How not to turn Baclosan from an effective muscle relaxant into a heavy drug?

Baclosan is a central muscle relaxant that acts on the neuromuscular transmission.

Is a derivative of gamma-aminobutyric acid. The medicine belongs to the group of medicines that have anti-inflammatory, myorelaxing and analgesic effects.

Form and Composition

The drug contains active substance Baclofen( 10 or 25 mg) and impurity elements in the form of potato starch, lactose, magnesium stearate, talka, ethyl cellulose and gelatin. Miorelaxant is made in the form of round biconvex tablets of white color.

For sale in polypropylene jars and cardboard packs of 50 pcs.

Formula Baclofen

Pharmacological profile

Exposure to the active component causes a decrease in the excitability of skeletal muscles and motor motility. The main active substance blocks the migration of nerve impulses and causes relaxation of the strained muscles due to:

• lowering the excitability of susceptible fibers of the limbs;
• inhibition of intermediate neurons.

It is believed that due to the blocking of mono- and polysynaptic reflexes, the level of excretion of generating amino acids( aspartate and glutamate) decreases.

This is due to the activation of presynaptic GABA receptors. Most often, the drug is used for neurological diseases, which are accompanied by pain in the muscles and cramps. The active substance is capable of drowning spinal and visceral reflexes and has analgesic effect.

All components of the drug are very well absorbed in the gastrointestinal tract. The active substance of the drug is able to pass through the placenta and is excreted in breast milk.

The highest saturation of muscle relaxant in the body is observed after two to three hours after administration. The ability to switch to plasma proteins is rather small - 30%.The process of metabolism takes place in the liver. Basically, metabolic products are excreted by the kidneys in an unconverted form.

The acceptable dosage is 80 -395 ng / ml. The limiting concentration of active substances is maintained in the plasma in an amount of 200 ng / ml for 8 hours.

About fifteen percent of the medication taken is subjected to a process of metabolism in the liver by deamination. The half-life is on average three to four hours. About 75-80% of the drug leaves with urine, 25-30% of the drug is excreted with feces. Complete elimination from the body occurs 72 hours after ingestion.

Mechanism of action

The mechanism of action of Baclosan tablets is to reduce the expansivity of the terminal sections of the supporting fibers and inhibit the intermediate neurons.

The active component of the drug is also capable of reducing the previous titanus of myothenic spindles. The migration of neuromuscular impulses is not disturbed.

Thus, the pain is reduced and all the spasmodic and convulsive symptoms are eliminated.

Indications and contraindications for the use of

Indications for the use of Baclosan tablets are very extensive:

• spinal cord diseases caused by injuries and infections;
• stroke;
• therapy for multiple sclerosis;
• cerebral palsy;
• myelitis, spinal cord tumors, syringomyelia, meningomyelitis and motor motoneuron disease;
• meningitis and previously suffered craniocerebral trauma;
• alcoholism and emotional distress;
• presence of cerebrovascular diseases. Contraindications to prescription:
  • presence of Parkinson's disease;
  • is nervousness and epilepsy;
  • intermittent convulsions;
  • Renal deficiency in lingering form;
  • acute susceptibility to the active substance of the drug;
  • pregnancy and the period of breastfeeding.
  For children under twelve years old and elderly patients, this muscle relaxant can be used only in special cases. With special attention the medicine is prescribed in the presence of cerebrovascular deficiency, atherosclerosis of cerebral vessels. The same is true for patients who have pitting disease of the stomach and duodenum.

  Instructions for Use

  Baclosan tablets are prescribed for internal use. You need to take medicine while eating. The initial dose of medication for adults is five milligrams. The frequency of use is three times a day.

  After each three days, it is necessary to increase the dose of the drug so that the total dosage for the whole day is from 30 to 75 mg. The amount of the drug should be increased until the time when there is a pronounced therapeutic effect.

  In any case, before starting the use of a drug it is worth consulting with your doctor.

  If you need to take the medicine in large doses( from 75 to 100 mg), tablets are prescribed with a dosage of 25 mg. The maximum daily dose of the drug should not be more than 100 mg.

  When taking medication in children, it is necessary to be extremely cautious. The dose should be started at a dose of 5 mg. This is half a tablet with a dosage of 10 mg. The frequency of admission for children, as for adults, is three times a day, during meals.

  If it is necessary to increase the amount of the drug taken, this should be done with a gradation increase. It is worth noting that the greatest amount of medication for children can be different, depending on the weight of the child and his age.

  The norms of the maximum permissible amount of medication taken for children are as follows:

  • from 12 months to 2 years - 10-20 mg per day;
  • from two to six years - 30 mg per day;
  • from six to ten years - 30-55 mg;
  • for children over 10 years of age, a dose of 2 mg per kg of body weight is prescribed.

  Cases of overdose

  Overdose with tablets Baclosan manifests itself with the following symptoms:

  1. Muscular hypotension .Since the therapeutic effect when taking the drug is designed to stabilize muscle tension, reception of a significant amount of medication leads to hypotension.
  2. Consciousness Disorders .It is manifested by the distortion of orientation in space and the violation of the functioning of the limbs. It is also possible to lower mental processes and poor understanding of what is happening.
  3. Backbone of respiratory deficiency .This is the most extreme case, in which a fatal outcome often occurs. With poor ventilation, the body is saturated with a small amount of oxygen, which increases the amount of carbon dioxide in the blood. Oppressed breathing causes a panic state, at which the respiratory process stops, which can lead to death.

  To date, a medicinal antidote has not been developed that could immediately stabilize the patient's condition. But for rescue of the patient a number of other actions are provided.

  First of all, you need to drink plenty of water. Also, it is necessary to induce vomiting( in case the overdose stage is initial).This is possible when taking a weak solution of potassium permanganate or warm salted water. In addition, the patient must take sorbents, which will help to remove toxins from the body.

  Adverse reactions

  Adverse reactions are manifested by vomiting, nausea, constipation, diarrhea, seizures, muscle weakness and acute asthenia. Also, dry mouth, urination, depression and apathy occur. With prolonged use of Baklosan, the manifestation of improper functioning of the kidneys is possible.

  When taking an increased drug dose of Baklosan, it is possible to develop a narcotic effect. At the same time there is a surge of strength, an increase in general tone, endurance and efficiency.

  Baclofen can not be combined with amphetamine, as this leads to increased euphoric sensations and prolongation of the drug effect.

  With the withdrawal of the drug, severe abstinence is possible, so the instruction for use for each patient should be made only by the attending physician.

  Special instructions

  With special precaution, the drug is prescribed in childhood( up to twelve years).The medication is contraindicated for use during the period of gestation and during breastfeeding.

  With prolonged renal deficiency, Baclosan is strictly contraindicated. If the liver is disturbed during the administration of the drug, continuous monitoring of liver transaminases should be carried out.

  During the course of treatment, alcohol intake is strictly contraindicated.

  Drug Interaction

  When combined with medications that affect the central nervous system, the activity of the latter is enhanced. Parallel reception with tricyclic antidepressants promotes regress of muscular tone.

  Synchronous reception of Baklosan and Carbidopa causes hallucinations and mixed consciousness.

  Practical experience of using

  The opinion of doctors and reviews of patients with multiple sclerosis who took the medicine Baclossan.

  Because of the likelihood of a narcotic effect, I prescribe this medicine only in rare cases. Of those patients who took it, the treatment course was normal, no side effects were reported.

  Oleg Dmitrievich, doctor neurologist

  This is a rather dangerous drug, I do not understand why it is in pharmacies in free access. I had to treat some patients whose drug addiction began precisely because of Baclosan.

  Irina Lvovna, narcologist

  Took this drug not as a drug, but as a narcotic. The dependence was specific. Three times a day for 75 mg caused me euphoria. I stopped taking it with difficulty.

  Valery, 37

  My grandfather prescribed this medication, as he was diagnosed with multiple sclerosis. I can not say that it was easier for him, he was constantly irritated and capricious. We switched to another drug.

  Inga, 24

  I have multiple sclerosis, I was appointed Baklosan. It was possible to stop the main symptomatology, but some manifestations of the disease still remained.

  Irina, 41

  I also took this medicine for multiple sclerosis. A little helped, but there was some dependence. Sometimes the symptoms of my illness were also accompanied by panic attacks. The dosage was not large( 85 mg).

  Andrey, 53

  According to patients' reviews and medical experience, it is clear that Baclosan is a dangerous medication that contributes to drug addiction. Take this medication with extreme caution and with strict adherence to the dosing regimen.
  

  Purchase and storage of

  Baclosan is available in the form of tablets, the average price of which is 250-270 rubles per package.

  The drug should be stored in a dark place at a temperature of no more than 25 degrees. The usefulness of the drug is three years. The medicine is released in pharmacies strictly according to the doctor's prescription.

  Analogs that can replace Baclosan:

  • Tolperisone( tablets 50 mg);
  • Tizalud( tablets 4 mg);
  • Mydocalm( tablets 50 mg;
  • Liorasal( ampoules 50 mg).