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Identification
NamePerampanel
Accession NumberDB08883
TypeSmall Molecule
GroupsApproved
Description

Perampanel is a noncompetitive AMPA glutamate receptor antagonist. It is marketed under the name Fycompa™ and is indicated as an adjunct in patients over 12 years old for the treatment of partial-onset seizures that may or may not occur with generalized seizures. The FDA label includes an important black-boxed warning of serious or life-threatening behavioral and psychiatric reactions in patients taking Fycompa™.

Structure
Thumb
Synonyms
3-(2-Cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one
perampanel
pérampanel
Perampanelum
External Identifiers
  • E-2007
  • E2007
  • ER-155055-90
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Fycompatablet12.0 mgoralEisai Limited2013-05-17Not applicableCanada
FycompakitEisai Inc.2012-10-22Not applicableUs
Fycompatablet2.0 mgoralEisai Limited2013-06-19Not applicableCanada
Fycompatablet12 mg/1oralEisai Inc.2012-10-22Not applicableUs
Fycompatablet10 mg/1oralEisai Inc.2012-10-22Not applicableUs
Fycompatablet10.0 mgoralEisai Limited2013-06-03Not applicableCanada
Fycompatablet8 mg/1oralEisai Inc.2012-10-22Not applicableUs
Fycompatablet8.0 mgoralEisai Limited2013-06-19Not applicableCanada
Fycompatablet6 mg/1oralEisai Inc.2012-10-22Not applicableUs
Fycompatablet6.0 mgoralEisai Limited2013-06-19Not applicableCanada
Fycompatablet4 mg/1oralEisai Inc.2012-10-22Not applicableUs
Fycompatablet4.0 mgoralEisai Limited2013-06-19Not applicableCanada
Fycompatablet2 mg/1oralEisai Inc.2012-10-22Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Perampanel hydrate
1571982-04-1
Thumb
  • InChI Key: PDWMJDKMSASBNE-UHFFFAOYSA-N
  • Monoisotopic Mass: 1450.517742513
  • Average Mass: 1451.617
DBSALT001824
Categories
UNIIH821664NPK
CAS number380917-97-5
WeightAverage: 349.393
Monoisotopic: 349.121512115
Chemical FormulaC23H15N3O
InChI KeyPRMWGUBFXWROHD-UHFFFAOYSA-N
InChI
InChI=1S/C23H15N3O/c24-15-17-8-4-5-11-20(17)21-14-18(22-12-6-7-13-25-22)16-26(23(21)27)19-9-2-1-3-10-19/h1-14,16H
IUPAC Name
2-{6'-oxo-1'-phenyl-1',6'-dihydro-[2,3'-bipyridine]-5'-yl}benzonitrile
SMILES
O=C1N(C=C(C=C1C1=CC=CC=C1C#N)C1=NC=CC=C1)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as bipyridines and oligopyridines. These are organic compounds containing two pyridine rings linked to each other.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPyridines and derivatives
Sub ClassBipyridines and oligopyridines
Direct ParentBipyridines and oligopyridines
Alternative Parents
Substituents
  • Bipyridine
  • 3-phenylpyridine
  • Benzonitrile
  • Dihydropyridine
  • Pyridinone
  • Monocyclic benzene moiety
  • Hydropyridine
  • Benzenoid
  • Heteroaromatic compound
  • Lactam
  • Nitrile
  • Carbonitrile
  • Azacycle
  • Organooxygen compound
  • Organonitrogen compound
  • Hydrocarbon derivative
  • Organic oxide
  • Cyanide
  • Organic oxygen compound
  • Organic nitrogen compound
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationUsed in patients over 12 years old for the treatment of partial-onset seizures that may or may not occur with generalized seizures.
PharmacodynamicsPerampanel is involved in inhibiting neuronal excitation in the central nervous system leading to such effects as decreased pyschomotor performance.
Mechanism of actionThe exact mechanism of action of perampanel in seizures is not yet determined, but it is known that perampanel decreases neuronal excitation by non-competitive ihibition of the AMPA receptor.
Related Articles
AbsorptionAfter oral adminitration, perampanel is absorbed rapidly and completely.
Volume of distribution

The volume of distribution of perampanel was not quantified.

Protein bindingPerampanel is 95-96% plasma protein bound with most binding to the plasma proteins α1-acid glycoprotein and albumin.
Metabolism

Perampanel is highly metabolized by CYP3A4 and/or CYP3A5 primary oxidation and by sequential glucuronidation.

Route of eliminationPerampanel is eliminated mostely in the feces (48%) and to a lesser exten in the urine (22%).
Half lifePerampanel has a long elmination half-life of about 105 hours.
Clearance

In healthy patients, perampanel has a clearance of about 12 mL/min.

ToxicityThe FDA label includes an important warning of serious or life-threatening behavioral and psychiatric adverse reactions including aggression, hostility, irritability, anger, and homicidal thoughts in patients taking perampanel.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Kit
Tabletoral10 mg/1
Tabletoral10.0 mg
Tabletoral12 mg/1
Tabletoral12.0 mg
Tabletoral2 mg/1
Tabletoral2.0 mg
Tabletoral4 mg/1
Tabletoral4.0 mg
Tabletoral6 mg/1
Tabletoral6.0 mg
Tabletoral8 mg/1
Tabletoral8.0 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6949571 No2001-06-082021-06-08Us
US8772497 No2006-05-162026-05-16Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityPractically insoluble in water.From FDA label.
Predicted Properties
PropertyValueSource
Water Solubility0.0056 mg/mLALOGPS
logP3.54ALOGPS
logP4.11ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)4.01ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area56.99 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity104.74 m3·mol-1ChemAxon
Polarizability38.03 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Francesco Fontana, “METHODS FOR PREPARING INTERMEDIATES OF PERAMPANEL.” U.S. Patent US20130109862, issued May 02, 2013.

US20130109862
General References
  1. Hanada T, Hashizume Y, Tokuhara N, Takenaka O, Kohmura N, Ogasawara A, Hatakeyama S, Ohgoh M, Ueno M, Nishizawa Y: Perampanel: a novel, orally active, noncompetitive AMPA-receptor antagonist that reduces seizure activity in rodent models of epilepsy. Epilepsia. 2011 Jul;52(7):1331-40. doi: 10.1111/j.1528-1167.2011.03109.x. Epub 2011 Jun 2. [PubMed:21635236 ]
External Links
ATC CodesN03AX22
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (611 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AlfentanilPerampanel may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
AlprazolamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
AmitriptylinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
AmobarbitalPerampanel may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
AmoxapinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
AripiprazolePerampanel may increase the central nervous system depressant (CNS depressant) activities of Aripiprazole.
AsenapinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
AzelastinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenPerampanel may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
BexaroteneThe serum concentration of Perampanel can be decreased when it is combined with Bexarotene.
BosentanThe serum concentration of Perampanel can be decreased when it is combined with Bosentan.
BrexpiprazolePerampanel may increase the central nervous system depressant (CNS depressant) activities of Brexpiprazole.
BrimonidinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
BromazepamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Bromazepam.
BrompheniraminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Brompheniramine.
BuprenorphinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BuspironePerampanel may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
ButabarbitalPerampanel may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
ButorphanolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
CarbamazepineThe serum concentration of Perampanel can be decreased when it is combined with Carbamazepine.
CarbinoxaminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Carbinoxamine.
CarisoprodolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Carisoprodol.
CetirizinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Cetirizine.
ChlordiazepoxidePerampanel may increase the central nervous system depressant (CNS depressant) activities of Chlordiazepoxide.
ChlorphenaminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Chlorphenamine.
ChlorpromazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Chlorpromazine.
ChlorzoxazonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
ClemastinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Clemastine.
ClobazamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
ClomipraminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Clomipramine.
ClonazepamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Clonazepam.
ClonidinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
ClorazepatePerampanel may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
ClozapinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
CyclizinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.
CyclobenzaprinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Cyclobenzaprine.
CyproheptadinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
DabrafenibThe serum concentration of Perampanel can be decreased when it is combined with Dabrafenib.
DantrolenePerampanel may increase the central nervous system depressant (CNS depressant) activities of Dantrolene.
DeferasiroxThe serum concentration of Perampanel can be decreased when it is combined with Deferasirox.
DesfluranePerampanel may increase the central nervous system depressant (CNS depressant) activities of Desflurane.
DesipraminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Desipramine.
DesloratadinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
Dexchlorpheniramine maleatePerampanel may increase the central nervous system depressant (CNS depressant) activities of Dexchlorpheniramine maleate.
DiazepamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
DienogestThe serum concentration of Dienogest can be decreased when it is combined with Perampanel.
DimenhydrinatePerampanel may increase the central nervous system depressant (CNS depressant) activities of Dimenhydrinate.
DiphenhydraminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Diphenhydramine.
DoxepinPerampanel may increase the central nervous system depressant (CNS depressant) activities of Doxepin.
DoxylaminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Doxylamine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Perampanel.
DroperidolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Droperidol.
EfavirenzPerampanel may increase the central nervous system depressant (CNS depressant) activities of Efavirenz.
EntacaponePerampanel may increase the central nervous system depressant (CNS depressant) activities of Entacapone.
EnzalutamideThe serum concentration of Perampanel can be decreased when it is combined with Enzalutamide.
EstazolamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
EszopiclonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Eszopiclone.
EthanolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthosuximidePerampanel may increase the central nervous system depressant (CNS depressant) activities of Ethosuximide.
EthotoinPerampanel may increase the central nervous system depressant (CNS depressant) activities of Ethotoin.
EtonogestrelThe serum concentration of Etonogestrel can be decreased when it is combined with Perampanel.
EzogabinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Ezogabine.
FelbamatePerampanel may increase the central nervous system depressant (CNS depressant) activities of Felbamate.
FentanylPerampanel may increase the central nervous system depressant (CNS depressant) activities of Fentanyl.
FexofenadinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Fexofenadine.
FlibanserinPerampanel may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
FlunarizinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
FlupentixolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
FluphenazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Fluphenazine.
FlurazepamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Flurazepam.
FosphenytoinThe serum concentration of Perampanel can be decreased when it is combined with Fosphenytoin.
GabapentinPerampanel may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
gabapentin enacarbilPerampanel may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Gamma Hydroxybutyric AcidPerampanel may increase the central nervous system depressant (CNS depressant) activities of Gamma Hydroxybutyric Acid.
GuanfacinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
HaloperidolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Haloperidol.
HydrocodonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydromorphonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
HydroxyzinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Hydroxyzine.
IloperidonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
ImipraminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Imipramine.
IsofluranePerampanel may increase the central nervous system depressant (CNS depressant) activities of Isoflurane.
KetaminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Ketamine.
LamotriginePerampanel may increase the central nervous system depressant (CNS depressant) activities of Lamotrigine.
LevetiracetamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Levetiracetam.
LevocabastinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.
LevocetirizinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.
LevonorgestrelThe serum concentration of Levonorgestrel can be decreased when it is combined with Perampanel.
LevorphanolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Levorphanol.
LoratadinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Loratadine.
LorazepamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Lorazepam.
LoxapinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
LurasidonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Perampanel.
MaprotilinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
MeclizinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Meclizine.
Medroxyprogesterone acetateThe serum concentration of Medroxyprogesterone Acetate can be decreased when it is combined with Perampanel.
MefloquineThe therapeutic efficacy of Perampanel can be decreased when used in combination with Mefloquine.
MeprobamatePerampanel may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
MetaxalonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
MethadonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Methadone.
MethocarbamolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Methocarbamol.
MethohexitalPerampanel may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
MethotrimeprazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethsuximidePerampanel may increase the central nervous system depressant (CNS depressant) activities of Methsuximide.
MetyrosinePerampanel may increase the sedative activities of Metyrosine.
MidazolamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Midazolam.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Perampanel.
MirtazapinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MitotaneThe serum concentration of Perampanel can be decreased when it is combined with Mitotane.
MorphinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Perampanel.
NalbuphinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Nalbuphine.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Perampanel.
NitrazepamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.
Nitrous oxidePerampanel may increase the central nervous system depressant (CNS depressant) activities of Nitrous oxide.
NorethisteroneThe serum concentration of Norethindrone can be decreased when it is combined with Perampanel.
NortriptylinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Nortriptyline.
OlanzapinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.
OlopatadinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
OrlistatThe serum concentration of Perampanel can be decreased when it is combined with Orlistat.
OrphenadrinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxazepamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Oxazepam.
OxcarbazepineThe serum concentration of Oxcarbazepine can be increased when it is combined with Perampanel.
OxycodonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
OxymorphonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
PaliperidonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Paliperidone.
ParaldehydePerampanel may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Perampanel is combined with Paroxetine.
PentazocinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Pentazocine.
PentobarbitalPerampanel may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
PerphenazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Perphenazine.
PethidinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
PhenobarbitalThe serum concentration of Perampanel can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Perampanel can be decreased when it is combined with Phenytoin.
PimozidePerampanel may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
PipotiazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Pipotiazine.
PizotifenPerampanel may increase the central nervous system depressant (CNS depressant) activities of Pizotifen.
PomalidomidePerampanel may increase the central nervous system depressant (CNS depressant) activities of Pomalidomide.
PramipexolePerampanel may increase the sedative activities of Pramipexole.
PregabalinPerampanel may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.
PrimidoneThe serum concentration of Perampanel can be decreased when it is combined with Primidone.
ProchlorperazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Prochlorperazine.
PromazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Promazine.
PromethazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Promethazine.
PropofolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Propofol.
ProtriptylinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
QuazepamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Quazepam.
QuetiapinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Quetiapine.
RamelteonPerampanel may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
RemifentanilPerampanel may increase the central nervous system depressant (CNS depressant) activities of Remifentanil.
ReserpinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Reserpine.
RifabutinThe serum concentration of Perampanel can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Perampanel can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Perampanel can be decreased when it is combined with Rifapentine.
RisperidonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Risperidone.
RopinirolePerampanel may increase the sedative activities of Ropinirole.
RotigotinePerampanel may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Perampanel.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Perampanel.
ScopolaminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Scopolamine.
Scopolamine butylbromidePerampanel may increase the central nervous system depressant (CNS depressant) activities of Scopolamine butylbromide.
SecobarbitalPerampanel may increase the central nervous system depressant (CNS depressant) activities of Secobarbital.
SevofluranePerampanel may increase the central nervous system depressant (CNS depressant) activities of Sevoflurane.
SiltuximabThe serum concentration of Perampanel can be decreased when it is combined with Siltuximab.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Perampanel.
St. John's WortThe serum concentration of Perampanel can be decreased when it is combined with St. John's Wort.
StiripentolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Stiripentol.
SufentanilPerampanel may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
SuvorexantPerampanel may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Tapentadol.
TasimelteonPerampanel may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
TemazepamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Temazepam.
TetrabenazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
ThalidomidePerampanel may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Thioridazine.
ThiothixenePerampanel may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
TiagabinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Tiagabine.
TizanidinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
TocilizumabThe serum concentration of Perampanel can be decreased when it is combined with Tocilizumab.
TolcaponePerampanel may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
TopiramatePerampanel may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
TramadolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Tramadol.
TriazolamPerampanel may increase the central nervous system depressant (CNS depressant) activities of Triazolam.
TrifluoperazinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
TrimipraminePerampanel may increase the central nervous system depressant (CNS depressant) activities of Trimipramine.
TriprolidinePerampanel may increase the central nervous system depressant (CNS depressant) activities of Triprolidine.
VigabatrinPerampanel may increase the central nervous system depressant (CNS depressant) activities of Vigabatrin.
ZaleplonPerampanel may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
ZiconotidePerampanel may increase the central nervous system depressant (CNS depressant) activities of Ziconotide.
ZiprasidonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Ziprasidone.
ZolpidemPerampanel may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZonisamidePerampanel may increase the central nervous system depressant (CNS depressant) activities of Zonisamide.
ZopiclonePerampanel may increase the central nervous system depressant (CNS depressant) activities of Zopiclone.
ZuclopenthixolPerampanel may increase the central nervous system depressant (CNS depressant) activities of Zuclopenthixol.
Food Interactions
  • Food slows perampanel's absorption rate but not extent.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Pdz domain binding
Specific Function:
Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inacti...
Gene Name:
GRIA1
Uniprot ID:
P42261
Molecular Weight:
101505.245 Da
References
  1. Hanada T, Hashizume Y, Tokuhara N, Takenaka O, Kohmura N, Ogasawara A, Hatakeyama S, Ohgoh M, Ueno M, Nishizawa Y: Perampanel: a novel, orally active, noncompetitive AMPA-receptor antagonist that reduces seizure activity in rodent models of epilepsy. Epilepsia. 2011 Jul;52(7):1331-40. doi: 10.1111/j.1528-1167.2011.03109.x. Epub 2011 Jun 2. [PubMed:21635236 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrateinducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
Comments
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Drug created on May 21, 2013 19:44 / Updated on June 25, 2016 01:51