Flurazepam

  • IUPAC :7- chloro-1- (2- diethylamino -ethyl ) -5 - (2- fluorophenyl) - 1,3- dihydro-2H- 1,4- benzodiazepin- 2-one
  • Latin: Flurazepamum

N05CD01

White rods or crystals

Benzodiazepines, hypnotics

  • 79.5 ° C
  • 190-220 ° C ( dihydrochloride)

Very slightly soluble in water; slightly soluble in ethanol; practically insoluble in diethyl ether

Attention

  • 980 mg · kg -1 ( LD50, rat, oral)
  • 879 mg · kg -1 ( LD50, Rat, oral, dihydrochloride)

Template: Infobox chemical / molecular formula search available

The flurazepam belongs to the long-acting benzodiazepines. It is used for short-term treatment of disorders of initiating and maintaining sleep.

Pharmacokinetics

The oral bioavailability of flurazepam is very good, it is almost complete absorption instead. In flurazepam is a prodrug. The substance is being implemented rapidly to the pharmacologically active metabolite Hydroxyethylflurazepam and Flurazepamaldehyd and a little less quick to Desalkylflurazepam, the metabolism is probably catalyzed by the cytochrome P450 CYP3A4 and CYP2C19 subgroups. In contrast to the other two metabolites accumulated Desalkylflurazepam whose plasma half-life between 50 and 100 hours. Desalkylflurazepam achieved with multiple doses of flurazepam after several days remains constant plasma concentrations. The maximum plasma concentration of flurazepam, after 1-3 hours, reaches its metabolites depending on which, after 0.5 to 96 hours.

Mechanism of action

Flurazepam reinforced in the central nervous system, the action of the endogenous neurotransmitter GABA. This is done by binding of flurazepam on the GABA receptor.

The effect of flurazepam reduces with an intake of more than 14 days. This is due to the control mechanism, in which the body tries to its original homeostasis restore be steady. In order to keep the effect constant, the dose should be gradually increased, which would lead to dependence.

Side effects

With prolonged use and high doses often leads to drowsiness, dizziness, confusion and memory problems, which also involves an increase in reaction time with them.

During the application of flurazepam may occur due to the enervating effect on the musculature to motion and unsteady gait.

Use in pregnancy and lactation

There is evidence for risks of the human fetus when taken during pregnancy, but the therapeutic benefit to the mother may outweigh. Flurazepam passes into breast milk. Is a regular intake necessary to the weaning is recommended.

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