Camazepam

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Not to be confused with clonazepam, clobazam, or cinolazepam.
Camazepam
Camazepam.svg
Camazepam3d.png
Systematic (IUPAC) name
7-chloro-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl N,N-dimethylcarbamate
Clinical data
Pregnancy
category
  •  ?
Legal status
Routes of
administration		 Oral
Pharmacokinetic data
Bioavailability 90%
Metabolism Hepatic
Biological half-life 6,4-10,5 hours
Excretion Renal
Identifiers
CAS Number 36104-80-0 YesY
ATC code N05BA15 (WHO)
PubChem CID: 37367
DrugBank DB01489 YesY
ChemSpider 34285 YesY
UNII HZ3XRH03C3 YesY
KEGG D07315 YesY
ChEMBL CHEMBL1095282 YesY
Chemical data
Formula C19H18ClN3O3
Molecular mass 371.8
  • ClC1=CC2=C(C=C1)N(C)C(C(N=C2C3=CC=CC=C3)OC(N(C)C)=O)=O
  • InChI=1S/C19H18ClN3O3/c1-22(2)19(25)26-17-18(24)23(3)15-10-9-13(20)11-14(15)16(21-17)12-7-5-4-6-8-12/h4-11,17H,1-3H3 YesY
  • Key:PXBVEXGRHZFEOF-UHFFFAOYSA-N YesY
  (verify)

Camazepam[1] is a benzodiazepine psychoactive drug, marketed under the brand names Albego, Limpidon and Paxor. It is the dimethyl carbamate ester of temazepam, a metabolite of diazepam.[2] While it possesses anxiolytic, anticonvulsant, skeletal muscle relaxant and hypnotic properties[3] it differs from other benzodiazepines in that its anxiolytic properties are particularly prominent but has comparatively limited anticonvulsant, hypnotic and skeletal muscle relaxant properties.

Pharmacology

Camazepam, like others benzodiazepines, produce a variety of therapeutic and adverse effects by binding to the benzodiazepine receptor site on the GABAA receptor and modulating the function of the GABA receptor, the most prolific inhibitory receptor within the brain. The GABA chemical and receptor system mediates inhibitory or calming effects of camazepam on the nervous system. Compared to other benzodiazepines, it has reduced side effects such as impaired cognition, reaction times and coordination.[4][5][6][7][8] which makes it best suited as an anxiolytic because of these reduced sides effects. Animal studies have shown camazepam and its active metabolites possess anticonvulsant properties.[9] Unlike other benzodiazepines it does not disrupt normal sleep patterns.[10] Camazepam has been shown in animal experiments to have a very low affinity for benzodiazepine receptors compared to other benzodiazepines.[11] Compared to temazepam, camazepam has shown roughly equal anxiolytic properties, and less anticonvulsant, sedative and motor-impairing properties.

Pharmacokinetics

Following oral administration, camazepam is almost completely absorbed into the bloodstream, with 90 percent bioavailability achieved in humans.[12] In the human camazepam is metabolised into the active metabolite temazepam.[13] Studies in dogs have shown that the half-life of the terminal elimination phase ranged from 6.4 to 10.5 h.[14]

Medical uses

Camazepam is indicated for the short-term treatment of insomnia and anxiety. As with other benzodiazepines, its use should be reserved for those patients in which the sleep disorder is severe, disabling or causes marked distress.

Adverse effects

With higher doses such as 40 mg of camazepam, impairments similar to those caused by other benzodiazepines manifest as disrupted sleep patterns and impaired cognitive performance.[15] Skin disorders have been reported with use of camazepam however.[16] Camazepam is believed to increase attention.[17]

Contraindications

Use of camazepam is contraindicated in subjects with known hypersensitivity to drug or allergy to other drugs in the benzodiazepine class or any excipients contained in the pharmaceutical form. Use of camazepam should be avoided or carefully monitored by medical professionals in individuals with the following conditions: myasthenia gravis, severe liver deficiencies (e.g., cirrhosis), severe sleep apnea, pre-existing respiratory depression or cronic pulmonary insufficiency.

See also

References

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External links

  1. ↑ DE Patent 2142181
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