Ketazolam

Drugbox
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 [cite journal | journal =Acta Crystallogr C | year =2001 |month=Jul | volume =57 | issue =Pt 7 | pages =848–50 | title =Ketazolam | author =Vega D |coauthors=Fernández D, Echeverría G | pmid =11443263 | doi =10.1107/S0108270101006175 ]

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width=150

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CAS_number=27223-35-4
ATC_prefix=N05
ATC_suffix=BA10
ATC_supplemental=
PubChem=33746
DrugBank=?
C=20 | H=17 | Cl=1 | N=2 | O=3
molecular_weight = 368.8
bioavailability= ?
metabolism = Hepatic
elimination_half-life= 26-200 hours
excretion = Renal
pregnancy_category = ?
legal_status = Schedule IV(US)
routes_of_administration= Oral

Ketazolam (marketed under the brand names Anseren, Ansieten, Ansietil, Marcen, Sedatival, Sedotime, Solatran, Unakalm) is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.

Availability

Ketazolam is not approved for sale in Australia, Canada, United Kingdom or the United States. [cite web |url=http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html#Ketazolam |title=Benzodiazepine Names |accessdaymonth=26 Aug |accessyear=2008 |publisher=The Tranquilliser Recovery and Awareness Place] In South Africa, GlaxoSmithKline markets ketazolam under its Solatran brand name. [cite web|url=http://home.intekom.com/pharm/smith_kb/solatran.html|title=SOLATRAN 15 (capsules) - SOLATRAN 30 (capsules)|accessdaymonth=26 Aug|accessyear=2008|date=12|year=1985|month=11|publisher=South African Electronic Package Inserts]

Pharmacokinetics

Ketazolam breaks down in the blood to diazepam which breaks down to demoxepam which breaks down to desmethyldiazepam. [cite journal | journal = Biomed Mass Spectrom. | year = 1984 | month = Jun| volume = 11| issue = 6| pages = 284| title = The decomposition of benzodiazepines during analysis by capillary gas chromatography/mass spectrometry| author = Joyce JR, Bal TS, Ardrey RE, Stevens HM, Moffat AC| pmid = 6743768| doi = 10.1002/bms.1200110607]

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. [cite journal | journal = | year =1980 |month=Nov | volume =41 | issue =11 | pages =386–92 | title =Double-blind comparison of ketazolam, diazepam and placebo in once-a-day vs t.i.d. dosing | author =Anhalt HS |coauthors=Young R, Roginsky M | pmid =6108319 ] [cite journal | journal =Clin Ther | year =1980 | volume =3 | issue =1 | pages =9–14 | title =Anxiolytic efficacy and safety of ketazolam compared with diazepam and placebo | author =Kim KK |coauthors=Sirman A, Trainor FS, Lee BY | pmid =6105920 ] [cite journal | journal =J Int Med Res | year =1976 | volume =4 | issue =1 | pages =50–4 | title =Double-blind placebo-controlled efficacy study of ketazolam (U-28,774) | author =Fabre LF Jr |coauthors= Harris RT | pmid =16791 ] [cite journal | journal =J Clin Pharmacol | year =1980 |month=Oct | volume =20 | issue =10 | pages =581–9 | title =Ketazolam and diazepam in anxiety: a controlled study | author =Rickels K |coauthors=Csanalosi I, Greisman P, Mirman MJ, Morris RJ, Weise CC, Weiss G | pmid =6108335 ] Ketazolam is also an effective antispasmodic drug and is used for the treatment of spasticity. [cite journal | journal =Arch Phys Med Rehabil | year =1986 |month=Aug | volume =67 | issue =8 | pages =556–7 | title =Ketazolam once daily for spasticity: double-blind cross-over study | author =Basmajian JV |coauthors=Shankardass K, Russell D | pmid =2874780 ] [cite journal | journal =Am J Phys Med Rehabil | year =1988 |month=Jun | volume =67 | issue =3 | pages =108–16 | title =Management of spasticity | author =Katz RT | pmid =3288246 | doi =10.1097/00002060-198806000-00004 ] [cite journal | journal =Arch Phys Med Rehabil | year =1984 |month=Nov | volume =65 | issue =11 | pages =698–701 | title =Ketazolam treatment for spasticity: double-blind study of a new drug | author =Basmajian JV |coauthors=Shankardass K, Russell D, Yucel V | pmid =6149738 ]

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. [cite journal | journal =Psychol Med Monogr Suppl | year =1988 | volume =13 | pages =1–55 | title =The natural history of tolerance to the benzodiazepines | author =Higgitt A |coauthors=Fonagy P, Lader M | pmid =2908516 ]

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
url= http://www.fda.gov/oc/opacom/reports/confusingnames.html|title= FDA Public Health Advisory - Consumers Filling U.S. Prescriptions Abroad May Get the Wrong Active Ingredient Because of Confusing Drug Names|accessdaymonth= 26 Aug|accessyear= 2006|author= Food and Drug Administration|authorlink= Food and Drug Administration|year= 2006|month= January|publisher= FDA (USA)]

Legal status

Ketazolam is a Schedule IV drug under the drugs misuse act. [cite web|url= http://www.dea.gov/pubs/scheduling.html|title= Drug Scheduling|accessdaymonth= 26 Aug|accessyear= 2008|author= Drug Enforcement Administration (USA)|authorlink=Drug Enforcement Administration|publisher= United States Government]

ee also

*Benzodiazepine
*List of benzodiazepines
*Benzodiazepine withdrawal syndrome

References