Key Features:
Muscle Relaxation: Tolrid Tablets harness the muscle relaxant properties of Tolperisone to effectively alleviate muscle stiffness and spasms. This makes it an ideal choice for individuals experiencing musculoskeletal discomfort due to various conditions.
Anti-Inflammatory Action: The inclusion of Diclofenac, a potent nonsteroidal anti-inflammatory drug (NSAID), ensures targeted relief from pain and inflammation. By inhibiting prostaglandin production, Diclofenac helps manage discomfort caused by inflammation, making Tolrid Tablets a valuable solution for conditions like arthritis and acute musculoskeletal injuries.
Comprehensive Relief: Tolrid Tablets offer a holistic approach to discomfort by addressing both the muscular and inflammatory components. This dual-action formula aims to enhance overall well-being and restore ease of movement.
Convenience: With a precise combination of Tolperisone and Diclofenac in each tablet, Tolrid simplifies your regimen, providing convenience without compromising on effectiveness. The tablets are easy to swallow, allowing for hassle-free integration into your daily routine.
Tolperisone –
1. Introduction
• Drug class: Centrally acting muscle relaxant
• Indication: Used mainly for muscle spasticity, muscle stiffness, and pain associated with neurological and musculoskeletal disorders.
• Structure: Tolperisone hydrochloride is a piperidine derivative, chemically related to lidocaine (local anesthetic).
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2. Pharmacological Actions
• Central Action:
• Inhibits voltage-gated sodium and calcium channels in neurons.
• Decreases excitability of spinal reflex arcs.
• Stabilizes neuronal membranes (like local anesthetics).
• Reduces mono- and polysynaptic reflex activity in the spinal cord.
• Peripheral Action:
• Mild vasodilatory effect (improves blood flow in muscles).
• Inhibits excessive muscle contractions without causing significant sedation (unlike benzodiazepines).
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3. Pharmacokinetics
• Absorption: Rapid but incomplete after oral administration (bioavailability ~17–20%).
• Metabolism: Extensively metabolized in the liver and kidneys.
• Excretion: Mainly via urine as metabolites.
• Half-life: ~2.5 hours.
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4. Indications
• Neurological conditions:
• Spasticity in stroke, multiple sclerosis, spinal cord injury.
• Orthopedic/Traumatic conditions:
• Muscle spasm after trauma, spondylosis, lumbar and cervical disc disease.
• Other uses:
• Adjunct therapy in vascular disorders (due to vasodilating effect).
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5. Dosage
• Usual adult dose: 150–450 mg/day, divided in 3 doses (e.g., 50–150 mg TDS after meals).
• Always titrated depending on tolerance and clinical response.
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6. Adverse Effects
• Common:
• Drowsiness, weakness, headache.
• GI upset (nausea, vomiting, abdominal pain).
• Rare but serious:
• Allergic reactions (rash, urticaria, anaphylaxis – especially in sensitive patients).
• Hypotension due to vasodilatory effect.
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7. Drug Interactions
• Caution with other CNS depressants (alcohol, benzodiazepines, opioids).
• CYP2D6/CYP2C19 substrates: May alter metabolism (though clinical significance is limited).
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8. Contraindications
• Hypersensitivity to Tolperisone.
• Severe hepatic or renal impairment.
• Myasthenia gravis.
• Not recommended in pregnancy & breastfeeding (insufficient safety data).
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9. Advantages
• Unlike benzodiazepines, minimal sedation.
• Better tolerated than other centrally acting relaxants.
• Improves muscle blood flow (vasodilation).
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10. Limitations
• Short half-life → frequent dosing needed.
• Variable absorption (food improves bioavailability).
• Reports of hypersensitivity reactions in some populations (particularly Europe, leading to restricted indications in some countries).
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11. Clinical Evidence
• Effective in post-stroke spasticity and lumbar/cervical spondylosis-related muscle spasms.
• Studies show improvement in muscle tone, pain relief, and mobility.
• Generally considered safe and effective when used appropriately.
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