Baclofene Drug Information [ Sanofi-Aventis ]

Table of content

Baclofene category:

• Human
• Gaba-Derivative Skeletal Muscle Relaxants
• Skeletal Muscle Relaxants

Active ingredients:

• Baclofen

Baclofene companies and manufacturers:

• Sanofi-Aventis

General Information

Baclofene forms, composition and dosages:

• Tablet; Oral; Baclofen 10 mg

Indications, usages and classification codes:

• M03BX01 - Baclofen

There is an additional general information about this medication active ingredient baclofen:

Pharmacological action

Baclofen is centrally acting muscle relaxant; GABA_B-receptor agonist. It depresses mono-and polysynaptic reflexes presumably by reducing the release of excitatory amino acids (glutamate and aspartate) from the terminals which occurs as a result of stimulation of presynaptic GABA-receptors. This medication does not affect the transmission of impulses in the nerve-muscle synapses; reduces skeletal muscle tone; has a moderate analgesic effect.

Pharmacokinetics

When administered orally baclofen is rapidly and completely absorbed from the gastrointestinal tract. C_max plasma levels achieved in 2-3 hours after administration. Plasma protein binding is about 30%. Baclofen crosses the placental barrier, excreted in breast milk; metabolized in the liver; excreted in the urine, mainly unchanged.

Why is Baclofene prescribed?

skeletal muscle spasticity in multiple sclerosis
spastic conditions of the spinal cord in diseases of infectious, degenerative, traumatic genesis
children cerebral palsy

Dosage and administration

For oral administration for adults at the beginning of treatment - 5 mg 3 times / day. For each 4-day treatment dose increased to 5 mg 3 times / day to the development of optimal therapeutic effect. Average daily dose is 30-75 mg, if necessary may increase up to 100-120 mg. The final daily dose is set individually so that together with the weakening of clonus and muscle spasms persisted muscle tone, which is sufficient for the implementation of active movements.
For patients with increased sensitivity to pharmaceutical drugs initial daily dose may be 5-10 mg, followed by a slower increase. For patients with renal insufficiency and during hemodialysis daily dose is 5 mg.
For children under 10 years daily dose is 0.75-2 mg / kg, over 10 years - 2.5 mg / kg. Treatment starts with a dose of 2.5 mg 4 times / day. Daily dose as for adults choose individually, increasing it every 3 days, in accordance with the clinical course of disease. Maintenance dose for children aged 1-2 years is 10-20 mg / day; for children aged 2-10 years - 30-60 mg / day.

Baclofene side effects

CNS and peripheral nervous system: drowsiness, dizziness (especially at the beginning of treatment); sometimes - apathy, fatigue, sleep disturbances, confusion; rarely - euphoria, depression, paresthesia, myalgia, muscle weakness, ataxia, tremor, nystagmus, accommodation disturbances, hallucinations; may be more frequent seizures and lowering the threshold of their appearance.
Digestive system: nausea, sometimes there are dry mouth, constipation, diarrhea, and in some cases - liver function abnormalities.
Cardiovascular system: sometimes - hypotension, deterioration of the cardiovascular system.
Other: sometimes - respiratory depression, rarely - dysuria, enuresis.
Side effects occur mainly at the beginning of treatment, with the rapid increase in dose, when administered a dose of 60 mg / day, as well as in elderly patients.

Contraindications

During pregnancy (especially in I trimester) baclofen can be used only for health reasons.

Special instructions

Selection of individual daily dose recommended in the hospital.
Side effects are often transient, may disappear or decrease at lower doses. The need to interrupt therapy is rare. Side effects of baclofen should be distinguished from symptoms of the disease which are treated. A cancellation of baclofen should be conducted gradually, reducing the dose for 1-2 weeks (except in cases of serious adverse events).
With careful use in cerebrovascular disorders, psychotic states, schizophrenia, stomach ulcers and duodenal ulcers, respiratory failure, violations of liver and kidney, as well as in elderly patients. If concomitant treatment of epilepsy should be under strict medical supervision and without interruption of adequate therapy by anticonvulsant drugs. Patients with dysuria after baclofen treatment can be observed hypertonicity of sphincter of the bladder and urine retention.
In patients with liver disease and diabetes should periodically monitor the level of hepatic transaminases, alkaline phosphatase and blood sugar.
During the treatment should refrain from potentially hazardous activities requiring increased attention and rapid psychomotor reactions.

Baclofene drug interactions

With the simultaneous application of baclofen increases the effects of antihypertensive drugs, ethanol.
In an application with tricyclic antidepressants can significantly decrease muscle tone.
There is a described case of toxic reactions caused by the action of baclofen (disturbance of consciousness, confusion, bradycardia, impaired visual acuity, hypotension, hypothermia) while using with ibuprofen in elderly patients with impaired renal function.
In an application with lithium therapy may be severe manifestations of hyperkinetic symptoms.
Patients suffering from Parkinson's disease while the application of baclofen with levodopa and carbidopa may have hallucinations, confusion, agitation.

Baclofene in case of emergency / overdose

Symptoms: vomiting, muscular hypotonia, drowsiness, impaired accommodation of the eye, coma, respiratory depression, convulsions.
Treatment: induction of vomiting or gastric lavage, taking activated charcoal, symptomatic and supportive therapy (mechanical ventilation, maintenance of cardiovascular activity). There is no specific antidote.

• Baclofene analogs
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