Tolperisone: A Typical Representative of a Class of Centrally Acting Muscle Relaxants with Less Sedative Side Effects

Abstract

Tolperisone, a piperidine derivative, is assigned to the group of centrally acting muscle relaxants and has been in clinical use now for decades. The review summarizes the known pharmacokinetics, pharmacodynamics, toxicology and side effects in humans and the clinical use of tolperisone. A future perspective for further exploration of this drug is given.

Muscle relaxants as alternative analgesics in the treatment of nonspecific back pain

“…: была установ-лена эффективность препарата в отношении мышечного спазма, миотонии и заболеваний периферических артерий [30]. С этого времени появилось более 130 публикаций, по-священных исследованиям толперизона при различных за-болеваниях.…”

“…Но уже через несколько лет клинического применения появились публи-кации о краткосрочных и долгосрочных эффектах толпери-зона при ревматических, ортопедических, травматологиче-ских, неврологических заболеваниях (например, детском церебральном параличе, черепно-мозговой травме, инсуль-те, рассеянном склерозе и различных формах спинальной травмы). Между тем к этому времени было опубликовано только 7 РКИ [30].…”

Acute toxicity profile of tolperisone in overdose: Observational poison centre-based study

“…4 In clinical studies tolperisone was well tolerated with minor side effects including nausea, headache, and dizziness. 1,5 Nevertheless, anaphylactic reactions have been reported and the European Medicines Agency therefore recommended restricting the use of tolperisone for the treatment of adults with post-stroke spasticity. 6,7 Although being a centrally acting muscle relaxant, a sedating effect was not observed in therapeutic dose.…”

“…2 This piperidine derivative (1-piperidino-2-methyl-3-(p-tolyl)-propan-3-on) has been used for decades mainly in Europe and Asia for the treatment of muscle spasticity of neurological origin and muscle pain and muscle spasms due to rheumatologic conditions. 1 Tolperisone has also been proposed for the treatment of peripheral vascular disease. 3 The precise mechanism of the muscle relaxing effect of tolperisone is not fully understood.…”

“…Tolperisone is a centrally acting muscle relaxant 1 with an additional vasodilating effect. 2 This piperidine derivative (1-piperidino-2-methyl-3-(p-tolyl)-propan-3-on) has been used for decades mainly in Europe and Asia for the treatment of muscle spasticity of neurological origin and muscle pain and muscle spasms due to rheumatologic conditions.…”