Nordazepam

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Nordazepam
Nordazepam.svg
Nordazepam3d.png
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 YesY
ATC code N05BA16
PubChem CID 2997
DrugBank none
ChemSpider 2890 YesY
UNII 67220MCM01 YesY
KEGG D08283 YesY
ChEBI CHEBI:111762 YesY
ChEMBL CHEMBL523 YesY
Chemical data
Formula C15H11ClN2O 
Mol. mass 270.71
 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 amnesic, 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]

Side effects[edit]

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[edit]

Benzodiazepines require special precaution if used in the elderly, during pregnancy, in children, alcohol- or drug-dependent individuals and individuals with comorbid psychiatric disorders.[3]

Pharmacology[edit]

Nordazepam is a partial agonist at the GABAA receptor, which makes it less potent than other benzodiazepines, particularly in its amnesic and muscle relaxing effects.[4] The elimination half life is between 36 and 200 hours, with wide variation among individuals, factors such as age and gender are known to impact it.[1]

Abuse[edit]

Nordazepam and other sedative hypnotic drugs are detected frequently in cases of people suspected of driving under the influence of drugs. Many drivers have blood levels far exceeding the therapeutic dose range suggesting a high degree of abuse potential for benzodiazepines. [5]

See also[edit]

External links[edit]

References[edit]

  1. ^ a b C. Heather Ashton (March 2007). "Benzodiazepine Equivalence Table". benzo.org.uk. Retrieved 2009-04-05. 
  2. ^ 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. 
  3. ^ Authier, N.; Balayssac, D.; Sautereau, M.; Zangarelli, A.; Courty, P.; Somogyi, AA.; Vennat, B.; Llorca, PM.; Eschalier, A. (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. 
  4. ^ 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. 
  5. ^ 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.