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 category	?
Legal status	DE: Anlage III (Prescription only) US: Schedule IV
Routes of administration	Oral
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic
Biological half-life	36-200 hours
Excretion	Renal
Identifiers
CAS Number	1088-11-5 Y
ATC code	N05BA16 (WHO)
PubChem	CID: 2997
DrugBank	[2]  N
ChemSpider	2890 Y
UNII	67220MCM01 Y
KEGG	D08283 Y
ChEBI	CHEBI:111762 Y
ChEMBL	CHEMBL523 Y
Chemical data
Formula	C15H11ClN2O
Molecular mass	270.71 g/mol
SMILES ClC1=CC2=C(C=C1)NC(CN=C2C3=CC=CC=C3)=O
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
NY (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.

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

Pharmacology

Nordazepam is a partial agonist at the GABA_A receptor, which makes it less potent than other benzodiazepines, particularly in its amnesic and muscle-relaxing effects. 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. More specifically, nordazepam is hydroxylated to active metabolites including oxazepam, and temazepam before finally being glucuronidated and excreted in the urine.

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. 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.

Recreational use

See also: Benzodiazepine misuse

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.

See also

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

External links

• Inchem - Nordazepam