Insumin: Full Drug Profile

Insumin - General Information

A benzodiazepine derivative used mainly as a hypnotic. [PubChem]

Pharmacology of Insumin

Insumin, 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.

Insumin for patients

To assure the safe and effective use of benzodiazepines, patients should be informed that, since benzodiazepines may produce psychological and physical dependence, it is advisable that they consult with their physician before either increasing the dose or abruptly discontinuing this drug.

Insumin Interactions

No information provided.

Insumin Contraindications

Flurazepam hydrochloride is contraindicated in patients with known hypersensitivity to the drug.

Usage in Pregnancy: Benzodiazepines may cause fetal damage when administered during pregnancy. An increased risk of congenital malformations associated with the use of diazepam and chlordiazepoxide during the first trimester of pregnancy has been suggested in several studies.

Flurazepam hydrochloride is contraindicated in pregnant women. Symptoms of neonatal depression have been reported; a neonate whose mother received 30 mg of flurazepam hydrochloride nightly for insomnia during the 10 days prior to delivery appeared hypotonic and inactive during the first four days of life. Serum levels of N1-desalkyl-flurazepam in the infant indicated transplacental circulation and implicate this long-acting metabolite in this case. If there is a likelihood of the patient becoming pregnant while receiving flurazepam, she would be warned of the potential risks to the fetus. Patients should be instructed to discontinue the drug prior to becoming pregnant. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered.

Additional information about Insumin

Insumin Indication

For short-term and intermittent use in patients with recurring insomnia and poor sleeping habits

Mechanism Of Action

Benzodiazepines bind nonspecifically to bezodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

Drug Interactions

Amprenavir Amprenavir increases the effect and toxicity of benzodiazepine

Food Interactions

Take without regard to meals.

Generic Name

Flurazepam

Synonyms

Flurazepam HCL

Drug Category

Anti-anxiety Agents; GABA Modulators; Hypnotics and Sedatives

Drug Type

Small Molecule; Illicit; Approved

Other Brand Names containing Flurazepam

Dalmane; Felison; Felmane; Flunox; Insumin; Noctosom; Paxane; Somnol; Stauroderm; Valdorm; Dalmadorm;

Absorption

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

Toxicity (Overdose)

Coma, confusion, low blood pressure, sleepiness

Protein Binding

83%

Biotransformation

Flurazepam is rapidly metabolized and is excreted primarily in the urine. Both hydroxyethyl flurazepam (the major metabolite) and N-desalkyl flurazepam are active. The N-desalkyl metabolite is slowly excreted in the urine as the conjugated form

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

Dosage Forms of Insumin

Tablet Oral

Chemical IUPAC Name

7-chloro-1-(2-diethylaminoethyl)-5-(2-fluorophenyl)-3H-1,4-benzodiazepin-2-one

Chemical Formula

C21H23ClFN3O

Flurazepam on Wikipedia

https://en.wikipedia.org/wiki/Flurazepam

Organisms Affected

Humans and other mammals