Brotizolam: Effects and side effects

How does Brotizolam work?

Brotizolam has a sedative, sleep-inducing and anxiety-relieving effect. As a representative of the benzodiazepine group of active ingredients, breadizolam mediates its effects via the so-called GABAA receptor.

Normally, this receptor is activated by the nerve messenger gamma-aminobutyric acid (GABA). This results in the effects mentioned above (sedation, anxiety relief, sleep promotion).

Brotizolam increases the likelihood that GABA will bind to the GABAA receptor.

In the human brain, GABA is the main messenger of inhibitory synapses (connections between nerve cells).

How long does it take for Brotizolam to work?

Brotizolam reaches its maximum concentration in the blood after about 45 minutes. The sleep-inducing effect usually occurs within 30 to 60 minutes.

What are the side effects of Brotizolam?

Common side effects of Brotizolam include fatigue, loss of performance, difficulty concentrating, and dizziness.

Brotizolam can significantly impair reaction even when taken properly. Therefore, you should not drive a motor vehicle or operate heavy machinery during the first few days of treatment. Observe how you react to the sleeping drug first.

Like all benzodiazepines, brotizolam can be addictive, so withdrawal symptoms may occur when you stop taking it.

For information on these and other side effects, see the package insert for your brotizolam medication. Contact your doctor or pharmacist if you develop or suspect any unwanted side effects.

When should you not take Brotizolam?

In general, you should not take Brotizolam in the following cases:

  • Hypersensitivity to the active ingredient or any of the other ingredients of the medication.
  • myasthenia gravis (autoimmune disease of the muscles)
  • severe disorders of respiratory function
  • severe liver dysfunction
  • acute poisoning with central depressants (e.g. alcohol, psychotropic drugs, sleeping pills)
  • drug, alcohol or medication addiction (current or past)
  • pregnancy and breastfeeding
  • in children and adolescents under 18 years of age

What does Brotizolam help against?

Brotizolam is used in Germany and Austria for the short-term treatment of problems falling asleep and staying asleep. The duration of therapy is generally limited to two weeks.

In Switzerland, the active ingredient is only used in animals: It is administered to cattle to increase their appetite, i.e., to stimulate the desire to eat.

How to take Brotizolam

Brotizolam is taken in the form of tablets. Adults usually take a half to whole tablet, which is equivalent to 0.125 and 0.250 milligrams of Brotizolam, respectively.

Elderly patients and those with impaired liver function or respiratory depression are given half a tablet (0.125 milligrams).

The sleeping pill is taken immediately before lying down, together with some liquid (preferably water). After that, you should make sure to sleep for seven to eight hours.

Use Brotizolam for as short a time as possible so that your body does not develop dependence. It may make it difficult to stop.

These drug interactions may occur with brotizolam

There are many known interactions with other drugs that have a depressant effect. These include:

  • Opioids: strong pain relievers, e.g., morphine, hydromorphone.
  • Antipsychotics: Agents for psychotic symptoms such as hallucinations, e.g., levomepromazine, olanzapine, quetiapine
  • Anxiolytics: anti-anxiety agents, e.g., gabapentin, pregabalin
  • Antiepileptic drugs: Epilepsy medications such as primidone and carbamazepine
  • older anti-allergic drugs such as dephenhydramine and hydroxyzine
  • Antifungals (e.g., ketoconazole and itraconazole).
  • Macrolide antibiotics (e.g., erythromycin and clarithromycin)
  • HIV medications (e.g., efavirenz and ritonavir)
  • Aprepitant (drug for chemotherapy-induced nausea and vomiting)
  • Grapefruit juice

CYP3A4 inducers have the opposite effect. These are substances that increase the activity of the degrading enzyme. This may reduce the sleep-inducing effect of brotizolam. Examples of CYP3A4 inducers are phenobarbital, phenytoin, and carbamazepine (all drugs for epilepsy), and the antibiotic rifampicin.

Brotizolam may potentiate the effects of muscle relaxants (muscle relaxants). This increases the risk of falls, particularly in elderly patients.

In combination with alcohol, the Brotizolam effect may change and intensify in an unpredictable way. Therefore, do not take the sleeping pill together with alcoholic beverages.

How to obtain medication with Brotizolam

The active ingredient is subject to prescription in Germany and Austria. In Switzerland, no human medicines containing Brotizolam are available.