Perampanel


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Partial seizures with or without secondary generalisation
Adult: As adjunctive therapy: Initially, 2 mg once daily at bedtime. Maintenance: 4-8 mg daily. Adjust doses in increments of 2 mg daily at intervals of at least every 2 weeks according to clinical response and tolerability. Max: 12 mg daily. Treatment recommendations may vary among countries and individual products (refer to specific product guidelines).
Child: As adjunctive therapy: 4-11 years <20 kg: Initially, 1 mg once daily at bedtime; may adjust in increments of 1 mg daily. Maintenance: 2-4 mg daily; depending upon the patient’s clinical response and tolerability at a dose of 4 mg daily, may adjust the dose in increments of 0.5 mg daily to 6 mg daily. Max: 6 mg daily; 20-<30 kg: Initially, 1 mg once daily at bedtime. Maintenance: 4-6 mg daily. May adjust doses in increments of 1 mg daily. Max: 8 mg daily; ≥30 kg: Same as adult dose. All doses are adjusted at intervals of at least every 2 weeks according to clinical response and tolerability. ≥12 years Same as adult dose. Treatment recommendations may vary among countries and individual products (refer to specific product guidelines).

Oral
Primary generalised tonic-clonic seizures
Adult: In patients with idiopathic generalised epilepsy: As adjunctive therapy: Initially, 2 mg once daily at bedtime. Maintenance: Up to 8 mg daily. Adjust doses in increments of 2 mg daily at intervals of at least every 2 weeks according to clinical response and tolerability. Max: 12 mg daily.
Child: In patients with idiopathic generalised epilepsy: As adjunctive therapy: 7-11 years <20 kg: Initially, 1 mg once daily at bedtime; may adjust in increments of 1 mg daily. Maintenance: 2-4 mg daily; depending upon the patient’s clinical response and tolerability at a dose of 4 mg daily, may adjust the dose in increments of 0.5 mg daily to 6 mg daily. Max: 6 mg daily; 20-<30 kg: Initially, 1 mg once daily at bedtime. Maintenance: 4-6 mg daily. Adjust in increments of 1 mg daily. Max: 8 mg daily; ≥30 kg: Initially, 2 mg once daily at bedtime. Maintenance: 4-8 mg daily. May adjust doses in increments of 2 mg daily. Max: 12 mg daily. All doses are adjusted at intervals of at least 2 weeks according to clinical response and tolerability. ≥12 years Same as adult dose. Treatment recommendations may vary among countries and individual products (refer to specific product guidelines).
Nhóm bệnh nhân đặc biệt
Patients taking moderate or strong CYP3A4 inducers (e.g. phenytoin, carbamazepine, oxcarbazepine, rifampicin): Titrate dose at intervals of at least 1 week.
Suy thận
Moderate or severe; in patients undergoing haemodialysis: Not recommended.
Suy gan
Mild or moderate (Child-Pugh class A or B): Max: 8 mg daily. Severe (Child-Pugh class C): Not recommended.
Cách dùng
May be taken with or without food.
Thận trọng
Patients who are at risk of falls or with history of substance abuse. Avoid abrupt withdrawal unless clearly necessary. Patients taking moderate or strong CYP3A4 inducers. Renal and hepatic impairment. Children and elderly. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: CNS effects (e.g. dizziness, fatigue, somnolence, gait disturbances, ataxia, balance disorder), increased risk of falls, increased risk of suicidal ideation and behaviour.
Ear and labyrinth disorders: Vertigo.
Eye disorders: Blurred vision, diplopia.
Gastrointestinal disorders: Nausea.
Investigations: Weight gain.
Metabolism and nutrition disorders: Decreased or increased appetite.
Musculoskeletal and connective tissue disorders: Back pain.
Nervous system disorders: Dysarthria.
Psychiatric disorders: Anxiety, confusional state.
Potentially Fatal: Serious psychiatric and behavioural reactions (e.g. aggression, hostility, irritability, anger, homicidal ideation and threats), severe cutaneous adverse reactions (e.g. Stevens-Johnson syndrome, drug reaction with eosinophilia and systemic symptoms).
PO: Z (Insufficient data to conclude its safety and risk during pregnancy. Generally not recommended.)
Thông tin tư vấn bệnh nhân
This drug may cause dizziness and drowsiness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Closely monitor for signs or symptoms of serious neuropsychiatric disorders or changes in mood, behaviour, or personality, particularly during dose adjustments, high-dose treatment, and for at least 1 month after the last dose. Observe seizure frequency or duration.
Quá liều
Symptoms: Altered mental status, somnolence, stupor, psychiatric or behavioural reactions, depressed level of consciousness, coma. Management: Supportive treatment. Monitor vital signs and observe the clinical status of the patient. Ensure an adequate airway, oxygenation, and ventilation.
Tương tác
May reduce the efficacy of levonorgestrel-containing contraceptives. Decreased plasma levels with moderate and strong CYP3A4 inducers (e.g. phenytoin, carbamazepine, oxcarbazepine, rifampicin). Increased risk of hepatotoxicity with other antiepileptic drugs. May decrease the exposure of midazolam. Increased exposure and prolonged half-life with CYP3A4 inhibitors (e.g. ketoconazole).
Tương tác với thức ăn
May increase the CNS depression effect with alcohol. Decreased plasma concentrations with St. John's wort. Food may delay absorption but not the extent of absorption.
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 postsynaptic neurons. Its exact mechanism of action for antiseizure activity is not yet determined; however, it is known to reduce excessive glutamatergic activity and neuronal excitation by blocking the activity of glutamate, the primary excitatory neurotransmitter in the CNS.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed. May delay absorption, but not the extent, with food. Time to peak plasma concentration: 0.5-2.5 hours (fasted state).
Distribution: Plasma protein binding: Approx 95-96%, mainly to albumin and α1-acid glycoprotein.
Metabolism: Extensively metabolised via oxidation, mainly by CYP3A4/5 isoenzymes (and to a lesser extent by CYP1A2 and CYP2B6), and sequential glucuronidation.
Excretion: Tab: Via faeces (48%) and urine (22%), primarily as oxidative and conjugated metabolites. Elimination half-life: Approx 105 hours.
Đặc tính

Chemical Structure Image
Perampanel

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 9924495, Perampanel. https://pubchem.ncbi.nlm.nih.gov/compound/Perampanel. Accessed Sept. 26, 2022.

Bảo quản
Store between 15-30°C. Do not freeze the oral susp.
Phân loại MIMS
Thuốc chống co giật
Phân loại ATC
N03AX22 - perampanel ; Belongs to the class of other antiepileptics.
Tài liệu tham khảo
Anon. Perampanel. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 08/09/2022.

Anon. Perampanel. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/09/2022.

Buckingham R (ed). Perampanel. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/09/2022.

Eisai New Zealand Ltd. Fycompa 2 mg, 4 mg, 6 mg, 8 mg, 10 mg and 12 mg Film Coated Tablets and Fycompa 2 mg/4 mL Oral Suspension data sheet 29 November 2021. Medsafe. http://www.medsafe.govt.nz. Accessed 07/09/2022.

Fycompa 0.5 mg/mL Oral Suspension (Eisai Europe Limited). MHRA. https://products.mhra.gov.uk. Accessed 07/09/2022.

Fycompa 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, 12 mg Film-coated Tablets (Eisai Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/09/2022.

Fycompa 6 mg Film-coated Tablets (Eisai Europe Limited). MHRA. https://products.mhra.gov.uk. Accessed 07/09/2022.

Fycompa Tablet, Suspension (Eisai Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/09/2022.

Joint Formulary Committee. Perampanel. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/09/2022.

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