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

Stem definitionDrug idCAS RN
1794 31828-71-4

Description:

MoleculeDescription

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:

DoseUnitRoute
0.80 g O
0.80 g P

ADMET properties:

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

Approvals:

DateAgencyCompanyOrphan
Dec. 18, 2018 EMA Lupin Europe GmbH
Dec. 30, 1985 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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
Oral herpes 139.70 48.15 44 1651 26030 63461297
Skin disorder 134.34 48.15 44 1651 29463 63457864
Cataract 112.87 48.15 46 1649 57007 63430320
Weight increased 111.62 48.15 75 1620 260717 63226610
Herpes zoster 99.67 48.15 47 1648 82415 63404912
Cellulitis 96.86 48.15 46 1649 81912 63405415
Immune thrombocytopenia 78.68 48.15 23 1672 10533 63476794
Contusion 68.36 48.15 45 1650 149999 63337328
Insomnia 55.91 48.15 46 1649 215206 63272121
Therapy non-responder 53.11 48.15 30 1665 75871 63411456

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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
Hyperlipidaemia 118.96 28.18 43 3091 26050 79715204
Oral herpes 116.82 28.18 43 3091 27411 79713843
Skin disorder 107.95 28.18 43 3091 33900 79707354
Cataract 94.77 28.18 47 3087 62073 79679181
Weight increased 85.13 28.18 77 3057 277309 79463945
Drug ineffective 82.32 28.18 149 2985 1080764 78660490
Herpes zoster 76.96 28.18 47 3087 93036 79648218
Cellulitis 65.36 28.18 45 3089 109015 79632239
Immune thrombocytopenia 58.11 28.18 23 3111 17782 79723472
Contusion 54.99 28.18 46 3088 148730 79592524
Therapy non-responder 43.63 28.18 33 3101 92272 79648982
Insomnia 40.58 28.18 49 3085 245121 79496133
Hypertension 29.20 28.18 49 3085 330943 79410311

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01BB02 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
ANTIARRHYTHMICS, CLASS I AND III
Antiarrhythmics, class Ib
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
CHEBI has role CHEBI:38070 antiarrhythmic agent

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

DiseaseRelationSNOMED_IDDOID
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
Second degree atrioventricular block contraindication 195042002
Disease of liver contraindication 235856003 DOID:409
Smokes tobacco daily contraindication 449868002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.01 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Sodium channel protein type 5 subunit alpha Ion channel BLOCKER IC50 4.53 WOMBAT-PK CHEMBL
Sodium channel protein type 2 subunit alpha Ion channel BLOCKER IC50 5.54 CHEMBL CHEMBL
Sodium channel protein type 4 subunit alpha Ion channel BLOCKER IC50 4.38 WOMBAT-PK CHEMBL
Sodium channel protein type 9 subunit alpha Ion channel BLOCKER Ki 4.89 CHEMBL CHEMBL
Sodium channel protein type 10 subunit alpha Ion channel BLOCKER IC50 4.25 CHEMBL CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5 CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 6.14 DRUG MATRIX
Sodium channel protein type 1 subunit alpha Ion channel IC50 4.96 CHEMBL
Solute carrier family 22 member 2 Transporter IC50 4.26 WOMBAT-PK
Potassium channel subfamily K member 3 Ion channel IC50 4.01 CHEMBL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 Ion channel IC50 3.51 WOMBAT-PK
Sodium channel subunit beta-1 Ion channel WOMBAT-PK
Sodium channel subunit beta-2 Ion channel WOMBAT-PK
Sodium channel subunit beta-3 Ion channel WOMBAT-PK
Sodium channel subunit beta-4 Ion channel WOMBAT-PK
Sodium channel protein type X alpha subunit Ion channel IC50 4.51 CHEMBL
Sodium channel protein type 9 subunit alpha Ion channel IC50 4.96 CHEMBL
Sodium channel protein type 1 subunit alpha Ion channel IC50 4.68 CHEMBL

External reference:

IDSource
4019837 VUID
N0000147925 NUI
D00639 KEGG_DRUG
5370-01-4 SECONDARY_CAS_RN
4019066 VANDF
4019837 VANDF
C0025887 UMLSCUI
CHEBI:6916 CHEBI
CHEMBL146855 ChEMBL_ID
CHEMBL558 ChEMBL_ID
CHEMBL147507 ChEMBL_ID
DB00379 DRUGBANK_ID
CHEMBL1200606 ChEMBL_ID
D008801 MESH_DESCRIPTOR_UI
4178 PUBCHEM_CID
3262 INN_ID
2629 IUPHAR_LIGAND_ID
1U511HHV4Z UNII
142138 RXNORM
1108 MMSL
5109 MMSL
d00300 MMSL
000630 NDDF
004485 NDDF
108500007 SNOMEDCT_US
372909002 SNOMEDCT_US
96298001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0527-4109 CAPSULE 250 mg ORAL ANDA 23 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0527-4109 CAPSULE 250 mg ORAL ANDA 23 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10135-730 CAPSULE 150 mg ORAL ANDA 22 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10135-731 CAPSULE 200 mg ORAL ANDA 22 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10135-732 CAPSULE 250 mg ORAL ANDA 22 sections
Mexiletine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 31722-036 CAPSULE 150 mg ORAL ANDA 17 sections
Mexiletine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 31722-037 CAPSULE 200 mg ORAL ANDA 17 sections
Mexiletine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 31722-038 CAPSULE 250 mg ORAL ANDA 17 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-624 CAPSULE 150 mg ORAL ANDA 19 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-624 CAPSULE 150 mg ORAL ANDA 19 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-624 CAPSULE 150 mg ORAL ANDA 19 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-625 CAPSULE 200 mg ORAL ANDA 19 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-625 CAPSULE 200 mg ORAL ANDA 19 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-625 CAPSULE 200 mg ORAL ANDA 19 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-626 CAPSULE 250 mg ORAL ANDA 19 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-626 CAPSULE 250 mg ORAL ANDA 19 sections
Mexiletine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-626 CAPSULE 250 mg ORAL ANDA 19 sections
MEXILETINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 50742-239 CAPSULE 150 mg ORAL ANDA 17 sections
MEXILETINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 50742-240 CAPSULE 200 mg ORAL ANDA 17 sections
MEXILETINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 50742-241 CAPSULE 250 mg ORAL ANDA 17 sections