Tolperisone

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Summary

Tolperisone is a muscle relaxant used to relieve spasticity after stroke in adults.

Generic Name
Tolperisone
DrugBank Accession Number
DB06264
Background

Tolperisone is an oral, centrally acting muscle relaxant. Its precise mechanism is not completely understood, though it blocks sodium and calcium channels. It possesses a high affinity for nervous system tissue, reaching highest concentrations in brain stem, spinal cord and peripheral nerves. Based on existing clinical data, Tolperisone is not sedating and does not interact with alcohol.

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 245.366
Monoisotopic: 245.177964365
Chemical Formula
C16H23NO
Synonyms
  • Tolperisone
External IDs
  • AV650
  • SPH-3047

Pharmacology

Indication

Investigated for use/treatment in neurologic disorders, spinal cord injuries, muscle spasm, back pain, and multiple sclerosis.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Not Available

Mechanism of action
Not Available
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Tolperisone is combined with 1,2-Benzodiazepine.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Tolperisone.
AcetophenazineThe risk or severity of adverse effects can be increased when Acetophenazine is combined with Tolperisone.
AclidiniumTolperisone may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
AgomelatineThe risk or severity of adverse effects can be increased when Tolperisone is combined with Agomelatine.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Tolperisone.
AlimemazineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Tolperisone.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Tolperisone.
AlosetronThe risk or severity of adverse effects can be increased when Alosetron is combined with Tolperisone.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Tolperisone.
Interactions
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Food Interactions
Not Available

Products

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Product Ingredients
IngredientUNIICASInChI Key
Tolperisone hydrochloride8Z075K2TIG3644-61-9ZBUVYROEHQQAKL-UHFFFAOYSA-N
International/Other Brands
Musclex / Viveo

Categories

ATC Codes
M03BX04 — TolperisoneM02AX06 — Tolperisone
Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
F5EOM0LD8E
CAS number
728-88-1
InChI Key
FSKFPVLPFLJRQB-UHFFFAOYSA-N
InChI
InChI=1S/C16H23NO/c1-13-6-8-15(9-7-13)16(18)14(2)12-17-10-4-3-5-11-17/h6-9,14H,3-5,10-12H2,1-2H3
IUPAC Name
2-methyl-1-(4-methylphenyl)-3-(piperidin-1-yl)propan-1-one
SMILES
CC(CN1CCCCC1)C(=O)C1=CC=C(C)C=C1

References

General References
Not Available
KEGG Drug
D08617
ChemSpider
5310
BindingDB
442744
RxNav
10639
ChEBI
93835
ChEMBL
CHEMBL1076211
Wikipedia
Tolperisone

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3RecruitingTreatmentBack Muscle Spasm / Back pain / Back Spasm Upper Back / Back Strain / Muscle Spasms / Pain, Acute1
2CompletedTreatmentBack pain / Back Pain Lower Back / Back Spasm Upper Back / Back Strain / Muscle Cramps / Muscle Spasms / Pain, Acute1
2TerminatedTreatmentSpasticity, Muscle2
1CompletedNot AvailableHealthy Subjects (HS)2
1CompletedOtherHealthy Subjects (HS)1
1CompletedTreatmentHealthy Subjects (HS)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral150 MG
Tablet, coatedOral50 mg
Tablet, film coatedOral50 mg
Tablet50 mg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.167 mg/mLALOGPS
logP3.75ALOGPS
logP3.57ChemAxon
logS-3.2ALOGPS
pKa (Strongest Acidic)16.51ChemAxon
pKa (Strongest Basic)8.78ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area20.31 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity76.35 m3·mol-1ChemAxon
Polarizability29.6 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
Data are limited to an in vitro study.
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Dalmadi B, Leibinger J, Szeberenyi S, Borbas T, Farkas S, Szombathelyi Z, Tihanyi K: Identification of metabolic pathways involved in the biotransformation of tolperisone by human microsomal enzymes. Drug Metab Dispos. 2003 May;31(5):631-6. [Article]

Drug created on March 19, 2008 16:20 / Updated on June 19, 2021 00:26