Bromazepam

Bromazepam
ATC Code N05BA08
Formula C14H10BrN3O
Molar Mass (g·mol−1) 316,15
Physical State solid
Melting Point (°C) 237-239
CAS Number 1812-30-2
PUB Number 2441
Drugbank ID DB01558
Solubility insoluble in water

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is classified as a psychotropic substance and was approved in Germany under the trade name Lexotanil® in 1977, but was withdrawn from the market in 2016.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

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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