Cloxazolam

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Cloxazolam
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Systematic (IUPAC) name
13-chloro- 2-(2-chlorophenyl)- 3-oxa- 6,9-diazatricyclo [8.4.0.02,6]tetradeca- 1(10),11,13-trien -8-one
Clinical data
Pregnancy
category
  •  ?
Routes of
administration		 Oral
Legal status
Legal status
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Biological half-life 65 Hours
Excretion Renal
Identifiers
CAS Number 24166-13-0
ATC code N05BA22 (WHO)
PubChem CID 2816
DrugBank ?
ChemSpider 2714
Chemical data
Formula C17H14Cl2N2O2
Molar mass 349.2[[Script error: No such module "String".]]
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Cloxazolam (marketed under brand name Sepazon, Olcadil (Brazil, Portugal and Spain), Akton (Belgium), Lubalix (Switzerland) is a drug which is a benzodiazepine derivative.[1] Cloxazolam is metabolised into the active metabolite chlordesmethyldiazepam (delorazepam).[2] It possesses anxiolytic,[3] anticonvulsant,[4] hypnotic,[5] sedative[6] and skeletal muscle relaxant properties.[7]

Indications

Cloxazolam's main use is as an anti-anxiety drug.[8]

Side effects

An increased heart rate may occur as an adverse effect of cloxazolam.[9]

Pharmacology

The pharmacological effects of cloxazolam are a result of mainly its active metabolites, thus cloxazolam is a prodrug. The main site of action of cloxazolam and its active metabolites are the benzodiazepine receptor.[10]

The pharmacological actions of benzodiazepines at the GABAa receptor are similar to those of neurosteroids. Neuroactive steroids are positive allosteric modulators of the GABAa receptor, enhancing GABA function and in turn have effects on mood and other functions. Many benzodiazepines (diazepam, medazepam, estazolam, temazepam, flunitrazepam and nitrazepam) potently inhibit the enzymes involved in the metabolism of neurosteroids. The tetrahydroxazole ring that cloxazolam and oxazolam have decreases the inhibitory potency of benzodiazepines on neurosteroids. Thus there could be subtle differences between cloxazolam and other benzodiazepines.[11]. However, because the parent prodrugs of cloxazolam and oxazolam were tested rather than the active metabolites, this is purely speculative.

See also

References

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External links

Benzodiazepine derivatives (N05BA, N05CD)
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Triazolobenzodiazepines
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  1. ↑ "Benzodiazepine Names". non-benzodiazepines.org.uk. Retrieved 2008-12-29. 
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  5. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  6. ↑ Brisse, B.; Tetsch, P.; Toye, A. (1980). "[Clinical study on stress protective action of cloxazolam in jaw surgery in double blind comparison to placebo (author's transl)]". Arzneimittelforschung. 30 (4): 679–82. PMID 6104969. 
  7. ↑ Ansseau, M.; von Frenckell, R. (1990). "Controlled comparison of two anxiolytic benzodiazepines, cloxazolam and bromazepam". Neuropsychobiology. 24 (1): 25–9. doi:10.1159/000119038. PMID 1983433. 
  8. ↑ Fischer-Cornelssen, KA. (1981). "Multicenter trials and complementary studies of cloxazolam, a new anxiolytic drug". Arzneimittelforschung. 31 (10): 1757–65. PMID 6119092. 
  9. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  10. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  11. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
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