- Eszopiclone is a single-isomer, nonbenzodiazepine, cyclopyrrolone agent that has demonstrated efficacy with both polysomnography (PSG) and patient-reported measures in non-elderly adults with chronic primary insomnia in long-term and short-term studies.
- Following oral administration in healthy adults, maximum eszopiclone plasma drug concentration (Tmax) occurs at 1 hour post-dose.7 Eszopiclone is primarily metabolized by CYP3A4 and CYP2E1 to (S)-N-desmethylzopiclone and (S)-zopiclone-N-oxide.
- The pharmacokinetics (PK) for eszopiclone are linear over the range of 1.0 to 6.0 mg daily in adults.
- Two Phase I studies were conducted in pediatric subjects with attention deficit hyperactivity disorder (ADHD) associated insomnia to characterize the safety and PK profile following single dose administration at bedtime.
- Pharmacokinetic modeling and simulation were used in the clinical development program for eszopiclone in pediatric insomnia, in part, as a basis for dose selection.
American Academy of Child & Adolescent Psychiatry (AACAP), Toronto, Ontario, October 2011
By G. Maier, Q. Lu, J. Blumer, B. Robertson, J. Zummo, Elizabeth Ludwig