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Cloxazolam

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Title: Cloxazolam  
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Subject: Gidazepam, List of benzodiazepines, Delorazepam, Adinazolam, Pinazepam
Collection: Anxiolytics, Chloroarenes, Gabaa Receptor Positive Allosteric Modulators, Lactams, Organochlorides, Oxazolobenzodiazepines, Prodrugs
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Cloxazolam

Cloxazolam
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
AHFS/Drugs.com
Pregnancy cat.
  • ?
Legal status
Routes Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Half-life 65 Hours
Excretion Renal
Identifiers
CAS number  YesY
ATC code N05
PubChem
DrugBank
ChemSpider  YesY
UNII  YesY
KEGG  YesY
ChEMBL  N
Chemical data
Formula C17H14Cl2N2O2 
Mol. mass 349.2
 N   

Cloxazolam[1] (marketed under brand name Sepazon, Olcadil (Brazil, Portugal and Spain), Akton (Belgium), Lubalix (Switzerland) is a drug which is a benzodiazepine derivative.[2] Cloxazolam is metabolised into the active metabolite chlordesmethyldiazepam (delorazepam).[3] It possesses anxiolytic,[4] anticonvulsant,[5] hypnotic,[6] sedative[7] and skeletal muscle relaxant properties.[8]

Contents

  • Indications 1
  • Side effects 2
  • Pharmacology 3
  • See also 4
  • References 5
  • External links 6

Indications

Cloxazolam's main use is as an anti-anxiety drug.[9]

Side effects

An increased heart rate may occur as an adverse effect of cloxazolam.[10]

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.[11]

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.[12] However, because the parent prodrugs of cloxazolam and oxazolam were tested rather than the active metabolites, this is purely speculative.

See also

References

  1. ^ DE Patent 1817923
  2. ^ "Benzodiazepine Names". non-benzodiazepines.org.uk. Retrieved 2008-12-29. 
  3. ^ Oliveira-Silva, D.; Oliveira, CH.; Mendes, GD.; Galvinas, PA.; Barrientos-Astigarraga, RE.; De Nucci, G. (Dec 2009). "Quantification of chlordesmethyldiazepam by liquid chromatography-tandem mass spectrometry: application to a cloxazolam bioequivalence study.". Biomed Chromatogr 23 (12): 1266–75.  
  4. ^ Kamioka, T.; Nakayama, I.; Akiyama, S.; Takagi, H. (Mar 1977). "Effects of oxazolam, cloxazolam, and CS-386, new anti-anxiety drugs, on socially induced suppression and aggression in pairs of monkeys.". Psychopharmacology (Berl) 52 (1): 17–23.  
  5. ^ Ito, M.; Miyajima, T.; Fujii, T.; Okuno, T. (Feb 2004). "Cloxazolam treatment for patients with intractable epilepsy.". Pediatr Neurol 30 (2): 111–4.  
  6. ^ Inoue, H.; Maeno, Y.; Iwasa, M.; Matoba, R.; Nagao, M. (Sep 2000). "Screening and determination of benzodiazepines in whole blood using solid-phase extraction and gas chromatography/mass spectrometry.". Forensic Sci Int 113 (1–3): 367–73.  
  7. ^ 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.  
  8. ^ Ansseau, M.; von Frenckell, R. (1990). "Controlled comparison of two anxiolytic benzodiazepines, cloxazolam and bromazepam". Neuropsychobiology 24 (1): 25–9.  
  9. ^ Fischer-Cornelssen, KA. (1981). "Multicenter trials and complementary studies of cloxazolam, a new anxiolytic drug". Arzneimittelforschung 31 (10): 1757–65.  
  10. ^ Boucsein, W.; Wendt-Suhl, G. (Mar 1982). "[Psychological and physiological effects of cloxazolam and diazepam under anxiety-evoking and control conditions on healthy subjects (author's transl)]". Pharmacopsychiatria 15 (2): 48–56.  
  11. ^ Nakatsuka, I.; Shimizu, H.; Asami, Y.; Katoh, T.; Hirose, A.; Yoshitake, A. (Jan 1985). "Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity". Life Sci 36 (2): 113–9.  
  12. ^ Usami N; Yamamoto T; Shintani S; Ishikura S; Higaki Y; Katagiri Y; Hara A. (Apr 2002). "Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines" (pdf). Biol Pharm Bull. 25 (4): 441–5.  

External links

  • Inchem.org - Cloxazolam


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