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Last Updated on February 19, 2017 by Dr.Derek Fhisher

Most popular brand: Lioresal
Active ingredient: Baclofen
Available dosage forms: 10, 25 mg

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Baclofen (Baclofen): instruction, and the use of a formula

Code CAS

Feature substance Baclofen

Muscle relaxants centrally acting.

A white or almost white crystalline powder, almost odorless. It is soluble in water, very little ; in methanol, and insoluble in chloroform.

Pharmacology

Mode of action -. Muscle relaxant, antispastic

It stimulates GABA _B – receptors, reduces the excitability of the terminal parts of afferent sensory fibers, inhibits the mono – and polisinapticheskie spinal reflexes, which leads to a decrease in muscle tension and analgesic effect.

When ingestion rapidly and almost completely absorbed from the gastrointestinal tract. C _max is achieved through a 2 – 3 hours Protein binding .; thirty%. It passes through the placental barrier, enters the breast milk. Approximately 15% biotransformed in the liver by deamination. T _1/2 ; 2,5 –. 4 hours Report mostly kidneys (70 – 80%) in unchanged form and as metabolites.

Application of the substance Baclofen

Inside: spasticity in multiple sclerosis, tumors and spinal cord diseases of infectious, degenerative and traumatic genesis (including syringomyelia, motor neuron disease, trauma), stroke, cerebral palsy, meningitis, head injury. alcoholism.

Intrathecal: severe chronic spasticity with spinal lesions (eg, due to trauma, multiple sclerosis), or brain inefficiency or intolerance with muscle relaxants therapy for oral.

Contraindications

Hypersensitivity, epilepsy, convulsions (in history), Parkinson’s disease, psychosis, chronic renal failure, pregnancy, lactation.

Restrictions on the use

Cerebrovascular insufficiency, cerebral atherosclerosis, gastric ulcer and duodenal ulcer, advanced age, children’s age (12 years).

Application of pregnancy and breastfeeding

is contraindicated in pregnancy.

Category effects on the fetus by FDA ;. is not defined

breast-feeding should be discontinued at the time of treatment.

Side effects of substance Baclofen

From the nervous system and sensory organs: drowsiness, insomnia, dizziness, headache, weakness, fatigue, confusion, impaired balance, decrease the rate of reaction, mental stimulation, euphoria, hallucinations, depression, nightmares, convulsions, reduced seizure threshold.

From the cardio – vascular system and blood (blood, hemostasis): decrease in blood pressure. palpitations, chest pain, collapse.

From the digestive tract: aversion to food, dysgeusia, nausea, vomiting, constipation / diarrhea, dyspepsia, abdominal pain.

With the genitourinary system: dysuria, enuresis, urinary retention; long-term use ; impairment of renal function.

From the respiratory system: sensation of nasal congestion and choking, respiratory depression.

Other: muscle pain, skin rash, itching, swelling of the feet, sweating, increased body mass index, a paradoxical reaction.

Interaction

With simultaneous use of baclofen increases the effects of antihypertensive drugs, ethanol.

Tricyclic antidepressants increase the decreased muscle tone. Levodopa and carbidopa increase the risk of hallucinations, confusion, agitation.

Overdose

Symptoms: vomiting, hypotonia, respiratory depression, convulsions, coma (after the return of consciousness muscular hypotonia may persist for 72 hours).

Treatment: induction of vomiting or gastric lavage, activated charcoal, symptomatic and supportive therapy (mechanical ventilation to maintain cardio – vascular activity.). There is no specific antidote.

Dosing and Administration

Inside, intrathecally. The mode set individually. Inside, the initial dose of ; 5 mg 3 times a day, then increase the dose every 3 days until optimal therapeutic effect (typically up to 30 – 75 mg / day). Patients over 65 years of age the dose should be increased with caution due to the increased risk of side effects. The maximum daily dose of ; 100 mg. The dose for children is set depending on the age and body weight.

Precautions Baclofen substances

In patients with liver disease and diabetes should periodically monitor the activity of liver transaminases, alkaline phosphatase. blood glucose levels.

To cancel baclofen should be gradually (may cause hallucinations and worsening spastic states). In the case of symptoms like chest pain, choking, collapse, hematuria, depression, confusion, hallucinations, skin rashes, seizures, blurred vision, a significant reduction in muscle strength, vomiting should immediately consult a doctor.

It should not be used during the drivers of vehicles and people skills relate to the high concentration of attention.

Trading names of drugs with working substance