'Flurazepam' (marketed under the brand names 'Dalmane' and 'Dalmadorm') is a drug which is a
benzodiazepine derivative. It possesses
anxiolytic,
anticonvulsant,
sedative and
skeletal muscle relaxant properties.
It has the longest
half-life of all of the benzodiazepines (40-250 hours), and may stay in the bloodstream for up to four days.
[1] Flurazepam is therefore unsuitable as a sleeping medication for some individuals due to next day sedation.
It is used for short-term treatment of patients with
insomnia.
The most common adverse effects are dizziness, drowsiness, lightheadedness and
ataxia. Flurazepam has abuse potential and should never be used with alcohol or any other substance that can cause drowsiness. Addictive and possibly fatal results may occur. Flurazepam users should only take this drug strictly as prescribed, and should only be taken directly before the user plans on sleeping a full night. Next day drowsiness is common.
Flurazepam is a Schedule IV drug under the
Convention on Psychotropic Substances[2].
Pharmacology
Flurazepam has a very long
elimination half life of 40-250 hours, which means the effects of Flurazepam after nighttime administration persist throughout the next day. Residual 'hangover' effects after nighttime administration of flurazepam, such as sleepiness, impaired psychomotor and
cognitive functions, may persist into the next day, which may impair the ability of users to drive safely and increase risks of falls and
hip fractures.
[1]
Flurazepam is
lipophilic, is metabolised hepatically via oxidative pathways. The main pharmacological effects of flurazepam are the enhancement of GABA at the GABA
A receptor.
[2]
Flurazepam shares cross tolerance with barbiturates and
barbiturates can easily be substituted for flurazepam in those who are habituated to barbiturate sedative hypnotics.
[3]
There is preferential storage of flurazepam in some organs including the heart. Absorption by any administered route and the risk of accumulation is significantly increased in the neonate, and there is clinical justification to recommend the withdrawal of flurazepam during pregnancy and breast feeding, as flurazepam is excreted in breast milk.
[4]
A hangover-like effect occurs with flurazepam with impairment of mental arithmetic abilities. After discontinuation of flurazepam a
rebound effect may occur about four days after discontinuation of medication.
[5] (See
benzodiazepine withdrawal syndrome)
Tolerance to the sedative sleep-inducing properties of flurazepam occurs after only seven days administration.
[6]
References
1. Residual effects of hypnotics: epidemiology and clinical implications., Vermeeren A., , , CNS Drugs., 2004
2. [Chemical and pharmacologic aspects of benzodiazepines], Oelschläger H., , , Schweiz Rundsch Med Prax., 1989
3. The use of flurazepam (dalmane) as a substitute for barbiturates and methaqualone/diphenhydramine (mandrax) in general practice., Rooke KC., , , J Int Med Res., 1976
4. Pharmacologic bases of use of benzodiazepines in peréinatal medicine., Olive G, , , Arch Fr Pediatr., 1977
5. A repeated dose comparison of three benzodiazepine derivative (nitrazepam, flurazepam and flunitrazepam) on subjective appraisals of sleep and measures of psychomotor performance the morning following night-time medication., Hindmarch I., , , Acta Psychiatr Scand., 1977
6. Efficacy and side effects of flurazepam, fosazepam, and nitrazepam as sleeping aids in psychogeriatric patients., Viukari M, , , Acta Psychiatr Scand., 1978
External links
★
Rx-List - Flurazepam
★
Inchem - Flurazepam