Identification

Name
Mexiletine
Accession Number
DB00379  (APRD00242)
Type
Small Molecule
Groups
Approved
Description

Antiarrhythmic agent pharmacologically similar to lidocaine. It may have some anticonvulsant properties. [PubChem]

Structure
Thumb
Synonyms
  • (+-)-1-(2,6-Dimethylphenoxy)propan-2-amine
  • (2RS)-1-(2,6-dimethylphenoxy)-2-aminopropane
  • 1-(2,6-Dimethylphenoxy)-2-propanamine
  • 1-(2',6'-Dimethylphenoxy)-2-aminopropane
  • 1-Methyl-2-(2,6-xylyloxy)ethanamine
  • Mexiletina
  • Mexilétine
  • Mexiletinum
External IDs
Kö 1173
Product Ingredients
IngredientUNIICASInChI Key
Mexiletine Hydrochloride606D60IS385370-01-4NFEIBWMZVIVJLQ-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alti-mexiletineCapsule100 mgOralAltimed Pharma Inc.1997-11-072001-09-05Canada
Alti-mexiletineCapsule200 mgOralAltimed Pharma Inc.1997-11-072001-09-05Canada
Mexitil Cap 100mgCapsule100 mgOralBoehringer Ingelheim (Canada) Ltd Ltee1985-12-312002-07-25Canada
Mexitil Cap 200mgCapsule200 mgOralBoehringer Ingelheim (Canada) Ltd Ltee1985-12-312002-07-25Canada
Teva-mexiletineCapsule100 mgOralTeva1997-03-17Not applicableCanada
Teva-mexiletineCapsule200 mgOralTeva1997-02-17Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mexiletine HydrochlorideCapsule150 mg/1OralAv Kare, Inc.2013-07-09Not applicableUs
Mexiletine HydrochlorideCapsule150 mg/1OralTeva1995-06-05Not applicableUs00093 8739 01 nlmimage10 9f364fb2
Mexiletine HydrochlorideCapsule150 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-03-16Not applicableUs
Mexiletine HydrochlorideCapsule250 mg/1OralCarilion Materials Management1995-06-05Not applicableUs00093 8741 01 nlmimage10 9a364d42
Mexiletine HydrochlorideCapsule200 mg/1OralAv Kare, Inc.2013-07-09Not applicableUs
Mexiletine HydrochlorideCapsule200 mg/1OralTeva1995-06-05Not applicableUs
Mexiletine HydrochlorideCapsule200 mg/1OralCarilion Materials Management1995-06-05Not applicableUs00093 8740 01 nlmimage10 a33651c2
Mexiletine HydrochlorideCapsule200 mg/1OralAvera Mc Kennan Hospital2015-10-26Not applicableUs
Mexiletine HydrochlorideCapsule250 mg/1OralTeva1995-06-05Not applicableUs
Mexiletine HydrochlorideCapsule250 mg/1OralAv Kare, Inc.2013-07-09Not applicableUs
International/Other Brands
Cirumimeru (Tsuruhara Seiyaku) / Mekiratin (Ohara Yakuhin) / Melate (Medisa Shinyaku) / Meldest (Taiyo Pharmaceutical) / Meletin (Taiwan Biotech) / Mequitolide (Towa Yakuhin) / Metorekicin (Choseido Pharmaceutical) / Mexicord (Polfa Grodzisk) / Mexitil (Boehringer Ingelheim) / Mexitilen (Boehringer Ingelheim) / Minsetil (Zdravlje) / Mobalen (Tatsumi Kagaku) / Mugadine (Yung Shin) / Olzoron (Kobayashi Kako) / Poeruten (Yoshindo) / Ritalmex (Valeant) / Teva-Mexiletine (Teva Neuroscience) / Toi (Kyorin Rimedio) / Tumetil (Boehringer Ingelheim)
Categories
UNII
1U511HHV4Z
CAS number
31828-71-4
Weight
Average: 179.2588
Monoisotopic: 179.131014171
Chemical Formula
C11H17NO
InChI Key
VLPIATFUUWWMKC-UHFFFAOYSA-N
InChI
InChI=1S/C11H17NO/c1-8-5-4-6-9(2)11(8)13-7-10(3)12/h4-6,10H,7,12H2,1-3H3
IUPAC Name
1-(2,6-dimethylphenoxy)propan-2-amine
SMILES
CC(N)COC1=C(C)C=CC=C1C

Pharmacology

Indication

For the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation.

Structured Indications
Pharmacodynamics

Mexiletine is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine has fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. It shortens the action potential duration, reduces refractoriness, and decreases Vmax in partially depolarized cells with fast response action potentials. Mexiletine either does not change the action potential duration, or decreases the action potential duration.

Mechanism of action

Mexiletine, like lidocaine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential, Phase 0. It achieves this reduced sodium current by inhibiting sodium channels. Mexiletine decreases the effective refractory period (ERP) in Purkinje fibers in the heart. The decrease in ERP is of lesser magnitude than the decrease in action potential duration (APD), which results in an increase in the ERP/APD ratio. It does not significantly affect resting membrane potential or sinus node automaticity, left ventricular function, systolic arterial blood pressure, atrioventricular (AV) conduction velocity, or QRS or QT intervals

TargetActionsOrganism
ASodium channel protein type 5 subunit alpha
inhibitor
Human
UAryl hydrocarbon receptor
agonist
Human
Absorption

Well absorbed (bioavailability 90%) from the gastrointenstinal tract.

Volume of distribution
  • 5 to 7 L/lg
Protein binding

50-60%

Metabolism

Primarily hepatic (85%) via CYP2D6 and CYP1A2 (primarily CYP2D6).

Route of elimination

Approximately 10% is excreted unchanged by the kidney. The urinary excretion of N-methylmexiletine in man is less than 0.5%.

Half life

10-12 hours

Clearance
Not Available
Toxicity

Symptoms of overdose include nausea, hypotension, sinus bradycardia, paresthesia, seizures, bundle branch block, AV heart block, asystole, ventricular tachyarrythmia, including ventricular fibrillation, cardiovascular collapse, and coma.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Mexiletine Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Mexiletine can be increased when it is combined with Abiraterone.Approved
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Mexiletine.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Mexiletine.Approved
AgomelatineThe serum concentration of Agomelatine can be increased when it is combined with Mexiletine.Approved, Investigational
AlaproclateThe metabolism of Mexiletine can be decreased when combined with Alaproclate.Experimental
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Mexiletine.Approved, Vet Approved
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Mexiletine.Approved, Investigational
AlosetronThe metabolism of Alosetron can be decreased when combined with Mexiletine.Approved, Withdrawn
Ambroxol acefyllinateThe metabolism of Ambroxol acefyllinate can be decreased when combined with Mexiletine.Experimental, Investigational
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Mexiletine.Approved, Withdrawn
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Mexiletine.Approved
AmiodaroneThe metabolism of Mexiletine can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Mexiletine.Approved
AnagrelideThe metabolism of Anagrelide can be decreased when combined with Mexiletine.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Mexiletine.Approved
ApixabanThe metabolism of Apixaban can be decreased when combined with Mexiletine.Approved
AprepitantThe serum concentration of Mexiletine can be increased when it is combined with Aprepitant.Approved, Investigational
ArtemetherThe metabolism of Mexiletine can be decreased when combined with Artemether.Approved
AsenapineThe metabolism of Asenapine can be decreased when combined with Mexiletine.Approved
AtazanavirThe metabolism of Mexiletine can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Mexiletine can be decreased when combined with Atomoxetine.Approved
AV650The metabolism of AV650 can be decreased when combined with Mexiletine.Approved, Investigational
AxitinibThe metabolism of Axitinib can be decreased when combined with Mexiletine.Approved, Investigational
AzelastineThe metabolism of Azelastine can be decreased when combined with Mexiletine.Approved
AzithromycinThe metabolism of Mexiletine can be decreased when combined with Azithromycin.Approved
BendamustineThe serum concentration of Bendamustine can be increased when it is combined with Mexiletine.Approved, Investigational
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Mexiletine.Approved
BetaxololThe metabolism of Betaxolol can be decreased when combined with Mexiletine.Approved
BoceprevirThe metabolism of Mexiletine can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Bortezomib can be decreased when combined with Mexiletine.Approved, Investigational
BosentanThe serum concentration of Mexiletine can be decreased when it is combined with Bosentan.Approved, Investigational
BromazepamThe metabolism of Bromazepam can be decreased when combined with Mexiletine.Approved, Illicit
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Mexiletine.Approved, Investigational
BupropionThe metabolism of Bupropion can be decreased when combined with Mexiletine.Approved
CaffeineThe metabolism of Caffeine can be decreased when combined with Mexiletine.Approved
CarbamazepineThe metabolism of Mexiletine can be increased when combined with Carbamazepine.Approved, Investigational
CarmustineThe metabolism of Carmustine can be decreased when combined with Mexiletine.Approved
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Mexiletine.Approved, Investigational
CelecoxibThe metabolism of Mexiletine can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Mexiletine can be increased when it is combined with Ceritinib.Approved
ChloroquineThe metabolism of Mexiletine can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Mexiletine.Approved, Vet Approved
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Mexiletine.Approved
CholecalciferolThe metabolism of Mexiletine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CilostazolThe metabolism of Cilostazol can be decreased when combined with Mexiletine.Approved
CimetidineThe metabolism of Mexiletine can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Cinacalcet can be decreased when combined with Mexiletine.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Mexiletine.Approved, Investigational
CisaprideThe metabolism of Cisapride can be decreased when combined with Mexiletine.Approved, Investigational, Withdrawn
CitalopramThe metabolism of Mexiletine can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Mexiletine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Mexiletine can be decreased when combined with Clemastine.Approved
ClenbuterolThe metabolism of Clenbuterol can be decreased when combined with Mexiletine.Approved, Investigational, Vet Approved
ClevidipineThe metabolism of Clevidipine can be decreased when combined with Mexiletine.Approved
ClobazamThe metabolism of Mexiletine can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Mexiletine.Approved, Vet Approved
ClonidineThe metabolism of Clonidine can be decreased when combined with Mexiletine.Approved
ClopidogrelThe metabolism of Clopidogrel can be decreased when combined with Mexiletine.Approved, Nutraceutical
ClotrimazoleThe metabolism of Mexiletine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Mexiletine.Approved
CobicistatThe serum concentration of Mexiletine can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Mexiletine can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Mexiletine can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated estrogensThe metabolism of Conjugated estrogens can be decreased when combined with Mexiletine.Approved
CrizotinibThe metabolism of Mexiletine can be decreased when combined with Crizotinib.Approved
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Mexiletine.Approved
CyclosporineThe metabolism of Mexiletine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Mexiletine can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Mexiletine can be decreased when it is combined with Dabrafenib.Approved
DacarbazineThe metabolism of Dacarbazine can be decreased when combined with Mexiletine.Approved, Investigational
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Mexiletine.Approved
DapoxetineThe metabolism of Mexiletine can be decreased when combined with Dapoxetine.Investigational
DarifenacinThe metabolism of Mexiletine can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Mexiletine can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Mexiletine can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe metabolism of Daunorubicin can be decreased when combined with Mexiletine.Approved
DeferasiroxThe serum concentration of Mexiletine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Mexiletine can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Desipramine can be decreased when combined with Mexiletine.Approved
DesvenlafaxineThe metabolism of Mexiletine can be decreased when combined with Desvenlafaxine.Approved
DeutetrabenazineThe metabolism of Deutetrabenazine can be decreased when combined with Mexiletine.Approved, Investigational
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Mexiletine.Approved, Illicit, Investigational, Withdrawn
DiazepamThe metabolism of Diazepam can be decreased when combined with Mexiletine.Approved, Illicit, Vet Approved
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Mexiletine.Approved, Vet Approved
DihydroergotamineThe metabolism of Mexiletine can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Mexiletine can be decreased when combined with Diltiazem.Approved
DinoprostoneThe metabolism of Dinoprostone can be decreased when combined with Mexiletine.Approved
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Mexiletine.Approved
DomperidoneThe metabolism of Domperidone can be decreased when combined with Mexiletine.Approved, Investigational, Vet Approved
DosulepinThe metabolism of Mexiletine can be decreased when combined with Dosulepin.Approved
DoxepinThe metabolism of Doxepin can be decreased when combined with Mexiletine.Approved
DoxorubicinThe metabolism of Mexiletine can be decreased when combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Mexiletine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Mexiletine can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Mexiletine can be decreased when combined with Duloxetine.Approved
DyphyllineThe metabolism of Dyphylline can be decreased when combined with Mexiletine.Approved
EliglustatThe metabolism of Mexiletine can be decreased when combined with Eliglustat.Approved
EltrombopagThe metabolism of Eltrombopag can be decreased when combined with Mexiletine.Approved
EnasidenibThe metabolism of Enasidenib can be decreased when combined with Mexiletine.Approved
EnzalutamideThe serum concentration of Mexiletine can be decreased when it is combined with Enzalutamide.Approved
ErgotamineThe metabolism of Ergotamine can be decreased when combined with Mexiletine.Approved
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Mexiletine.Approved, Investigational
ErythromycinThe metabolism of Mexiletine can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe metabolism of Mexiletine can be decreased when combined with Escitalopram.Approved, Investigational
EstradiolThe metabolism of Estradiol can be decreased when combined with Mexiletine.Approved, Investigational, Vet Approved
EstroneThe metabolism of Estrone can be decreased when combined with Mexiletine.Approved
Estrone sulfateThe metabolism of Estrone sulfate can be decreased when combined with Mexiletine.Approved
EthanolThe metabolism of Ethanol can be decreased when combined with Mexiletine.Approved
EtoperidoneThe metabolism of Mexiletine can be decreased when combined with Etoperidone.Withdrawn
EtoposideThe metabolism of Etoposide can be decreased when combined with Mexiletine.Approved
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Mexiletine.Approved, Investigational
EtravirineThe serum concentration of Mexiletine can be decreased when it is combined with Etravirine.Approved
FluconazoleThe metabolism of Mexiletine can be decreased when combined with Fluconazole.Approved
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Mexiletine.Approved
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Mexiletine.Approved, Illicit
FluorouracilThe metabolism of Fluorouracil can be decreased when combined with Mexiletine.Approved
FluoxetineThe metabolism of Mexiletine can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlutamideThe metabolism of Flutamide can be decreased when combined with Mexiletine.Approved
FluvoxamineThe metabolism of Mexiletine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Mexiletine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Mexiletine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Mexiletine can be decreased when it is combined with Fosphenytoin.Approved
FrovatriptanThe metabolism of Frovatriptan can be decreased when combined with Mexiletine.Approved, Investigational
Fusidic AcidThe serum concentration of Mexiletine can be increased when it is combined with Fusidic Acid.Approved
GenisteinThe metabolism of Genistein can be decreased when combined with Mexiletine.Investigational
GrepafloxacinThe metabolism of Grepafloxacin can be decreased when combined with Mexiletine.Investigational, Withdrawn
GuanabenzThe metabolism of Guanabenz can be decreased when combined with Mexiletine.Approved, Investigational
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Mexiletine.Approved
HesperetinThe metabolism of Hesperetin can be decreased when combined with Mexiletine.Approved
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Mexiletine.Approved
IcotinibThe metabolism of Icotinib can be decreased when combined with Mexiletine.Approved, Investigational
IdelalisibThe serum concentration of Mexiletine can be increased when it is combined with Idelalisib.Approved
IloperidoneThe metabolism of Iloperidone can be decreased when combined with Mexiletine.Approved
ImatinibThe metabolism of Imatinib can be decreased when combined with Mexiletine.Approved
ImipramineThe metabolism of Imipramine can be decreased when combined with Mexiletine.Approved
ImiquimodThe metabolism of Imiquimod can be decreased when combined with Mexiletine.Approved, Investigational
IndalpineThe metabolism of Mexiletine can be decreased when combined with Indalpine.Investigational, Withdrawn
IndinavirThe metabolism of Mexiletine can be decreased when combined with Indinavir.Approved
IsavuconazoniumThe metabolism of Mexiletine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Mexiletine can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Mexiletine can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Mexiletine can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Mexiletine can be increased when it is combined with Ivacaftor.Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Mexiletine.Approved
KetoconazoleThe metabolism of Mexiletine can be decreased when combined with Ketoconazole.Approved, Investigational
LeflunomideThe metabolism of Leflunomide can be decreased when combined with Mexiletine.Approved, Investigational
LevobupivacaineThe metabolism of Levobupivacaine can be decreased when combined with Mexiletine.Approved, Investigational
LevomilnacipranThe metabolism of Mexiletine can be decreased when combined with Levomilnacipran.Approved
LidocaineThe metabolism of Lidocaine can be decreased when combined with Mexiletine.Approved, Vet Approved
LobeglitazoneThe metabolism of Mexiletine can be decreased when combined with Lobeglitazone.Approved, Investigational
LomefloxacinThe metabolism of Lomefloxacin can be decreased when combined with Mexiletine.Approved, Investigational
LopinavirThe metabolism of Mexiletine can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Mexiletine.Approved
LovastatinThe metabolism of Mexiletine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Mexiletine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Mexiletine can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Mexiletine can be decreased when combined with Lumefantrine.Approved
LumiracoxibThe metabolism of Lumiracoxib can be decreased when combined with Mexiletine.Approved, Investigational
MalathionThe metabolism of Malathion can be decreased when combined with Mexiletine.Approved, Investigational
ManidipineThe metabolism of Mexiletine can be decreased when combined with Manidipine.Approved, Investigational
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Mexiletine.Approved
MelatoninThe metabolism of Melatonin can be decreased when combined with Mexiletine.Approved, Nutraceutical, Vet Approved
MenadioneThe metabolism of Menadione can be decreased when combined with Mexiletine.Approved, Nutraceutical
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Mexiletine.Investigational, Withdrawn
MethadoneThe metabolism of Methadone can be decreased when combined with Mexiletine.Approved
MethotrimeprazineThe metabolism of Mexiletine can be decreased when combined with Methotrimeprazine.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Mexiletine.Approved, Investigational, Vet Approved
MetoprololThe metabolism of Mexiletine can be decreased when combined with Metoprolol.Approved, Investigational
MianserinThe metabolism of Mianserin can be decreased when combined with Mexiletine.Approved, Investigational
MidostaurinThe metabolism of Mexiletine can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Mexiletine can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe metabolism of Mexiletine can be decreased when combined with Milnacipran.Approved
MirabegronThe metabolism of Mexiletine can be decreased when combined with Mirabegron.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Mexiletine.Approved
MitotaneThe serum concentration of Mexiletine can be decreased when it is combined with Mitotane.Approved
muraglitazarThe metabolism of muraglitazar can be decreased when combined with Mexiletine.Investigational
NabumetoneThe metabolism of Nabumetone can be decreased when combined with Mexiletine.Approved
NaproxenThe metabolism of Naproxen can be decreased when combined with Mexiletine.Approved, Vet Approved
NefazodoneThe metabolism of Mexiletine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Mexiletine can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Mexiletine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Mexiletine can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Mexiletine can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Mexiletine.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Mexiletine.Approved
NilotinibThe metabolism of Mexiletine can be decreased when combined with Nilotinib.Approved, Investigational
Nitric OxideThe metabolism of Nitric Oxide can be decreased when combined with Mexiletine.Approved
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Mexiletine.Approved
OlanzapineThe metabolism of Olanzapine can be decreased when combined with Mexiletine.Approved, Investigational
OlaparibThe metabolism of Mexiletine can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Omeprazole can be decreased when combined with Mexiletine.Approved, Investigational, Vet Approved
OndansetronThe metabolism of Ondansetron can be decreased when combined with Mexiletine.Approved
OsimertinibThe serum concentration of Mexiletine can be increased when it is combined with Osimertinib.Approved
OxaliplatinThe metabolism of Oxaliplatin can be decreased when combined with Mexiletine.Approved, Investigational
OxtriphyllineThe metabolism of Oxtriphylline can be decreased when combined with Mexiletine.Approved
PalbociclibThe serum concentration of Mexiletine can be increased when it is combined with Palbociclib.Approved
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Mexiletine.Approved, Investigational
PanobinostatThe serum concentration of Mexiletine can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Mexiletine.Approved
ParoxetineThe metabolism of Mexiletine can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe metabolism of Pazopanib can be decreased when combined with Mexiletine.Approved
Peginterferon alfa-2bThe serum concentration of Mexiletine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Mexiletine.Approved
PentobarbitalThe metabolism of Mexiletine can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoxifyllineThe serum concentration of Pentoxifylline can be increased when it is combined with Mexiletine.Approved, Investigational
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Mexiletine.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Mexiletine.Withdrawn
PhenobarbitalThe metabolism of Mexiletine can be increased when combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Mexiletine can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideThe metabolism of Pimozide can be decreased when combined with Mexiletine.Approved
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Mexiletine.Approved, Investigational
PirfenidoneThe serum concentration of Pirfenidone can be increased when it is combined with Mexiletine.Approved, Investigational
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Mexiletine.Approved
PosaconazoleThe metabolism of Mexiletine can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PraziquantelThe metabolism of Praziquantel can be decreased when combined with Mexiletine.Approved, Vet Approved
PrimaquineThe metabolism of Primaquine can be decreased when combined with Mexiletine.Approved
PrimidoneThe metabolism of Mexiletine can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Mexiletine.Approved, Vet Approved
ProguanilThe metabolism of Proguanil can be decreased when combined with Mexiletine.Approved
PromazineThe metabolism of Promazine can be decreased when combined with Mexiletine.Approved, Vet Approved
PropafenoneThe metabolism of Propafenone can be decreased when combined with Mexiletine.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Mexiletine.Approved, Investigational, Vet Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Mexiletine.Approved, Investigational
PyrazinamideThe metabolism of Pyrazinamide can be decreased when combined with Mexiletine.Approved
QuazepamThe serum concentration of Mexiletine can be increased when it is combined with Quazepam.Approved, Illicit
QuinidineThe metabolism of Mexiletine can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Quinine can be decreased when combined with Mexiletine.Approved
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Mexiletine.Approved, Investigational
RanitidineThe metabolism of Ranitidine can be decreased when combined with Mexiletine.Approved
RanolazineThe metabolism of Mexiletine can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineThe serum concentration of Rasagiline can be increased when it is combined with Mexiletine.Approved
ResveratrolThe metabolism of Resveratrol can be decreased when combined with Mexiletine.Approved, Experimental, Investigational
RifabutinThe metabolism of Mexiletine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Mexiletine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Mexiletine can be increased when combined with Rifapentine.Approved
RiluzoleThe metabolism of Riluzole can be decreased when combined with Mexiletine.Approved, Investigational
RitonavirThe metabolism of Ritonavir can be decreased when combined with Mexiletine.Approved, Investigational
RizatriptanThe metabolism of Rizatriptan can be decreased when combined with Mexiletine.Approved
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Mexiletine.Investigational, Withdrawn
RolapitantThe metabolism of Mexiletine can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Ropinirole can be decreased when combined with Mexiletine.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Mexiletine.Approved
RotigotineThe metabolism of Rotigotine can be decreased when combined with Mexiletine.Approved
RucaparibThe metabolism of Rucaparib can be decreased when combined with Mexiletine.Approved, Investigational
SaquinavirThe metabolism of Mexiletine can be decreased when combined with Saquinavir.Approved, Investigational
SelegilineThe metabolism of Selegiline can be decreased when combined with Mexiletine.Approved, Investigational, Vet Approved
SertralineThe metabolism of Mexiletine can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Mexiletine can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Mexiletine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Mexiletine can be increased when it is combined with Simeprevir.Approved
SorafenibThe metabolism of Mexiletine can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Mexiletine can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Mexiletine can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Mexiletine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrineThe metabolism of Tacrine can be decreased when combined with Mexiletine.Investigational, Withdrawn
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Mexiletine.Approved
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Mexiletine.Approved
TelaprevirThe metabolism of Mexiletine can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Mexiletine can be decreased when combined with Telithromycin.Approved
TemafloxacinThe metabolism of Temafloxacin can be decreased when combined with Mexiletine.Withdrawn
Tenofovir disoproxilThe metabolism of Mexiletine can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Mexiletine.Approved, Investigational, Vet Approved
TeriflunomideThe serum concentration of Mexiletine can be decreased when it is combined with Teriflunomide.Approved
ThalidomideThe metabolism of Thalidomide can be decreased when combined with Mexiletine.Approved, Investigational, Withdrawn
TheobromineThe metabolism of Theobromine can be decreased when combined with Mexiletine.Approved, Investigational
TheophyllineThe metabolism of Theophylline can be decreased when combined with Mexiletine.Approved
ThiabendazoleThe metabolism of Thiabendazole can be decreased when combined with Mexiletine.Approved, Vet Approved
ThioridazineThe metabolism of Thioridazine can be decreased when combined with Mexiletine.Approved, Withdrawn
ThiotepaThe metabolism of Mexiletine can be decreased when combined with Thiotepa.Approved
ThiothixeneThe metabolism of Thiothixene can be decreased when combined with Mexiletine.Approved
TiclopidineThe metabolism of Mexiletine can be decreased when combined with Ticlopidine.Approved
TipranavirThe metabolism of Mexiletine can be decreased when combined with Tipranavir.Approved, Investigational
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Mexiletine.Approved
TocilizumabThe serum concentration of Mexiletine can be decreased when it is combined with Tocilizumab.Approved
ToremifeneThe metabolism of Toremifene can be decreased when combined with Mexiletine.Approved, Investigational
TranylcypromineThe metabolism of Mexiletine can be decreased when combined with Tranylcypromine.Approved
TriamtereneThe metabolism of Triamterene can be decreased when combined with Mexiletine.Approved
TrifluoperazineThe metabolism of Trifluoperazine can be decreased when combined with Mexiletine.Approved
UlipristalThe metabolism of Ulipristal can be decreased when combined with Mexiletine.Approved
VadimezanThe metabolism of Vadimezan can be decreased when combined with Mexiletine.Investigational
VemurafenibThe serum concentration of Mexiletine can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Mexiletine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Verapamil can be decreased when combined with Mexiletine.Approved
VoriconazoleThe metabolism of Mexiletine can be decreased when combined with Voriconazole.Approved, Investigational
VoxilaprevirThe metabolism of Voxilaprevir can be decreased when combined with Mexiletine.Approved
WarfarinThe metabolism of Warfarin can be decreased when combined with Mexiletine.Approved
ZileutonThe metabolism of Zileuton can be decreased when combined with Mexiletine.Approved, Investigational, Withdrawn
ZimelidineThe metabolism of Mexiletine can be decreased when combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Ziprasidone can be decreased when combined with Mexiletine.Approved
ZolmitriptanThe metabolism of Zolmitriptan can be decreased when combined with Mexiletine.Approved, Investigational
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Mexiletine.Approved
ZucapsaicinThe metabolism of Mexiletine can be decreased when combined with Zucapsaicin.Approved
Food Interactions
  • Take with food to reduce irritation.

References

Synthesis Reference

Margarita Ortiz-Marciales, Kun Huang, Viatcheslav Stepanenko, Melvin De Jesus, Wildeliz Correa, "Method of synthesizing enantiopure mexiletine analogues and novel b-thiophenoxy and pyridyl ethers." U.S. Patent US08012901, issued September 06, 2011.

US08012901
General References
Not Available
External Links
Human Metabolome Database
HMDB14523
KEGG Compound
C07220
PubChem Compound
4178
PubChem Substance
46505491
ChemSpider
4034
BindingDB
50117271
ChEBI
6916
ChEMBL
CHEMBL558
Therapeutic Targets Database
DAP000505
PharmGKB
PA450488
IUPHAR
2629
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Mexiletine
ATC Codes
C01BB02 — Mexiletine
AHFS Codes
  • 24:04.04.08 — Class Ib Antiarrythmics
FDA label
Download (1.21 MB)
MSDS
Download (47.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceDrug-induced QT Interval Prolongation / Pharmacodynamics / Pharmacokinetics1
1CompletedTreatmentIBS1
2CompletedTreatmentAmputations / Pain, Chronic1
2CompletedTreatmentBlepharospasm / Dystonias / Spasms1
2CompletedTreatmentCharcot Marie Tooth Disease1
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Peripheral Nervous System Diseases1
2CompletedTreatmentMyotonia / Non-dystrophic Myotonias1
2CompletedTreatmentNon Dystrophic Myotonia1
2CompletedTreatmentSporadic Amyotrophic Lateral Sclerosis1
2CompletedTreatmentSteinert's Disease1
2RecruitingTreatmentSporadic Amyotrophic Lateral Sclerosis1
3CompletedPreventionArrythmias / Cardiovascular Disease (CVD) / Heart Arrest / Heart Diseases / Myocardial Infarction (MI) / Severe ventricular arrhythmias1
3CompletedTreatmentArrythmias / Cardiovascular Disease (CVD) / Death, Sudden,Cardiac / Heart Diseases / Severe ventricular arrhythmias / Ventricular Arrythmias / Ventricular Tachycardia (VT)1
3CompletedTreatmentDiabetic Neuropathies / Pain / Paresthesia1
3CompletedTreatmentMyotonia Congenita / Non-dystrophic Myotonias / Paramyotonia Congenita1
4Active Not RecruitingTreatmentCryptogenic Sensory Polyneuropathy1
4CompletedTreatmentMuscle Cramps in Amyotrophic Lateral Sclerosis1

Pharmacoeconomics

Manufacturers
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Boehringer ingelheim
Packagers
Dosage forms
FormRouteStrength
CapsuleOral100 mg
CapsuleOral200 mg
CapsuleOral150 mg/1
CapsuleOral200 mg/1
CapsuleOral250 mg/1
Prices
Unit descriptionCostUnit
Mexitil 250 mg capsule1.85USD capsule
Mexiletine HCl 250 mg capsule1.6USD capsule
Mexiletine 250 mg capsule1.54USD capsule
Mexiletine HCl 200 mg capsule1.38USD capsule
Mexiletine 200 mg capsule1.33USD capsule
Mexitil 200 mg capsule1.23USD capsule
Novo-Mexiletine 200 mg Capsule1.19USD capsule
Mexiletine HCl 150 mg capsule1.16USD capsule
Mexiletine 150 mg capsule1.11USD capsule
Novo-Mexiletine 100 mg Capsule0.89USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)203-205 °CPhysProp
water solubility8.25 mg/mLNot Available
logP2.15MANNHOLD,R ET AL. (1990)
pKa9.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.538 mg/mLALOGPS
logP2.17ALOGPS
logP2.46ChemAxon
logS-2.5ALOGPS
pKa (Strongest Basic)9.52ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area35.25 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity54.97 m3·mol-1ChemAxon
Polarizability21.17 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9382
Caco-2 permeable+0.7357
P-glycoprotein substrateNon-substrate0.6711
P-glycoprotein inhibitor INon-inhibitor0.8781
P-glycoprotein inhibitor IINon-inhibitor0.9484
Renal organic cation transporterNon-inhibitor0.7849
CYP450 2C9 substrateNon-substrate0.8191
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateNon-substrate0.5463
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.941
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.9132
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6004
Ames testNon AMES toxic0.6357
CarcinogenicityNon-carcinogens0.7796
BiodegradationNot ready biodegradable0.9261
Rat acute toxicity2.6338 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8982
hERG inhibition (predictor II)Non-inhibitor0.6563
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-0a4i-9100000000-6d40293ed4e486f9cf9e
GC-MS Spectrum - CI-BGC-MSsplash10-0a4i-9300000000-147905f020f0139cfe20
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9400000000-d9f9d0eeea2a47e42771
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9300000000-76838bfcf2fd2b0e2b17
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9400000000-c5920fd67439f418b86f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9500000000-b5f13a7a078d1c192691
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9500000000-24a61cef86793ffcf760
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9400000000-d740cc5fc7a9b2b380a6
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01q9-0900000000-083bab651324c62f4cd5
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01q9-0900000000-feace6e16ed93a4bd13e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9400000000-94985b5db6692d615971
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9300000000-c1e103780c7df279dc6c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9400000000-d077857c1d4a1d567c03
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9500000000-9ef54de393ed768d242f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9500000000-9a364fda721f96e6e368

Taxonomy

Description
This compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenol ethers
Sub Class
Not Available
Direct Parent
Phenol ethers
Alternative Parents
m-Xylenes / Phenoxy compounds / Alkyl aryl ethers / Organopnictogen compounds / Monoalkylamines / Hydrocarbon derivatives
Substituents
Phenol ether / Xylene / M-xylene / Phenoxy compound / Alkyl aryl ether / Monocyclic benzene moiety / Ether / Amine / Hydrocarbon derivative / Primary amine
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
aromatic ether, primary amino compound (CHEBI:6916)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated sodium channel activity involved in sa node cell action potential
Specific Function
This protein 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 pr...
Gene Name
SCN5A
Uniprot ID
Q14524
Uniprot Name
Sodium channel protein type 5 subunit alpha
Molecular Weight
226937.475 Da
References
  1. Valdivia CR, Ackerman MJ, Tester DJ, Wada T, McCormack J, Ye B, Makielski JC: A novel SCN5A arrhythmia mutation, M1766L, with expression defect rescued by mexiletine. Cardiovasc Res. 2002 Aug 1;55(2):279-89. [PubMed:12123767]
  2. Chinushi M, Tagawa M, Sugiura H, Komura S, Hosaka Y, Washizuka T, Aizawa Y: Ventricular tachyarrhythmias in a canine model of LQT3: arrhythmogenic effects of sympathetic activity and therapeutic effects of mexiletine. Circ J. 2003 Mar;67(3):263-8. [PubMed:12604879]
  3. Fabritz L, Kirchhof P, Franz MR, Nuyens D, Rossenbacker T, Ottenhof A, Haverkamp W, Breithardt G, Carmeliet E, Carmeliet P: Effect of pacing and mexiletine on dispersion of repolarisation and arrhythmias in DeltaKPQ SCN5A (long QT3) mice. Cardiovasc Res. 2003 Mar 15;57(4):1085-93. [PubMed:12650887]
  4. Wang HW, Zheng YQ, Yang ZF, Li CZ, Liu YM: Effect of mexiletine on long QT syndrome model. Acta Pharmacol Sin. 2003 Apr;24(4):316-20. [PubMed:12676070]
  5. Napolitano C, Bloise R, Priori SG: Gene-specific therapy for inherited arrhythmogenic diseases. Pharmacol Ther. 2006 Apr;110(1):1-13. Epub 2005 Sep 15. [PubMed:16168489]
  6. Shimizu W, Antzelevitch C, Suyama K, Kurita T, Taguchi A, Aihara N, Takaki H, Sunagawa K, Kamakura S: Effect of sodium channel blockers on ST segment, QRS duration, and corrected QT interval in patients with Brugada syndrome. J Cardiovasc Electrophysiol. 2000 Dec;11(12):1320-9. [PubMed:11196553]
  7. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Transcription regulatory region dna binding
Specific Function
Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phase I and II xenobiotic chemical metabolizing enzyme genes...
Gene Name
AHR
Uniprot ID
P35869
Uniprot Name
Aryl hydrocarbon receptor
Molecular Weight
96146.705 Da
References
  1. Hu W, Sorrentino C, Denison MS, Kolaja K, Fielden MR: Induction of cyp1a1 is a nonspecific biomarker of aryl hydrocarbon receptor activation: results of large scale screening of pharmaceuticals and toxicants in vivo and in vitro. Mol Pharmacol. 2007 Jun;71(6):1475-86. Epub 2007 Feb 27. [PubMed:17327465]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Nakajima M, Kobayashi K, Shimada N, Tokudome S, Yamamoto T, Kuroiwa Y: Involvement of CYP1A2 in mexiletine metabolism. Br J Clin Pharmacol. 1998 Jul;46(1):55-62. [PubMed:9690950]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Nakajima M, Kobayashi K, Shimada N, Tokudome S, Yamamoto T, Kuroiwa Y: Involvement of CYP1A2 in mexiletine metabolism. Br J Clin Pharmacol. 1998 Jul;46(1):55-62. [PubMed:9690950]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid 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 oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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 ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:34