Tolperisone

Tolperisone

Systematic (IUPAC) name
2-methyl-1-(4-methylphenyl)-3-(1-piperidyl)propan-1-one
Clinical data
AHFS/Drugs.com	International Drug Names
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	728-88-1 Y
ATC code	M03BX04
PubChem	CID 5511
UNII	F5EOM0LD8E Y
KEGG	D08617 Y
Chemical data
Formula	C16H23NO
Mol. mass	245.36 g/mol
SMILES	eMolecules & PubChem
Y(what is this?)  (verify)

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

Clinical use

Typically, tolperisone is indicated in the treatment of acute muscle spasms in back pain and spasticity in neurological diseases.

Manufacturer claims

Tolperisone is currently marketed in Europe as a centrally-acting muscle relaxant, which reportedly has special advantages over other drugs of its class, in that it reportedly does not cause drowsiness or lethargy, according to some manufacturers.^[1]

Besides claiming "tolperisone has an excellent efficacy and safety profile", these manufacturers also state^[1] tolperisone has the unique property of mediating muscle relaxation "without concomitant sedation" and it does not cause incoordination, weakness, mental confusion or withdrawal phenomena, in contrast to other muscle relaxants.

== Indications ==

Tolperisone is reportedly used in the typical treatment of the following conditions:

• Pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the pyramidal tract, multiple sclerosis, myelopathy, encephalomyelitis)
• Spastic paralysis and other encephalopathies manifested with muscular dystonia
• Spondylosis
• Spondylarthrosis
• Cervical and lumbar syndromes
• Arthrosis of the large joints
• Obliterating atherosclerosis of the extremity vessels
• Diabetic angiopathy
• Thromboangiitis obliterans
• Raynaud's syndrome'Bold text

Contraindications and cautions

Manufacturers report that tolperisone should not be used in the following conditions:

• Myasthenia
• Children under 1 years of age
• Pregnancy
• Breastfeeding

Side effects and adverse reactions

Some people using tolperisone have reported^[2] the following reactions:

• In hypersensitivity: muscle weakness, headache, arterial hypotension, nausea, vomiting, dyspepsia.
• Skin allergic reactions: skin rash, hives, Quincke's edema, anaphylactic shock.

The side effects and reactions listed above may not include all effects reported by the drug's manufacturer.

Interactions

Tolperisone is believed to have few interactions with other medicines, but this does not rule out any interactions that may not have been reported to caregivers thus far.

Some manufacturers have stated tolperisone may enhance the effects of other neuromuscular blocking agents.

Dosage

A blister package of Mydocalm 50mg tablets intended for distribution in the Slovak Republic

According to various sources, the typical oral adult dose for tolperisone is 150-450 mg in a 24-hour period, divided into two or three portions. It is highly advised that dosage information be confirmed by information provided from the manufacturer and prescriber.

More detailed dosage information^[3] is as follows:

Adults over 12 years old:

• Oral: 50-150 mg every 8 hours
• IM: 100 mg every 12 hours.
• IV: 100 mg over 24 hours.

Pediatric dosage (minimum weight of 20 kg, minimum age 6 years):

• Oral dosage: 1.0 mg/kg every 8 hours.

Neonatal dosage (minimum weight of 3 kg)

• 2.5 mg/kg every 8 hours.

Also see

• Tolperisone at Drug Info Systems (www.druginfosys.com)
• Papers and safety and efficacy studies of tolperisone at BioInfo
• Tolperisone at Sanochemia Austria

External links

• 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". Eur J Pharmacol 538 (1–3): 5–14. doi:10.1016/j.ejphar.2006.03.034. PMID 16650844. 
• 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". J Pharmacol Exp Ther 315 (3): 1237–46. doi:10.1124/jpet.105.089805. PMID 16126840. 
• Ribi C, Vermeulen C, Hauser C (2003). "Anaphylactic reactions to tolperisone (Mydocalm)". Swiss Med Wkly 133 (25–26): 369–71. PMID 12947534. 

Footnotes

1. ^ ^{a b} http://www.sanochemia.at/en/research-development/product-pipeline/tolperisone/#c1779
2. ^ http://www.drugs-pro.com/other/mydocalm.html
3. ^ http://www.druginfosys.com/Drug.aspx?drugCode=1078&drugName=Tolperisone%20(HCl)&type=9