tolperisone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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:

None

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 52.45 29.93 11 805 2690 63485516
Serotonin syndrome 48.67 29.93 17 799 28665 63459541

FDA Adverse Event Reporting System (Male)

None

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
Respiratory alkalosis 46.36 34.10 10 657 4301 79739420
Serotonin syndrome 44.55 34.10 16 651 45011 79698710

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 D002491 Central Nervous System Agents
MeSH PA D009125 Muscle Relaxants, Central
MeSH PA D009465 Neuromuscular Agents
MeSH PA D018373 Peripheral Nervous System Agents

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 Unclassified IC50 5.47 DRUG MATRIX

External reference:

IDSource
F5EOM0LD8E UNII
N0000167236 NUI
D01507 KEGG_DRUG
3644-61-9 SECONDARY_CAS_RN
C0040382 UMLSCUI
CHEBI:93835 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