Bromazepam

ATC CodeN05BA08
CAS number1812-30-2
PUB number2441
Drugbank IDDB01558
Empirical formulaC14H10BrN3O
Molar mass (g·mol−1)316,15
Physical statesolid
Melting point (°C)237-239

Basics

Bromazepam is an active ingredient from the benzodiazepine group, which is used to treat severe anxiety or panic attacks or insomnia due to its antianxiety and sedative properties. It is also used to relieve alcohol and opiate withdrawal symptoms.

Because of its rapid absorption and onset of action, bromazepam has a greater potential for abuse compared to other benzodiazepines, according to many psychiatric experts.

It is classified as a psychotropic substance and was approved in Germany under the trade name Lexotanil® in 1977, but was withdrawn from the market in 2016. Lexotanil® is still available in Switzerland and Austria.

Pharmacology

Pharmacodynamics

The drug binds to the GABA-A receptor, causing a conformational change and potentiating the inhibitory GABA-Aergic effects. As a result, the depressant, antianxiety, anticonvulsant, and muscle relaxant effects are induced.

Pharmacokinetics

After oral ingestion, bioavailability is 84%. The maximum plasma level is reached after 1-4 hours. The drug circulates 70% protein-bound and has a half-life of 10-20 hours. Bromazepam is broken down in the liver via oxidative pathways and excretion occurs in the urine.

Contraindications

Bromazepam should not be used in case of:

  • Hypersensitivity
  • dependence on CNS depressant substances including alcohol
  • Sleep apnea
  • myasthenia gravis
  • Severe hepatic insufficiency
  • severe respiratory insufficiency
  • Pregnancy and lactation

Drug interactions

When used concomitantly with centrally sedating drugs, alcohol, and muscle relaxants, the depressant, respiratory, and hemodynamic (blood flow mechanics) effects may be mutually potentiated.

Toxicity

Side effects

Side effects commonly encountered at the start of therapy include fatigue, dizziness, lightheadedness, lowered blood pressure, impaired concentration, impaired reaction times, and headache.
Das Risiko einer psychischen und körperlichen Abhängigkeitsentwicklung besteht bereits nach wenigen Wochen mit täglicher Einnahme und bei einem raschen Absetzen können Entzugserscheinungen auftreten.

Toxicological data

High doses over a prolonged period of time may result in articulation difficulties and unsteadiness of movement and gait.

Markus Falkenstätter, BSc

Markus Falkenstätter, BSc

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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