Ketazolam Explained

Watchedfields:changed
Verifiedrevid:447550624
Iupac Name:11-chloro-2,8-dimethyl-12b-phenyl-6H-[1,3]oxazino[3,2-d][1,4]benzodiazepine-4,7-dione[1]
Width:175
Width2:150
Legal Br:B1
Legal Br Comment:[2]
Legal Ca:Schedule IV
Legal De:Rx-only/Anlage III
Legal Us:Schedule IV
Routes Of Administration:Oral
Metabolism:Hepatic
Elimination Half-Life:26–200 hours
Excretion:Renal
Cas Number:27223-35-4
Atc Prefix:N05
Atc Suffix:BA10
Pubchem:33746
Drugbank:DB01587
Chemspiderid:31110
Unii:92A214MD7Y
Kegg:D04650
C:20
H:17
Cl:1
N:2
O:3
Smiles:ClC1=CC2=C(N(C)C(CN3C(C=C(C)OC32C4=CC=CC=C4)=O)=O)C=C1
Stdinchi:1S/C20H17ClN2O3/c1-13-10-18(24)23-12-19(25)22(2)17-9-8-15(21)11-16(17)20(23,26-13)14-6-4-3-5-7-14/h3-11H,12H2,1-2H3
Stdinchikey:PWAJCNITSBZRBL-UHFFFAOYSA-N

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.[3] [4] [5] [6] Ketazolam is also an effective antispasmodic drug and is used for the treatment of spasticity.[7] [8] [9]

Availability

Ketazolam is not approved for sale in Norway, Australia, United Kingdom or the United States.[10] In South Africa, GlaxoSmithKline markets ketazolam under its Solatran brand name.[11] In Canada, ketazolam is listed in schedule IV of the Controlled Drugs and Substances Act, along with other benzodiazepines.[12]

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.[13]

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.[14]

Pharmacokinetics

Ketazolam breaks down in the blood to diazepam which breaks down to demoxepam which breaks down to desmethyldiazepam.[15]

Warnings

The U.S. Food and Drug Administration warns that in Spain, ketazolam marketed as Marcen may sometimes be mistakenly confused with Narcan.[16]

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.[17]

Notes and References

  1. Vega D, Fernández D, Echeverría G . Ketazolam . Acta Crystallographica Section C . 57 . Pt 7 . 848–850 . July 2001 . 11443263 . 10.1107/S0108270101006175 .
  2. Web site: Anvisa . Brazilian Health Regulatory Agency . 2023-03-31 . RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial . Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control. live . https://web.archive.org/web/20230803143925/https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 . 2023-08-03 . 2023-08-16 . . pt-BR . 2023-04-04.
  3. Anhalt HS, Young R, Roginsky M . 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 . 6108319 .
  4. Kim KK, Sirman A, Trainor FS, Lee BY . Anxiolytic efficacy and safety of ketazolam compared with diazepam and placebo . Clinical Therapeutics . 3 . 1 . 9–14 . 1980 . 6105920 .
  5. Fabre LF, Harris RT . Double-blind placebo-controlled efficacy study of ketazolam (U-28,774) . The Journal of International Medical Research . 4 . 1 . 50–54 . 1976 . 16791 . 10.1177/030006057600400107 . 26311555 .
  6. Rickels K, Csanalosi I, Greisman P, Mirman MJ, Morris RJ, Weise CC, Weiss G . Ketazolam and diazepam in anxiety: a controlled study . Journal of Clinical Pharmacology . 20 . 10 . 581–589 . October 1980 . 6108335 . 10.1002/j.1552-4604.1980.tb01673.x . 6597368 .
  7. Basmajian JV, Shankardass K, Russell D . Ketazolam once daily for spasticity: double-blind cross-over study . Archives of Physical Medicine and Rehabilitation . 67 . 8 . 556–557 . August 1986 . 2874780 .
  8. Katz RT . Management of spasticity . American Journal of Physical Medicine & Rehabilitation . 67 . 3 . 108–116 . June 1988 . 3288246 . 10.1097/00002060-198806000-00004 . 45292155 .
  9. Basmajian JV, Shankardass K, Russell D, Yucel V . Ketazolam treatment for spasticity: double-blind study of a new drug . Archives of Physical Medicine and Rehabilitation . 65 . 11 . 698–701 . November 1984 . 6149738 .
  10. Web site: Benzodiazepine Names . 26 August 2008 . The Tranquilliser Recovery and Awareness Place . dead . https://web.archive.org/web/20081208054743/http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html . 8 December 2008 .
  11. Web site: SOLATRAN 15 (capsules) - SOLATRAN 30 (capsules). 26 August 2008. 12 November 1985. South African Electronic Package Inserts. 2 June 2019. https://web.archive.org/web/20190602153230/http://home.intekom.com/pharm/smith_kb/solatran.html. dead.
  12. Web site: Controlled Drugs and Substances Act. laws-lois.justice.gc.ca . https://web.archive.org/web/20131215170432/http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-26.html . 2013-12-15.
  13. Higgitt A, Fonagy P, Lader M . The natural history of tolerance to the benzodiazepines . Psychological Medicine. Monograph Supplement . 13 . 1–55 . 1988 . 2908516 . 10.1017/S0264180100000412 . 38037200 .
  14. Authier N, Balayssac D, Sautereau M, Zangarelli A, Courty P, Somogyi AA, Vennat B, Llorca PM, Eschalier A . 6 . Benzodiazepine dependence: focus on withdrawal syndrome . Annales Pharmaceutiques Françaises . 67 . 6 . 408–413 . November 2009 . 19900604 . 10.1016/j.pharma.2009.07.001 .
  15. Joyce JR, Bal TS, Ardrey RE, Stevens HM, Moffat AC . The decomposition of benzodiazepines during analysis by capillary gas chromatography/mass spectrometry . Biomedical Mass Spectrometry . 11 . 6 . 284–289 . June 1984 . 6743768 . 10.1002/bms.1200110607 .
  16. Web site: FDA Public Health Advisory - Consumers Filling U.S. Prescriptions Abroad May Get the Wrong Active Ingredient Because of Confusing Drug Names . 26 August 2006 . Food and Drug Administration . Food and Drug Administration . January 2006 . FDA (USA) . https://web.archive.org/web/20060812000720/https://www.fda.gov/oc/opacom/reports/confusingnames.html . 12 August 2006 . dead .
  17. Web site: Drug Scheduling. 26 August 2008. Drug Enforcement Administration (USA). Drug Enforcement Administration. United States Government. 27 May 2018. https://web.archive.org/web/20180527230806/https://www.dea.gov/pubs/scheduling.html. dead.

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