Overview
| Generic Names: | Flurazepam HCL |
|---|---|
| Trade Names: | Dalmadorm; Dalmane; Felison; Felmane; Flunox; Insumin; Noctosom; Paxane; Somnol; Stauroderm; Valdorm |
| PharmGKB Accession Id: | PA449681 |
Description
A benzodiazepine derivative used mainly as a hypnotic. PubChem (source: Drug Bank)
Indication
For short-term and intermittent use in patients with recurring insomnia and poor sleeping habits (source: Drug Bank)
ATC Therapeutic Category
- N05CD:Benzodiazepine derivatives
Pharmacology, Interactions, and Contraindications
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. (source: Drug Bank)
Pharmacology
Flurazepam, 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. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Take without regard to meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
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 (source: Drug Bank)
Protein Binding
83% (source: Drug Bank)
Absorption
Flurazepam hydrochloride is rapidly (30 minutes) absorbed from the gastrointestinal tract (source: Drug Bank)
Toxicity
Coma, confusion, low blood pressure, sleepiness (source: Drug Bank)
Isomeric SMILES Code:
CCN(CC)CCN1c2ccc(cc2C(=NCC1=O)c3ccccc3F)Cl (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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CYP2E1 |
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Publications |
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GABRA1 |
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Publications |
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GABRB2 |
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Publications |
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GABRG2 |
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Publications |
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SLC22A2 |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| GABRA1 |
|
(source: Drug Bank) |
| GABRA2 |
|
(source: Drug Bank) |
| GABRA3 |
|
(source: Drug Bank) |
| GABRA4 |
|
(source: Drug Bank) |
| GABRA5 |
|
(source: Drug Bank) |
| GABRA6 |
|
(source: Drug Bank) |
| GABRB1 |
|
(source: Drug Bank) |
| GABRB2 |
|
(source: Drug Bank) |
| GABRB3 |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| amprenavir |
|
Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank) |
| cimetidine |
|
Cimetidine increases the effect of the benzodiazepine (source: Drug Bank) |
| clozapine |
|
Increased risk of toxicity (source: Drug Bank) |
| fluconazole |
|
Fluconazole increases the effect of the benzodiazepine (source: Drug Bank) |
| fosamprenavir |
|
Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank) |
| indinavir |
|
The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| itraconazole |
|
The imidazole increases the effect of the benzodiazepine (source: Drug Bank) |
| ketoconazole |
|
The imidazole increases the effect of the benzodiazepine (source: Drug Bank) |
| mephenytoin |
|
Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank) |
| nelfinavir |
|
The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| omeprazole |
|
Omeprazole increases the effect of benzodiazepine (source: Drug Bank) |
| phenytoin |
|
Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank) |
| ritonavir |
|
The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| saquinavir |
|
The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| voriconazole |
|
The imidazole increases the effect of the benzodiazepine (source: Drug Bank) |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.
