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

Identification

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Name
Tolperisone
Accession Number
DB06264
Type
Small Molecule
Groups
Investigational
Description

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.

Structure
Thumb
Synonyms
Not Available
External IDs
AV650 / SPH-3047
Product Ingredients
IngredientUNIICASInChI Key
Tolperisone hydrochloride8Z075K2TIG3644-61-9ZBUVYROEHQQAKL-UHFFFAOYSA-N
International/Other Brands
Musclex / Viveo
Categories
UNII
F5EOM0LD8E
CAS number
728-88-1
Weight
Average: 245.366
Monoisotopic: 245.177964365
Chemical Formula
C16H23NO
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

Pharmacology

Indication

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

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
Toxicity
Not Available
Affected organisms
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
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Tolperisone is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Tolperisone.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Methoxyamphetamine is combined with Tolperisone.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Tolperisone is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Tolperisone.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of adverse effects can be increased when Tolperisone is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Tolperisone.
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Tolperisone.
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.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

General References
Not Available
External Links
KEGG Drug
D08617
ChemSpider
5310
ChEBI
93835
ChEMBL
CHEMBL1076211
Wikipedia
Tolperisone
ATC Codes
M03BX04 — TolperisoneM02AX06 — Tolperisone

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers2
2CompletedTreatmentBack Pain / Back Pain Lower Back / Back Spasm Upper Back / Back Strain / Muscle Cramps / Muscle Spasms / Pain, Acute1
2TerminatedTreatmentMuscle Spasticity2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
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

Taxonomy

Classification
Not classified

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. [PubMed:12695352]

Drug created on March 19, 2008 10:20 / Updated on September 06, 2019 05:06