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Tolperisone Uses, Dosage, Side Effects, Interactions, Pregnancy

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.

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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

Investigated for use/treatment in neurologic disorders, spinal cord injuries, muscle spasm, back pain, and multiple sclerosis.
Symptomatic treatment of post-stroke spasticity in adults.
Spondylosis
Spondylarthrosis
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
Neurolathyrism
Trapezitis
Rehabilitation programmes
Periarthritis
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

Allergy
Myasthenia gravis
Use in children
Children
History of allerg
Hypersensitivity
Lactation
Pregnancy
Renal impairement
Liver didease

Dosage of Tolperisone

Tolperisone (HCl)’s dosage details are as follows

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
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

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Common

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

Rare

Anxiety
change in vision
seizures
abnormal or fast heart rate
tremors
weight loss
chest pain or tightness
confusion
cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps

Drug Interactions of Tolperisone

Allopurinol
Probenecid
Methocarbamol
Tetracyclines

Pregnancy & Lactation of Tolperisone

TGA pregnancy category C ,FDA Pregnancy Catagory N (unknown)

Pregnancy

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.

Lactation

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.

References