấn bệnh nhân
This drug may cause dizziness and somnolence, if affected, do not drive or operate machinery. Avoid abrupt withdrawal.
MonitoringParameters
Monitor seizure frequency and duration, suicidality (during therapy and for at least 1 mth after discontinuation), wt.
Tương tác
Increased metabolism w/ other antiepileptics that are CYP3A inducers (e.g. carbamazepine, oxcarbazepine, phenytoin). May decrease the efficacy of OCs. Decreased concentrations w/ strong CYP enzyme inducers (e.g. rifampicin). Increased risk of CNS-related adverse effect of other CNS depressants (e.g. benzodiazepines, opiate analgesics, barbiturates, sedating antihistamines).
Food Interaction
Increased sedative and cognitive effects w/ alcohol. Decreased concentrations w/ St. John’s wort.
Tác dụng
Description: Perampanel is a selective, non-competitive antagonist of the ionotropic α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptor on post-synaptic neurons. Its exact mechanism of action is not yet determined, however, it is known to reduce neuronal excitation by blocking the activity of glutamate, the primary excitatory neurotransmitter in the CNS.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed. Time to peak plasma concentration: 0.5-2.5 hr.
Distribution: Plasma protein binding: Approx 95%, mainly to albumin and α1-acid glycoprotein.
Metabolism: Extensively metabolised via oxidation, mainly by CYP3A4/5 enzymes (and to a lesser extent by CYP1A2 and CYP2B6 enzymes), w/ sequential glucuronidation.
Excretion: Via urine and faeces, as oxidative and conjugated metabolites. Elimination half-life: Approx 105 hr.
Đặc tính

Chemical Structure Image
Perampanel

Source: National Center for Biotechnology Information. PubChem Database. Perampanel, CID=9924495, https://pubchem.ncbi.nlm.nih.gov/compound/Perampanel (accessed on Jan. 22, 2020)

Bảo quản
Store between 15-30°C.
Phân loại MIMS
Phân loại ATC
N03AX22 - perampanel ; Belongs to the class of other antiepileptics.
References
Anon. Perampanel. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/04/2017.

Anon. Perampanel. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/04/2017.

Buckingham R (ed). Perampanel. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2017.

Fycompa Tablet and Suspension (Eisai Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/04/2017.

Joint Formulary Committee. Perampanel. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2017.

Thông báo miễn trừ trách nhiệm: Thông tin này được MIMS biên soạn một cách độc lập dựa trên thông tin của Perampanel từ nhiều nguồn tài liệu tham khảo và được cung cấp chỉ cho mục đích tham khảo. Việc sử dụng điều trị và thông tin kê toa có thể khác nhau giữa các quốc gia. Vui lòng tham khảo thông tin sản phẩm trong MIMS để biết thông tin kê toa cụ thể đã qua phê duyệt ở quốc gia đó. Mặc dù đã rất nỗ lực để đảm bảo nội dung được chính xác nhưng MIMS sẽ không chịu trách nhiệm hoặc nghĩa vụ pháp lý cho bất kỳ yêu cầu bồi thường hay thiệt hại nào phát sinh do việc sử dụng hoặc sử dụng sai các thông tin ở đây, về nội dung thông tin hoặc về sự thiếu sót thông tin, hoặc về thông tin khác. © 2021 MIMS. Bản quyền thuộc về MIMS. Phát triển bởi MIMS.com
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in