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mexiletine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	1794	31828-71-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: mexiletine dl-mexiletine (+/-)-Mexiletine (RS)-Mexiletine mexiletine hydrochloride mexiletin hydrochloride mexiletine HCl mexiletin HCl	Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties. Molecular weight: 179.26 Formula: C11H17NO CLOGP: 2.57 LIPINSKI: 0 HAC: 2 HDO: 1 TPSA: 35.25 ALOGS: -2.52 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

mexiletine
dl-mexiletine
(+/-)-Mexiletine
(RS)-Mexiletine
mexiletine hydrochloride
mexiletin hydrochloride
mexiletine HCl
mexiletin HCl

Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.

Molecular weight: 179.26
Formula: C11H17NO
CLOGP: 2.57
LIPINSKI: 0
HAC: 2
HDO: 1
TPSA: 35.25
ALOGS: -2.52
ROTB: 3

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.80	g	O
0.80	g	P

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	95.63 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	9.90 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	9.50 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	87 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	8.30 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	5.90 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.36 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 18, 2018	EMA	Lupin Europe GmbH
Dec. 30, 1985	FDA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Body tinea	254.66	48.15	44	1651	1841	63485486
Inhibitory drug interaction	230.13	48.15	43	1652	2806	63484521
Infection susceptibility increased	227.21	48.15	44	1651	3477	63483850
Glucose tolerance impaired	199.79	48.15	44	1651	6533	63480794
Poor quality sleep	187.58	48.15	52	1643	19883	63467444
Purpura	175.78	48.15	44	1651	11341	63475986
Impaired quality of life	172.25	48.15	45	1650	13738	63473589
Bone density decreased	164.88	48.15	44	1651	14568	63472759
Impaired work ability	157.08	48.15	44	1651	17431	63469896
Hyperlipidaemia	152.15	48.15	44	1651	19527	63467800

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Ventricular tachycardia	99.12	21.82	40	1656	26539	34928696
Drug ineffective	44.56	21.82	79	1617	456672	34498563
Tracheitis	30.21	21.82	7	1689	707	34954528
Treatment failure	23.75	21.82	19	1677	46678	34908557
Myoclonus	22.61	21.82	12	1684	14713	34940522

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Body tinea	231.72	28.18	43	3091	1811	79739443
Infection susceptibility increased	201.84	28.18	43	3091	3678	79737576
Inhibitory drug interaction	188.64	28.18	42	3092	4411	79736843
Glucose tolerance impaired	168.65	28.18	43	3091	8041	79733213
Poor quality sleep	152.54	28.18	50	3084	22672	79718582
Bone density decreased	147.29	28.18	43	3091	13304	79727950
Impaired quality of life	144.11	28.18	43	3091	14343	79726911
Purpura	131.17	28.18	43	3091	19484	79721770
Impaired work ability	126.82	28.18	42	3092	19639	79721615
Ventricular tachycardia	119.23	28.18	49	3085	41886	79699368

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C01BB02	CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class Ib
CHEBI has role	CHEBI:38070	antiarrhythmic agent
FDA EPC	N0000175426	Antiarrhythmic
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D026941	Sodium Channel Blockers
MeSH PA	D061567	Voltage-Gated Sodium Channel Blockers

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Ventricular arrhythmia	indication	44103008
Myotonic disorder	indication	193237003	DOID:450
Myocardial infarction	contraindication	22298006	DOID:5844
Complete atrioventricular block	contraindication	27885002
Sick sinus syndrome	contraindication	36083008	DOID:13884
Low blood pressure	contraindication	45007003
Chronic heart failure	contraindication	48447003
Epilepsy	contraindication	84757009	DOID:1826
Cardiogenic shock	contraindication	89138009
Liver function tests abnormal	contraindication	166603001

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.01	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN	BLOCKER	IC50	4.53	WOMBAT-PK	CHEMBL
Sodium channel protein type 2 subunit alpha	Ion channel	Q99250	SCN2A_HUMAN	BLOCKER	IC50	5.54	CHEMBL	CHEMBL
Sodium channel protein type 4 subunit alpha	Ion channel	P35499	SCN4A_HUMAN	BLOCKER	IC50	4.38	WOMBAT-PK	CHEMBL
Sodium channel protein type 9 subunit alpha	Ion channel	Q15858	SCN9A_HUMAN	BLOCKER	Ki	4.89	CHEMBL	CHEMBL
Sodium channel protein type 10 subunit alpha	Ion channel	Q9Y5Y9	SCNAA_HUMAN	BLOCKER	IC50	4.25	CHEMBL	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.14	DRUG MATRIX
Sodium channel protein type 1 subunit alpha	Ion channel	P35498	SCN1A_HUMAN		IC50	4.96	CHEMBL
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	4.26	WOMBAT-PK
Potassium channel subfamily K member 3	Ion channel	O14649	KCNK3_HUMAN		IC50	4.01	CHEMBL

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External reference:

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ID	Source
000630	NDDF
004485	NDDF
108500007	SNOMEDCT_US
1108	MMSL
142138	RXNORM
1U511HHV4Z	UNII
2629	IUPHAR_LIGAND_ID
3262	INN_ID
372909002	SNOMEDCT_US
4019066	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Mexiletine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8739	CAPSULE	150 mg	ORAL	ANDA	20 sections
Mexiletine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8739	CAPSULE	150 mg	ORAL	ANDA	20 sections
Mexiletine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8740	CAPSULE	200 mg	ORAL	ANDA	20 sections
Mexiletine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8740	CAPSULE	200 mg	ORAL	ANDA	20 sections
Mexiletine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8741	CAPSULE	250 mg	ORAL	ANDA	20 sections
Mexiletine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8741	CAPSULE	250 mg	ORAL	ANDA	20 sections
Mexiletine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4107	CAPSULE	150 mg	ORAL	ANDA	23 sections
Mexiletine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4107	CAPSULE	150 mg	ORAL	ANDA	23 sections
Mexiletine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4108	CAPSULE	200 mg	ORAL	ANDA	23 sections
Mexiletine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4108	CAPSULE	200 mg	ORAL	ANDA	23 sections

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