- Overview
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Overview
| Generic Names: | DAP; Methyldiazepinone |
|---|---|
| Trade Names: | Alboral; Aliseum; Alupram; Amiprol; An-Ding; Ansiolin; Ansiolisina; Apaurin; Apo-Diazepam; Apozepam; Armonil; Assival; Atensine; Atilen; Bensedin; Bialzepam; Calmocitene; Calmpose; Cercine; Ceregulart; Diacepan; Dialag; Dialar; Diapam; Diastat; Diazemuls; Diazemulus; Diazepam Intensol; Diazepan; Diazetard; Dienpax; Dipam; Dipezona; Dizac; Domalium; Duksen; Duxen; E-Pam; Eridan; Eurosan; Evacalm; Faustan; Faustan,; Freudal; Frustan; Gewacalm; Gihitan; Kabivitrum; Kiatrium; LA III; La-Iii; Lamra; Lembrol; Levium; Liberetas; Mandrozep; Morosan; Neurolytril; Noan; Novazam; Novo-Dipam; Paceum; Pacitran; Paranten; Paxate; Paxel; Plidan; Pms-Diazepam; Pro-Pam; Q-Pam; Q-Pam Relanium; Quetinil; Quiatril; Quievita; Relaminal; Relanium; Renborin; Ruhsitus; Saromet; Sedapam; Sedipam; Seduksen; Seduxen; Serenack; Serenamin; Serenzin; Servizepam; Setonil; Sibazon; Sibazone; Solis; Sonacon; Stesolid; Stesolin; Tensopam; Tranimul; Tranqdyn; Tranquase; Tranquirit; Tranquo-Puren; Tranquo-Tablinen; Umbrium; Unisedil; Usempax Ap; Valaxona; Valeo; Valiquid; Valitran; Valium; Valrelease; Vatran; Velium; Vival; Vivol; Zetran; Zipan |
| PharmGKB Accession Id: | PA449283 |
Description
A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of gamma-aminobutyric acid activity. It is used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome. (From Martindale, The Extra Pharmacopoeia, 30th ed, p589) (source: Drug Bank)
Indication
Used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome. (source: Drug Bank)
ATC Therapeutic Category
- N05BA:Benzodiazepine derivatives
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABA<sub>A</sub>) 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
Diazepam, a benzodiazepine, generates the same active metabolite as chlordiazepoxide and clorazepate. In animals, diazepam appears to act on parts of the limbic system, the thalamus and hypothalamus, and induces calming effects. Diazepam, unlike chlorpromazine and reserpine, has no demonstrable peripheral autonomic blocking action, nor does it produce extrapyramidal side effects; however, animals treated with diazepam do have a transient ataxia at higher doses. Diazepam was found to have transient cardiovascular depressor effects in dogs. Long-term experiments in rats revealed no disturbances of endocrine function. Injections into animals have produced localized irritation of tissue surrounding injection sites and some thickening of veins after intravenous use. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Avoid excessive quantities of coffee or tea (caffeine).
Avoid taking with grapefruit or grapefruit juice as grapefruit can significantly increase serum levels of this product.
Take with food.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic via the Cytochrome P450 enzyme system. The main active metabolite is desmethyldiazepam, in addition to minor active metabolites including temazepam and oxazepam. (source: Drug Bank)
Protein Binding
98.5% (source: Drug Bank)
Absorption
Essentially complete, with a bioavailability of 93%. (source: Drug Bank)
Toxicity
Symptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored. (source: Drug Bank)
Isomeric SMILES Code:
CN1c2ccc(cc2C(=NCC1=O)c3ccccc3)Cl (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
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CYP2C19 |
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Publications |
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CYP2E1 |
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Publications |
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CYP3A |
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Publications |
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CYP3A4 |
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Publications |
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CYP3A5 |
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Publications |
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DBI |
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Publications |
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GABRA1 |
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Publications |
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GABRA6 |
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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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TSPO |
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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 |
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(source: Drug Bank) |
| GABRA2 |
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(source: Drug Bank) |
| GABRA3 |
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(source: Drug Bank) |
| TSPO |
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(source: Drug Bank) |
PharmGKB Curated Pathways
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
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fluoxetine |
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Publications |
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) |
| clarithromycin |
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The macrolide increases the effect of the benzodiazepine (source: Drug Bank) |
| clozapine |
|
Increased risk of toxicity (source: Drug Bank) |
| digoxin |
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The benzodiazepine increases the effect of digoxin (source: Drug Bank) |
| erythromycin |
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The macrolide increases the effect of the benzodiazepine (source: Drug Bank) |
| fluconazole |
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Fluconazole increases the effect of the benzodiazepine (source: Drug Bank) |
| fosamprenavir |
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Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank) |
| indinavir |
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The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| itraconazole |
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The imidazole increases the effect of the benzodiazepine (source: Drug Bank) |
| ketoconazole |
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The imidazole increases the effect of the benzodiazepine (source: Drug Bank) |
| mephenytoin |
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Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank) |
| nelfinavir |
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The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| omeprazole |
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Omeprazole increases the effect of benzodiazepine (source: Drug Bank) |
| phenytoin |
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Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank) |
| rifampin |
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Rifampin decreases the effect of benzodiazepine (source: Drug Bank) |
| ritonavir |
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The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| saquinavir |
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The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| voriconazole |
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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.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
