TOLPIDOL 150

Indications

• Muscle spasms
• Spasticity associated with neurological conditions
• Musculoskeletal pain

Dosage

Children: Refer to the BNF for Children for specific dosing information.

Adults: Refer to the BNF for specific dosing information.

Mechanism of action

Tolperisone is believed to exert its muscle relaxant effects through the inhibition of presynaptic release of excitatory neurotransmitters, leading to a reduction in skeletal muscle tone. It also acts on voltage-gated sodium channels and may have some effects on calcium channels, contributing to its muscle relaxant properties.

Pharmacodynamics

Tolperisone demonstrates muscle relaxant effects without significant sedation. It works by modulating the activity of spinal reflexes responsible for muscle contraction. This results in a decrease in muscle spasticity and rigidity, improving overall muscle function and comfort in patients with conditions that cause muscle hyperactivity.

Pharmacokinetics

Tolperisone is well absorbed after oral administration, with peak plasma concentrations typically occurring within 1 to 2 hours. It undergoes extensive hepatic metabolism, primarily through cytochrome P450 enzymes. The elimination half-life ranges from 4 to 8 hours, and it is excreted mainly in urine. The pharmacokinetics may be influenced by factors such as liver function and age.

Contra-indications

• Myasthenia gravis
• Severe hepatic impairment
• Hypersensitivity to tolperisone or any of the excipients

Adverse effects

• Drowsiness
• Nausea
• Vomiting
• Diarrhea
• Rash
• Hypotension
• Allergic reactions

Interactions

• Caution when used with other CNS depressants, such as alcohol, benzodiazepines, and opioids, as these may enhance the sedative effects of tolperisone
• May interact with antihypertensive agents, potentially leading to increased hypotensive effects

Precautions

• Use with caution in patients with a history of seizure disorders
• Monitor for signs of respiratory depression, especially in patients with pre-existing respiratory conditions
• Caution in elderly patients, who may be more sensitive to the effects of tolperisone

Pregnancy

Safety during pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Tolperisone is excreted in breast milk. Caution is advised when administering to breastfeeding women.

Storage

Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.

Formulations

• Tolperisone hydrochloride tablet
• Tolperisone hydrochloride solution for injection