Definition
A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.
Description
Eszopiclone, marketed by Sepracor under the brand-name Lunesta, is a nonbenzodiazepine hypnotic agent (viz., a sedative) used as a treatment for insomnia. Eszopiclone is the active stereoisomer of zopiclone, and belongs to the class of drugs known as cyclopyrrones. Its main selling point is that it is approved by the U.S. Food and Drug Administration for long-term use, unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia.
General Information
- Metabolism: Following oral administration, eszopiclone is extensively metabolized by oxidation and demethylation. Route of Elimination: Up to 75% of an oral dose of racemic zopiclone is excreted in the urine, primarily as metabolites. Half Life: 6 hours
- Uses/Sources: For the treatment of insomnia
- Symptoms: Side effects include viral infection, dry mouth, dizziness, hallucinations, infection, rash, and unpleasant taste, with this relationship clearest for unpleasant taste depending on doses.
- 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 Gamma-aminobutyric acid receptor subunit alpha-6 Translocator protein GABA-A receptor (anion channel) Sphingosine 1-phosphate receptor 3 |
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