Tolperisone is a centrally acting muscle relaxant used primarily for the symptomatic treatment of spasticity and muscle spasms associated with various neurological and musculoskeletal conditions. It is a piperidine derivative with a unique mechanism that differentiates it from other muscle relaxants. In the Indian context, it is widely prescribed for conditions like cervical spondylosis, low back pain, and post-stroke spasticity.
Adult: 50-150 mg three times daily (tid). The usual starting dose is 50 mg tid, which can be increased to 100 mg tid or 150 mg tid based on response and tolerability.
Note: To be taken orally with or after food to minimize gastrointestinal discomfort. Tablets should be swallowed whole with a glass of water. Do not crush or chew.
Tolperisone exerts its spasmolytic effect through multiple mechanisms. Its primary action is the blockade of voltage-gated sodium channels in the membranes of peripheral nerve fibers (both motor and sensory), leading to a reduction in the frequency and amplitude of action potentials. This stabilizes nerve membranes and reduces excessive neuronal firing that causes muscle spasticity and pain.
Pregnancy: Category C: Animal studies have shown teratogenic effects. There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Driving: May impair alertness, reaction time, and motor coordination. Patients should be cautioned against driving or operating machinery until their individual response is known.
| CYP2D6 Inhibitors (e.g., Fluoxetine, Paroxetine, Quinidine) | Increased tolperisone plasma levels, risk of toxicity (CNS depression, hypotension). | Major |
| CYP2C19 Inhibitors (e.g., Omeprazole, Fluconazole) | Potential increase in tolperisone levels. | Moderate |
| Other CNS Depressants (e.g., Alcohol, Benzodiazepines, Opioids, Baclofen) | Additive sedative effects, impaired alertness and coordination. | Major |
| Antihypertensives | Potentiated hypotensive effect. | Moderate |
| Levodopa | Theoretical antagonism of effect; use with caution in Parkinsonism. | Moderate |
Same composition (Tolperisone (50mg)), different brands: