Baclofen

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The active ingredient baclofen is one of the most important drugs for increased skeletal muscle tension (spasticity). It was first produced in 1962 and is now included in numerous medicines. It is generally considered to be well tolerated, but in rare cases it can lead to tiredness and gastrointestinal complaints. Children and pregnant women should only take baclofen after consulting their doctor. Here you can read everything you need to know about baclofen.

This is how baclofen works

The human skeletal muscles are activated or inhibited by certain messenger substances (neurotransmitters). Normally, these messenger substances are released according to the external circumstances. A certain messenger substance, the so-called gamma-aminobutyric acid (GABA), is the most important inhibiting messenger substance in the central nervous system (brain and spinal cord). Among other things, GABA ensures sleep and relaxation of the muscles and suppresses muscle cramps.

In diseases or injuries to the nervous system, this controlled balance is disturbed and GABA is sometimes not sufficiently effective. The result: The nervous system is overexcitable, and multiple sclerosis and spasticity (unnatural, constant tension of the muscles) can occur.

The active ingredient baclofen attacks a specific GABA docking point (GABA-B receptor) and mimics its effect. This receptor is specifically responsible for muscle tension. The affected muscles relax and the spasticity is relieved.

Baclofen uptake, breakdown and excretion

The active ingredient baclofen is quickly and almost completely absorbed from the intestine into the blood. However, the amount of baclofen that reaches the actual site of action (central nervous system) is relatively small. In the case of very severe spasticity, the active ingredient is therefore introduced directly into the liquor (fluid in the brain) so that high concentrations can be achieved at the site of action.

The active ingredient is excreted unchanged through the kidneys.

When is baclofen used?

The areas of application (indications) for baclofen include:

• Skeletal muscle spasticity due to multiple sclerosis
• Skeletal muscle spasticity due to brain injury or dysfunction

This is how baclofen is used

Baclofen is usually taken in pill form. For better tolerability, the active ingredient should be taken with a meal. If symptoms are severe, baclofen can also be infused directly into the cerebrospinal fluid.

The maximum dose of baclofen in adults is 75 milligrams per day (rarely up to 120 milligrams). This amount should be achieved by slowly increasing the dose, whereby an individual dose must be found for each person treated. You usually start with five milligrams three times a day and then increase the dose until the symptoms have improved significantly.

Children and adolescents receive a reduced dose.

Treatment with the active ingredient baclofen is usually a long-term treatment. The drug must be discontinued "gradually". This means that you have to gradually reduce the dose over a period of about two to three weeks.

What are the side effects of baclofen?

Baclofen can cause side effects such as gastrointestinal problems, tiredness or drowsiness (during the day), especially at the beginning of treatment.

Occasionally, that is, less than one percent of those treated, may experience dry mouth, visual disturbances, headaches and tremors, among other things.

What should be considered when taking baclofen?

The active ingredient should only be used with caution if the patient suffers from impaired renal function, severe mental illness or acute states of confusion. This is especially true if there is poisoning with alcohol or sleeping pills.

Contraindications

Baclofen medication should not be used if the person being treated has convulsions (epilepsy) or severe kidney problems.

Interactions

Baclofen and other centrally active substances (such as alcohol, sleeping pills, anti-depression drugs or strong pain relievers) can mutually reinforce their effects and side effects.

The active substance baclofen can increase the effects of antihypertensive agents, which is why a dose adjustment may be necessary.

Driving and using machines

Since baclofen can impair the ability to react, active participation in road traffic and the use of heavy machinery should be avoided, especially when starting therapy. This is especially true when consuming alcohol at the same time.

Age restrictions

The active ingredient baclofen can also be used in children under strict medical supervision.

pregnancy and breast feeding period

There is very little experience with the use of baclofen during pregnancy and breastfeeding. Two cases of use in pregnancy are known. There were severe withdrawal symptoms in the newborn and epileptic seizures in one baby.

If in doubt, the attending physician should decide whether the individual benefit of the treatment outweighs the risk.

A strict risk-benefit analysis should also be carried out during breastfeeding. Experts suspect that baclofen passes into breast milk. The consequences for the infant are unknown.

The active ingredient diazepam is a better tried and tested alternative during pregnancy and breastfeeding.

How to get baclofen medication

Medicines containing baclofen require a prescription, as the care of patients with multiple sclerosis and spasticity, including regular monitoring of the success of the therapy, is very important. This is why you can only get such drugs in the pharmacy with a prescription from your doctor.

How long has baclofen been known?

The active ingredient baclofen was synthesized for the first time in 1962 and was initially used to treat convulsive disorders (epilepsy). The active ingredient was also said to have a pain-relieving effect.

It was not until ten years later that it was recognized that it was effective in treating multiple sclerosis and spasticity caused by injuries to the spinal cord and brain. Baclofen is now only used in this area.

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