Clonazepam

Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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The active ingredient clonazepam is an antispasmodic and sedative from the benzodiazepine group. It is primarily used against seizures in epileptics, but like other benzodiazepines it also relieves anxiety and promotes sleep. Here you can read everything you need to know about the effects and use of clonazepam, interactions and side effects.

This is how clonazepam works

The nerve cells of the brain communicate with each other via messenger substances, so-called neurotransmitters. A nerve cell releases these exciting or inhibiting neurotransmitters at a contact point (synapse) and the downstream cell, which perceives the messenger substance via docking points (receptors), is subsequently excited or inhibited. Each nerve cell can only form and release one type of neurotransmitter.

One of the most important inhibiting messenger substances is GABA (gamma-aminobutyric acid). This neurotransmitter binds to GABA receptors, among other things. These can be influenced by many substances, for example unspecifically by alcohol or specifically by barbiturate sleeping pills such as phenobarbital. Benzodiazepines such as clonazepam also bind to the GABA receptor. They strengthen the effect of the naturally present GABA and are therefore suitable as sleeping pills, sedatives and antispasmodics.

Uptake, breakdown and excretion of clonazepam

After ingestion, the active ingredient enters the blood through the intestines, where it reaches the highest levels after one to four hours. Because of its fat solubility, it accumulates preferentially in the brain. In the liver, clonazepam is converted into ineffective breakdown products and then excreted mainly via the kidneys with the urine, and to a lesser extent also with the stool. After a day and a half, the level of clonazepam in the body has halved again.

When is clonazepam used?

In Germany, clonazepam is only approved for the treatment of various forms of epilepsy, both in adults and in children (including infants).

In other countries as well as in Germany “off-label” (outside of the areas of application approved here), clonazepam is also used to treat anxiety disorders, sleepwalking and movement disorders (restless legs syndrome, cramps in the masticatory muscles, unsteady sitting).

In general, benzodiazepines should not be taken for a longer period than a few weeks, because they are addictive and can lose their effectiveness over time (tolerance development). Long-term therapy with clonazepam may be necessary, especially in the case of severe epilepsy and other chronic diseases that cannot be treated sufficiently well with other active ingredients.

This is how clonazepam is used

Treatment with clonazepam should be started gradually:

Adults start with 0.5 milligrams of clonazepam twice daily; then the dosage is slowly increased over several weeks until the optimum effect is achieved. The total daily dose of eight milligrams - divided into three to four individual doses - should not be exceeded. It is taken independently of meals with sufficient liquid.

Younger patients receive a reduced dose. Children under six years of age and patients with swallowing disorders can also take clonazepam drops instead of the tablets.

As with other anti-convulsive drugs, treatment should not be stopped abruptly, as this could lead to seizures. To stop treatment, the dosage must be reduced gradually ("tapering off").

What are the side effects of clonazepam?

The side effects of clonazepam are comparable to those of other benzodiazepines: tiredness, sleepiness, fatigue, dizziness, light-headedness and weakness can often be expected - especially at the beginning of treatment and at higher doses.

Occasionally, clonazepam side effects such as a decrease in blood platelet count, loss of libido, impotence, headache, chest pain, larynx swelling, nausea, abdominal pain, rash, itching, redness, hair loss, and urinary incontinence are also seen.

What should be considered when taking clonazepam?

If clonazepam is used in addition to other active ingredients against epilepsy, lower doses of the active ingredients are usually sufficient because of the mutual reinforcement of their effects.

Medicines that lead to higher concentrations of degrading enzymes in the liver (so-called enzyme inducers) can thereby increase the breakdown of clonazepam and thus reduce its effect. Some of these drugs are also used in epilepsy, such as phenobarbital, phenytoin, carbamazepine, and oxcarbazepine.

Because of the risk of unpredictable interactions, alcohol should never be consumed during treatment with clonazepam.

Clonazepam should not be used during pregnancy, as the active ingredient can cause deformities in the child, as well as dependency of the infant and problems during childbirth.

Clonazepam is excreted in breast milk. If use during breastfeeding is absolutely necessary, women should stop breastfeeding beforehand.

How to get medication with clonazepam

Preparations with single-dose dosage forms (e.g. tablets) that contain no more than two milligrams of clonazepam per single dose and no more than 250 milligrams of clonazepam per pack may be prescribed by the doctor on a normal drug prescription. Higher dosed drugs fall under the Narcotics Act: They can only be prescribed on a yellow narcotics prescription.

Since when is clonazepam known?

After the market launch of the first benzodiazepine (chlordiazepoxide in 1960) by the pharmaceutical company Hoffmann-La Roche, numerous other benzodiazepines with different properties and action profiles were developed. The active ingredient clonazepam was patented in 1964. From 1975 he was expelled in the USA.

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