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词条 Ketazolam
释义

  1. Therapeutic uses

  2. Availability

  3. Tolerance and physical dependence

  4. Contraindications and special caution

  5. Pharmacokinetics

  6. Warnings

  7. Legal status

  8. References

{{Drugbox
| 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]
| image = Ketazolam.svg
| width = 175
| image2 = Ketazolam3d.png
| width2 = 150
| tradename =
| Drugs.com = {{drugs.com|CONS|ketazolam}}
| pregnancy_category =
| legal_CA = Schedule IV
| legal_DE = Rx-only/Anlage III
| legal_US = Schedule IV
| routes_of_administration = Oral
| bioavailability =
| metabolism = Hepatic
| elimination_half-life = 26–200 hours
| excretion = Renal
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 27223-35-4
| ATC_prefix = N05
| ATC_suffix = BA10
| PubChem = 33746
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB01587
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 31110
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 92A214MD7Y
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D04650
| C=20 | H=17 | Cl=1 | N=2 | O=3
| molecular_weight = 368.8
| smiles = ClC1=CC2=C(N(C)C(CN3C(C=C(C)OC32C4=CC=CC=C4)=O)=O)C=C1
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| 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_Ref = {{stdinchicite|correct|chemspider}}
| 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 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]

References

1. ^{{cite journal | journal = Acta Crystallogr C |date=July 2001 | volume = 57 | issue = Pt 7 | pages = 848–50 | title = Ketazolam | author = Vega D |author2=Fernández D |author3=Echeverría G | pmid = 11443263 | doi = 10.1107/S0108270101006175}}
2. ^{{cite journal | journal = The Journal of Clinical Psychiatry|date=November 1980 | 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 |author2=Young R |author3=Roginsky M | pmid =6108319 }}
3. ^{{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 |author2=Sirman A |author3=Trainor FS |author4=Lee BY | pmid =6105920 }}
4. ^{{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 |author2=Harris RT | pmid =16791 }}
5. ^{{cite journal | journal =J Clin Pharmacol |date=October 1980 | volume =20 | issue =10 | pages =581–9 | title =Ketazolam and diazepam in anxiety: a controlled study | author =Rickels K |author2=Csanalosi I |author3=Greisman P |author4=Mirman MJ |author5=Morris RJ |author6=Weise CC |author7=Weiss G | pmid =6108335 | doi=10.1002/j.1552-4604.1980.tb01673.x}}
6. ^{{cite journal | journal =Arch Phys Med Rehabil |date=August 1986 | volume =67 | issue =8 | pages =556–7 | title =Ketazolam once daily for spasticity: double-blind cross-over study | author =Basmajian JV |author2=Shankardass K |author3=Russell D | pmid =2874780 }}
7. ^{{cite journal | journal =Am J Phys Med Rehabil |date=June 1988 | volume =67 | issue =3 | pages =108–16 | title =Management of spasticity | author =Katz RT | pmid =3288246 | doi =10.1097/00002060-198806000-00004 }}
8. ^{{cite journal | journal =Arch Phys Med Rehabil |date=November 1984 | volume =65 | issue =11 | pages =698–701 | title =Ketazolam treatment for spasticity: double-blind study of a new drug | author =Basmajian JV |author2=Shankardass K |author3=Russell D |author4=Yucel V | pmid =6149738 }}
9. ^{{cite web|url=http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html#Ketazolam |title=Benzodiazepine Names |accessdate=26 August 2008 |publisher=The Tranquilliser Recovery and Awareness Place |deadurl=yes |archiveurl=https://web.archive.org/web/20081208054743/http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html |archivedate= 8 December 2008 |df= }}
10. ^{{cite web|url=http://home.intekom.com/pharm/smith_kb/solatran.html|title=SOLATRAN 15 (capsules) - SOLATRAN 30 (capsules)|accessdate=26 August 2008|date=12 November 1985|publisher=South African Electronic Package Inserts}}
11. ^http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-26.html#h-29 {{webarchive|url=https://web.archive.org/web/20131215170432/http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-26.html |date=2013-12-15 }}
12. ^{{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 |author2=Fonagy P |author3=Lader M | pmid =2908516 | doi =10.1017/S0264180100000412 }}
13. ^{{Cite journal | last1 = Authier | first1 = N. | last2 = Balayssac | first2 = D. | last3 = Sautereau | first3 = M. | last4 = Zangarelli | first4 = A. | last5 = Courty | first5 = P. | last6 = Somogyi | first6 = AA. | last7 = Vennat | first7 = B. | last8 = Llorca | first8 = PM. | last9 = Eschalier | first9 = A. | title = Benzodiazepine dependence: focus on withdrawal syndrome. | journal = Ann Pharm Fr | volume = 67 | issue = 6 | pages = 408–13 |date=Nov 2009 | doi = 10.1016/j.pharma.2009.07.001 | pmid = 19900604 }}
14. ^{{cite journal | journal = Biomed Mass Spectrom. |date=June 1984| volume = 11| issue = 6| pages = 284–9| title = The decomposition of benzodiazepines during analysis by capillary gas chromatography/mass spectrometry|vauthors=Joyce JR, Bal TS, Ardrey RE, Stevens HM, Moffat AC | pmid = 6743768| doi = 10.1002/bms.1200110607}}
15. ^{{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 |accessdate=26 August 2006 |author=Food and Drug Administration |authorlink=Food and Drug Administration |date=January 2006 |publisher=FDA (USA) |archiveurl=https://web.archive.org/web/20060812000720/http://www.fda.gov/oc/opacom/reports/confusingnames.html |archivedate=12 August 2006 |deadurl=yes |df= }}
16. ^{{cite web|url= http://www.dea.gov/pubs/scheduling.html|title= Drug Scheduling|accessdate= 26 August 2008|author= Drug Enforcement Administration (USA)|authorlink=Drug Enforcement Administration|publisher= United States Government}}
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