Chemistry:Ketazolam

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Short description: Chemical compound
Ketazolam
Ketazolam.svg
Ketazolam3d.png
Clinical data
AHFS/Drugs.comMicromedex Detailed Consumer Information
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
MetabolismHepatic
Elimination half-life26–200 hours
ExcretionRenal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC20H17ClN2O3
Molar mass368.8 g·mol−1
3D model (JSmol)
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Ketazolam (marketed under the brand names Anseren, Ansieten, Ansietil, Marcen, Sedatival, Sedotime, Solatran and Unakalm) is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.

Therapeutic uses

It is used for the treatment of anxiety and has similar effectiveness compared to diazepam. Ketazolam also appears to produce reduced levels of side effects such as sedation compared with diazepam and the side effects when they occur tend to be milder.[2][3][4][5] Ketazolam is also an effective antispasmodic drug and is used for the treatment of spasticity.[6][7][8]

Availability

Ketazolam is not approved for sale in Norway , Australia , United Kingdom or the United States .[9] In South Africa , GlaxoSmithKline markets ketazolam under its Solatran brand name.[10] In Canada, ketazolam is listed in schedule IV of the Controlled Drugs and Substances Act, along with other benzodiazepines.[11]

Tolerance and physical dependence

Chronic use of ketazolam as with other benzodiazepines can lead to physical dependence and the appearance of the benzodiazepine withdrawal syndrome upon cessation of use or decrease in dose. Tolerance to ketazolam's therapeutic effects occurs over a period of 15 days.[12]

Contraindications and special caution

Benzodiazepines require special precaution if used in the elderly, during pregnancy, in children, alcohol or drug-dependent individuals and individuals with comorbid psychiatric disorders.[13]

Pharmacokinetics

Ketazolam breaks down in the blood to diazepam which breaks down to demoxepam which breaks down to desmethyldiazepam.[14]

Warnings

The U.S. Food and Drug Administration warns that in Spain, ketazolam marketed as Marcen may sometimes be mistakenly confused with Narcan.[15]

Legal status

Ketazolam is a List 3 drug under the Betäubungsmittelgesetz, like almost all benzodiazepines in Germany. Ketazolam is a List II drugs of the Opium Law in the Netherlands. Ketazolam is a Schedule IV drug under the Controlled Substances Act in the US.[16]

References

  1. ↑ "Ketazolam". Acta Crystallographica Section C 57 (Pt 7): 848–850. July 2001. doi:10.1107/S0108270101006175. PMID 11443263. 
  2. ↑ "Double-blind comparison of ketazolam, diazepam and placebo in once-a-day vs t.i.d. dosing". The Journal of Clinical Psychiatry 41 (11): 386–392. November 1980. PMID 6108319. 
  3. ↑ "Anxiolytic efficacy and safety of ketazolam compared with diazepam and placebo". Clinical Therapeutics 3 (1): 9–14. 1980. PMID 6105920. 
  4. ↑ "Double-blind placebo-controlled efficacy study of ketazolam (U-28,774)". The Journal of International Medical Research 4 (1): 50–54. 1976. doi:10.1177/030006057600400107. PMID 16791. 
  5. ↑ "Ketazolam and diazepam in anxiety: a controlled study". Journal of Clinical Pharmacology 20 (10): 581–589. October 1980. doi:10.1002/j.1552-4604.1980.tb01673.x. PMID 6108335. 
  6. ↑ "Ketazolam once daily for spasticity: double-blind cross-over study". Archives of Physical Medicine and Rehabilitation 67 (8): 556–557. August 1986. PMID 2874780. 
  7. ↑ "Management of spasticity". American Journal of Physical Medicine & Rehabilitation 67 (3): 108–116. June 1988. doi:10.1097/00002060-198806000-00004. PMID 3288246. 
  8. ↑ "Ketazolam treatment for spasticity: double-blind study of a new drug". Archives of Physical Medicine and Rehabilitation 65 (11): 698–701. November 1984. PMID 6149738. 
  9. ↑ "Benzodiazepine Names". The Tranquilliser Recovery and Awareness Place. http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html#Ketazolam. 
  10. ↑ "SOLATRAN 15 (capsules) - SOLATRAN 30 (capsules)". South African Electronic Package Inserts. 12 November 1985. http://home.intekom.com/pharm/smith_kb/solatran.html. 
  11. ↑ "Controlled Drugs and Substances Act". http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-26.html#h-29. 
  12. ↑ "The natural history of tolerance to the benzodiazepines". Psychological Medicine. Monograph Supplement 13: 1–55. 1988. doi:10.1017/S0264180100000412. PMID 2908516. 
  13. ↑ "Benzodiazepine dependence: focus on withdrawal syndrome". Annales Pharmaceutiques Françaises 67 (6): 408–413. November 2009. doi:10.1016/j.pharma.2009.07.001. PMID 19900604. 
  14. ↑ "The decomposition of benzodiazepines during analysis by capillary gas chromatography/mass spectrometry". Biomedical Mass Spectrometry 11 (6): 284–289. June 1984. doi:10.1002/bms.1200110607. PMID 6743768. 
  15. ↑ Food and Drug Administration (January 2006). "FDA Public Health Advisory - Consumers Filling U.S. Prescriptions Abroad May Get the Wrong Active Ingredient Because of Confusing Drug Names". FDA (USA). https://www.fda.gov/oc/opacom/reports/confusingnames.html. 
  16. ↑ Drug Enforcement Administration (USA). "Drug Scheduling". United States Government. http://www.dea.gov/pubs/scheduling.html. 



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