Tizanidine (Tizanidinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Alpha-adrenomimetics

Included in the formulation
  • Sirdalud®
    pills inwards 
    Novartis Pharma AG     Switzerland
  • Sirdalud® MR
    capsules inwards 
    Novartis Pharma AG     Switzerland
  • Tizalud
    pills inwards 
    VEROPHARM SA     Russia
  • Tizanidine
    pills inwards 
    Berezovsky Pharmaceutical Plant, ZAO     Russia
  • Tizanidine
    pills inwards 
    VERTEKS, AO     Russia
  • Tizanidine-Teva
    pills inwards 
    Teva Pharmaceutical Enterprises Co., Ltd.     Israel
  • Tizanil®
    pills inwards 
    Simpex Pharma Pvt Ltd.     India
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    ONLS

    VED

    АТХ:

    M.03.B.X   Other muscle relaxants of central action

    M.03.B.X.02   Tizanidine

    Pharmacodynamics:

    By stimulating α2receptors inhibits the release of amino acids that stimulate the N-methyl-D-aspartate receptors in the spinal cord, thereby suppressing the postsynaptic mechanisms of interneuronal connections in the spinal cord, The hypertonicity of the transverse striated muscles.

    Reduces muscular resistance in passive movements, suppresses clonic convulsions, strengthens arbitrary muscle contractions.

    Pharmacokinetics:

    After oral administration, it is completely absorbed in the gastrointestinal tract, but due to rapid metabolism during primary passage in the liver, the bioavailability of the drug is no more than 34%. The maximum concentration in blood plasma is achieved after 1 hour.The connection with plasma proteins is 30%.

    Metabolism in the liver to inactive metabolites.

    The half-life is 2-4 hours. Elimination by the kidneys.

    Indications:

    It is used to treat multiple sclerosis, chronic myelopathy, stroke, degenerative diseases of the spinal cord, with painful spasms of skeletal muscles due to osteochondrosis.

    ICD-10

    VI.G35-G37.G35   Multiple sclerosis

    VI.G80-G83.G82.4   Spasmodic tetraplegia

    VI.G80-G83.G82.1   Spastic paraplegia

    VI.G80-G83.G81   Hemiplegia

    VI.G90-G99.G95.9   Disease of spinal cord, unspecified

    XIII.M40-M43.M42   Osteocondritis of the spine

    Contraindications:

    Asthenic bulbar paralysis, individual intolerance.

    Carefully:

    Violations of the functions of the liver and kidneys.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside for 2-6 mg 3-4 times / day with a slow increase in the dose to 12-24 mg / day for 3-4 reception.

    The highest daily dose: 6 mg.

    The highest single dose: 36 mg.

    Side effects:

    Central and peripheral nervous system: insomnia, hallucinations, dizziness.

    The cardiovascular system: arterial hypotension, bradycardia.

    Digestive system: dry mouth, dyspeptic disorders.

    Musculoskeletal system: rarely - myasthenia gravis.

    Allergic reactions.

    Overdose:

    Vomiting, arterial hypotension, miosis, coma.

    Treatment is symptomatic.

    Interaction:

    Simultaneous use with antihypertensive agents increases the risk of bradycardia and arterial hypotension.

    Simultaneous use with CYP 1A2 inhibitors (ciprofloxacin, fluvoxamine) increases the risk of hypotension.

    Alcohol and drugs that depress the central nervous system and strengthen the sedative effect.

    Special instructions:

    Monitoring of the functional activity of the kidneys, the content of transaminases in the blood plasma.

    Persons receiving tizanidine, care should be taken when driving vehicles and working with moving machinery.

    Instructions
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