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

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 1 Flurazepam Mechanism of Action 2 Flurazepam Absorption 3 Flurazepam Toxicity 4 Protein Binding 5 Biotransformation 6 Half Life Flurazepam 7 Brand names for Flurazepam

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

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