Introduction
A benzodiazepine derivative used mainly as a hypnotic.
Uses
Flurazepam is a long-acting benzodiazepine with a rapid onset of action that is commonly used to treat insomnia.
For short-term and intermittent use in patients with recurring insomnia and poor sleeping habits
Associated Conditions
Pharmacodynamics
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.
Mechanism of Action
Flurazepam binds to an allosteric site on GABA-A receptors. Binding potentiates the action of GABA on GABA-A receptors by opening the chloride channel within the receptor, causing chloride influx and hyperpolarization.
Absorption
Flurazepam hydrochloride is rapidly (30 minutes) absorbed from the gastrointestinal tract
Protein Binding
83%
Route of Elimination
Flurazepam is rapidly metabolized and is excreted primarily in the urine. Less than 1% of the dose is excreted in the urine as N1-desalkyl-flurazepam.
Half Life
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
Toxicity
Coma, confusion, low blood pressure, sleepiness
Food Interactions
- Avoid alcohol.
- Take with or without food. The absorption is unaffected by food.
Dosage
Elderly or debilitated: 15 mg is usually sufficient for a therapeutic response.
Children: Not recommended.
In hepatic and renal impairment: Dosage may need to be reduced in patients with impaired hepatic or renal function.
