| Indication | For the treatment of insomnia |
| Pharmacodynamics | Eszopiclone is a nonbenzodiazepine hypnotic, pyrrolopyrazine derivative of the cyclopyrrolone class and is indicated for the short-term treatment of insomnia. While Eszopiclone is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Eszopiclone binds selectively to the brain alpha subunit of the GABA A omega-1 receptor. |
| Mechanism of action | The mechanism of action of Eszopiclone is not completely understood. It is thought that Eszopiclone acts on the benzodiazepine receptors as an agonist and interacts with GABA-receptor complexes. |
| Absorption | Rapidly absorbed following oral administration |
| Volume of distribution | Not Available |
| Protein binding | 52-59% |
| 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 |
| Clearance | Not Available |
| Toxicity | Side effects include viral infection, dry mouth, dizziness, hallucinations, infection, rash, and unpleasant taste, with this relationship clearest for unpleasant taste depending on doses. |