Tolperisone

Centrally acting muscle relaxant

ATC code: M03BX04

Brand names: Mydocalm

Updated 24 Sep 2026 · Methodology

Indications

Muscle spasticity

Second line

Post-stroke spasticity in adults is the only indication the left tolperisone after its 2012 Article 31 review. The evidence base is modest: in the one study of acceptable quality the Ashworth score improved by 32% against 14% on placebo, with the effect stronger at 300–450 mg daily. The adult dose in the SmPC is 150–450 mg a day in three doses, taken after food because absorption falls on an empty stomach. Safety and efficacy in children are not established. In moderate renal or hepatic impairment the dose is titrated individually; in severe impairment the drug is not used. Work on post-stroke spasticity does not come down to a tablet: rehabilitation and positioning carry it, and focal spasticity is treated with botulinum toxin.

Sources

ICD-10: R25.2 · ICD-11: MB47.3

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

Acute painful muscle spasm

Not recommended

In Russia tolperisone is prescribed for painful muscle spasm in the back and neck, often alongside an NSAID, and it is registered for that. In the European Union the indication was removed: in 2012 the CHMP reviewed every tolperisone indication and kept only post-stroke spasticity in adults. The reason lies in data quality: studies from the 1960s and 1970s fall below today's standard, and the material on locomotor diseases, vascular diseases, rehabilitation after surgery and Little's disease was called limited and unconvincing. The second reason is safety: more than half of the spontaneous adverse reaction reports were hypersensitivity reactions, from skin rash to anaphylactic shock, while trials had shown almost none. Injectable forms were revoked across the EU. One practical point stands apart: the label states that tolperisone potentiates niflumic acid, and with concomitant use the dose of that or another NSAID is reduced. If tolperisone has been prescribed as a course for back pain, consider seeking a second opinion.

Sources

ICD-10: M62.8 · ICD-11: MB47.3

Peripheral artery disease

Not recommended

For decades tolperisone was prescribed in obliterative vascular disease: intermittent claudication, diabetic angiopathy, thromboangiitis obliterans, Raynaud's disease. The logic was to relieve vascular spasm. In the 2012 review the judged the data for these indications limited and unconvincing and removed the vascular indications from European labels, leaving only post-stroke spasticity in adults. Work on peripheral artery disease runs differently: stopping smoking, structured walking, control of blood pressure, lipids and glucose, an antiplatelet drug, and revascularisation in critical ischaemia. A muscle relaxant answers none of that, while the risk of hypersensitivity reactions stays. If tolperisone has been suggested for circulation, consider seeking a second opinion.

Sources

ICD-10: I73.9 · ICD-11: BD40

How to read tiers A–F

AStrong evidence – first or second line in international guidelines
BRecommended in selected cases
CStudy data contradict each other
DBenefit not proven, no documented harm
FDocumented harm, or risk without benefit

Mechanism of action

The exact mechanism of tolperisone is not established. It is thought to act in the brain and spinal cord, stabilising neuronal membranes and reducing the flow of impulses that keep muscle contracted and rigid. Structurally the molecule sits close to lidocaine, and that is more than theory: in a patient hypersensitive to lidocaine the label demands caution because of possible cross-reactions. Its sedative potential is low. The pharmacokinetic side matters more in prescribing: in a study with dextromethorphan tolperisone raised levels of drugs metabolised by CYP2D6, and its own bioavailability falls when taken on an empty stomach, so it is swallowed after meals.

Safety

Contraindications

Hypersensitivity to tolperisone or to the chemically similar eperisone, or to any excipient
Myasthenia gravis
Breastfeeding
Relative contraindication: pregnancy, especially the first trimester

Serious adverse effects

Anaphylactic reaction and anaphylactic shock
Angioedema with tachycardia, hypotension and dyspnoea
Cross-reactions in patients hypersensitive to lidocaine
Anaemia, lymphadenopathy
Seizure, confusion

Common adverse effects

Hypersensitivity reactions: erythema, rash, urticaria, pruritus
Headache, dizziness, somnolence, disturbance in attention
Nausea, abdominal pain, dry mouth, diarrhoea
Muscular weakness, low blood pressure, hyperhidrosis

Pregnancy: can you take Tolperisone?

Animal studies found no teratogenic effect of tolperisone, and human clinical data are missing. The European label rules out use in pregnancy, especially in the first trimester, unless the expected benefit clearly outweighs the possible risk to the fetus. In practice that means tolperisone is not the choice for back pain in a pregnant woman: the indication it is most often prescribed for has already been removed in the European Union.

Breastfeeding: can you take Tolperisone?

Whether tolperisone passes into human breast milk is unknown, so the European label lists breastfeeding among the contraindications.

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Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

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Frequently asked

What is Tolperisone used for?

Tolperisone is evaluated for the following indications with varying evidence strength: Muscle spasticity (evidence tier B), Acute painful muscle spasm (evidence tier D), Peripheral artery disease (evidence tier F). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Tolperisone?

Common side effects of Tolperisone (≥ 1 in 100): Hypersensitivity reactions: erythema, rash, urticaria, pruritus, Headache, dizziness, somnolence, disturbance in attention, Nausea, abdominal pain, dry mouth, diarrhoea, Muscular weakness, low blood pressure, hyperhidrosis. See the Safety section for uncommon and serious reactions.

Is Tolperisone safe during pregnancy?

Is Tolperisone compatible with breastfeeding?

Whether tolperisone passes into human breast milk is unknown, so the European label lists breastfeeding among the contraindications.

Who should not take Tolperisone?

Tolperisone is contraindicated in: Hypersensitivity to tolperisone or to the chemically similar eperisone, or to any excipient; Myasthenia gravis; Breastfeeding; Relative contraindication: pregnancy, especially the first trimester. Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

GRLS

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