Each hard gelatin capsule contains: Eperisone Hydrochloride (as sustained release pellets) 150 mg, Excipients q.s.
Skelemus 150 SR capsules are advocated for skeletal muscle spasm associated with painful musculoskeletal disorders. The empirical formula of Eperisone hydrochloride is C17H26ClNO and its molecular weight is 295.85.
Excipients/Inactive Ingredients: Non Pareil seeds, Hypromellose BP, Citric acid monohydrate USP, Ethyl cellulose USP, Purified talc BP, Methyl Alcohol USP, Isopropyl alcohol BP, Purified water BP.
Pharmacology: Pharmacodynamics: Eperisone Hydrochloride acts by relaxing both skeletal muscles and vascular smooth muscles, and demonstrates a variety of effects such as reduction of myotonia, improvement of circulation, and suppression of the pain reflex. The drug inhibits the vicious cycle of myotonia by decreasing pain, ischemia, and hypertonia in skeletal muscles, thus alleviating stiffness and spasticity, and facilitating muscle movement. Eperisone Hydrochloride additionally possesses analgesic action at the level of spinal cord. Eperisone Hydrochloride also improves dizziness and tinnitus associated with cerebrovascular disorders or cervical spondylosis. When eperisone is advocated alone in the treatment of spastic paralysis in patients with cerebral apoplexy, it improves the cybex torque curve and electromyogram and facilitates voluntary movements such as flexion and extension of the extremities, without reducing the muscle force. Eperisone Hydrochloride causes muscle relaxation and analgesia by acting at the level of spinal cord; it depresses both monosynaptic and polysynaptic reflexes. It dilates the blood vessels due to calcium antagonistic action on the vascular smooth muscles and muscular sympatholytic actions.
Pharmacokinetics: Eperisone Hydrochloride is very well absorbed but the immediate release drug produces low and variable-plasma concentrations due to extensive first-pass metabolism in intestine. The minimum plasma levels demonstrating a myotonolytic effect are estimated to be 300 ng/ml. However, the muscle relaxant action may depend more on the concentrations achieved in target organs rather than the plasma levels per se. Eperisone Hydrochloride is metabolized to seven metabolites via oxidation and carbonyl reduction in human liver microsome. Among them, M3 and M4 are the primary major metabolites which are generated by CYPs. Eperisone is excreted in breast milk and in urine. The elimination half-life of eperisone is 1.6-1.8 hours.
Skelemus 150 SR capsules are indicated for improvement of myotonic conditions caused by the following diseases: neck-shoulder-arm syndrome, scapulohumeral periarthritis and low back pain.
Spastic paralysis caused by the following diseases: Cerebrovascular disorders, spastic spinal paralysis, cervical spondylosis, post-surgical sequelae (including cerebrospinal tumor), sequelae of trauma (spinal injury and head injury), amyotrophic lateral sclerosis, infantile cerebral palsy, spinocerebellar degeneration, spinal vascular disorders, subacute myelo-optico neuropathy (SMON) and other encephalomyopathies.
ADULTS: Skelemus 150 SR is recommended once daily.
Mode of Administration: The mode of administration is Oral.
Overdosage can cause seizures, ventricular tachycardia and coma have been reported in an infant.
Eperisone Hydrochloride Sustained Release capsules 150mg is contraindicated in patients with hypersensitivity to any of the ingredients. It is not advocated in small children below 18 months of age and during lactation.
Eperisone Hydrochloride Sustained Release capsules 150mg is contraindicated in patients with hypersensitivity to any of the ingredients. It is not advocated in small children below 18 months of age and during lactation. Eperisone Hydrochloride Sustained Release capsules 150mg should be administered with caution in acidpeptic disease, impaired renal or liver functions, blood dyscrasias, and hypersensitivity to aspirin or other nonsteroidal anti-inflammatory drugs (NSAIDs). Patients taking Eperisone Hydrochloride Sustained Release capsules 150mg should be cautioned against engaging in potentially hazardous activities requiring alertness eg, operating machinery or driving a car. Avoid alcoholic beverages whilst taking Eperisone Hydrochloride Sustained Release capsules 150mg.
Methocarbamol, aspirin, methotrexate, digoxin, cyclosporin, angiotensin converting enzyme (ACE) inhibitors, diuretics, lithium and warfarin are to be coadministered with due precaution with Eperisone Hydrochloride Sustained Release capsules 150mg.
Eperisone Hydrochloride Sustained Release capsules 150mg should be administered with caution in acid-peptic disease, impaired renal or liver functions, blood dyscrasias, and hypersensitivity to aspirin or other NSAIDs. Since weakness, lightheadedness, sleepiness or other symptoms may occur with Eperisone Hydrochloride, the patients should be cautioned against engaging in potentially hazardous activities requiring alertness eg, operating machinery or driving a car. Data on safety and efficacy of Eperisone Hydrochloride in children is not adequate. Lower dose of Eperisone Hydrochloride is advocated in the elderly. Avoid alcoholic beverages whilst taking Eperisone Hydrochloride Sustained Release capsules 150mg. It must be coadministered with methocarbamol with due precaution.
Methacarbamol, aspirin, methotrexate, digoxin, cyclosporin, angiotensin converting enzyme (ACE) inhibitors, diuretics, lithium and warfarin are to be coadministered with due precaution with Eperisone Hydrochloride Sustained Release capsules 150mg.
Effects on ability to drive and use machines: Patients taking Eperisone Hydrochloride Sustained Release capsules 150mg should be cautioned against engaging in potentially hazardous activities requiring alertness eg, operating machinery or driving a car.
Use in Children: Safety in children has not been established (insufficient clinical experience).
Eperisone Hydrochloride Sustained Release capsules 150mg should be used in pregnant women (C; eperisone, not known) only if absolutely required.
Eperisone Hydrochloride Sustained Release capsules 150mg can cause acute allergic reactions such as redness, itching, urticaria, edema of the face or other parts and dyspnea, etc.
Renal: Proteinuria, elevation of blood urea nitrogen (BUN).
Hematologic: Anemia.
Hypersensitivity: Rash, pruritus, erythema exudativum multiforme, oculo-mucocutaneous syndrome (Stevens Johnson Syndrome, Toxic Epidermal Necrolysis).
Psychoneurologic: Sleepiness, insomnia, headache, numbness in the extremities, stiffness and tremor in the extremities.
Gastrointestinal: Nausea, vomiting, anorexia, stomach discomfort, abdominal pain, diarrhea, constipation, thirst, stomatitis, feeling of enlarged abdomen.
Urinary: Urinary retention, urinary incontinence, feeling of residual urine.
General: Weakness, lightheadedness, generalized fatigue, muscle hypotonia, dizziness.
Others: Hot flushes, diaphoresis, edema.
Eperisone Hydrochloride Sustained Release capsules 150mg can cause disturbance of visual accommodation when coadministered with methocarbamol.
Protect from light & moisture.
Store below 25°C in a dry place.
Shelf Life: 24 Months.
M03BX09 - eperisone ; Belongs to the class of other centrally-acting muscle relaxants.
SR cap 150 mg (white to off white spherical to oval pellets filled in unprinted size '1' hard gelatin capsules with red opaque cap and yellow opaque body) x 3 x 5's.
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