Tolperisone

Tolperisone

Clinical data
Trade names	Mydocalm and others
AHFS/Drugs.com	International Drug Names
Routes of administration	Oral, parenteral
ATC code	M02AX06 (WHO) M03BX04 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Metabolism	Liver, kidney
Elimination half-life	1st phase: 2 hrs 2nd phase: 12 hrs
Excretion	Renal
Identifiers
IUPAC name 2-methyl-1-(4-methylphenyl)-3-(1-piperidyl)propan-1-one
CAS Number	728-88-1 Y
PubChem CID	5511
UNII	F5EOM0LD8E
KEGG	D08617 Y
ChEMBL	ChEMBL1076211 N
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C16H23NO
Molar mass	245.36 g/mol
3D model (JSmol)	Interactive image
SMILES C1CCCN(C1)CC(C(C2=CC=C(C=C2)C)=O)C
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 N Key:FSKFPVLPFLJRQB-UHFFFAOYSA-N N
NY (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

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.

Other possible uses include:

• Spondylosis
• Spondylarthrosis
• Cervical and lumbar syndromes
• Arthrosis of the large joints
• Obliterating atherosclerosis of the extremity vessels
• Diabetic angiopathy
• Thromboangiitis obliterans
• Raynaud's syndrome

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.

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. Allergic reactions occur in fewer than 0.1% of patient and include skin rash, hives, Quincke's edema, and in some cases anaphylactic shock.

Overdose

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

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.

Mechanism of action

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

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.

See also

• Chemically and mechanistically related drugs: eperisone, inaperisone, lanperisone, silperisone