 | |
 | |
| Clinical data | |
|---|---|
| Trade names | Mydocalm and others |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral,parenteral |
| ATC code | |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Metabolism | Liver, kidney |
| Eliminationhalf-life | 1st phase: 2 hrs 2nd phase: 12 hrs |
| Excretion | Renal |
| Identifiers | |
| |
| CAS Number |
|
| PubChemCID | |
| DrugBank |
|
| ChemSpider |
|
| UNII | |
| KEGG |
|
| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.010.889 |
| Chemical and physical data | |
| Formula | C16H23NO |
| Molar mass | 245.366 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
 N Y (what is this?) (verify) | |
Tolperisone (trade nameMydocalm among others) is a centrally actingskeletal muscle relaxant used for the treatment of increasedmuscle tone associated withneurological diseases. It has been used since the 1960s.[1][2]
Tolperisone is indicated for use in the treatment of pathologically increased tone of theskeletal muscle caused by neurological diseases (damage of thepyramidal tract,multiple sclerosis,myelopathy,encephalomyelitis) and ofspastic paralysis and otherencephalopathies manifested with muscular dystonia.[3][4]
Other possible uses include:[citation needed]
Manufacturers report that tolperisone should not be used in patients withmyasthenia 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.[3][4]
In 2012, following concerns about safety and efficacy, an "article 31 referral"[5] was triggered at theEuropean Medicines Agency (EMA). After the review and a subsequent re-examination, the Agency concluded that the benefits of tolperisone-containing medicines given orally continue to outweigh their risks. However, there is weak support for tolperisone's efficacy, specifically due to the prevalence of hypersensitivity symptoms such as flushing, rash, severe skin itchiness (with raised lumps), wheezing, difficulty breathing and swallowing, fast heartbeat, and fast decrease in blood pressure (basically anaphylaxis). The EMA recommends that tolperisone use be restricted to the treatment of adults with post-stroke spasticity (stiffness). The EMA also advises cessation of advertising, only using tolperisone orally, updating patient information leaflets, and changing to another medicine for existing users.[6]
Adverse effects occur in fewer than 1% of patients and include muscle weakness, headache, arterialhypotension, nausea, vomiting,dyspepsia, and dry mouth. All effects are reversible.[3][4] Allergic reactions occur in fewer than 0.1% of patient and include skin rash,hives,Quincke's edema, and in some casesanaphylactic shock.[3][7][8][9]
Excitability has been noted after ingestion of high doses by children.[3] In suicide studies of three isolated cases, it is believed that ingestion of tolperisone was the cause of death.[10]
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 ornonsteroidal anti-inflammatory drugs (NSAIDs) may make a dose reduction necessary in some patients.[3][4]
Tolperisone is a centrally acting skeletal muscle relaxant that acts at thereticular formation in thebrainstem[3] by blockingvoltage-gated sodium andcalcium channels.[11][12]
Tolperisone is absorbed nearly completely from the gut and reaches itspeak 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.[3]
Tolperisone is apiperidine derivative.
Tolperisone was developed in the 1960s in Hungary.[2]
Brand names include Biocalm, Miderizone, Mydeton, Mydocalm, Mydoflex, Myolax, Myoxan, Tolson, Topee, and Viveo.
Chemically related drugs with similarmechanism of action:
Muscle relaxants (drug class):