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modified on 29 April 2009 at 06:07 ••• 2,954 views

Flurazepam

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Flurazepam, a benzodiazepine derivative, is a hypnotic agent which does not appear to decrease dream time as measured by rapid eye movements (REM). Furthermore, it decreases sleep latency and number of awakenings for a consequent increase in total sleep time. Flurazepam is mainly used for short-term and intermittent use in patients with recurring insomnia and poor sleeping habits

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Flurazepam
Systematic (IUPAC) name
9-chloro-2-(2-diethylaminoethyl)-
6-(2-fluorophenyl)-2,5-diazabicyclo[5.4.0]undeca-
5,8,10,12-tetraen-3-one
Identifiers
CAS number 17617-23-1
ATC code N05CD01
PubChem 3393
DrugBank APRD00983
Chemical data
Formula C21H23ClFN3O 
Mol. mass 387.88 g/mol
Pharmacokinetic data
Bioavailability 83%
Metabolism Hepatic
Half life 40–250 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

X (Contraindicated in pregnancy)

Legal status

Schedule IV(US)

Routes Oral


Contents

Flurazepam Mechanism of Action

Benzodiazepines bind nonspecifically to bezodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

Flurazepam Absorption

Flurazepam hydrochloride is rapidly (30 minutes) absorbed from the gastrointestinal tract.

Flurazepam Toxicity

Coma, confusion, low blood pressure and sleepiness.

Protein Binding

83%

Biotransformation

Flurazepam is rapidly metabolized and is excreted primarily in the urine. Both hydroxyethyl flurazepam (the major metabolite) and N-desalkyl flurazepam are active. The N-desalkyl metabolite is slowly excreted in the urine as the conjugated form.

Half Life Flurazepam

The mean apparent half-life of flurazepam is 2.3 hours. The half life of elimination of N1-des-alkyl- flurazepam ranged from 47 to 100 hours.

Brand names for Flurazepam

  • Dalmadorm
  • Dalmane
  • Felison
  • Felmane
  • Flunox
  • Insumin
  • Noctosom
  • Paxane
  • Somnol
  • Stauroderm
  • Valdorm