Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C16H23NO.ClH |
| Molecular Weight | 281.821 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC(CN1CCCCC1)C(=O)C2=CC=C(C)C=C2
InChI
InChIKey=ZBUVYROEHQQAKL-UHFFFAOYSA-N
InChI=1S/C16H23NO.ClH/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;1H
DescriptionCurator's Comment: description was created based on several sources, including
https://pharmacybook.net/mydocalm/ | http://en.remedy-info.com/ovr0_midokalm.html | https://www.ncbi.nlm.nih.gov/pubmed/18482024 | https://www.ncbi.nlm.nih.gov/pubmed/232053
Curator's Comment: description was created based on several sources, including
https://pharmacybook.net/mydocalm/ | http://en.remedy-info.com/ovr0_midokalm.html | https://www.ncbi.nlm.nih.gov/pubmed/18482024 | https://www.ncbi.nlm.nih.gov/pubmed/232053
Tolperisone is a centrally acting muscle relaxant first synthesized in 1956 and used in clinical practice since the 1960’s. Tolperisone is an aryl alkyl β-aminoketone with an asymmetric carbon atom α to the carbonyl group. The dextrorotatory enantiomer was reported less effective, however, no detailed analyses of the enantiomers are available. The precise mechanism of action of tolperisone is not fully known. The most prominent effect of tolperisone is its inhibitory action on pathways of spinal reflexes. It suppresses the mono and polysynaptic reflex transmission by both pre-synaptic and post-synaptic mechanisms.
CNS Activity
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| [Neuropharmacological studies on tolperisone hydrochloride (author's transl)]. | 1979 Oct |
|
| Tolperisone--a novel modulator of ionic currents in myelinated axons. | 2001 Dec |
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| Simultaneous determination of tolperisone and lidocaine by high performance liquid chromatography. | 2001 Dec |
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| Use of vancomycin silica stationary phase in packed capillary electrochromatography I. Enantiomer separation of basic compounds. | 2001 Feb |
|
| [Spastic syndrome. More mobile again after stroke]. | 2001 Mar 8 |
|
| Comparison of two intracranial self-stimulation (ICSS) paradigms in C57BL/6 mice: head-dipping and place-learning. | 2001 Nov 29 |
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| Separation of basic drug enantiomers by capillary electrophoresis using ovoglycoprotein as a chiral selector: comparison of chiral resolution ability of ovoglycoprotein and completely deglycosylated ovoglycoprotein. | 2001 Sep |
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| [Fibromyalgia problem case. Monotherapy is mostly insufficient]. | 2002 Apr 25 |
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| Effect of muscle relaxants on experimental jaw-muscle pain and jaw-stretch reflexes: a double-blind and placebo-controlled trial. | 2003 |
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| Prophylactic tolperisone for post-exercise muscle soreness causes reduced isometric force--a double-blind randomized crossover control study. | 2003 |
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| [Fibromyalgia also has psychological origins. "Often harmony seeking perfectionists"]. | 2003 May 1 |
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| [A study of mydocalm efficiency in the treatment of chronic headache of tension]. | 2005 |
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| A comparative study of the action of tolperisone on seven different voltage dependent sodium channel isoforms. | 2006 May 24 |
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| Grand rounds: an outbreak of toxic hepatitis among industrial waste disposal workers. | 2007 Jan |
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| Determination of eperisone in human plasma by liquid chromatography-ESI-tandem mass spectrometry. | 2007 Sep |
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| Cannabinoids in the management of spasticity associated with multiple sclerosis. | 2008 Oct |
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| [IGOST guideline for pharmacotherapy of low back pain]. | 2010 Aug 12 |
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| Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method. | 2010 Dec |
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| Classification of drugs based on properties of sodium channel inhibition: a comparative automated patch-clamp study. | 2010 Dec 20 |
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| Differential effects of painful and non-painful stimulation on tactile processing in fibromyalgia syndrome and subjects with masochistic behaviour. | 2010 Dec 28 |
|
| Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. | 2011 Jul 14 |
|
| Comparative study of therapeutic response to baclofen vs tolperisone in spasticity. | 2017 Mar |
Sample Use Guides
In Vivo Use Guide
Sources: https://pharmacybook.net/mydocalm/
The usual dose is Mydocalm (tolperisone) 150 mg, 1-3 times a day. It should be taken after meal. The maximum daily dose is 450 mg
Route of Administration:
Oral
The sodium channel blocking effects of Tolperisone was characterized in electrophysiological experiments on dorsal root ganglion (DRG) cells. DRG cells were acutely dissociated from rat DRG of 6-day-old male rats. Tolperisone (0, 40, 80, 160, 320, and 640 mkM) dissolved in the extracellular solution were applied onto the cells via multibarreled ejection pipettes controlled by electromagnetic valves. Currents were recorded from fast-kinetics tetrodotoxin-sensitive DRG cells.
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NCI_THESAURUS |
C29696
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3644-61-9
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100000084637
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SUB04912MIG
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222-876-5
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C84220
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8Z075K2TIG
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92965
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DTXSID2045868
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DBSALT002004
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m10951
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CHEMBL1076211
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ACTIVE MOIETY
SUBSTANCE RECORD
