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Identification
NameRufinamide
Accession NumberDB06201
TypeSmall Molecule
GroupsApproved
DescriptionRufinamide is a triazole derivative and an anticonvulsant medication to treat seizure disorders like Lennox-Gastuat syndrome, a form of childhood epilepsy. Clinical trials suggest its efficacy in the treatment of partial seizures.
Structure
Thumb
Synonyms
Banzel
RUF 331
Xilep
External Identifiers
  • CGP 33101
  • E 2080
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BanzelTablet, film coated200 mg/1OralEisai Inc.2008-11-14Not applicableUs
BanzelTablet200 mgOralEisai Limited2011-08-29Not applicableCanada
BanzelTablet, film coated400 mg/1OralEisai Inc.2008-11-14Not applicableUs
BanzelTablet400 mgOralEisai Limited2011-09-01Not applicableCanada
BanzelSuspension40 mg/mLOralEisai Inc.2011-03-03Not applicableUs
BanzelSuspension40 mgOralEisai LimitedNot applicableNot applicableCanada
BanzelTablet100 mgOralEisai Limited2011-10-20Not applicableCanada
InovelonTablet, film coated100 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated400 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated200 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated100 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated400 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated100 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonSuspension40 mg/mlOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated200 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated200 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated400 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated100 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated400 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated200 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated400 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated100 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated400 mgOralEisai Ltd2007-01-16Not applicableEu
InovelonTablet, film coated200 mgOralEisai Ltd2007-01-16Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
InovelonEisai Inc.
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIWFW942PR79
CAS number106308-44-5
WeightAverage: 238.1935
Monoisotopic: 238.066617308
Chemical FormulaC10H8F2N4O
InChI KeyPOGQSBRIGCQNEG-UHFFFAOYSA-N
InChI
InChI=1S/C10H8F2N4O/c11-7-2-1-3-8(12)6(7)4-16-5-9(10(13)17)14-15-16/h1-3,5H,4H2,(H2,13,17)
IUPAC Name
1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4-carboxamide
SMILES
NC(=O)C1=CN(CC2=C(F)C=CC=C2F)N=N1
Pharmacology
IndicationAdjunct therapy for treatment of seizures associated with Lennox-Gastaut syndrome.
Structured Indications
PharmacodynamicsAt high concentrations will inhibit action of mGluR5 subtype receptors thus preventing the production of glutamate.
Mechanism of actionRufinamide is a triazole derivative antiepileptic that prolongs the inactive state of voltage gated sodium channels thus stabilizing membranes, ultimately blocking the spread of partial seizure activity.
TargetKindPharmacological actionActionsOrganismUniProt ID
Metabotropic glutamate receptor 5Proteinunknown
inhibitor
HumanP41594 details
Sodium channel protein type 9 subunit alphaProteinunknown
modulator
HumanQ15858 details
Related Articles
AbsorptionThe oral suspension and tablet are bioequivalent on a mg per mg basis. Rufinamide is well absorbed but the rate is slow and the extent of absorption decreases as dose is increases. Based on urinary excretion, the extent of absorption was at least 85% following oral administration of a single dose of 600 mg rufinamide tablet under fed conditions. Bioavailability= 70%-85% (decreases with increasing doses); Tmax, fed and fasted states= 4-6 hours; Cmax, 10 mg/kg/day= 4.01 µL/mL; Cmax, 30mg/kg/day= 8.68 µL/mL; AUC (0h-12h), 10mg/kg/day= 37.8±47 µg·h/mL; AUC (0h-12h), 30mg/kg/day= 89.3±59 µg·h/mL.
Volume of distribution

Rufinamide was evenly distributed between erythrocytes and plasma. The apparent volume of distribution is dependent upon dose and varies with body surface area. The apparent volume of distribution was about 50 L at 3200 mg/day.
Volume of distribution is similar between adults and children and is non-linear.

Protein binding26.3% - 34.8% with 90% binding to albumin (27%).
Metabolism

Rufinamide is extensively metabolized but has no active metabolites. Metabolism by carboxyesterases into inactive metabolite CGP 47292, a carboxylic acid derivative, via hydrolysis is the primary biotransformation pathway. A few minor additional metabolites were detected in urine, which appeared to be acyl-glucuronides of CGP 47292. The cytochrome P450 enzyme system or glutathiones are not involved with the metabolism of rufinamide. Rufinamide is a weak inhibitor of CYP 2E1. Rufinamide is a weak inducer of CYP 3A4 enzymes.

SubstrateEnzymesProduct
Rufinamide
Not Available
CGP 47292Details
Route of eliminationRenally (91%; 66% as CGP 47292, 2% as unchanged drug) and fecally (9%) eliminated.
Half lifeElimination half-life, healthy subjects and patients with epilepsy = 6-10 hours.
ClearanceNot Available
ToxicityThe most commonly observed adverse reactions (≥10% and greater than placebo) were headache, dizziness, fatigue, somnolence, and nausea.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,1,1,2 TetrafluoroethaneThe risk or severity of adverse effects can be increased when Rufinamide is combined with 1,1,1,2 Tetrafluoroethane.Investigational
7-NitroindazoleThe risk or severity of adverse effects can be increased when Rufinamide is combined with 7-Nitroindazole.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Aceprometazine.Approved
adipiplonThe risk or severity of adverse effects can be increased when Rufinamide is combined with adipiplon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Agomelatine.Approved, Investigational
AlfaxaloneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Rufinamide is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Alphacetylmethadol.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Alprazolam.Approved, Illicit, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Amitriptyline.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Amobarbital.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Amperozide.Experimental
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Rufinamide.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Asenapine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Azaperone.Vet Approved
AzelastineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Azelastine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Rufinamide is combined with Baclofen.Approved
BarbitalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Barbital.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Benzocaine.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Rufinamide is combined with Benzyl alcohol.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Rufinamide is combined with Brexpiprazole.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Brimonidine.Approved
BromazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Bromazepam.Approved, Illicit
BrompheniramineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Brotizolam.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Bupivacaine.Approved, Investigational
BuprenorphineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Rufinamide is combined with Buspirone.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Butabarbital.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Butalbital.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Rufinamide is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Butethal.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Butorphanol.Approved, Illicit, Vet Approved
CarbamazepineThe serum concentration of Carbamazepine can be decreased when it is combined with Rufinamide.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Rufinamide is combined with Carfentanil.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Carisoprodol.Approved
CetirizineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Chloral hydrate.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Chlordiazepoxide.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Chlormezanone.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Chloroprocaine.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Chlorphenamine.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Chlorpromazine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Chlorprothixene.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Chlorzoxazone.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Cinchocaine.Approved, Vet Approved
ClemastineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clemastine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clobazam.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Rufinamide is combined with clomethiazole.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clomipramine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clonidine.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clorazepate.Approved, Illicit
ClozapineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clozapine.Approved
CocaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Cocaine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Codeine.Approved, Illicit
CyclizineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Cyclobenzaprine.Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Cyproheptadine.Approved
DantroleneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dapiprazole.Approved
deramciclaneThe risk or severity of adverse effects can be increased when Rufinamide is combined with deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Desflurane.Approved
DesipramineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Desipramine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Desloratadine.Approved, Investigational
DetomidineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Detomidine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dexbrompheniramine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dexmedetomidine.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dezocine.Approved
DiazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Diazepam.Approved, Illicit, Vet Approved
DifenoxinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dihydromorphine.Experimental, Illicit
DimenhydrinateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dimenhydrinate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Diphenhydramine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Diphenoxylate.Approved, Illicit
DoramectinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Doramectin.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Doxepin.Approved
DoxylamineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Doxylamine.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Rufinamide is combined with DPDPE.Investigational
DroperidolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Droperidol.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Drotebanol.Experimental, Illicit
DyclonineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Dyclonine.Approved
EcgonineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ecgonine.Experimental, Illicit
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when Rufinamide is combined with ECGONINE METHYL ESTER.Experimental
EcopipamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Rufinamide is combined with Efavirenz.Approved, Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Enflurane.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Rufinamide is combined with Entacapone.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Estazolam.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Eszopiclone.Approved
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Rufinamide.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ethchlorvynol.Approved, Illicit, Withdrawn
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Rufinamide.Approved
EthosuximideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ethyl carbamate.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ethylmorphine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Etifoxine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Etomidate.Approved
EtorphineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Etorphine.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Felbamate.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fexofenadine.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Flibanserin.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fludiazepam.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Flunitrazepam.Approved, Illicit
FlupentixolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fluphenazine.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Flurazepam.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fluspirilene.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fluticasone Propionate.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fluvoxamine.Approved, Investigational
FosphenytoinThe serum concentration of Rufinamide can be decreased when it is combined with Fosphenytoin.Approved
FospropofolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fospropofol.Approved, Illicit
GabapentinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Gabapentin.Approved, Investigational
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Rufinamide is combined with gabapentin enacarbil.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Rufinamide is combined with Gamma Hydroxybutyric Acid.Approved, Illicit
GepironeThe risk or severity of adverse effects can be increased when Rufinamide is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Glutethimide.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Halazepam.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Haloperidol.Approved
HalothaneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Halothane.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Heroin.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Hexobarbital.Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Hydromorphone.Approved, Illicit
HydroxyzineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Hydroxyzine.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Iloperidone.Approved
ImipramineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Imipramine.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Isoflurane.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ketamine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ketobemidone.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Lamotrigine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Levobupivacaine.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Rufinamide is combined with Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Levomethadyl Acetate.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Levorphanol.Approved
LidocaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Lidocaine.Approved, Vet Approved
LithiumThe risk or severity of adverse effects can be increased when Rufinamide is combined with Lithium.Approved
LofentanilThe risk or severity of adverse effects can be increased when Rufinamide is combined with Lofentanil.Illicit
LoratadineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Lorazepam.Approved
LoxapineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Loxapine.Approved
Lu AA21004The risk or severity of adverse effects can be increased when Rufinamide is combined with Lu AA21004.Investigational
LurasidoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Lurasidone.Approved
Magnesium SulfateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Magnesium Sulfate.Approved, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Maprotiline.Approved
MeclizineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Meclizine.Approved
MedetomidineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Medetomidine.Vet Approved
MefloquineThe therapeutic efficacy of Rufinamide can be decreased when used in combination with Mefloquine.Approved
MelatoninThe risk or severity of adverse effects can be increased when Rufinamide is combined with Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Melperone.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Meprobamate.Approved, Illicit
MesoridazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Mesoridazine.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Metaxalone.Approved
MethadoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methadyl Acetate.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methaqualone.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methohexital.Approved
MethotrimeprazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methoxyflurane.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methsuximide.Approved
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methylphenobarbital.Approved
MianserinThe therapeutic efficacy of Rufinamide can be decreased when used in combination with Mianserin.Approved
MidazolamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Midazolam.Approved, Illicit
MirtazapineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Mirtazapine.Approved
MolindoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Molindone.Approved
MorphineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Morphine.Approved, Investigational
NabiloneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Nabilone.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Nalbuphine.Approved
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Rufinamide.Approved
NitrazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Nitrazepam.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Nitrous oxide.Approved, Vet Approved
NorethisteroneThe serum concentration of Norethisterone can be decreased when it is combined with Rufinamide.Approved
NormethadoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Nortriptyline.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Olanzapine.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Olopatadine.Approved
OndansetronThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Rufinamide is combined with Opium.Approved, Illicit
OrlistatThe serum concentration of Rufinamide can be decreased when it is combined with Orlistat.Approved, Investigational
OrphenadrineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Rufinamide is combined with Osanetant.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Oxazepam.Approved
OxetacaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Oxetacaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Rufinamide is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Oxybuprocaine.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Oxymorphone.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Paliperidone.Approved
ParaldehydeThe risk or severity of adverse effects can be increased when Rufinamide is combined with Paraldehyde.Approved
PentazocineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pentazocine.Approved, Vet Approved
PentobarbitalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pentobarbital.Approved, Vet Approved
PerampanelThe risk or severity of adverse effects can be increased when Rufinamide is combined with Perampanel.Approved
PerazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Rufinamide is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pethidine.Approved
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Rufinamide.Approved
PhenoxyethanolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Phenoxyethanol.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Rufinamide.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pimozide.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pipamperone.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pipotiazine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pomalidomide.Approved
PramocaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Prazepam.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pregabalin.Approved, Illicit, Investigational
PregnanoloneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pregnanolone.Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Prilocaine.Approved
PrimidoneThe serum concentration of Rufinamide can be decreased when it is combined with Primidone.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Procaine.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Prochlorperazine.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Promazine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Promethazine.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Proparacaine.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Propofol.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Propoxycaine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Protriptyline.Approved
PSD502The risk or severity of adverse effects can be increased when Rufinamide is combined with PSD502.Investigational
QuazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Quazepam.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Quetiapine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ramelteon.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Rufinamide is combined with Remifentanil.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Remoxipride.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Reserpine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Risperidone.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ritanserin.Investigational
RomifidineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Romifidine.Vet Approved
RopivacaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ropivacaine.Approved
S-EthylisothioureaThe risk or severity of adverse effects can be increased when Rufinamide is combined with S-Ethylisothiourea.Experimental
Sage 547The risk or severity of adverse effects can be increased when Rufinamide is combined with Sage 547.Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Rufinamide.Approved
ScopolamineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Scopolamine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Secobarbital.Approved, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Rufinamide is combined with Sertindole.Approved, Withdrawn
SevofluraneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Sevoflurane.Approved, Vet Approved
Sodium oxybateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Sodium oxybate.Approved
StiripentolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Rufinamide is combined with Sufentanil.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Sulpiride.Approved
SuvorexantThe risk or severity of adverse effects can be increased when Rufinamide is combined with Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tandospirone.Investigational
TapentadolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tapentadol.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tasimelteon.Approved
TemazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Temazepam.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tetrabenazine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tetracaine.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tetrodotoxin.Investigational
ThalidomideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Rufinamide is combined with Thiopental.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Thioridazine.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Thiothixene.Approved
TiagabineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tiapride.Investigational
TiletamineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tiletamine.Vet Approved
TizanidineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tizanidine.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tolcapone.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Rufinamide is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tramadol.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tranylcypromine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Trazodone.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Triazolam.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Trifluoperazine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Triflupromazine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Triprolidine.Approved
Uc1010The risk or severity of adverse effects can be increased when Rufinamide is combined with Uc1010.Investigational
Valproic AcidThe serum concentration of Rufinamide can be increased when it is combined with Valproic Acid.Approved, Investigational
VigabatrinThe risk or severity of adverse effects can be increased when Rufinamide is combined with Vigabatrin.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Vortioxetine.Approved
XylazineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Xylazine.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Rufinamide is combined with Zaleplon.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ziconotide.Approved
ZiprasidoneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Ziprasidone.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Rufinamide is combined with Zolazepam.Vet Approved
ZolpidemThe risk or severity of adverse effects can be increased when Rufinamide is combined with Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Rufinamide is combined with Zopiclone.Approved
ZotepineThe risk or severity of adverse effects can be increased when Rufinamide is combined with Zotepine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Rufinamide is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
  • Food increases plasma concentrations of rufinamide and slightly decreases half-life (by 3%)
References
Synthesis Reference

Emanuele ATTOLINO, Lino COLOMBO, Ilaria MORMINO, Pietro ALLEGRINI, “METHOD FOR THE PREPARATION OF RUFINAMIDE.” U.S. Patent US20100234616, issued September 16, 2010.

US20100234616
General References
  1. Arroyo S: Rufinamide. Neurotherapeutics. 2007 Jan;4(1):155-62. [PubMed:17199032 ]
  2. Hakimian S, Cheng-Hakimian A, Anderson GD, Miller JW: Rufinamide: a new anti-epileptic medication. Expert Opin Pharmacother. 2007 Aug;8(12):1931-40. [PubMed:17696794 ]
  3. Authors unspecified: Rufinamide: CGP 33101, E 2080, RUF 331, Xilep. Drugs R D. 2005;6(4):249-52. [PubMed:15991887 ]
  4. Wier HA, Cerna A, So TY: Rufinamide for pediatric patients with Lennox-Gastaut syndrome: a comprehensive overview. Paediatr Drugs. 2011 Apr 1;13(2):97-106. doi: 10.2165/11586920-000000000-00000. [PubMed:21351809 ]
External Links
ATC CodesN03AF03
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (562 KB)
MSDSDownload (76.7 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9777
Caco-2 permeable-0.5301
P-glycoprotein substrateNon-substrate0.7407
P-glycoprotein inhibitor INon-inhibitor0.9422
P-glycoprotein inhibitor IINon-inhibitor0.9633
Renal organic cation transporterNon-inhibitor0.6685
CYP450 2C9 substrateNon-substrate0.8452
CYP450 2D6 substrateNon-substrate0.8723
CYP450 3A4 substrateNon-substrate0.5567
CYP450 1A2 substrateNon-inhibitor0.5
CYP450 2C9 inhibitorNon-inhibitor0.8201
CYP450 2D6 inhibitorNon-inhibitor0.8454
CYP450 2C19 inhibitorNon-inhibitor0.5561
CYP450 3A4 inhibitorNon-inhibitor0.7995
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5438
Ames testAMES toxic0.6126
CarcinogenicityNon-carcinogens0.8415
BiodegradationNot ready biodegradable0.9945
Rat acute toxicity2.5067 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9484
hERG inhibition (predictor II)Non-inhibitor0.7869
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
SuspensionOral40 mg
SuspensionOral40 mg/mL
TabletOral100 mg
TabletOral200 mg
TabletOral400 mg
Tablet, film coatedOral200 mg/1
Tablet, film coatedOral400 mg/1
Tablet, film coatedOral100 mg
Tablet, film coatedOral200 mg
Tablet, film coatedOral400 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6740669 Yes2003-05-142023-05-14Us
US7750028 Yes1999-04-192019-04-19Us
US8076362 Yes1998-12-082018-12-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityInsoluble FDA label
logP0.835MSDS
Predicted Properties
PropertyValueSource
Water Solubility0.642 mg/mLALOGPS
logP0.95ALOGPS
logP1.27ChemAxon
logS-2.6ALOGPS
pKa (Strongest Acidic)12.69ChemAxon
pKa (Strongest Basic)-1.1ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area73.8 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity67.07 m3·mol-1ChemAxon
Polarizability20.42 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as triazole carboxylic acids and derivatives. These are heterocyclic compounds containing a triazole ring substituted by at least one carboxylic acid group (or a derivative thereof).
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzoles
Sub ClassTriazoles
Direct ParentTriazole carboxylic acids and derivatives
Alternative Parents
Substituents
  • 1,2,3-triazole carboxylic acid or derivatives
  • Phenylmethylamine
  • Halobenzene
  • Fluorobenzene
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Vinylogous amide
  • Primary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Glutamate receptor activity
Specific Function:
G-protein coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling activates a phosphatidylinositol-calcium second messenger system and generates a calcium-activated chloride current. Plays an important role in the regulation of synaptic ...
Gene Name:
GRM5
Uniprot ID:
P41594
Molecular Weight:
132467.635 Da
References
  1. Wier HA, Cerna A, So TY: Rufinamide for pediatric patients with Lennox-Gastaut syndrome: a comprehensive overview. Paediatr Drugs. 2011 Apr 1;13(2):97-106. doi: 10.2165/11586920-000000000-00000. [PubMed:21351809 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
modulator
General Function:
Voltage-gated sodium channel activity
Specific Function:
Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-sensitive Na(+) channel isoform. Plays a role in pain mechanisms, es...
Gene Name:
SCN9A
Uniprot ID:
Q15858
Molecular Weight:
226370.175 Da
References
  1. Suter MR, Kirschmann G, Laedermann CJ, Abriel H, Decosterd I: Rufinamide attenuates mechanical allodynia in a model of neuropathic pain in the mouse and stabilizes voltage-gated sodium channel inactivated state. Anesthesiology. 2013 Jan;118(1):160-72. doi: 10.1097/ALN.0b013e318278cade. [PubMed:23221868 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Triglyceride lipase activity
Specific Function:
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl-CoA ester. Hydrolyzes the methyl ester group of cocaine to form benzoylecgonine. Catalyzes the transesterification of cocaine to form cocaethylene. Displays fatty acid ethyl ester synthase activity,...
Gene Name:
CES1
Uniprot ID:
P23141
Molecular Weight:
62520.62 Da
References
  1. Williams ET, Carlson JE, Lai WG, Wong YN, Yoshimura T, Critchley DJ, Narurkar M: Investigation of the metabolism of rufinamide and its interaction with valproate. Drug Metab Lett. 2011 Dec;5(4):280-9. [PubMed:22022867 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
Comments
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Drug created on March 19, 2008 10:17 / Updated on December 06, 2016 03:56