Definition
A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent.
Description
Temazepam is only found in individuals that have used or taken this drug. It is a benzodiazepine that acts as a gamma-aminobutyric acid modulator and anti-anxiety agent. [PubChem]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 (GABAA) 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.
Top Gene Interactions
General Information
- Metabolism: Hepatic. Temazepam is completely metabolized through conjugation prior to excretion. The major metabolite is the O-conjugate of temazepam (90%). Route of Elimination: Temazepam was completely metabolized through conjugation prior to excretion; 80% to 90% of the dose appeared in the urine. Half Life: 10-20 hours
- Uses/Sources: Officially indicated for severe insomnia and other severe or disabling sleep disorders. For the short-term treatment of insomnia (generally 7-10 days).
- Health Effects: They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive.
- Treatment: If the patient is conscious, vomiting should be induced mechanically or with emetics. Gastric lavage should be employed utilizing concurrently a cuffed endotracheal tube if the patient is unconscious to prevent aspiration and pulmonary complications. Maintenance of adequate pulmonary ventilation is essential. The use of pressor agents intravenously may be necessary to combat hypotension. Fluids should be administered intravenously to encourage diuresis. (L1712)
- Route of Exposure: Oral, well absorbed, minimal first-pass metabolism.
Toxicity
- Carcinogenicity: 3, not classifiable as to its carcinogenicity to humans. (L135)
- Toxicity: LD50: 1963 mg/kg (oral, mice) (L1338) LD50: 1833 mg/kg (oral, rat) (L1338) LD50: >2400 mg/kg (oral, rabbit) (L1338)
Mechanism of Action
Target Name | Mechanism of Action | References |
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Gamma-aminobutyric acid receptor subunit alpha-1 Gamma-aminobutyric acid receptor subunit alpha-2 Gamma-aminobutyric acid receptor subunit alpha-3 Gamma-aminobutyric acid receptor subunit alpha-4 Gamma-aminobutyric acid receptor subunit alpha-5 Gamma-aminobutyric acid receptor subunit alpha-6 Gamma-aminobutyric acid receptor subunit beta-1 Gamma-aminobutyric acid receptor subunit beta-2 Gamma-aminobutyric acid receptor subunit beta-3 Gamma-aminobutyric acid receptor subunit delta Gamma-aminobutyric acid receptor subunit gamma-2 Gamma-aminobutyric acid receptor subunit gamma-3 Gamma-aminobutyric acid receptor subunit pi Gamma-aminobutyric acid receptor subunit rho-1 Gamma-aminobutyric acid receptor subunit rho-2 Gamma-aminobutyric acid receptor subunit gamma-1 Gamma-aminobutyric acid receptor subunit rho-3 Gamma-aminobutyric acid receptor subunit theta Gamma-aminobutyric acid receptor subunit epsilon GABA-A receptor (anion channel) |
17016423 2867566 20138190 6738302 17139284 18384456 11752090 |
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Translocator protein | 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 (GABAA) 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. |
17016423 7911332 17139284 16959136 12850901 |
Temazepam Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Hepatitis C | 3.83 |
|
Osteosarcoma | 3.67 |
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Torsades de pointes | 3.28 |
|
Prostatic Neoplasms | 2.65 |
|
Breast carcinoma | 2.59 |
|