Nordazepam

Nordazepam

Systematic (IUPAC) name
7-chloro-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one
Clinical data
AHFS/Drugs.com	International Drug Names
Pregnancy cat.	?
Legal status	Schedule IV(US)
Routes	Oral
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic
Half-life	36-200 hours[1]
Excretion	Renal
Identifiers
CAS number	1088-11-5 Y
ATC code	N05BA16
PubChem	CID 2997
DrugBank	none
ChemSpider	2890 Y
UNII	67220MCM01 Y
KEGG	D08283 Y
ChEBI	CHEBI:111762 N
ChEMBL	CHEMBL523 Y
Chemical data
Formula	C15H11ClN2O
Mol. mass	270.71
SMILES	eMolecules & PubChem
InChI InChI=1S/C15H11ClN2O/c16-11-6-7-13-12(8-11)15(17-9-14(19)18-13)10-4-2-1-3-5-10/h1-8H,9H2,(H,18,19) Y Key:AKPLHCDWDRPJGD-UHFFFAOYSA-N Y
N(what is this?)  (verify)

Nordazepam (marketed under brand names Nordaz, Stilny, Madar, Vegesan, and Calmday), also known as desoxydemoxepam, nordiazepam and desmethyldiazepam, is a 1,4-benzodiazepine derivative. Like other benzodiazepine derivatives, it has anticonvulsant, anxiolytic, muscle relaxant and sedative properties. However, it is used primarily in the treatment of anxiety. It is an active metabolite of diazepam, chlordiazepoxide, clorazepate, prazepam, pinazepam, and medazepam.^[2][3]

Side effects

Common side effects of nordazepam include somnolence, which is more common in elderly patients and/or people on high dose regimens. Hypotonia, which is much less common, is also associated with high doses and/or old age.

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.^[4]

Pharmacology

Nordazepam is a partial agonist at the benzodiazepine receptor, which makes it less potent than other benzodiazepines.^[5] The elimination half life is between 36 and 200 hours.^[1]

Abuse

See also: Benzodiazepine drug misuse

Nordazepam and other sedative hypnotic drugs are detected frequently in cases of people suspected of driving under the influence of drugs. Zolpidem and zopiclone are also found in high numbers of suspected drugged drivers. Many drivers have blood levels far exceeding the therapeutic dose range suggesting a high degree of abuse potential for benzodiazepines and zolpidem and zopiclone. ^[6] (Note: Zolpidem and Zopiclone are not Benzodiazepines, but rather nonbenzodiazepine hypnotic drugs intended for sleep, nonetheless they are GABAergic drugs that impair cognitive function to a degree dangerous for driving; all CNS depressants have the ability to severely impair motor function, reaction time, and judgement.)

See also

• Benzodiazepine
• Benzodiazepine dependence
• Benzodiazepine withdrawal syndrome
• Long term effects of benzodiazepines

External links

• Inchem - Nordazepam

References

1. ^ ^{a b} C. Heather Ashton (March 2007). "Benzodiazepine Equivalence Table". benzo.org.uk. http://www.benzo.org.uk/bzequiv.htm. Retrieved 2009-04-05. 
2. ^ Biam. "NORDAZEPAM" (in French). http://www3.biam2.org/www1/Sub2655.html. Retrieved 18 October 2005. 
3. ^ Ator NA, Griffiths RR (September 1997). "Selectivity in the generalization profile in baboons trained to discriminate lorazepam: benzodiazepines, barbiturates and other sedative/anxiolytics". J. Pharmacol. Exp. Ther. 282 (3): 1442–57. PMID 9316858. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=9316858. 
4. ^ Authier, N.; Balayssac, D.; Sautereau, M.; Zangarelli, A.; Courty, P.; Somogyi, AA.; Vennat, B.; Llorca, PM. et al. (November 2009). "Benzodiazepine dependence: focus on withdrawal syndrome". Ann Pharm Fr 67 (6): 408–413. doi:10.1016/j.pharma.2009.07.001. PMID 19900604. 
5. ^ Gobbi M, Barone D, Mennini T, Garattini S (May 1987). "Diazepam and desmethyldiazepam differ in their affinities and efficacies at 'central' and 'peripheral' benzodiazepine receptors". J. Pharm. Pharmacol. 39 (5): 388–91. PMID 2886589. 
6. ^ Jones AW; Holmgren A, Kugelberg FC. (April 2007). "Concentrations of scheduled prescription drugs in blood of impaired drivers: considerations for interpreting the results". Ther Drug Monit. 29 (2): 248–60. doi:10.1097/FTD.0b013e31803d3c04. PMID 17417081.