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

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 REM rebound does not occur when the durgs are withdrawn.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

Dry mouth
muscle trembling, jerking, or stiffness
agitation
anxiety
changes in vision, including blurred vision
dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
Chest pain or tightness
trembling or shaking of the hands or feet
stomach pain or cramping
diarrhea
headache
stomach pain;
back pain, joint or muscle pain.
problems with your vision (including color vision);
sudden chest pain or trouble breathing;
pain or swelling in one or both legs;
migraine headache;
pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or

More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
difficulty with moving
headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in chest
discomfort in arms, shoulders, neck or upper back
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
rust colored urine
decreased amount of urine

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Rare

Anxiety
change in vision
chest pain or tightness
confusion
cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps
muscle spasm or jerking of all extremities
nervousness

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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