Oxazepam

Oxazepam
ATC Code N05BA04
Formula C15H11ClN2O2
Melting Point (°C) 205
PKS Value 1.55; 10.9
CAS Number 604-75-1
PUB Number 4616
Drugbank ID DB00842

Basics

Oxazepam is a medium-acting member of the benzodiazepine class with a slow onset of action. Oxazepam is indicated for the treatment of anxiety disorders and for short-term relief of anxiety symptoms. It can also be used to treat alcohol withdrawal symptoms. The substance is taken perorally in the form of tablets.

The substance was developed and marketed in 1965 by Dr. Karl Thomae GmbH (now Boehringer Ingelheim).


Pharmacology

Pharmacodynamics

Benzodiazepines, including oxazepam, exert their sedative and anxiolytic effects by enhancing the action of endogenous GABA, the primary inhibitory neurotransmitter in the CNS. In doing so, it binds to the GABA chloride channel as a positive allosteric modulator. This promotes the binding of GABA to the channel and enhances the inhibitory effect. Compared to other benzodiazepines, oxazepam has relatively low potency and moderate duration of action.

Pharmacokinetics

Oxazepam is administered orally only and reaches peak plasma concentration after approximately 3 hours. It is 89% bound to serum albumin. The elimination half-life is about 8 hours. According to a British study, oxazepam is absorbed most slowly and has the slowest onset of action of all commonly used benzodiazepines. The substance is not broken down via the cytochrome P450 system, which is why it can be used without problems even in patients with severely impaired liver function.

Interactions

Oxazepam is itself an active substance and, unlike other commonly used benzodiazepines, does not need to be converted in the liver beforehand. This makes the occurrence of interactions rather unlikely.

Toxicity

Side effects

  • Dizziness
  • Drowsiness
  • Headache
  • Memory impairment
  • Paradoxical excitation
  • Anterograde amnesia

Oxazepam can cause tolerance, physical dependence, addiction, and benzodiazepine withdrawal syndrome. Withdrawal from oxazepam or other benzodiazepines often results in withdrawal symptoms similar to those of alcohol and barbiturate withdrawal. The higher the dose and the longer the drug is taken, the greater the risk of experiencing unpleasant withdrawal symptoms. However, withdrawal symptoms can occur even at normal doses and after short-term use. Treatment with benzodiazepines should be discontinued as soon as possible by slow and gradual dose reduction.

Contraindications

Use of oxazepam during pregnancy may cause a number of serious side effects in the unborn and newborn. Therefore, the substance should be administered only when clearly needed.

Toxicological data

LD50, rat, oral: >8000 mg/kg

LD50, mouse, oral: 1540 mg/kg

Sources

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

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