Tolperisone is an oral centrally acting muscle relaxant. Tolperisone is a centrally acting muscle relaxant that has been used for the symptomatic treatment of spasticity and muscle spasm . Its precise mechanism is not completely understood, though it blocks sodium and calcium channels. It possesses a high affinity for nervous system tissue, reaching highest concentrations in brain stem, spinal cord and peripheral nerves. Based on existing clinical data, Tolperisone is not sedating and does not interact with alcohol.
Voltage-gated Na+ channels (VGSC, Na) are critically important for electrogenesis and nerve impulse conduction. Certain Na+ channel isoforms are predominantly expressed in peripheral sensory neurons associated with pain sensation, and the expression and functional properties of Na in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation.
Mechanism of Action of Tolperisone
Being, centrally acting muscle relaxant, tolperisone acts at the level of spinal cord by blocking sodium channels and calcium channels. Tolperisone exerts its spinal reflex inhibitory action predominantly via a pre synaptic inhibition of the transmitter release from the primary afferent endings via a combined action on voltage-gated sodium and calcium channels.
Tolperisone increases the blood supply to skeletal muscles; this action is noteworthy since a muscle contracture may compress the small blood vessels and induce an ischemia leading to release of pain stimulating compounds.Tolperisone causes preferential antinociceptive activity against thermal stimulation that is likely to be attributed to its local anesthetic action.Tolperisone causes muscle relaxation by its action on central nervous system. It also leads to membrane stabilization & has analgesic activity. This muscle relaxation is dose dependant.
A heterogeneous group of drugs used to produce muscle relaxation, excepting the neuromuscular blocking agents. They have their primary clinical and therapeutic uses in the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. They have been used also for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in MULTIPLE SCLEROSIS.
Indications of Tolperisone
Tolperisone is indicated for use in the treatment of pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the pyramidal tract, multiple sclerosis, myelopathy, encephalomyelitis) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.
Other possible uses include
- Cervical and lumbar syndromes
- Arthrosis of the large joints
- Obliterating atherosclerosis of the extremity vessels
- Diabetic angiopathy
- Thromboangiitis obliterans
- Raynaud’s syndrome
- Low back pain syndrome6
- Painful reflex muscle spasm
- Post-cerebral stroke spasticity
- Rehabilitation programmes
- Muscle spasm,spasticity due to scliosis.
- Parkinson’s disease
- Paresthesia, muscle pain, coordination disorder, tremor, rigidity, dystonia, ataxia, nystagmus, strabismus, dysarthria, epileptic seizure
Contra indications of Tolperisone
Use in children
- History of allerg
- Renal impairement
- Liver didease
Dosage of Tolperisone
Tolperisone (HCl)’s dosage details are as follows
|100 mg||100 (100)||12 hourly||IM|
|100 mg||100 (100)||24 hourly||IV|
|50 to 150 mg||100 (100)||8 hourly||PO|
Paedriatic Dosage (20kg)
|0.66 to 1.33 mg/kg||1 (0.995)||8 hourly||Oral||Dose for above 6 Yrs of children|
Neonatal Dosage (3kg)
|1.66 to 3.33 mg/kg||2.5 (2.495)||8 hourly||Oral|
Side Effects of Tolperisone
The Most common
- Loss of muscle coordination
- skin color change, mild diarrhea
- mild nausea
- loss of appetite
- vaginal discharge and itching
- swelling of feet or legs
- chest pain
- Frequently passing urine ,Excitement
- Visual disturbance
- diarrhea or loose stools
- difficulty with breathing
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- difficulty with moving
- headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- change in vision
- abnormal or fast heart rate
- weight loss
- chest pain or tightness
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- extra heartbeats
- mood or mental changes
- muscle pain or cramps
Drug Interactions of Tolperisone
Pregnancy & Lactation of Tolperisone
TGA pregnancy category C ,FDA Pregnancy Catagory N (unknown)
It is not known if tolperisone is safe and effective for use in pregnant women. Tell your doctor if you’re pregnant or plan to become pregnant. Tolperisone should be used during pregnancy only if the potential benefit justifies the potential risk.
Call your doctor right away if you become pregnant while taking this drug.
It isn’t known if tolperisone passes into breast milk. If it does, it may cause side effects in a child who is breastfed. Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication.