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
category
  •  ?
Legal status
Routes of
administration
Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Biological half-life 36-200 hours[1]
Excretion Renal
Identifiers
CAS Number 1088-11-5 YesY
ATC code N05BA16 (WHO)
PubChem CID: 2997
DrugBank [2] [2] N
ChemSpider 2890 YesY
UNII 67220MCM01 YesY
KEGG D08283 YesY
ChEBI CHEBI:111762 YesY
ChEMBL CHEMBL523 YesY
Chemical data
Formula C15H11ClN2O
Molecular mass 270.71 g/mol
 NYesY (what is this?)  (verify)

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.[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] In fact, changes in liver function associated with aging or diseases such as cirrhosis, may lead to impaired clearance of nordazepam.[5]

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.[6] 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.[7]

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.[8] 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.[9]

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.[10]

See also

References

  1. 1.0 1.1 C. Heather Ashton (March 2007). "Benzodiazepine Equivalence Table". benzo.org.uk. Retrieved 2009-04-05.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  2. "DrugBank. Showing metabolite Nordiazepam (DBMET00113)". DrugBank. DrugBank Version 4.3. Retrieved 1 December 2015.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  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.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
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  8. Olive G, Rey E (1983). "[Benzodiazepines and pregnancy. Transplacental passage, labor and lactation]". L'Encéphale (in French). 9 (4 Suppl 2): 87B–96B. PMID 6144535. |access-date= requires |url= (help) <templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
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External links