Last Updated on March 16, 2024
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Baclofen
The active ingredient Baclofen is one of the most important drugs in increased skeletal muscle tension (spasticity). It was made in 1962 for the first time and is now included in many medications. He is generally well tolerated, can lead to fatigue and gastrointestinal symptoms in rare cases, however. Children and pregnant women should take Baclofen only after consultation with the doctor. Here you can read everything about Baclofen.
How Baclofen works
The human skeletal muscle is activated or inhibited by certain chemical messengers (neurotransmitters). Normally, these messengers are released according to the external circumstances. A specific chemical messenger, called gamma-aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the central nervous system (brain and spinal cord). GABA provides inter alia for sleep and muscle relaxation and suppresses muscle spasms.
In diseases or injuries of the nervous system that controlled balance is disturbed and GABA sometimes not sufficiently effective. The result: The nervous system is hyperexcitable, and there may be multiple sclerosis and spasticity (unnatural, resistant strain of the muscles)
The active ingredient Baclofen engages a particular docking site of GABA at (GABA B receptor) and mimics the effect. This receptor is specifically responsible for muscle tension. So there is a relaxation of the affected muscles, and spasticity is alleviated.
Pharmacokinetics and metabolism of Baclofen
The active ingredient Baclofen is rapidly and almost completely absorbed from the intestine into the blood. However, the amount of Baclofen, reaches the actual site of action (central nervous system), relatively low. For very severe spasticity of the drug is therefore (fluid in the brain) is introduced directly into the cerebrospinal fluid, thus high concentrations can be achieved at the site.
The active substance is excreted unchanged by the kidneys.
When is Baclofen used?
Among the areas of application (indications) of Baclofen include:
- spasticity of the skeletal muscles through
- spasticity of skeletal muscle due to injury or disease of the spinal cord
- spasticity of skeletal muscle due to injury or dysfunction of the brain
How Baclofen is used
Normally occupied Baclofen in the form of tablets. For better tolerability of the drug should be taken with a meal. In case of severe symptoms Baclofen can also be introduced as an infusion directly into the cerebrospinal fluid of the brain.
The Baclofen dosage in adults is a maximum of 75 milligrams daily (rarely up to 120 milligrams). This amount should be achieved by slowly increasing the dose, whereby an individual dose must be found for each treated. It usually starts with five milligrams three times a day and then increasing the dose until the symptoms have improved significantly.
Children and young people receive a reduced dose.
Normally it is in the treatment with the drug Baclofen to a long-term treatment. The discontinuation of the drug must be “tapered off”. This means that you have to reduce the dose over a period of about two to three weeks gradually.
What are the side effects Baclofen?
Especially at the beginning of treatment may cause side effects such as Baclofen gastrointestinal problems, fatigue or drowsiness (daytime).
Sometimes, ie in less than one percent of those treated, it may lead to, among other things, and tremors.
What should I watch for while taking Baclofen?
The drug should be used with caution when the patient is suffering from renal impairment, severe mental illness or acute confusion states. This is especially true if a poisoning with alcohol or sleeping pills is present.
Contraindications
medication Baclofen may not be applied when the treated suffers from epilepsy () or severe renal impairment.
Interaction
Baclofen and other centrally acting Substanten (such as alcohol, sleeping pills, antidepressants or strong painkillers) can be mutually reinforcing in their effects and side effects.
The drug Baclofen may increase the effect of blood pressure-lowering drugs, which is why a dose adjustment may be necessary.
Driving and using machines
Since Baclofen can affect the ability to react, should in particular be dispensed at baseline to an active participation in traffic and operating heavy machinery. This is especially true with simultaneous consumption of alcohol.
Parental
The drug Baclofen can also be used in children under strict medical supervision.
Pregnancy and lactation
The scope of experience on the use of Baclofen in pregnancy and lactation is very low. Two cases of use in pregnancy are known. It came in at the newborn to severe withdrawal symptoms and a baby to epileptic seizures.
In case of doubt, the treating physician should decide whether the individual benefits of treatment outweigh the risks.
Even during lactation should be a strict benefit-risk assessment. Experts suggest that Baclofen passes into breast milk. The consequences for the infant are unknown.
A better proven alternative in pregnancy and lactation is the active substance is acting temporarily eases tensions in low doses.
How to get Baclofen
medication Baclofen are only available on prescription, since the care of patients with multiple sclerosis and spasticity is very important, including a regular therapy success monitoring. You get such drugs therefore in the pharmacy with a prescription from a doctor.
Since when Baclofen is known?
The drug Baclofen was synthesized in 1962 for the first time and initially used to treat seizure disorders (epilepsy) used. Also an analgesic effect was said the drug.
It was not until ten years later (1972) was recognized its good effect in multiple sclerosis and spasticity, which are based on spinal cord and brain injuries. Meanwhile, Baclofen only applied to this area.