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| '''Tolperisone''', a [[piperidine]] derivative, is a centrally acting [[muscle relaxant]]. Brand names include '''Mydocalm''' and '''Mydeton'''. | | '''Tolperisone''', a [[piperidine]] derivative, is a centrally acting [[muscle relaxant]]. Brand names include '''Mydocalm''' and '''Mydeton'''. |
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| {{Drugbox | | ==External links== |
| | Verifiedfields = changed | | * {{cite journal | author = Hofer D, Lohberger B, Steinecker B, Schmidt K, Quasthoff S, Schreibmayer W | title = A comparative study of the action of tolperisone on seven different voltage dependent sodium channel isoforms. | journal = Eur J Pharmacol | volume = 538 | issue = 1-3 | pages = 5-14 | year = 2006 | id = PMID 16650844}} |
| | Watchedfields = changed | | * {{cite journal | author = Kocsis P, Farkas S, Fodor L, Bielik N, Thán M, Kolok S, Gere A, Csejtei M, Tarnawa I | title = Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels. | journal = J Pharmacol Exp Ther | volume = 315 | issue = 3 | pages = 1237-46 | year = 2005 | id = PMID 16126840}} |
| | verifiedrevid = 451425253 | | * {{cite journal | author = Ribi C, Vermeulen C, Hauser C | title = Anaphylactic reactions to tolperisone (Mydocalm). | journal = Swiss Med Wkly | volume = 133 | issue = 25-26 | pages = 369-71 | year = 2003 | id = PMID 12947534}} |
| | IUPAC_name = 2-methyl-1-(4-methylphenyl)-3-(1-piperidyl)propan-1-one | |
| | image = Tolperisone-2d-skeletal.png | |
| | width = 150 | |
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| <!--Clinical data-->
| | {{medicine-stub}} |
| | tradename = Mydocalm and others
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| | Drugs.com = {{drugs.com|international|tolperisone}}
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| | pregnancy_category=
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| | legal_status = Rx-only
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| | routes_of_administration = Oral, [[parenteral]]
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| <!-- Pharmacokinetic data -->
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| | bioavailability =
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| | protein_bound =
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| | metabolism = Liver, kidney
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| | elimination_half-life = 1st phase: 2 hrs<br />2nd phase: 12 hrs
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| | excretion = [[Kidney|Renal]]
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| <!--Identifiers-->
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| | CAS_number_Ref = {{cascite|correct|??}}
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| | CAS_number = 728-88-1
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| | ATC_prefix = M02
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| | ATC_suffix = AX06
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| | ATC_supplemental = {{ATC|M03|BX04}}
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| | PubChem = 5511
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| | ChEMBL_Ref = {{ebicite|changed|EBI}}
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| | ChEMBL = 1076211
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| | DrugBank_Ref = {{drugbankcite|correct|drugbank}}
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| | UNII_Ref = {{fdacite|correct|FDA}}
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| | UNII = F5EOM0LD8E
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| | KEGG_Ref = {{keggcite|correct|kegg}}
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| | KEGG = D08617
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| <!--Chemical data-->
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| | C=16 | H=23 | N=1 | O=1
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| | molecular_weight = 245.36 g/mol
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| | smiles = C1CCCN(C1)CC(C(C2=CC=C(C=C2)C)=O)C
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| | StdInChI_Ref = {{stdinchicite|changed|chemspider}}
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| | StdInChI = 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
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| | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
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| | StdInChIKey = FSKFPVLPFLJRQB-UHFFFAOYSA-N
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| }}
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| __Notoc__
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| {{SI}}
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| {{CMG}}
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| ==Overview==
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| '''Tolperisone''', a [[piperidine]] derivative, is a centrally acting [[muscle relaxant]]. Trade names include '''Biocalm''', '''Muscodol''', '''Mydeton''', '''Mydocalm''', '''Myolax''', '''Myoxan''' and '''Viveo'''.
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| == Clinical use ==
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| In Tolperisone is indicated for use in the treatment of pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the [[pyramidal tract]], [[multiple sclerosis]], [[myelopathy]], [[encephalomyelitis]]) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.<ref name="Austria-Codex">{{cite book|title=Austria-Codex|editor=Jasek, W|publisher=Österreichischer Apothekerverlag|location=Vienna|year=2007|edition=62nd|pages=5510–1|isbn=978-3-85200-181-4|language=German}}</ref><ref name="Midocalm-ro">{{ cite web | url = http://www.info-medic.ro/midocalm/ | title = Midocalm | publisher = InfoMedic| location = Romania}}</ref>
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| Other possible uses include:{{fact|date=May 2012}}
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| *[[Spondylosis]]
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| *Spondylarthrosis
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| *Cervical and lumbar syndromes
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| *[[Arthrosis]] of the large joints
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| *[[atherosclerosis|Obliterating atherosclerosis]] of the extremity vessels
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| *[[Diabetic angiopathy]]
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| *[[Thromboangiitis obliterans]]
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| *[[Raynaud's syndrome]]
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| == Contraindications and cautions ==
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| Manufacturers report that tolperisone should not be used in patients with [[myasthenia gravis]]. Only limited data are available regarding the safety in children, youths, during pregnancy and breastfeeding. It is not known whether tolperisone is excreted into mother's milk.<ref name="Austria-Codex" /><ref name="Midocalm-ro" />
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| == Side effects ==
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| Adverse effects occur in fewer than 1% of patients and include muscle weakness, headache, arterial [[hypotension]], nausea, vomiting, [[dyspepsia]], and dry mouth. All effects are reversible.<ref name="Austria-Codex" /><ref name="Midocalm-ro" />
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| Allergic reactions occur in fewer than 0.1% of patient and include skin rash, [[hives]], [[Quincke's edema]], and in some cases [[anaphylactic shock]].<ref name="Austria-Codex" /><ref>{{ cite journal | author = Ribi C, Vermeulen C, Hauser C | title = Anaphylactic reactions to tolperisone (Mydocalm) | journal = Swiss Medical Weekly | volume = 133 | issue = 25–26 | pages = 369–371 | year = 2003 | pmid = 12947534 }}</ref><ref name="pmid14587432">{{cite journal |author=Kwaśniewski A, Korbuszewska-Gontarz B, Mika S |title=[Mydocalm causing anaphylaxis] |language=Polish |journal=Pneumonol Alergol Pol |volume=71 |issue=5-6 |pages=250–2 |year=2003 |pmid=14587432 |doi= |url= |accessdate=2014-12-17}}</ref><ref name="pmid21905508">{{cite journal |author=Glück J, Rymarczyk B, Rogala B |title=An immediate hypersensitivity reaction caused by tolperisone hydrochloride |journal=J Investig Allergol Clin Immunol |volume=21 |issue=5 |pages=411–2 |year=2011 |pmid=21905508 |doi= |url= |accessdate=2014-12-17}}</ref>
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| == Overdose ==
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| Excitability has been noted after ingestion of high doses by children.<ref name="Austria-Codex" />
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| In suicide studies of three isolated cases, it is believed that ingestion of tolperisone was the cause of death.<ref>{{ cite journal | author = Sporkert, F.; Brunel, C.; Augsburger, M. P.; Mangin, P. | title = Fatal tolperisone poisoning: Autopsy and toxicology findings in three suicide cases | journal = Forensic Science International | year = 2012 | volume = 215 | issue = 1 | pages = 101–104 | doi = 10.1016/j.forsciint.2011.05.025 | pmid = 21683537 }}</ref>
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| == Interactions ==
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| Tolperisone does not have a significant potential for interactions with other pharmaceutical drugs. It cannot be excluded that combination with other centrally acting muscle relaxants, [[benzodiazepine]]s or [[non-steroidal anti-inflammatory drug]]s (NSAIDs) may make a dose reduction necessary in some patients.<ref name="Austria-Codex" /><ref name="Midocalm-ro" />
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| == Mechanism of action ==
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| Tolperisone is a centrally acting muscle relaxant that acts at the [[reticular formation]] in the brain stem<ref name="Austria-Codex" /> by blocking [[Voltage-gated sodium channel|voltage-gated sodium]] and [[Voltage-gated calcium channel|calcium channels]].<ref>{{ cite journal | author = Kocsis P, Farkas S, Fodor L, Bielik N, Thán M, Kolok S, Gere A, Csejtei M, Tarnawa I | title = Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels | journal = Journal of Pharmacology and Experimental Therapeutics | volume = 315 | issue = 3 | pages = 1237–1246 | year = 2005 | pmid = 16126840 | doi = 10.1124/jpet.105.089805 }}</ref><ref>{{ cite journal | author = Hofer D, Lohberger B, Steinecker B, Schmidt K, Quasthoff S, Schreibmayer W | title = A comparative study of the action of tolperisone on seven different voltage dependent sodium channel isoforms | journal = European Journal of Pharmacology | volume = 538 | issue = 1–3 | pages = 5–14 | year = 2006 | pmid = 16650844 | doi = 10.1016/j.ejphar.2006.03.034 }}</ref>
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| == Pharmacokinetics ==
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| Tolperisone is absorbed nearly completely from the gut and reaches its [[peak (pharmacology)|peak]] blood plasma concentration after 1.5 hours. It is extensively metabolised in the liver and kidneys. The substance is excreted via the kidneys in two phases; the first with a half-life of two hours, and the second with a half-life of 12 hours.<ref name="Austria-Codex" />
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| == See also ==
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| * Chemically and mechanistically related drugs: [[eperisone]], [[inaperisone]], [[lanperisone]], [[silperisone]]
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| == References ==
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| {{reflist|2}}
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| == External links ==
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| * {{ cite web | url = http://lib.bioinfo.pl/meid:189350 | title = Tolperisone: Administration & Dosage - Papers | publisher = BioInfo | location = Poland }}{{dead link|date=December 2013}}
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| {{Muscle relaxants}} | | {{Muscle relaxants}} |
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| [[Category:Piperidines]] | | [[hu:Tolperizon]] |
| [[Category:Muscle relaxants]] | | [[ro:Tolperison]] |
| [[Category:Aromatic ketones]]
| | {{WikiDoc Sources}} |
