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PeraMpanel

Description Indications Dose titration Interactions Special populations Behavioural and cognitive effects in patients with epilepsy Psychiatric use
PeraMpanel
PeraMpanel structure
CAS No.
380917-97-5
Chemical Name:
PeraMpanel
Synonyms
E 2007;CS-1116;Perampane;PeraMpanel;ER 155055-90;PeraMpanel-D5;PERAMPANEL API;PeraMpanel-13C6;Perampanel(E2007);Perampanel Impurity
CBNumber:
CB12598797
Molecular Formula:
C23H15N3O
Formula Weight:
349.38
MOL File:
380917-97-5.mol

PeraMpanel Properties

Boiling point:
619.1±55.0 °C(Predicted)
Density 
1.31±0.1 g/cm3(Predicted)
pka
4.73±0.19(Predicted)
FDA UNII
H821664NPK
NCI Drug Dictionary
perampanel

PeraMpanel price More Price(2)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 23003 Perampanel ≥98% 380917-97-5 10mg $124 2021-03-22 Buy
Cayman Chemical 23003 Perampanel 380917-97-5 5mg $65 2021-03-22 Buy

PeraMpanel Chemical Properties,Uses,Production

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.

Behavioural and cognitive effects in patients with epilepsy

For this third- generation agent, clinical experience is still limited, and little is known about its positive and negative psychotropic properties, and their implications for the management of behavioural symptoms in patients with epilepsy. There are initial reports of behavioural disturbances (especially depression, anxiety, irritability, and psychosis), which seem to be dose- related and tend to appear within the first weeks of treatment. Reports of cognitive effects (mainly affecting memory) are relatively rare.

Psychiatric use

Perampanel has no indications for the treatment of psychiatric disorders. There is insufficient experience with perampanel to draw any conclusion regarding its psychotropic profile.

Description

In October 2012, the US FDA approved perampanel for the treatment of partial onset seizures in epileptic patients who are at least 12 years old. Perampanel is the first AMPA receptor antagonist to receive FDA approval as an AED. AMPA glutamate receptors are found primarily on postsynaptic neurons in the brain. As a selective, noncompetitive antagonist of AMPA, parampanel prevents ion channel opening and reduces propagation of action potential. Parampanel was discovered through lead optimization of a commercially available compound, 2,4-diphenyl-4H-[1,3,4]oxadiazin-5-one, which was identified by high-throughput screening of a compound collection employing a rat cortical neuron AMPA-induced cell-death assay. Modifications of aromatic rings at positions 1, 3, and 5 while changing the core to pyridone led to parampanel which inhibited AMPA-induced calcium influx (IC50=60 nM). Parampanel had a minimum effective oral dose of 2 mg/kg in an AMPA-induced mouse seizure model. The synthesis of parampanel was accomplished via a 6-step route utilizing Suzuki–Miyaura couplings and modified Ullmann reactions for incorporation of aryl groups.

Originator

Eisai (Japan)

Definition

ChEBI: A member of the class of bipyridines that is 2,3'-bipyridin-6'-one substituted at positions 1' and 5' by phenyl and 2-cyanophenyl groups respectively. Used as an adjunctive therapy for the treatment of partial-onset seizures in patients with epilepsy.

brand name

Fycompa

PeraMpanel Preparation Products And Raw materials

Raw materials

Preparation Products


PeraMpanel Suppliers

Global( 129)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 37282 58
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 8882 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29960 58
Shochem(Shanghai) Co.,Ltd
86-21-50800795
info@shochem.com CHINA 289 58
Zhuozhou Wenxi import and Export Co., Ltd
+8613111626072 (WhatsApp)
Wechat: +8613111626072 Wickr me: waynehu zzwenxi@126.com CHINA 13187 58
ShenZhen Ipure Biology import and export company co.,ltd
18071025641 18071025641
eric@ipurechemical.com CHINA 11336 58
AFINE CHEMICALS LIMITED
008657185134551
008657185134895 info@afinechem.com CHINA 15559 58

Related articles


View Lastest Price from PeraMpanel manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-07-13 Perampanel
380917-97-5
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
2021-07-10 Perampanel
380917-97-5
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
2019-09-02 PeraMpanel
380917-97-5
US $7.00 / KG 1KG 99% JD 474 career henan chemical co

380917-97-5(PeraMpanel)Related Search:


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  • 380917-97-5
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  • API
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