PeraMpanel

Product Name:

PeraMpanel

Synonyms:

PeraMpanel;E 2007;ER 155055-90;PeraMpanel-D5;PeraMpanel-13C6;3-(2-Cyanophenyl)-1-phenyl-5-(2-pyridyl)-1,2-dihydropyridin-2-one;3-(2-Cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one;2-(2-oxo-1-phenyl-5-(pyridin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile

CAS:

MF:

C23H15N3O

MW:

349.3847

EINECS:

691-969-4

Product Categories:

API;Inhibitors;-

Mol File:

380917-97-5.mol

 

PeraMpanel Chemical Properties

 

Safety Information

MSDS Information

 

PeraMpanel Usage And Synthesis

Description

Perampanel (licensed in 2012) is a third- generation AED known with the proprietary brand name of Fycompa® (Eisai, Hatfield) in the UK and Banzel® (Eisai, Hatfield) in the USA.

Indications

Epilepsy: Adjunctive treatment of focal seizures with or without secondary generalization and primary generalized tonic- clonic seizures.

Dose titration

Epilepsy— adjunctive therapy: 2 mg nocte for at least 14 days, then increased by 2 mg every 14 or more days; usual maintenance 4– 8 mg nocte (max. 12 mg nocte).

Interactions

With AEDs

• Some AEDs known as CYP450 3A enzyme inducers (carbamazepine, oxcarbazepine, phenytoin) have been shown to increase perampanel clearance and consequently to decrease plasma concentrations of perampanel. Carbamazepine, a known potent enzyme inducer, reduced perampanel levels by two- thirds in a study performed on healthy subjects
• In the epilepsy population pharmacokinetic analysis, perampanel was found to decrease the clearance of oxcarbazepine by 26%. Oxcarbazepine is rapidly metabolized by cytosolic reductase enzyme to the active metabolite, monohydroxycarbazepine. The effect of perampanel on monohydroxycarbazepine concentrations is not known.

With other drugs

• Strong inducers of cytochrome P450, such as rifampicin and St John’s Wort (Hypericum perforatum), are expected to decrease perampanel concentrations.
• In healthy subjects, the CYP3A4 inhibitor ketoconazole increases perampanel exposure.
• Perampanel can make certain hormonal contraceptives such as levonorgestrel less effective.
• Decrease in exposure of midazolam may be caused by perampanel.

With alcohol/food

• Drinking alcohol while taking perampanel can affect a patients’ alertness and ability to drive or use tools or machines. It can also aggravate irritability, confusion, and depression.
• There are no specific foods that must be excluded from diet when taking perampanel.

Special populations

Hepatic impairment

• Increase at intervals of at least 2 weeks, up to a maximum of 8 mg daily, in mild- to- moderate impairment.
• Avoid in severe impairment.

Renal impairment
Avoid in moderate or severe impairment.

Pregnancy

• There are limited amount of data available on the use of perampanel in pregnant women and the potential risk for humans is unknown.
• Perampanel is not recommended in pregnancy and female patients must use a reliable method of contraception to avoid becoming pregnant while being treated with perampanel (this should be continued for 1 month after stopping treatment).
• As perampanel can make certain hormonal contraceptives such as levonorgestrel less effective, other forms of safe and effective contraception (such as a condom or coil) should be used when taking perampanel (this should be continued for 1 month after stopping treatment).
• Perampanel has been found to be present in milk in animal studies and it is recommended that breastfeeding should be avoided.