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
Structure for Tolperisone (DB06264)
- 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.
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- Contraindications & Blackbox Warnings
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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
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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.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Tolperisone is combined with 1,2-Benzodiazepine. Acetazolamide The risk or severity of CNS depression can be increased when Acetazolamide is combined with Tolperisone. Acetophenazine The risk or severity of CNS depression can be increased when Acetophenazine is combined with Tolperisone. Agomelatine The risk or severity of CNS depression can be increased when Tolperisone is combined with Agomelatine. Alfentanil The risk or severity of CNS depression can be increased when Alfentanil is combined with Tolperisone. Alimemazine The risk or severity of CNS depression can be increased when Alimemazine is combined with Tolperisone. Almotriptan The risk or severity of CNS depression can be increased when Almotriptan is combined with Tolperisone. Alosetron The risk or severity of CNS depression can be increased when Alosetron is combined with Tolperisone. Alprazolam The risk or severity of CNS depression can be increased when Alprazolam is combined with Tolperisone. Alverine The risk or severity of CNS depression can be increased when Alverine is combined with Tolperisone. 
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- Not Available
Products
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Ingredient UNII CAS InChI Key Tolperisone hydrochloride 8Z075K2TIG 3644-61-9 ZBUVYROEHQQAKL-UHFFFAOYSA-N - International/Other Brands
- Musclex / Viveo
Categories
- ATC Codes
- M03BX04 — Tolperisone
- M03BX — Other centrally acting agents
- M03B — MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
- M03 — MUSCLE RELAXANTS
- M — MUSCULO-SKELETAL SYSTEM
- Drug Categories
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 Substrates
- Ketones
- Muscle Relaxants
- Muscle Relaxants, Centrally Acting Agents
- Musculo-Skeletal System
- Neuromuscular Agents
- Peripheral Nervous System Agents
- Propiophenones
- Pyridines
- Topical Products for Joint and Muscular Pain
- 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
- External Links
- KEGG Drug
- D08617
- ChemSpider
- 5310
- BindingDB
- 442744
- 10639
- ChEBI
- 93835
- ChEMBL
- CHEMBL1076211
- Wikipedia
- Tolperisone
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Completed Treatment Acute Pain / Back Muscle Spasm / Back pain / Back Spasm Upper Back / Back Strain / Muscle Spasms 1 3 Recruiting Treatment Back Pain Lower Back 1 2 Completed Treatment Acute Pain / Back pain / Back Pain Lower Back / Back Spasm Upper Back / Back Strain / Muscle Cramps / Muscle Spasms 1 2 Terminated Treatment Spasticity, Muscle 2 1 Completed Not Available Healthy Subjects (HS) 2 1 Completed Other Healthy Subjects (HS) 1 1 Completed Treatment Healthy Subjects (HS) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral 150 MG Tablet, coated Oral 50 mg Tablet, film coated Oral 50 mg Tablet 50 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.167 mg/mL ALOGPS logP 3.75 ALOGPS logP 3.57 Chemaxon logS -3.2 ALOGPS pKa (Strongest Acidic) 16.51 Chemaxon pKa (Strongest Basic) 8.78 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 20.31 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 76.35 m3·mol-1 Chemaxon Polarizability 29.6 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - 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
- 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 at March 19, 2008 16:20 / Updated at June 19, 2021 00:26