Tolperisone

Tolperisone
Systematic (IUPAC) name
2-methyl-1-(4-methylphenyl)-3-(1-piperidyl)propan-1-one
Clinical data
Trade names Mydocalm and others
AHFS/Drugs.com International Drug Names
Routes of
administration		 Oral, parenteral
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Metabolism Liver, kidney
Biological half-life 1st phase: 2 hrs
2nd phase: 12 hrs
Excretion Renal
Identifiers
CAS Number 728-88-1 YesY
ATC code M02AX06 (WHO) M03BX04 (WHO)
PubChem CID 5511
UNII F5EOM0LD8E YesY
KEGG D08617 YesY
ChEMBL CHEMBL1076211 N
Chemical data
Formula C16H23NO
Molar mass 245.36 g/mol
 NYesY (what is this?)  (verify)

Tolperisone, a piperidine derivative, is a centrally acting muscle relaxant. Trade names include Biocalm, Muscodol, Mydeton, Mydocalm, Mydoflex, Myolax, Myoxan and Viveo.

Clinical use

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.[1][2]

Other possible uses include:

Contraindications and cautions

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.[1][2]

Side effects

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.[1][2] Allergic reactions occur in fewer than 0.1% of patient and include skin rash, hives, Quincke's edema, and in some cases anaphylactic shock.[1][3][4][5]

Overdose

Excitability has been noted after ingestion of high doses by children.[1] In suicide studies of three isolated cases, it is believed that ingestion of tolperisone was the cause of death.[6]

Interactions

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, benzodiazepines or non-steroidal anti-inflammatory drugs (NSAIDs) may make a dose reduction necessary in some patients.[1][2]

Mechanism of action

Tolperisone is a centrally acting muscle relaxant that acts at the reticular formation in the brain stem[1] by blocking voltage-gated sodium and calcium channels.[7][8]

Pharmacokinetics

Tolperisone is absorbed nearly completely from the gut and reaches its 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.[1]

See also

References

  1. 1 2 3 4 5 6 7 8 Jasek, W, ed. (2007). Austria-Codex (in German) (62nd ed.). Vienna: Österreichischer Apothekerverlag. pp. 5510–1. ISBN 978-3-85200-181-4.
  2. 1 2 3 4 "Midocalm". Romania: InfoMedic.
  3. ↑ Ribi C, Vermeulen C, Hauser C (2003). "Anaphylactic reactions to tolperisone (Mydocalm)". Swiss Medical Weekly 133 (25–26): 369–371. PMID 12947534.
  4. ↑ Kwaśniewski A, Korbuszewska-Gontarz B, Mika S (2003). "[Mydocalm causing anaphylaxis]". Pneumonologia i Alergologia Polska (in Polish) 71 (5–6): 250–2. PMID 14587432.
  5. ↑ Glück J, Rymarczyk B, Rogala B (2011). "An immediate hypersensitivity reaction caused by tolperisone hydrochloride". J Investig Allergol Clin Immunol 21 (5): 411–2. PMID 21905508.
  6. ↑ Sporkert, F.; Brunel, C.; Augsburger, M. P.; Mangin, P. (2012). "Fatal tolperisone poisoning: Autopsy and toxicology findings in three suicide cases". Forensic Science International 215 (1): 101–104. doi:10.1016/j.forsciint.2011.05.025. PMID 21683537.
  7. ↑ Kocsis P, Farkas S, Fodor L, Bielik N, Thán M, Kolok S, Gere A, Csejtei M, Tarnawa I (2005). "Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels". Journal of Pharmacology and Experimental Therapeutics 315 (3): 1237–1246. doi:10.1124/jpet.105.089805. PMID 16126840.
  8. ↑ Hofer D, Lohberger B, Steinecker B, Schmidt K, Quasthoff S, Schreibmayer W (2006). "A comparative study of the action of tolperisone on seven different voltage dependent sodium channel isoforms". European Journal of Pharmacology 538 (1–3): 5–14. doi:10.1016/j.ejphar.2006.03.034. PMID 16650844.


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