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Identification
NameMexiletine
Accession NumberDB00379  (APRD00242)
TypeSmall Molecule
GroupsApproved
DescriptionAntiarrhythmic 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 Identifiers
  • Kö 1173
Approved 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 mgoralTeva Canada Limited1997-03-17Not applicableCanada
Teva-mexiletinecapsule200 mgoralTeva Canada Limited1997-02-17Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mexiletine Hydrochloridecapsule200 mg/1oralCarilion Materials Management1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule150 mg/1oralTeva Pharmaceuticals USA Inc1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule200 mg/1oralAv Kare, Inc.2013-07-09Not applicableUs
Mexiletine Hydrochloridecapsule150 mg/1oralCarilion Materials Management1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule200 mg/1oralTeva Pharmaceuticals USA Inc1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule250 mg/1oralAv Kare, Inc.2013-07-09Not applicableUs
Mexiletine Hydrochloridecapsule250 mg/1oralCarilion Materials Management1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule250 mg/1oralTeva Pharmaceuticals USA Inc1995-06-05Not applicableUs
Mexiletine Hydrochloridecapsule150 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-16Not applicableUs
Mexiletine Hydrochloridecapsule150 mg/1oralAv Kare, Inc.2013-07-09Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CirumimeruTsuruhara Seiyaku
MekiratinOhara Yakuhin
MelateMedisa Shinyaku
MeldestTaiyo Pharmaceutical
MeletinTaiwan Biotech
MequitolideTowa Yakuhin
MetorekicinChoseido Pharmaceutical
MexicordPolfa Grodzisk
MexitilBoehringer Ingelheim
MexitilenBoehringer Ingelheim
MinsetilZdravlje
MobalenTatsumi Kagaku
MugadineYung Shin
OlzoronKobayashi Kako
PoerutenYoshindo
RitalmexValeant
Teva-MexiletineTeva Neuroscience
ToiKyorin Rimedio
TumetilBoehringer Ingelheim
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Mexiletine Hydrochloride
5370-01-4
Thumb
  • InChI Key: NFEIBWMZVIVJLQ-UHFFFAOYNA-N
  • Monoisotopic Mass: 215.10769191
  • Average Mass: 215.72
DBSALT000449
Categories
UNII1U511HHV4Z
CAS number31828-71-4
WeightAverage: 179.2588
Monoisotopic: 179.131014171
Chemical FormulaC11H17NO
InChI KeyInChIKey=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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenol ethers
Direct ParentPhenol ethers
Alternative Parents
Substituents
  • Phenol ether
  • Alkyl aryl ether
  • Ether
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation.
PharmacodynamicsMexiletine 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 actionMexiletine, 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
Related Articles
AbsorptionWell absorbed (bioavailability 90%) from the gastrointenstinal tract.
Volume of distribution
  • 5 to 7 L/lg
Protein binding50-60%
Metabolism

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

SubstrateEnzymesProduct
Mexiletine
2-hydroxymexiletineDetails
Mexiletine
p-hydroxymexiletineDetails
Route of eliminationApproximately 10% is excreted unchanged by the kidney. The urinary excretion of N-methylmexiletine in man is less than 0.5%.
Half life10-12 hours
ClearanceNot Available
ToxicitySymptoms 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
PathwayCategorySMPDB ID
Mexiletine Action PathwayDrug actionSMP00329
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
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.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point203-205 °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 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
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 ReferencesNot Available
External Links
ATC CodesC01BB02
AHFS Codes
  • 24:04.04.08
PDB EntriesNot Available
FDA labelDownload (1.21 MB)
MSDSDownload (47.1 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Mexiletine can be increased when it is combined with Abiraterone.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Mexiletine.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Mexiletine.
AgomelatineThe serum concentration of Agomelatine can be increased when it is combined with Mexiletine.
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Mexiletine.
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Mexiletine.
AlosetronThe metabolism of Alosetron can be decreased when combined with Mexiletine.
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Mexiletine.
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Mexiletine.
AmiodaroneThe metabolism of Amiodarone can be decreased when combined with Mexiletine.
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Mexiletine.
AmoxapineThe metabolism of Mexiletine can be decreased when combined with Amoxapine.
AnagrelideThe metabolism of Anagrelide can be decreased when combined with Mexiletine.
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Mexiletine.
ApixabanThe metabolism of Apixaban can be decreased when combined with Mexiletine.
AprepitantThe serum concentration of Mexiletine can be increased when it is combined with Aprepitant.
AprepitantThe metabolism of Aprepitant can be decreased when combined with Mexiletine.
ArtemetherThe metabolism of Mexiletine can be decreased when combined with Artemether.
ASA404The metabolism of ASA404 can be decreased when combined with Mexiletine.
AsenapineThe metabolism of Asenapine can be decreased when combined with Mexiletine.
AtazanavirThe metabolism of Mexiletine can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Mexiletine can be decreased when combined with Atomoxetine.
AV650The metabolism of AV650 can be decreased when combined with Mexiletine.
AxitinibThe metabolism of Axitinib can be decreased when combined with Mexiletine.
AzelastineThe metabolism of Azelastine can be decreased when combined with Mexiletine.
AzithromycinThe metabolism of Mexiletine can be decreased when combined with Azithromycin.
BendamustineThe serum concentration of Bendamustine can be increased when it is combined with Mexiletine.
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Mexiletine.
BetaxololThe metabolism of Betaxolol can be decreased when combined with Mexiletine.
BexaroteneThe serum concentration of Mexiletine can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Mexiletine can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Mexiletine can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Mexiletine can be decreased when it is combined with Bosentan.
BromazepamThe metabolism of Bromazepam can be decreased when combined with Mexiletine.
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Mexiletine.
BupropionThe metabolism of Bupropion can be decreased when combined with Mexiletine.
CaffeineThe metabolism of Mexiletine can be decreased when combined with Caffeine.
CarbamazepineThe metabolism of Mexiletine can be increased when combined with Carbamazepine.
CarmustineThe metabolism of Carmustine can be decreased when combined with Mexiletine.
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Mexiletine.
CelecoxibThe metabolism of Mexiletine can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Mexiletine can be increased when it is combined with Ceritinib.
ChloroquineThe metabolism of Mexiletine can be decreased when combined with Chloroquine.
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Mexiletine.
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Mexiletine.
CholecalciferolThe metabolism of Mexiletine can be decreased when combined with Cholecalciferol.
CilostazolThe metabolism of Cilostazol can be decreased when combined with Mexiletine.
CimetidineThe metabolism of Mexiletine can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Cinacalcet can be decreased when combined with Mexiletine.
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Mexiletine.
CisaprideThe metabolism of Cisapride can be decreased when combined with Mexiletine.
CitalopramThe metabolism of Mexiletine can be decreased when combined with Citalopram.
ClarithromycinThe metabolism of Mexiletine can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Mexiletine can be decreased when combined with Clemastine.
ClenbuterolThe metabolism of Clenbuterol can be decreased when combined with Mexiletine.
ClevidipineThe metabolism of Clevidipine can be decreased when combined with Mexiletine.
ClobazamThe metabolism of Mexiletine can be decreased when combined with Clobazam.
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Mexiletine.
ClonidineThe metabolism of Clonidine can be decreased when combined with Mexiletine.
ClopidogrelThe metabolism of Clopidogrel can be decreased when combined with Mexiletine.
ClotrimazoleThe metabolism of Mexiletine can be decreased when combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Mexiletine.
ClozapineThe metabolism of Mexiletine can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Mexiletine can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Mexiletine can be decreased when combined with Cocaine.
ConivaptanThe serum concentration of Mexiletine can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe metabolism of Conjugated Equine Estrogens can be decreased when combined with Mexiletine.
CrizotinibThe metabolism of Mexiletine can be decreased when combined with Crizotinib.
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Mexiletine.
CyclosporineThe metabolism of Mexiletine can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Mexiletine can be decreased when it is combined with Cyproterone acetate.
DabrafenibThe serum concentration of Mexiletine can be decreased when it is combined with Dabrafenib.
DacarbazineThe metabolism of Dacarbazine can be decreased when combined with Mexiletine.
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Mexiletine.
DapoxetineThe metabolism of Mexiletine can be decreased when combined with Dapoxetine.
DarifenacinThe metabolism of Mexiletine can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Mexiletine can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Mexiletine can be increased when it is combined with Dasatinib.
DasatinibThe metabolism of Dasatinib can be decreased when combined with Mexiletine.
DaunorubicinThe metabolism of Daunorubicin can be decreased when combined with Mexiletine.
DeferasiroxThe serum concentration of Mexiletine can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Mexiletine can be decreased when combined with Delavirdine.
DesipramineThe metabolism of Desipramine can be decreased when combined with Mexiletine.
DexamethasoneThe serum concentration of Mexiletine can be decreased when it is combined with Dexamethasone.
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Mexiletine.
DiazepamThe metabolism of Diazepam can be decreased when combined with Mexiletine.
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Mexiletine.
DihydroergotamineThe metabolism of Mexiletine can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Mexiletine can be decreased when combined with Diltiazem.
DinoprostoneThe metabolism of Dinoprostone can be decreased when combined with Mexiletine.
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Mexiletine.
DisulfiramThe metabolism of Mexiletine can be decreased when combined with Disulfiram.
DomperidoneThe metabolism of Domperidone can be decreased when combined with Mexiletine.
DoxepinThe metabolism of Doxepin can be decreased when combined with Mexiletine.
DoxorubicinThe metabolism of Mexiletine can be decreased when combined with Doxorubicin.
DoxycyclineThe metabolism of Mexiletine can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Mexiletine can be decreased when combined with Dronedarone.
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Mexiletine.
DuloxetineThe metabolism of Mexiletine can be decreased when combined with Duloxetine.
DyphyllineThe metabolism of Dyphylline can be decreased when combined with Mexiletine.
EfavirenzThe serum concentration of Mexiletine can be decreased when it is combined with Efavirenz.
EliglustatThe metabolism of Mexiletine can be decreased when combined with Eliglustat.
EltrombopagThe metabolism of Eltrombopag can be decreased when combined with Mexiletine.
EnzalutamideThe serum concentration of Mexiletine can be decreased when it is combined with Enzalutamide.
ErgotamineThe metabolism of Ergotamine can be decreased when combined with Mexiletine.
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Mexiletine.
ErythromycinThe metabolism of Mexiletine can be decreased when combined with Erythromycin.
EscitalopramThe metabolism of Mexiletine can be decreased when combined with Escitalopram.
Eslicarbazepine acetateThe serum concentration of Mexiletine can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe metabolism of Estradiol can be decreased when combined with Mexiletine.
EstroneThe metabolism of Estrone can be decreased when combined with Mexiletine.
Estrone sulfateThe metabolism of Estrone sulfate can be decreased when combined with Mexiletine.
EthanolThe metabolism of Ethanol can be decreased when combined with Mexiletine.
EtoperidoneThe metabolism of Mexiletine can be decreased when combined with Etoperidone.
EtoposideThe metabolism of Etoposide can be decreased when combined with Mexiletine.
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Mexiletine.
EtravirineThe serum concentration of Mexiletine can be decreased when it is combined with Etravirine.
FenfluramineThe metabolism of Mexiletine can be decreased when combined with Fenfluramine.
FluconazoleThe metabolism of Mexiletine can be decreased when combined with Fluconazole.
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Mexiletine.
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Mexiletine.
FluorouracilThe metabolism of Fluorouracil can be decreased when combined with Mexiletine.
FluoxetineThe metabolism of Mexiletine can be decreased when combined with Fluoxetine.
FlutamideThe metabolism of Flutamide can be decreased when combined with Mexiletine.
FluvoxamineThe metabolism of Mexiletine can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Mexiletine can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Mexiletine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Mexiletine can be decreased when it is combined with Fosphenytoin.
FrovatriptanThe metabolism of Frovatriptan can be decreased when combined with Mexiletine.
Fusidic AcidThe serum concentration of Mexiletine can be increased when it is combined with Fusidic Acid.
GenisteinThe metabolism of Genistein can be decreased when combined with Mexiletine.
GrepafloxacinThe metabolism of Grepafloxacin can be decreased when combined with Mexiletine.
GuanabenzThe metabolism of Guanabenz can be decreased when combined with Mexiletine.
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Mexiletine.
HesperetinThe metabolism of Hesperetin can be decreased when combined with Mexiletine.
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Mexiletine.
IdelalisibThe serum concentration of Mexiletine can be increased when it is combined with Idelalisib.
IloperidoneThe metabolism of Iloperidone can be decreased when combined with Mexiletine.
ImatinibThe metabolism of Mexiletine can be decreased when combined with Imatinib.
ImipramineThe metabolism of Imipramine can be decreased when combined with Mexiletine.
ImiquimodThe metabolism of Imiquimod can be decreased when combined with Mexiletine.
IndalpineThe metabolism of Mexiletine can be decreased when combined with Indalpine.
IndinavirThe metabolism of Mexiletine can be decreased when combined with Indinavir.
IsavuconazoniumThe metabolism of Mexiletine can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Mexiletine can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Mexiletine can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Mexiletine can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Mexiletine can be increased when it is combined with Ivacaftor.
IxazomibThe metabolism of Ixazomib can be decreased when combined with Mexiletine.
KetoconazoleThe metabolism of Mexiletine can be decreased when combined with Ketoconazole.
LeflunomideThe metabolism of Leflunomide can be decreased when combined with Mexiletine.
LevobupivacaineThe metabolism of Levobupivacaine can be decreased when combined with Mexiletine.
LevomilnacipranThe metabolism of Mexiletine can be decreased when combined with Levomilnacipran.
LidocaineThe metabolism of Mexiletine can be decreased when combined with Lidocaine.
LomefloxacinThe metabolism of Lomefloxacin can be decreased when combined with Mexiletine.
LopinavirThe metabolism of Mexiletine can be decreased when combined with Lopinavir.
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Mexiletine.
LovastatinThe metabolism of Mexiletine can be decreased when combined with Lovastatin.
Lu AA21004The metabolism of Mexiletine can be decreased when combined with Lu AA21004.
LuliconazoleThe serum concentration of Mexiletine can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Mexiletine can be decreased when it is combined with Lumacaftor.
LumefantrineThe metabolism of Mexiletine can be decreased when combined with Lumefantrine.
LumiracoxibThe metabolism of Lumiracoxib can be decreased when combined with Mexiletine.
MalathionThe metabolism of Malathion can be decreased when combined with Mexiletine.
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Mexiletine.
MelatoninThe metabolism of Melatonin can be decreased when combined with Mexiletine.
MenadioneThe metabolism of Menadione can be decreased when combined with Mexiletine.
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Mexiletine.
MethadoneThe metabolism of Methadone can be decreased when combined with Mexiletine.
MethotrimeprazineThe metabolism of Mexiletine can be decreased when combined with Methotrimeprazine.
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Mexiletine.
MetoprololThe metabolism of Mexiletine can be decreased when combined with Metoprolol.
MianserinThe metabolism of Mianserin can be decreased when combined with Mexiletine.
MifepristoneThe metabolism of Mexiletine can be decreased when combined with Mifepristone.
MilnacipranThe metabolism of Mexiletine can be decreased when combined with Milnacipran.
MirabegronThe metabolism of Mexiletine can be decreased when combined with Mirabegron.
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Mexiletine.
MitotaneThe serum concentration of Mexiletine can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Mexiletine can be decreased when it is combined with Modafinil.
muraglitazarThe metabolism of muraglitazar can be decreased when combined with Mexiletine.
NabumetoneThe metabolism of Nabumetone can be decreased when combined with Mexiletine.
NafcillinThe serum concentration of Mexiletine can be decreased when it is combined with Nafcillin.
NaproxenThe metabolism of Naproxen can be decreased when combined with Mexiletine.
NefazodoneThe metabolism of Mexiletine can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Mexiletine can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Mexiletine can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Mexiletine can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Mexiletine can be decreased when combined with Nicardipine.
NicotineThe metabolism of Nicotine can be decreased when combined with Mexiletine.
NifedipineThe metabolism of Nifedipine can be decreased when combined with Mexiletine.
NilotinibThe metabolism of Mexiletine can be decreased when combined with Nilotinib.
Nitric OxideThe metabolism of Nitric Oxide can be decreased when combined with Mexiletine.
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Mexiletine.
OlanzapineThe metabolism of Mexiletine can be decreased when combined with Olanzapine.
OlaparibThe metabolism of Mexiletine can be decreased when combined with Olaparib.
OmeprazoleThe metabolism of Omeprazole can be decreased when combined with Mexiletine.
OndansetronThe metabolism of Ondansetron can be decreased when combined with Mexiletine.
OsimertinibThe serum concentration of Mexiletine can be increased when it is combined with Osimertinib.
OxaliplatinThe metabolism of Oxaliplatin can be decreased when combined with Mexiletine.
OxtriphyllineThe metabolism of Oxtriphylline can be decreased when combined with Mexiletine.
PalbociclibThe serum concentration of Mexiletine can be increased when it is combined with Palbociclib.
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Mexiletine.
PanobinostatThe metabolism of Mexiletine can be decreased when combined with Panobinostat.
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Mexiletine.
ParoxetineThe metabolism of Mexiletine can be decreased when combined with Paroxetine.
PazopanibThe metabolism of Pazopanib can be decreased when combined with Mexiletine.
Peginterferon alfa-2bThe serum concentration of Mexiletine can be decreased when it is combined with Peginterferon alfa-2b.
PentamidineThe metabolism of Pentamidine can be decreased when combined with Mexiletine.
PentobarbitalThe metabolism of Mexiletine can be increased when combined with Pentobarbital.
PentoxifyllineThe serum concentration of Pentoxifylline can be increased when it is combined with Mexiletine.
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Mexiletine.
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Mexiletine.
PhenobarbitalThe metabolism of Mexiletine can be increased when combined with Phenobarbital.
PhenytoinThe serum concentration of Mexiletine can be decreased when it is combined with Phenytoin.
PimozideThe metabolism of Pimozide can be decreased when combined with Mexiletine.
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Mexiletine.
PirfenidoneThe serum concentration of Pirfenidone can be increased when it is combined with Mexiletine.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Mexiletine.
PosaconazoleThe metabolism of Mexiletine can be decreased when combined with Posaconazole.
PraziquantelThe metabolism of Praziquantel can be decreased when combined with Mexiletine.
PrimaquineThe metabolism of Primaquine can be decreased when combined with Mexiletine.
PrimidoneThe metabolism of Mexiletine can be increased when combined with Primidone.
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Mexiletine.
ProguanilThe metabolism of Proguanil can be decreased when combined with Mexiletine.
PromazineThe metabolism of Promazine can be decreased when combined with Mexiletine.
PropafenoneThe metabolism of Propafenone can be decreased when combined with Mexiletine.
PropofolThe metabolism of Propofol can be decreased when combined with Mexiletine.
PropranololThe metabolism of Propranolol can be decreased when combined with Mexiletine.
PyrazinamideThe metabolism of Pyrazinamide can be decreased when combined with Mexiletine.
QuazepamThe serum concentration of Mexiletine can be increased when it is combined with Quazepam.
QuinidineThe metabolism of Mexiletine can be decreased when combined with Quinidine.
QuinineThe metabolism of Quinine can be decreased when combined with Mexiletine.
RamelteonThe metabolism of Ramelteon can be decreased when combined with Mexiletine.
RanitidineThe metabolism of Ranitidine can be decreased when combined with Mexiletine.
RanolazineThe metabolism of Mexiletine can be decreased when combined with Ranolazine.
RasagilineThe serum concentration of Rasagiline can be increased when it is combined with Mexiletine.
ResveratrolThe metabolism of Resveratrol can be decreased when combined with Mexiletine.
RifabutinThe metabolism of Mexiletine can be increased when combined with Rifabutin.
RifampicinThe metabolism of Mexiletine can be increased when combined with Rifampicin.
RifapentineThe metabolism of Mexiletine can be increased when combined with Rifapentine.
RiluzoleThe metabolism of Riluzole can be decreased when combined with Mexiletine.
RitonavirThe metabolism of Mexiletine can be decreased when combined with Ritonavir.
RizatriptanThe metabolism of Rizatriptan can be decreased when combined with Mexiletine.
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Mexiletine.
RolapitantThe metabolism of Mexiletine can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Mexiletine can be decreased when combined with Ropinirole.
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Mexiletine.
RotigotineThe metabolism of Rotigotine can be decreased when combined with Mexiletine.
SaquinavirThe metabolism of Mexiletine can be decreased when combined with Saquinavir.
SelegilineThe metabolism of Selegiline can be decreased when combined with Mexiletine.
SertralineThe metabolism of Sertraline can be decreased when combined with Mexiletine.
SildenafilThe metabolism of Mexiletine can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Mexiletine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Mexiletine can be increased when it is combined with Simeprevir.
SorafenibThe metabolism of Mexiletine can be decreased when combined with Sorafenib.
St. John's WortThe serum concentration of Mexiletine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Mexiletine can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Mexiletine can be decreased when combined with Sulfisoxazole.
TacrineThe metabolism of Tacrine can be decreased when combined with Mexiletine.
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Mexiletine.
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Mexiletine.
TelaprevirThe metabolism of Mexiletine can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Mexiletine can be decreased when combined with Telithromycin.
TemafloxacinThe metabolism of Temafloxacin can be decreased when combined with Mexiletine.
TenofovirThe metabolism of Mexiletine can be decreased when combined with Tenofovir.
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Mexiletine.
TeriflunomideThe serum concentration of Mexiletine can be decreased when it is combined with Teriflunomide.
ThalidomideThe metabolism of Thalidomide can be decreased when combined with Mexiletine.
TheobromineThe metabolism of Theobromine can be decreased when combined with Mexiletine.
TheophyllineThe metabolism of Theophylline can be decreased when combined with Mexiletine.
ThiabendazoleThe metabolism of Thiabendazole can be decreased when combined with Mexiletine.
ThioridazineThe metabolism of Thioridazine can be decreased when combined with Mexiletine.
ThiotepaThe metabolism of Mexiletine can be decreased when combined with Thiotepa.
ThiothixeneThe metabolism of Thiothixene can be decreased when combined with Mexiletine.
TiclopidineThe metabolism of Mexiletine can be decreased when combined with Ticlopidine.
TipranavirThe metabolism of Mexiletine can be decreased when combined with Tipranavir.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Mexiletine.
TocilizumabThe serum concentration of Mexiletine can be decreased when it is combined with Tocilizumab.
ToremifeneThe metabolism of Toremifene can be decreased when combined with Mexiletine.
TranylcypromineThe metabolism of Mexiletine can be decreased when combined with Tranylcypromine.
TrazodoneThe metabolism of Mexiletine can be decreased when combined with Trazodone.
TriamtereneThe metabolism of Triamterene can be decreased when combined with Mexiletine.
TrifluoperazineThe metabolism of Trifluoperazine can be decreased when combined with Mexiletine.
UlipristalThe metabolism of Ulipristal can be decreased when combined with Mexiletine.
VemurafenibThe serum concentration of Mexiletine can be increased when it is combined with Vemurafenib.
VenlafaxineThe metabolism of Mexiletine can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Mexiletine can be decreased when combined with Verapamil.
VilazodoneThe metabolism of Mexiletine can be decreased when combined with Vilazodone.
VoriconazoleThe metabolism of Mexiletine can be decreased when combined with Voriconazole.
VortioxetineThe metabolism of Mexiletine can be decreased when combined with Vortioxetine.
WarfarinThe metabolism of Warfarin can be decreased when combined with Mexiletine.
ZileutonThe metabolism of Zileuton can be decreased when combined with Mexiletine.
ZimelidineThe metabolism of Mexiletine can be decreased when combined with Zimelidine.
ZiprasidoneThe metabolism of Mexiletine can be decreased when combined with Ziprasidone.
ZolmitriptanThe metabolism of Zolmitriptan can be decreased when combined with Mexiletine.
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Mexiletine.
Food Interactions
  • Take with food to reduce irritation.

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 protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is respon...
Gene Name:
SCN5A
Uniprot ID:
Q14524
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 (such as the CYP1A1 gene). Mediates biochemical and toxic effects of halogenated aromatic hydrocarbons. Involved in cell-cycle regulation. Likely to play an important role in the development and matu...
Gene Name:
AHR
Uniprot ID:
P35869
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
substrateinhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
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 or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
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 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
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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23