tolperisone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
2703 728-88-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tolperisone
  • mideton
  • mydeton
  • mydetone
  • dl-Tolperisone
  • tolperisone hydrochloride
  • (+/-)-Tolperisone
  • tolperisone HCl
A centrally acting muscle relaxant that has been used for the symptomatic treatment of spasticity and muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1211)
  • Molecular weight: 245.37
  • Formula: C16H23NO
  • CLOGP: 3.83
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 20.31
  • ALOGS: -3.17
  • ROTB: 4

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 19.50 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AKT2,AXL,BRAF,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1 33
kinase-selectivity-class AXL,BRAF,EIF2AK3,GRK2,SIK2,TTK 6
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

None

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
Respiratory alkalosis 69.47 31.06 14 943 3434 90624056
Serotonin syndrome 62.80 31.06 21 936 37866 90589624
Pelvic fracture 44.36 31.06 13 944 15206 90612284
Drug interaction 38.56 31.06 28 929 276425 90351065
Lymphopenia 31.30 31.06 11 946 22870 90604620

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
Enzyme inhibition 73.60 45.56 8 147 76 42621104

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
Enzyme inhibition 71.50 32.47 9 844 144 110588302
Respiratory alkalosis 61.06 32.47 13 840 5708 110582738
Serotonin syndrome 56.29 32.47 20 833 59133 110529313
Pelvic fracture 44.59 32.47 12 841 14142 110574304

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M02AX06 MUSCULO-SKELETAL SYSTEM
TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
Other topical products for joint and muscular pain
ATC M03BX04 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
Other centrally acting agents
MeSH PA D009125 Muscle Relaxants, Central
MeSH PA D009465 Neuromuscular Agents
CHEBI has role CHEBI:35480 analgesic

Related Drugs by ATC class:

M02AX Other topical products for joint and muscular pain 3 drugs
dimethyl sulfoxideidrocilamidetolazoline
M03BX Other centrally acting agents 9 drugs
baclofencyclobenzaprineeperisonefenyramidolmephenesinpridinoltetrazepamthiocolchicosidetizanidine

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

DiseaseRelationSNOMED_IDDOID
Spasticity indication 221360009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.68 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
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 8.25 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.34 DRUG MATRIX
SMR1-alpha3 Unclassified Ki 5.69 DRUG MATRIX
BetaB2-crystallin Structural IC50 5.47 DRUG MATRIX

External reference:

IDSource
F5EOM0LD8E UNII
N0000167236 NUI
D01507 KEGG_DRUG
3644-61-9 SECONDARY_CAS_RN
C0040382 UMLSCUI
CHEBI:749126 CHEBI
CHEMBL1076211 ChEMBL_ID
5511 PUBCHEM_CID
DB06264 DRUGBANK_ID
CHEMBL1395150 ChEMBL_ID
D014049 MESH_DESCRIPTOR_UI
3298 INN_ID
10639 RXNORM
004185 NDDF
004186 NDDF
1172426007 SNOMEDCT_US
703717006 SNOMEDCT_US
703718001 SNOMEDCT_US

Pharmaceutical products:

None