Details of the Drug

General Information of Drug (ID: DMCTE9R)

Drug Name

Mexiletine

Synonyms

Mexiletene; Mexiletina; Mexiletinum; Mexilitine; Mexityl; Mexiletine HCL; KO1173; KO-1173; KOE-1173; Mexiletina [INN-Spanish]; Mexiletine (INN); Mexiletine [INN:BAN]; Mexiletinum [INN-Latin]; Mexitil (TN); (+-)-1-(2,6-dimethylphenoxy)propan-2-amine; (2RS)-1-(2,6-dimethylphenoxy)-2-aminopropane; 1-(2',6'-Dimethylphenoxy)-2-aminopropane; 1-(2,6-Dimethylphenoxy)-2-propanamine; 1-(2,6-dimethylphenoxy)propan-2-amine; 1-Methyl-2-(2,6-xylyloxy)ethylamine; 1-methyl-2-(2,6-xylyloxy)ethanamine; 2-(2-Aminopropoxy)-1,3-DiMethyl-Benzene Hydrochloride; 2-(2-aminopropoxy)-1,3-dimethylbenzene

Indication

Disease Entry	ICD 11	Status	REF
Ventricular tachycardia	BC71	Approved	[1]
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Therapeutic Class

Antiarrhythmic Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

179.26

Logarithm of the Partition Coefficient (xlogp)

2.1

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [2]
Bioavailability: 87% of drug becomes completely available to its intended biological destination(s) [3]
Clearance: The drug present in the plasma can be removed from the body at the rate of 8.3 mL/min/kg [4]
Elimination: 9.5% of drug is excreted from urine in the unchanged form [2]
Half-life: The concentration or amount of drug in body reduced by one-half in 10 - 12 hours [4]
Metabolism: The drug is metabolized via the hepatic []
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 95.6312 micromolar/kg/day [5]
Unbound Fraction: The unbound fraction of drug in plasma is 0.36% [4]
Vd: The volume of distribution (Vd) of drug is 5-7 L/kg []

Adverse Drug Reaction (ADR)

ADR Term	Variation	Related DOT	DOT ID	REF
Drug toxicity	Not Available	CYP2D6	OTZJC802	[6]
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Chemical Identifiers

Formula: C11H17NO
IUPAC Name: 1-(2,6-dimethylphenoxy)propan-2-amine
Canonical SMILES: CC1=C(C(=CC=C1)C)OCC(C)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
InChIKey: VLPIATFUUWWMKC-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 4178
ChEBI ID: CHEBI:6916
CAS Number: 31828-71-4
DrugBank ID: DB00379
TTD ID: D0X0RI
VARIDT ID: DR00695
INTEDE ID: DR1079
ACDINA ID: D00428

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated sodium channel alpha Nav1.5 (SCN5A)	TTZOVE0	SCN5A_HUMAN	Blocker	[7]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[8]
Cytochrome P450 2E1 (CYP2E1)	DEVDYN7	CP2E1_HUMAN	Substrate	[9]
Cytochrome P450 2D6 (CYP2D6)_{Main DME}	DECB0K3	CP2D6_HUMAN	Substrate	[10]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Substrate	[11]
Cytochrome P450 2B6 (CYP2B6)	DEPKLMQ	CP2B6_HUMAN	Substrate	[9]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Cytochrome P450 2D6 (CYP2D6)	OTZJC802	CP2D6_HUMAN	Drug Response	[6]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Mexiletine (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Sodium bicarbonate	DMMU6BJ	Moderate	as urine pH determines the ionization state of weakly acidic or weakly alkaline drugs. Mexiletine caused by Sodium bicarbonate mediated altered urine pH.	Acidosis [5C73]	[12]
Emapalumab	DMZG5WL	Moderate	Altered metabolism of Mexiletine due to Emapalumab alters the formation of CYP450 enzymes.	Adaptive immunity immunodeficiency [4A01]	[13]
Siltuximab	DMGEATB	Moderate	Altered metabolism of Mexiletine due to Siltuximab alters the formation of CYP450 enzymes.	Anemia [3A00-3A9Z]	[13]
Dronedarone	DMA8FS5	Moderate	Decreased metabolism of Mexiletine caused by Dronedarone mediated inhibition of CYP450 enzyme.	Angina pectoris [BA40]	[14]
Aminophylline	DML2NIB	Major	Decreased metabolism of Mexiletine caused by Aminophylline mediated inhibition of CYP450 enzyme.	Asthma [CA23]	[15]
Roflumilast	DMPGHY8	Moderate	Decreased metabolism of Mexiletine caused by Roflumilast mediated inhibition of CYP450 enzyme.	Asthma [CA23]	[13]
Obeticholic acid	DM3Q1SM	Moderate	Decreased metabolism of Mexiletine caused by Obeticholic acid mediated inhibition of CYP450 enzyme.	Autoimmune liver disease [DB96]	[16]
Ofloxacin	DM0VQN3	Minor	Decreased metabolism of Mexiletine caused by Ofloxacin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[17]
Ciprofloxacin XR	DM2NLS9	Minor	Decreased metabolism of Mexiletine caused by Ciprofloxacin XR mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[17]
Norfloxacin	DMIZ6W2	Minor	Decreased metabolism of Mexiletine caused by Norfloxacin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[17]
Levobupivacaine	DM783CH	Moderate	Decreased metabolism of Mexiletine caused by Levobupivacaine mediated inhibition of CYP450 enzyme.	Corneal disease [9A76-9A78]	[13]
Oxtriphylline	DMLHSE3	Major	Decreased metabolism of Mexiletine caused by Oxtriphylline mediated inhibition of CYP450 enzyme.	Cough [MD12]	[15]
Sertraline	DM0FB1J	Moderate	Decreased metabolism of Mexiletine caused by Sertraline mediated inhibition of CYP450 enzyme.	Depression [6A70-6A7Z]	[18]
Fluoxetine	DM3PD2C	Moderate	Decreased metabolism of Mexiletine caused by Fluoxetine mediated inhibition of CYP450 enzyme.	Depression [6A70-6A7Z]	[18]
Paroxetine	DM5PVQE	Moderate	Decreased metabolism of Mexiletine caused by Paroxetine mediated inhibition of CYP450 enzyme.	Depression [6A70-6A7Z]	[18]
Duloxetine	DM9BI7M	Moderate	Decreased metabolism of Mexiletine caused by Duloxetine mediated inhibition of CYP450 enzyme.	Depression [6A70-6A7Z]	[19]
SODIUM CITRATE	DMHPD2Y	Moderate	as urine pH determines the ionization state of weakly acidic or weakly alkaline drugs. Mexiletine caused by SODIUM CITRATE mediated altered urine pH.	Discovery agent [N.A.]	[12]
PMID28870136-Compound-49	DMTUC9E	Moderate	Decreased metabolism of Mexiletine caused by PMID28870136-Compound-49 mediated inhibition of CYP450 enzyme.	Discovery agent [N.A.]	[20]
Mephenytoin	DM5UGDK	Moderate	Increased metabolism of Mexiletine caused by Mephenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[21]
Stiripentol	DMMSDOY	Moderate	Decreased metabolism of Mexiletine caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[13]
Fosphenytoin	DMOX3LB	Moderate	Increased metabolism of Mexiletine caused by Fosphenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[21]
Ethotoin	DMXWOCP	Moderate	Increased metabolism of Mexiletine caused by Ethotoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[21]
Mirabegron	DMS1GYT	Moderate	Decreased metabolism of Mexiletine caused by Mirabegron mediated inhibition of CYP450 enzyme.	Functional bladder disorder [GC50]	[22]
Darifenacin	DMWXLYZ	Moderate	Decreased metabolism of Mexiletine caused by Darifenacin mediated inhibition of CYP450 enzyme.	Functional bladder disorder [GC50]	[23]
Terbinafine	DMI6HUW	Moderate	Decreased metabolism of Mexiletine caused by Terbinafine mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[24]
Simeprevir	DMLUA9D	Moderate	Decreased metabolism of Mexiletine caused by Simeprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[25]
Rifampin	DMA8J1G	Moderate	Increased metabolism of Mexiletine caused by Rifampin mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[26]
Cobicistat	DM6L4H2	Moderate	Decreased metabolism of Mexiletine caused by Cobicistat mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[13]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Mexiletine caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[27]
Darunavir	DMN3GCH	Moderate	Decreased metabolism of Mexiletine caused by Darunavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[28]
Cinacalcet	DMCX0K3	Moderate	Decreased metabolism of Mexiletine caused by Cinacalcet mediated inhibition of CYP450 enzyme.	Hyper-parathyroidism [5A51]	[28]
Pirfenidone	DM6VZFQ	Moderate	Decreased metabolism of Mexiletine caused by Pirfenidone mediated inhibition of CYP450 enzyme.	Idiopathic interstitial pneumonitis [CB03]	[13]
Givosiran	DM5PFIJ	Moderate	Decreased metabolism of Mexiletine caused by Givosiran mediated inhibition of CYP450 enzyme.	Inborn porphyrin/heme metabolism error [5C58]	[29]
Berotralstat	DMWA2DZ	Moderate	Decreased metabolism of Mexiletine caused by Berotralstat mediated inhibition of CYP450 enzyme.	Innate/adaptive immunodeficiency [4A00]	[30]
Ramelteon	DM7IW9J	Moderate	Decreased metabolism of Mexiletine caused by Ramelteon mediated inhibition of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[31]
Tasimelteon	DMLOQ1V	Moderate	Decreased metabolism of Mexiletine caused by Tasimelteon mediated inhibition of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[32]
Polyethylene glycol	DM4I1JP	Moderate	Increased risk of lowers seizure threshold by the combination of Mexiletine and Polyethylene glycol.	Irritable bowel syndrome [DD91]	[33]
Alosetron	DML2A03	Moderate	Decreased metabolism of Mexiletine caused by Alosetron mediated inhibition of CYP450 enzyme.	Irritable bowel syndrome [DD91]	[34]
Dacomitinib	DMOH8VY	Moderate	Decreased metabolism of Mexiletine caused by Dacomitinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[35]
Lumefantrine	DM29GAD	Moderate	Decreased metabolism of Mexiletine caused by Lumefantrine mediated inhibition of CYP450 enzyme.	Malaria [1F40-1F45]	[28]
Vemurafenib	DM62UG5	Moderate	Decreased metabolism of Mexiletine caused by Vemurafenib mediated inhibition of CYP450 enzyme.	Melanoma [2C30]	[36]
Exjade	DMHPRWG	Moderate	Decreased metabolism of Mexiletine caused by Exjade mediated inhibition of CYP450 enzyme.	Mineral absorption/transport disorder [5C64]	[37]
Panobinostat	DM58WKG	Moderate	Decreased metabolism of Mexiletine caused by Panobinostat mediated inhibition of CYP450 enzyme.	Multiple myeloma [2A83]	[38]
Fedratinib	DM4ZBK6	Moderate	Decreased metabolism of Mexiletine caused by Fedratinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[13]
Imatinib	DM7RJXL	Moderate	Decreased metabolism of Mexiletine caused by Imatinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[39]
Droperidol	DM0DXA8	Major	Increased risk of prolong QT interval by the combination of Mexiletine and Droperidol.	Nausea/vomiting [MD90]	[40]
Rolapitant	DM8XP26	Moderate	Decreased metabolism of Mexiletine caused by Rolapitant mediated inhibition of CYP450 enzyme.	Nausea/vomiting [MD90]	[41]
Bupropion	DM5PCS7	Major	Increased risk of lowers seizure threshold by the combination of Mexiletine and Bupropion.	Nicotine use disorder [6C4A]	[42]
Lorcaserin	DMG6OYJ	Moderate	Decreased metabolism of Mexiletine caused by Lorcaserin mediated inhibition of CYP450 enzyme.	Obesity [5B80-5B81]	[43]
Rasagiline	DM3WKQ4	Major	Decreased metabolism of Mexiletine caused by Rasagiline mediated inhibition of CYP450 enzyme.	Parkinsonism [8A00]	[28]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Mexiletine caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[44]
Lindane	DMB8CNL	Moderate	Increased risk of lowers seizure threshold by the combination of Mexiletine and Lindane.	Pediculosis [1G00]	[45]
ABIRATERONE	DM8V75C	Moderate	Decreased metabolism of Mexiletine caused by ABIRATERONE mediated inhibition of CYP450 enzyme.	Prostate cancer [2C82]	[46]
Ustekinumab	DMHTYK3	Moderate	Altered metabolism of Mexiletine due to Ustekinumab alters the formation of CYP450 enzymes.	Psoriasis [EA90]	[13]
Celecoxib	DM6LOQU	Moderate	Decreased metabolism of Mexiletine caused by Celecoxib mediated inhibition of CYP450 enzyme.	Rheumatoid arthritis [FA20]	[47]
Tocilizumab	DM7J6OR	Moderate	Altered metabolism of Mexiletine due to Tocilizumab alters the formation of CYP450 enzymes.	Rheumatoid arthritis [FA20]	[13]
Canakinumab	DM8HLO5	Moderate	Altered metabolism of Mexiletine due to Canakinumab alters the formation of CYP450 enzymes.	Rheumatoid arthritis [FA20]	[13]
Rilonacept	DMGLUQS	Moderate	Altered metabolism of Mexiletine due to Rilonacept alters the formation of CYP450 enzymes.	Rheumatoid arthritis [FA20]	[13]
Golimumab	DMHZV7X	Moderate	Altered metabolism of Mexiletine due to Golimumab alters the formation of CYP450 enzymes.	Rheumatoid arthritis [FA20]	[13]
Chlorpromazine	DMBGZI3	Moderate	Decreased metabolism of Mexiletine caused by Chlorpromazine mediated inhibition of CYP450 enzyme.	Schizophrenia [6A20]	[28]
Asenapine	DMSQZE2	Moderate	Decreased metabolism of Mexiletine caused by Asenapine mediated inhibition of CYP450 enzyme.	Schizophrenia [6A20]	[48]
Tizanidine	DMR2IQ4	Major	Decreased metabolism of Mexiletine caused by Tizanidine mediated inhibition of CYP450 enzyme.	Tonus and reflex abnormality [MB47]	[49]
Nalidixic acid	DMRM0JV	Minor	Decreased metabolism of Mexiletine caused by Nalidixic acid mediated inhibition of CYP450 enzyme.	Urinary tract infection [GC08]	[17]
Enoxacin	DMYTE6L	Minor	Decreased metabolism of Mexiletine caused by Enoxacin mediated inhibition of CYP450 enzyme.	Urinary tract infection [GC08]	[17]
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⏷ Show the Full List of 64 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Allura red AC dye	E00338	33258	Colorant
D&C red no. 28	E00491	6097185	Colorant
FD&C blue no. 1	E00263	19700	Colorant
FD&C blue no. 2	E00446	2723854	Colorant
Isopropyl alcohol	E00070	3776	Antimicrobial preservative; Solvent
Quinoline yellow WS	E00309	24671	Colorant
Sunset yellow FCF	E00255	17730	Colorant
Ammonia	E00007	222	Alkalizing agent
Butyl alcohol	E00011	263	Flavoring agent; Solvent
Ferrosoferric oxide	E00231	14789	Colorant
Magnesium stearate	E00208	11177	lubricant
Propylene glycol	E00040	1030	Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
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⏷ Show the Full List of 14 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Mexiletine 150 mg capsule	150 mg	Oral Capsule	Oral
Mexiletine 200 mg capsule	200 mg	Oral Capsule	Oral
Mexiletine 250 mg capsule	250 mg	Oral Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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