Drug/Small Molecule:
temazepam

2D structure

Overview

Generic Names: Hydroxydiazepam; Methyloxazepam; N-Methyloxazepam; Oxydiazepam
Trade Names: Apo-Temazepam; Cerepax; Crisonar; Euhypnos; Euipnos; Gelthix; Levanxene; Levanxol; Levanzene; Mabertin; Normison; Novo-Temazepam; Perdorm; Planum; Remestan; Restoril; Signopam; Temaz
PharmGKB Accession Id: PA451608

Description

A benzodiazepine that acts as a gamma-aminobutyric acid modulator and anti-anxiety agent. PubChem (source: Drug Bank)

Indication

For the short-term treatment of insomnia (generally 7-10 days). (source: Drug Bank)

ATC Therapeutic Category

  • N05CD:Benzodiazepine derivatives

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Benzodiazepines bind nonspecifically to benzodiazepine receptors, which 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 the inhibitory neurotransmitter 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

Temazepam is a benzodiazepine used as a hypnotic agent in the management of insomnia. Temazepam produces CNS depression at limbic, thalamic, and hypothalamic levels of the CNS. Temazepam increases the affinity of the neurotransmitter gamma-aminobutyric acid (GABA) for GABA receptors by binding to benzodiazepine receptors. Results are sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolytic action. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Avoid avocado.
Avoid excessive quantities of coffee or tea (Caffeine). (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Temazepam is completely metabolized through conjugation prior to excretion. The major metabolite is the O-conjugate of temazepam (90%). (source: Drug Bank)

Protein Binding

96% (source: Drug Bank)

Absorption

Well absorbed, minimal first-pass metabolism. (source: Drug Bank)

Isomeric SMILES Code:

CN1C2=C(C=C(C=C2)Cl)C(=N[C@@H](C1=O)O)C3=CC=CC=C3 (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C19
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
GABRA1
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
GABRB2
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  • PD
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
GABRG2
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Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
UGT2B7
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  • PK
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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
TSPO Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
clozapine Uncurated Annotation Increased risk of toxicity (source: Drug Bank)
mephenytoin Uncurated Annotation Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
phenytoin Uncurated Annotation Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00231
KEGG Drug ID:
D00370
PubChem Compound ID:
5391
PubChem Substance ID:
156664

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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