Baclofen (Baclophenum)

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

Means that affect neuromuscular transmission

Included in the formulation
  • Baclosan®
    pills inwards 
    Pharmaceutical factory "POLFARMA" JSC     Poland
  • Liorasal® Intrathecal
    Novartis Pharma AG     Switzerland
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

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

    Pharmacodynamics:

    This substance is an agonist GABABreceptors. Due to the activation of these receptors, inhibition of excitatory neurotransmitter release occurs (aspartate and glutamate) by neurons, as a result, the tone of skeletal muscles decreases.

    Pharmacokinetics:

    Adsorption in the gastrointestinal tract is high, the maximum concentration in the blood is achieved 2-3 hours after admission. Connection with plasma proteins - 30%. Metabolized in the liver, excretion of the kidneys mainly in an unchanged form. Half-Elimination (half-life) - 2-4 hours.

    Indications:

    Spastic conditions of skeletal muscles that accompany multiple sclerosis, head trauma, spinal diseases of degenerative, infectious, traumatic and tumor etiology, cerebral palsy, strokes. Alcoholism (affective disorders).

    ICD-10

    V.F10-F19.F10.2   Mental and behavioral disorders caused by alcohol use - addiction syndrome

    VI.G00-G09.G03.9   Meningitis, unspecified

    VI.G10-G13.G12.2   Disease of the motor neuron

    VI.G35-G37.G35   Multiple sclerosis

    VI.G80-G83.G80   Cerebral palsy

    VI.G80-G83.G83   Other paralytic syndromes

    VI.G90-G99.G93   Other brain damage

    VI.G90-G99.G95   Other diseases of the spinal cord

    VI.G90-G99.G95.0   Syringomyelia and syringobulbia

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

    IX.I60-I69.I64   Stroke not specified as a hemorrhage or infarction

    XVIII.R25-R29.R25.2   Cramp and spasm

    XIX.S00-S09   Head injuries

    XIX.T08-T14.T09.3   Trauma of spinal cord at unspecified level

    Contraindications:

    Epilepsy, mental disorders, Parkinson's disease, convulsions (in the anamnesis); xrenal diseases; hypersensitivity; pregnancy; lactation period.

    Carefully:

    Kidney diseases.

    Cerebrovascular insufficiency.

    Stomach ulcer or duodenal ulcer.

    Elderly or children's (under 12 years) age.

    Diabetes.

    Dysfunction of the liver. Patients with liver diseases should periodically monitor the level of hepatic transaminases, alkaline phosphatase.

    Pregnancy and lactation:

    Category Food and Drug Administration (US Food and Drug Administration) - C. Contraindicated in pregnancy. Penetrates into breast milk. For the duration of treatment, breastfeeding should be discontinued.Possible convulsive paroxysms in newborns, whose mothers during pregnancy took baclofen.

    Dosing and Administration:

    Orally, with food. Adults / children - 5 mg 3 times a day, followed by an increase in the dose every 3 days by 5 mg to achieve the effect (no more than 20-25 mg 3 times a day). The dose is raised until the appearance of a therapeutic effect (adults / children 6-10 years - 30-75 mg per day for adults, children 1-2 years - 10-20 mg per day, children 2-6 years - 20-30 mg per day) , the maximum daily dose of 100 mg. In chronic renal failure and hemodialysis, the daily dose is 5 mg. Cancel gradually (within 1-2 weeks).

    Side effects:

    From the digestive system: dry mouth, diarrhea, constipation, nausea, impaired liver function, aversion to food, perversion of taste, pain in the abdomen.

    From the nervous system and sensory organs: apathy, sleep disorder, confusion, nystagmus, tremor, depression, ataxia, there may be an increase in seizures and a decrease in the threshold of their occurrence, myalgia, hallucinations, fatigue, imbalance, accommodation disorder.

    From the cardiovascular system: decrease in blood pressure, palpitation, chest pain, collapse.

    From the genitourinary system: dysuria, enuresis, urinary retention; with prolonged use - a violation of kidney function.

    On the part of the respiratory system: sensation of stuffy nose and suffocation, respiratory depression.

    Other: muscular pain, hypersensitivity, skin rash, itching, swelling of the feet, sweating, weight gain, paradoxical reaction.

    Overdose:

    Nystagmus, muscle hypotension, vomiting, confusion, convulsions, strabismus, coma, respiratory depression, miosis, diplopia (after the return of consciousness, muscle hypotension may persist for 72 hours).

    Treatment - with respiratory depression - artificial ventilation of the lungs. In other cases, diuretics, copious drinking, induction of vomiting or gastric lavage, reception of activated charcoal, symptomatic and maintenance therapy (maintenance of cardiovascular activity). There is no specific antidote.

    Interaction:

    Lithium salts are hyperkinesis.

    Means that reduce the sugar content - an increase in the concentration of glucose in the blood.

    Lithium salts, muscle relaxants - a decrease in muscle tone.

    Levodopa / levodopa + carbidopa - hallucinations, agitation, confusion.

    With simultaneous application baclofen enhances the effect of antihypertensive drugs, ethanol.

    Tricyclic antidepressants increase the decrease in muscle tone.

    Special instructions:

    Side effects of the drug are contiguous with the symptoms of the disease, and therefore need close monitoring of the doctor when selecting a dose.

    In the treatment of patients with epilepsy, antiepileptic drugs are canceled.

    For the period of taking the drug should refrain from actions that require concentration of attention.

    In patients with liver diseases and diabetes mellitus, it is necessary to periodically monitor the activity of hepatic transaminases, alkaline phosphatase, blood glucose level.

    Cancel baclofen should be gradually (there may be hallucinations and exacerbation of spastic conditions). In case of symptoms such as chest pain, choking, collapse, hematuria, depression, confusion, hallucinations, skin rash, convulsions, visual impairment, significant reduction in muscle strength, vomiting, you should immediately consult a doctor.

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