Flurazepam; Indications/Uses, Dosage, Side Effects, Interactions, Pregnancy

Flurazepam
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Flurazepam is a member of the benzodiazepines and a long-acting depressor of the central nervous system (CNS) with sedative and hypnotic effects. Flurazepam binds to a specific site on the benzodiazepine-gamma-aminobutyric acid (GABA)-A-chloride ionophore receptor complex located on the neuronal membrane. Binding causes an allosteric modification of the receptor thereby enhancing the affinity of GABA to the receptor leading to an increase in the frequency of chloride-channel opening events, which leads to an increase in chloride ion conductance, neuronal hyperpolarization, inhibition of the action potential, and a decrease in neuronal excitability. By modulating binding of the GABA inhibitory neurotransmitter to GABA-A receptors in the ascending reticular activating system, flurazepam blocks arousal of the cortical and limbic system, thereby exerting its sedative and hypnotic effect.

Flurazepam is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. It produces a metabolite with a long half-life, which may stay in the bloodstream for days.

Mechanism of Action of Flurazepam

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.

The exact sites and mode of action of the benzodiazepines are unknown. The drugs appear to act at the limbic, thalamic, and hypothalamic levels of the CNS, producing anxiolytic, sedative, hypnotic, skeletal muscle relaxant, and anticonvulsant effects. The effects of benzodiazepines may be mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). Benzodiazepines are capable of producing all levels of CNS depression from mild sedation to hypnosis to coma.
Anxiolytic and possibly paradoxical CNS stimulatory effects of benzodiazepines are postulated to result from release of previously suppressed responses (disinhibition). After usual doses of benzodiazepines for several days, the drugs cause a moderate decrease in rapid eye movement (REM) sleep. REM rebound does not occur when the durgs are withdrawn. Stage 3 and 4 sleep are markedly reduced by usual doses of the drugs; the clinical importance of these sleep stage alterations has not been established. 

Indications of Flurazepam

  • Sleeplessness
  • Insomnia
  • For short-term and intermittent use in patients with recurring insomnia and poor sleeping habits
  • Anti-Anxiety Agents, Benzodiazepine; GABA Modulators; Sedatives, Nonbarbiturate
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Contra-Indications of Flurazepam

  • Myasthenia gravis
  • Acute intoxication with alcohol, narcotics, or other psychoactive substances
  • Ataxia
  • Severe hypoventilation
  • Acute narrow-angle glaucoma
  • Severe liver deficiencies (hepatitis and liver cirrhosis decrease elimination by a factor of 2)
  • Mental Disorder with Loss of Normal Personality & Reality
  • Having Thoughts of Suicide
  • Drug abuse
  • Severe Chronic Obstructed Lung Disease
  • Temporarily Stops Breathing While Sleeping
  • Shock
  • Pregnancy
  • Hypersensitivity or allergy to any drug in the benzodiazepine class

Dosage of Flurazepam

Strengths: 15 mg; 30 mg

Insomnia

  • 15 mg orally once a day at bedtime for women and 15 or 30 mg orally once a day at bedtime for men

Side Effects of Flurazepam

The most common

More common

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Rare

Drug Interactions of Flurazepam

Flurazepam may interact with following drug, supplements, & may change the efficacy of the drug

  • ACE inhibitors, Adrenergic neurone blockers, Angiotensin II receptor antagonists, Beta blockers, Calcium channel blockers, Clonidine, Diazoxide, Diuretics, Hydralazine, Methyldopa, Minoxidil, Nitrates, Sodium Nitroprusside – enhanced hypotensive effect
  • Alcohol, barbiturates, opiates, antihistamines, antipsychotics – increased sedative effect in combination with benzodiazepines.
  • Cimetidine – metabolism of benzodiazepines inhibited by cimetidine (increased plasma concentration)
  • Disulfiram – metabolism of benzodiazepines inhibited by disulfiram (increased sedative effects)
  • Fluvoxamine – plasma concentration of some benzodiazepines increased by fluvoxamine
  • Levodopa – benzodiazepines possibly antagonize effects of levodopa
  • Moxonidine – sedative effects possibly increased when benzodiazepines given with moxonidine
  • Olanzapine – increased risk of hypotension, bradycardia and respiratory depression when parenteral benzodiazepines given with intramuscular olanzapine
  • Phenytoin – benzodiazepines possibly increase or decrease the plasma concentration of phenytoin
  • Rifampicin – metabolism of benzodiazepines possibly accelerated by rifampicin (reduced plasma concentration)
  • Sodium oxybate – benzodiazepines enhance effects of sodium oxybate (avoid concomitant use)

Pregnancy Catagory of Flurazepam

FDA Pregnancy Category N – Not classified.

Pregnancy

Benzodiazepines may cause fetal damage when administered during pregnancy. Therefore, flurazepam should not be used during pregnancy. Women should be warned of the potential risks to the fetus if they become pregnant while taking flurazepam.

Lactation

It is not known if flurazepam crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using flurazepam.

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References

 

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