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Ketazolam

Chemical compound


Chemical compound

FieldValue
Watchedfieldschanged
verifiedrevid447550624
IUPAC_name11-chloro-2,8-dimethyl-12b-phenyl-6*H*-[1,3]oxazino[3,2-d][1,4]benzodiazepine-4,7-dione
imageKetazolam.svg
image_classskin-invert-image
width175
image2Ketazolam3d.png
image_class2bg-transparent
width2150
Drugs.com
legal_BRB1
legal_BR_comment
legal_CASchedule IV
legal_DERx-only/Anlage III
legal_USSchedule IV
routes_of_administrationOral
metabolismHepatic
elimination_half-life26–200 hours
excretionRenal
CAS_number_Ref
CAS_number27223-35-4
ATC_prefixN05
ATC_suffixBA10
PubChem33746
DrugBank_Ref
DrugBankDB01587
ChemSpiderID_Ref
ChemSpiderID31110
UNII_Ref
UNII92A214MD7Y
KEGG_Ref
KEGGD04650
C20H=17Cl=1N=2O=3
smilesClC1=CC2=C(N(C)C(CN3C(C=C(C)OC32C4=CC=CC=C4)=O)=O)C=C1
StdInChI_Ref
StdInChI1S/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_Ref
StdInChIKeyPWAJCNITSBZRBL-UHFFFAOYSA-N

| Drugs.com =

| elimination_half-life = 26–200 hours

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. Ketazolam is also an effective antispasmodic drug and is used for the treatment of spasticity.

Availability

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

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.

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.

Pharmacokinetics

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

Warnings

The U.S. Food and Drug Administration warns that in Spain, ketazolam marketed as Marcen may sometimes be mistakenly confused with Narcan.{{cite web |access-date=26 August 2006 |author-link=Food and Drug Administration |archive-url=https://web.archive.org/web/20060812000720/https://www.fda.gov/oc/opacom/reports/confusingnames.html |archive-date=12 August 2006 |url-status=dead

References

References

  1. (July 2001). "Ketazolam". Acta Crystallographica Section C.
  2. Anvisa. (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial". [[Diário Oficial da União]].
  3. (November 1980). "Double-blind comparison of ketazolam, diazepam and placebo in once-a-day vs t.i.d. dosing". The Journal of Clinical Psychiatry.
  4. (1980). "Anxiolytic efficacy and safety of ketazolam compared with diazepam and placebo". Clinical Therapeutics.
  5. (1976). "Double-blind placebo-controlled efficacy study of ketazolam (U-28,774)". The Journal of International Medical Research.
  6. (October 1980). "Ketazolam and diazepam in anxiety: a controlled study". Journal of Clinical Pharmacology.
  7. (August 1986). "Ketazolam once daily for spasticity: double-blind cross-over study". Archives of Physical Medicine and Rehabilitation.
  8. (June 1988). "Management of spasticity". American Journal of Physical Medicine & Rehabilitation.
  9. (November 1984). "Ketazolam treatment for spasticity: double-blind study of a new drug". Archives of Physical Medicine and Rehabilitation.
  10. "Benzodiazepine Names". The Tranquilliser Recovery and Awareness Place.
  11. (12 November 1985). "SOLATRAN 15 (capsules) - SOLATRAN 30 (capsules)". South African Electronic Package Inserts.
  12. "Controlled Drugs and Substances Act".
  13. (1988). "The natural history of tolerance to the benzodiazepines". Psychological Medicine. Monograph Supplement.
  14. (November 2009). "Benzodiazepine dependence: focus on withdrawal syndrome". Annales Pharmaceutiques Françaises.
  15. (June 1984). "The decomposition of benzodiazepines during analysis by capillary gas chromatography/mass spectrometry". Biomedical Mass Spectrometry.
  16. Drug Enforcement Administration (USA). "Drug Scheduling". United States Government.
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