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Baclofen is a muscle relaxant drug. Miorelaxant central action; agonist of GABA B receptors. Oppressing Mono-and polysynaptic reflexes, apparently due to the reduced allocation of excitatory amino acids (glutamate and aspartate) of cord that occurs as a result of stimulation of presinapticakih GABA-receptors. Does not affect the transmission of impulses in nerve-muscle synapses. Provides tone skeletal muscles. Provides moderate analgesic effect. Amid the drug improves mobility and functional activity of the patients.

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Pharmacokinetics.

After intake of baclofen rapidly and completely absorbed from the digestive tract. Therapeutic concentration is 80-395 ng/ml. C max is 500-600 ng/ml achieved through 2-3 h after administration of the drug, then the concentration of baclofen in the plasma is maintained at the level of 200 ng/ml within distribution of Linking blood plasma is about 30%. Baclofen penetrates through the placental barrier, out of breast milk.

Metabolism.

About 15% of the dose is metabolized in the liver by deamidization. Baclofen return with urine (70-80%) in unmodified form or in the form of metabolites, 20-30% return with faeces. After intake is completely eliminated from the body within 72 hours. lethargy skeletal muscles in multiple sclerosis; convulsive of brain diseases of different origin.

The dosage.

Set individually. Adults appoint drug in the initial dose of 5 mg 3 times per day; for each 4-day treatment of single dose of 5 mg (reception frequency 3 times/day) to the development of an optimal therapeutic effect. The maximum daily dose of 60-75 mg. Take medication while eating.

Side effect.

The central nervous system and peripheral nervous system: drowsiness, dizziness (especially at the beginning of treatment); rarely, lethargy, fatigue, sleep disturbance, depression. parestesia, ataxy, tremor, nystagmus, ccomodation violation; in some cases, convulsions (in predisposed patients).
on the part of the digestive system: nausea; Sometimes, dry mouth, constipation, diarrhea; in some cases, violations of the liver.
Cardiovascular system: arterial gipotenzia. Other: respiratory depression.

Contraindications.

  • Psychosis;
  • Parkinson’s disease;
  • Epilepsy;
  • Hypersensitivity to baklofen.

Pregnancy and lactation.

During pregnancy (especially in the first trimester), Baclofen can be used only for health reasons. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.Special instructions. Be wary drug in patients with gastric ulcers stomach and duodenal ulcers and those over 60 years old. Side effects are often transitory nature, may disappear or decrease with decreasing dose.
Influence on the ability to drive vehicles and management mechanisms. Patients receiving Baclofen should refrain from potentially dangerous activities related to attention and quick emotional reactions.

Drug interactions.

Together with the use of Baclofen enhances the effect of drugs that affect the CENTRAL NERVOUS SYSTEM, gipotenziveh funds. Together with the use of Baclofen with tricyclic antidepressants may have a significant reduction in muscle tone. In patients with Parkinson’s disease while appointing Baclofen with levodopa and karbidopoj may experience hallucinations, sputannosti consciousness, agitation. The drug should be stored in a dry, the dark place at a temperature of no higher than 25° c. Shelf life is 5 years.

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