Why is Clonazepam a Benzodiazepine


ClonazepamDrug groupsBenzodiazepine Clonazepam is an active ingredient from the group of benzodiazepines with antispasmodic, depressant and anti-anxiety properties. The effects are based on the amplification of the effects of the inhibitory neurotransmitter GABA in the brain by binding to the GABA receptor. Clonazepam is mainly used in Switzerland to treat epilepsy. In some countries, however, it is also approved for the treatment of psychiatric illnesses such as panic disorders. Clonazepam has a long half-life between 30 to 40 hours and is a substrate of CYP3A4. Possible adverse effects include, for example, fatigue, drowsiness, psychiatric disorders, paradoxical reactions, addiction, muscle weakness, visual disturbances, respiratory depression and withdrawal symptoms. Like other benzodiazepines, clonazepam can be abused as a depressant intoxicant and become addictive.

synonym: ClonazepamumPhEur

Products

Clonazepam is available in tablet, solution for injection and oral drops (Rivotril®). It has been approved in Switzerland since 1973. In the US it is marketed as Klonopin®.

Structure and properties

Clonazepam (C.15H10ClN3O3, Mr = 315.7 g / mol) is a slightly yellowish, crystalline powder that is practically insoluble in water. It is a 5-aryl-1,4-benzodiazepine which carries a nitro group. Clonazepam is a chlorinated derivative of Nitrazepam (Mogadon®).

Effects

Clonazepam (ATC N03AE01) has antispasmodic, depressant and anti-anxiety properties. The effects are based on the allosteric binding to the postsynaptic GABA receptor, the opening of chloride channels and the amplification of the effects of GABA, the most important inhibitory neurotransmitter in the brain. Clonazepam has a long half-life between 30 to 40 hours.

Mechanism of action of the benzodiazepines, click to enlarge. Illustration © PharmaWiki

Indications

For the treatment of epilepsy and epileptic fits (status epilepticus). In some countries also for the treatment of psychiatric illnesses such as panic disorders.

dosage

According to the specialist information. The dose is set individually. The drugs are usually given two to three times a day.

Abuse

Like other benzodiazepines, clonazepam can also be misused as a central depressant intoxicant. It can lead to dependency and, upon withdrawal, cause withdrawal symptoms.

Contraindications
  • Hypersensitivity
  • Respiratory failure
  • Severe hepatic insufficiency
  • Drug, drug and alcohol addiction
  • Myasthenia gravis

The complete precautionary measures can be found in the medicinal product information sheet.

Interactions

Clonazepam is a substrate for CYP3A4. Drug interactions have been described with the following substances:

unwanted effects

Possible adverse effects include, for example, fatigue, drowsiness, psychiatric disorders, paradoxical reactions, addiction, muscle weakness, visual disturbances, respiratory depression and withdrawal symptoms.

see also

Benzodiazepines

literature
  • Pharmaceutical product information (CH, USA, D)
  • Browne T.R. Clonazepam. A review of a new anticonvulsant drug. Arch Neurol, 1976, 33 (5), 326-32 Pubmed
  • European Pharmacopoeia PhEur
  • Nardi A.E. et al. Clonazepam for the treatment of panic disorder. Curr Drug Targets, 2013, 14 (3), 353-64 Pubmed
  • Nardi A.E., Perna G. Clonazepam in the treatment of psychiatric disorders: an update. Int Clin Psychopharmacol, 2006, 21 (3), 131-42 Pubmed
  • Rosenbaum J.F. The development of clonazepam as a psychotropic: the massachusetts general hospital experience. J Clin Psychiatry, 2004, 65 Suppl 5, 3-6 Pubmed
author

Conflicts of Interest: None / Independent. The author has no relationships with the manufacturers and is not involved in the sale of the products mentioned.

additional Information
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This article was last changed on February 18, 2020.
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