Nordazepam

Nordazepam

Nordazepam
Systematic (IUPAC) name
7-chloro-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one
Clinical data
AHFS/Drugs.com
Pregnancy
category
  • ?
Legal status
Routes of
administration
Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Biological half-life 36-200 hours[1]
Excretion Renal
Identifiers
CAS Registry Number  Y
ATC code N05
PubChem CID:
DrugBank  N
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI  Y
ChEMBL  Y
Chemical data
Formula C15H11ClN2O
Molecular mass 270.71
 N   

Nordazepam (marketed under brand names Nordaz, Stilny, Madar, Vegesan, and Calmday), also known as desoxydemoxepam 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]

Contents

  • Side effects 1
  • Contraindications and special caution 2
  • Pharmacology 3
  • Pregnancy and nursing mothers 4
  • Recreational use 5
  • See also 6
  • References 7
  • External links 8

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.[3] In fact, changes in liver function associated with aging or diseases such as cirrhosis, may lead to impaired clearance of nordazepam.[4]

Pharmacology

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.[5] Its 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] More specifically, nordazepam is hydroxylated to active metabolites including oxazepam, and temazepam before finally being glucuronidated and excreted in the urine.[6]

Pregnancy and nursing mothers

Nordazepam, like other benzodiazepines, easily crosses the placental barrier, so the drug should not be administered during the first trimester of pregnancy.[7] In case of serious medical reasons, nordazepam can be given in late pregnancy, but the baby, due to the pharmacological action of the drug, may experience side effects such as hypothermia, hypotonia, and sometimes mild respiratory depression. Since nordazepam and other benzodiazepines are excreted in breast milk, the molecule should not be administered to mothers who are breastfeeding. Discontinuing of breast-feeding is indicated for regular intake by the mother.[8]

Recreational use

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 benzodiazepines are commonly used in doses higher than the recommended doses.[9]

See also

References

  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.  
  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.  
  4. ^ Klotz U, Müller-Seydlitz P (January 1979). "Altered elimination of desmethyldiazepam in the elderly". British Journal of Clinical Pharmacology 7 (1): 119–20.  
  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.  
  6. ^ Marland, A (Jan–Feb 1999). "The urinary elimination profiles of diazepam and its metabolites, nordiazepam, temazepam, and oxazepam, in the equine after a 10-mg intramuscular dose.". J Anal Toxicol 23 (1): 29–34.  
  7. ^ Olive G, Rey E (1983). "[Benzodiazepines and pregnancy. Transplacental passage, labor and lactation]". L'Encéphale (in French) 9 (4 Suppl 2): 87B–96B.  
  8. ^ Dusci LJ, Good SM, Hall RW, Ilett KF (January 1990). "Excretion of diazepam and its metabolites in human milk during withdrawal from combination high dose diazepam and oxazepam". British Journal of Clinical Pharmacology 29 (1): 123–6.  
  9. ^ 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.  

External links

  • Inchem - Nordazepam