II. Mechanism
- Nonbenzodiazepine Hypnotic Agent (Benzodiazepine Receptor Agonist)
- Acts at Gamma-Aminobutyric Acid receptors
- Isomer of Zopiclone (Imovane)
- Schedule IV Controlled Substance
III. Indication
IV. Dosing
- Starting dose: 1 mg orally at bedtime
- Maximum dosing of 1 mg indications
- Severe liver disease
- Concurrent use of CYP 3A4 inhibitor
- Maximum dosing of 2 mg indications
- Older patients (age over 65 years old): 1 mg
- Maximum of 3 mg indications
- Younger, healthy patients
V. Precautions
- These agents have a duration of effect that extends past the time patients awaken
- Eszopiclone (Lunesta) at 3 mg dose can impair driving, coordination and memory for up to 11 hours
- In 2014 FDA released a safety warning to limit maximum dosing of Lunesta
- Start at 1 mg in all patients (similar to the 2013 Ambien warning)
- http://www.fda.gov/Drugs/DrugSafety/ucm397260.htm
VI. Pharmacokinetics
VII. Adverse effects
- Nonbenzodiazepine Hypnotic Agent for common effects
-
Metallic Taste
- Reported in up to 34% of patients on 3 mg
- Very bothersome - discontinuation is common
- Amnesia
- Hallucinations
- Worsening depression
VIII. Resources
Images: Related links to external sites (from Bing)
Related Studies
eszopiclone (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
ESZOPICLONE 1 MG TABLET | Generic | $0.19 each |
ESZOPICLONE 2 MG TABLET | Generic | $0.18 each |
ESZOPICLONE 3 MG TABLET | Generic | $0.12 each |
lunesta (on 12/16/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
LUNESTA 3 MG TABLET | Generic | $0.12 each |
Ontology: Eszopiclone (C1436328)
Definition (NCI) | A nonbenzodiazepine, cyclopyrrolone and active stereoisomer of zopiclone with hypnotic and sedative activity and without significant anxiolytic activity. Although the exact mechanism of action remains to be fully elucidated, eszopiclone is able to bind to and activate the omega-1 subtype of the alpha subunit of the gamma-aminobutyric acid-benzodiazepine GABA receptor complex (GABA-A), a chloride ionophore complex in the central nervous system (CNS). This leads to the opening of chloride channels, causing hyperpolarization, inhibition of neuronal firing, and enhancement of the inhibitory effect of GABA. This eventually leads to a hypnotic effect and allows for an induction of sleep. |
Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
MSH | C515051 |
SnomedCT | 409421001, 409420000 |
English | eszopiclone, (+)-(5S)-6(chloropyridine-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolo(3,4-b)-pyrazin-5-yl-4-methyl-piperazine-1-carboxylate, eszopiclone (medication), (S)-Zopiclone, (+)-(5S)-6-(5-Chloropyridin-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolo(3,4-b)pyrazin-5-yl 4-methylpiperazine-1-carboxylate, ESZOPICLONE, eszopiclone [Chemical/Ingredient], Eszopiclone (product), Eszopiclone (substance), Eszopiclone |
Spanish | eszopiclona (producto), eszopiclona (sustancia), eszopiclona |
Ontology: Lunesta (C1579761)
Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
MSH | C515051 |
English | Lunesta |