Flurazepamum

Uses

Flurazepamum is a hypnotic agent useful for the treatment of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakening. Flurazepamum can be used effectively in patients with recurring insomnia or poor sleeping habits, and in acute or chronic medical situations requiring restful sleep. Sleep laboratory studies have objectively determined that Flurazepamum is effective for at least 28 consecutive nights of drug administration. Since insomnia is often transient and intermittent, short-term use is usually sufficient. Prolonged use of hypnotics is usually not used and should only be undertaken concomitantly with appropriate evaluation of the patient.

Flurazepamum is also used to associated treatment for these conditions: Insomnia

How Flurazepamum works

Flurazepamum 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.

Dosage

Flurazepamum dosage

Oral-Short-term management of insomnia

• Adult: 15-30 mg at night.
• Child: ≥15 yr 15 mg at night.
• Elderly: Max: 15 mg at night.

Side Effects

Increased risk of hazardous sleep-related activities (e.g. sleep-driving), drowsiness, light-headedness, dizziness, confusion, anterograde amnesia, headache, fatigue, reduced alertness, numbed emotions, apnoea, dyspnoea, muscle weakness, ataxia, slurred speech, double vision, vertigo, hypotension, skin rashes, GI and visual disturbances, excessive salivation, changes in libido, urinary retention.

Toxicity

Coma, confusion, low blood pressure, sleepiness

Precaution

Patient with chronic pulmonary insufficiency, personality disorder, depression, resp disease, impaired gag reflex, history of alcohol or drug addiction. Renal and hepatic impairment. Children (<15 yr), elderly or debilitated patient. Lactation.

Interaction

May enhance CNS depressant effect with antidepressants, antipsychotics, general anaesth, hypnotics or sedatives, opioid analgesics. Flurazepamum clearance may be reduced by cimetidine, and may be increased by rifampicin.

Food Interaction

• Avoid alcohol.
• Take with or without food. The absorption is unaffected by food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Flurazepamum Drug Interaction

Moderate: aripiprazole, aripiprazole, lorazepam, lorazepam, duloxetine, duloxetine, escitalopram, escitalopram, pregabalin, pregabalin, fluoxetine, fluoxetine, quetiapine, quetiapine, alprazolam, alprazolamUnknown: amphetamine / dextroamphetamine, amphetamine / dextroamphetamine, cholecalciferol, cholecalciferol

Flurazepamum Disease Interaction

Major: acute alcohol intoxication, closed-angle glaucoma, drug dependence, renal/liver disease, respiratory depression, seizuresModerate: depression, obesity, paradoxical reactions

Elimination Route

Flurazepamum hydrochloride is rapidly (30 minutes) absorbed from the gastrointestinal tract

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

Elimination Route

Flurazepamum 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.

Pregnancy & Breastfeeding use

Category X: Studies in animals or human beings have demonstrated fetal abnormalities or there is evidence of fetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Contraindication

Patient with pre-existing CNS depression or coma, resp depression, acute pulmonary insufficiency, myasthenia gravis, sleep apnoea, chronic psychosis or obsessional states. Pregnancy.

Acute Overdose

Symptoms: Mental confusion, somnolence, lethargy, dysarthria, impaired vision, dystonia to ataxia, unconsciousness, central resp and/or circulatory depression, coma.

Management: Symptomatic and supportive treatment. Induce vomiting or gastric lavage if taken within 1 hr. May admin activated charcoal to reduce absorption. Flumazenil may be used as an adjunct to proper management.

Storage Condition

Store between 15-30°C.

Innovators Monograph

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