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modified on 29 April 2009 at 07:34 ••• 4,538 views

Nitrazepam

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Nitrazepam is used to treat short-term sleeping problems (insomnia), such as difficulty falling asleep, frequent awakenings during the night, and early-morning awakening. Nitrazepam is a type of benzodiazepine drug. It is a powerful hypnotic drug which possesses strong sedative, anxiolytic, amnestic, anticonvulsant, and skeletal muscle relaxant properties. Nitrazepam shortens the time required to fall asleep and lengthens the duration of sleep. It is also useful for the management of myoclonic seizures.

Nitrazepam.svg.png
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Nitrazepam
Systematic (IUPAC) name
9-nitro- 6-phenyl- 2,5-diazabicyclo [5.4.0] undeca- 5,8,10,12- tetraen- 3-one
Identifiers
CAS number 146-22-5
ATC code N05CD02
PubChem 4506
DrugBank none
ChemSpider 4350
Chemical data
Formula C15H11N3O3 
Mol. mass 281.3 g/mol
Pharmacokinetic data
Bioavailability 53-94%
Metabolism Hepatic
Half life 16-38 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

D(AU) D(US)

Legal status

Schedule IV (International)

Routes Oral


Contents

Mechanism of Action

Nitrazepam belongs to a group of medicines called benzodiazepines. It acts on benzodiazepine receptors in the brain which are associated with the GABA receptors causing an enhanced binding of GABA (gamma amino butyric acid) to GABAA receptors. GABA is a major inhibitory neurotransmitter in the brain, involved in inducing sleepiness, muscular relaxation and control of anxiety and fits, and slows down the central nervous system. The anticonvulsant properties of nitrazepam and other benzodiazepines may be in part or entirely due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors. Sustained repetitive firing seems to be limited by benzodiazepines effect of slowing recovery of sodium channels from inactivation.

Absorption

Bioavailability is 53-94% following oral administration.

Toxicity

Nitrazepam is a drug which is very frequently involved in drug intoxication, including overdose. Nitrazepam overdose may result in stereotypical symptoms of benzodiazepine overdose including intoxication, impaired balance, slurred speech. In cases of severe overdose this may progress to a comatose state with the possibility of death.


Half Life

15-38 hours (mean elimination half life 26 hours).


Brand names for Nitrazepam

  • Alodorm
  • Apo-nitrazepam tablets BP
  • Apodorm
  • Atempol
  • Benzalin
  • Calsamin
  • Calsmin
  • Cerson
  • Dormicum
  • Dormin-5
  • Dormo-puren
  • Dumolid
  • Eatan
  • Eatan n
  • Epibenzalin
  • Epinelbon
  • Eunoctin
  • Eunoktin
  • Gerson
  • Hipnax
  • Hipsal
  • Ibrovek
  • Imeson
  • Imesont
  • Insomin
  • Ipersed
  • LA 1 (VAN)
  • Magadon
  • Megadon
  • Mitidin
  • Mogadan
  • Mogadon
  • Mogadone
  • Nelbon
  • Nelmat
  • Neozepam
  • Neuchlonic
  • Nitrados
  • Nitravet
  • Nitrazadon
  • Nitrazepam-10
  • Nitrazepam-5
  • Nitrempax
  • Nitrenpax
  • Noctesed
  • Pacisyn
  • Paxisyn
  • Pelson
  • Persopit
  • Radedorm
  • Relact
  • Remnos
  • Sandoz nitrazepam
  • Somitran
  • Somnased
  • Somnibel
  • Somnite
  • Sonebon
  • Sonebon tofraniln a
  • Sonnolin
  • Surem
  • Trazenin
  • Unisomnia