Description
Quazepam is only found in individuals that have used or taken this drug. It is a drug which is a benzodiazepine derivative. It induces impairment of motor function and has hypnotic properties. Quazepam is used to treat insomnia.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.
General Information
- Metabolism: Hepatic. Half Life: 39 hours
- Uses/Sources: Quazepam is indicated for the treatment of insomnia including sleep induction and sleep maintenance. [Wikipedia]
- Health Effects: They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive.
- Symptoms: Rebound insomnia, and Benzodiazepine withdrawal syndrome. [Wikipedia]
- Treatment: General supportive measures should be employed, along with intravenous fluids, and an adequate airway maintained. Hypotension may be combated by the use of norepinephrine or metaraminol. Dialysis is of limited value. Flumazenil (Anexate) is a competitive benzodiazepine receptor antagonist that can be used as an antidote for benzodiazepine overdose. In particular, flumazenil is very effective at reversing the CNS depression associated with benzodiazepines but is less effective at reversing respiratory depression. Its use, however, is controversial as it has numerous contraindications. It is contraindicated in patients who are on long-term benzodiazepines, those who have ingested a substance that lowers the seizure threshold, or in patients who have tachycardia or a history of seizures. As a general rule, medical observation and supportive care are the mainstay of treatment of benzodiazepine overdose. Although benzodiazepines are absorbed by activated charcoal, gastric decontamination with activated charcoal is not beneficial in pure benzodiazepine overdose as the risk of adverse effects often outweigh any potential benefit from the procedure. It is recommended only if benzodiazepines have been taken in combination with other drugs that may benefit from decontamination. Gastric lavage (stomach pumping) or whole bowel irrigation are also not recommended.
- Route of Exposure: Bioavailability is 29-35% following oral administration.
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Gamma-aminobutyric acid receptor subunit alpha-2 Gamma-aminobutyric acid receptor subunit alpha-3 Gamma-aminobutyric acid receptor subunit alpha-5 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 epsilon Translocator protein GABA-A receptor (anion channel) |
6738302 2892106 17139284 2867566 3017690 17016423 |
|
Gamma-aminobutyric acid receptor subunit alpha-1 | 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. |
17139284 17016423 |