Ketazolam

Ketazolam

Ketazolam
Systematic (IUPAC) name
11-chloro-8,12b-dihydro-2,8-dimethyl-12b-phenyl-4H-[1,3]oxazino[3,2-d][1,4]benzodiazepine-4,7(6H)-dione[1]
Clinical data
AHFS/Drugs.com
Pregnancy cat.
  • ?
Legal status
Routes Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Half-life 26-200 hours
Excretion Renal
Identifiers
CAS number  YesY
ATC code N05
PubChem
DrugBank
ChemSpider  YesY
UNII  YesY
KEGG  YesY
Chemical data
Formula C20H17ClN2O3 
Mol. mass 368.8
 YesY   

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 a reduced level 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 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]

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References

  1. ^ Vega D; Fernández D; Echeverría G (July 2001). "Ketazolam". Acta Crystallogr C 57 (Pt 7): 848–50.  
  2. ^ Anhalt HS; Young R; Roginsky M (November 1980). "Double-blind comparison of ketazolam, diazepam and placebo in once-a-day vs t.i.d. dosing". The Journal of clinical psychiatry 41 (11): 386–92.  
  3. ^ Kim KK; Sirman A; Trainor FS; Lee BY (1980). "Anxiolytic efficacy and safety of ketazolam compared with diazepam and placebo". Clin Ther 3 (1): 9–14.  
  4. ^ Fabre LF Jr; Harris RT (1976). "Double-blind placebo-controlled efficacy study of ketazolam (U-28,774)". J Int Med Res 4 (1): 50–4.  
  5. ^ Rickels K; Csanalosi I; Greisman P; Mirman MJ; Morris RJ; Weise CC; Weiss G (October 1980). "Ketazolam and diazepam in anxiety: a controlled study". J Clin Pharmacol 20 (10): 581–9.  
  6. ^ Basmajian JV; Shankardass K; Russell D (August 1986). "Ketazolam once daily for spasticity: double-blind cross-over study". Arch Phys Med Rehabil 67 (8): 556–7.  
  7. ^ Katz RT (June 1988). "Management of spasticity". Am J Phys Med Rehabil 67 (3): 108–16.  
  8. ^ Basmajian JV; Shankardass K; Russell D; Yucel V (November 1984). "Ketazolam treatment for spasticity: double-blind study of a new drug". Arch Phys Med Rehabil 65 (11): 698–701.  
  9. ^ "Benzodiazepine Names". The Tranquilliser Recovery and Awareness Place. Retrieved 26 August 2008. 
  10. ^ "SOLATRAN 15 (capsules) - SOLATRAN 30 (capsules)". South African Electronic Package Inserts. 12 November 1985. Retrieved 26 August 2008. 
  11. ^ http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-26.html#h-29
  12. ^ Higgitt A; Fonagy P; Lader M (1988). "The natural history of tolerance to the benzodiazepines". Psychol Med Monogr Suppl 13: 1–55.  
  13. ^ Authier, N.; Balayssac, D.; Sautereau, M.; Zangarelli, A.; Courty, P.; Somogyi, AA.; Vennat, B.; Llorca, PM.; Eschalier, A. (Nov 2009). "Benzodiazepine dependence: focus on withdrawal syndrome.". Ann Pharm Fr 67 (6): 408–13.  
  14. ^ Joyce JR, Bal TS, Ardrey RE, Stevens HM, Moffat AC (June 1984). "The decomposition of benzodiazepines during analysis by capillary gas chromatography/mass spectrometry". Biomed Mass Spectrom. 11 (6): 284–9.  
  15. ^  
  16. ^