Description
Zopiclone is only found in individuals that have used or taken this drug. It is a novel hypnotic agent used in the treatment of insomnia. Its mechanism of action is based on modulating benzodiazepine receptors. In addition to zopiclone's benzodiazepine pharmacological properties it also has some barbiturate like properties. Zopiclone exerts its action by binding on the benzodiazepine receptor complex and modulation of the GABABZ receptor chloride channel macromolecular complex. Both zopiclone and benzodiazepines act indiscriminately at the benzodiazepine binding site on α1, α2, α3 and α5 GABAA containing receptors as full agonists causing an enhancement of the inhibitory actions of GABA to produce the therapeutic (hypnotic and anxiolytic) and adverse effects of zopiclone.
Top Gene Interactions
General Information
- Metabolism: Extensively metabolized in the liver via decarboxylation (major pathway), demethylation, and side chain oxidation. Metabolites include an N-oxide derivative (weakly active; approximately 12% of a dose) and an N-desmethyl metabolite (inactive; approximately 16%). Approximately 50% of a dose is converted to other inactive metabolites via decarboxylation. Hepatic microsomal enzymes are apparently not involved in zopiclone clearance. Half Life: Elimination half life is approximately 5 hours (range 3.8 to 6.5 hours) and is prolonged to 11.9 hours in patients with hepatic insufficiency.
- Uses/Sources: For the short-term treatment of insomnia.
- Health Effects: They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive.
- Symptoms: Rare individual instances of fatal outcomes following overdose with racemic zopiclone have been reported in European postmarketing reports, most often associated with overdose with other CNS-depressant agent. Signs and symptoms of overdose effects of CNS depressants can be expected to present as exaggerations of the pharmacological effects noted in preclinical testing.
- Route of Exposure: Rapidly absorbed following oral administration.
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
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-5 |
6135616 19942638 18973287 15291009 20303942 |
|
Translocator protein | Zopiclone exerts its action by binding on the benzodiazepine receptor complex and modulation of the GABABZ receptor chloride channel macromolecular complex. |
17139284 17016423 |
Zopiclone Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Acute lymphoblastic leukemia | 4.3 |
|
Rhabdomyolysis | 4.3 |
|
Nervous System Diseases | 3.83 |
|
Kidney disease | 3.51 |
|