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Drug Notebook

Generic Name: eszopiclone

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Lunesta
An anxiolytic - treats Insomnia
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eszopiclone
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(e ZOP i klone)

Drug Interactions

Metabolized principally by CYP3A4 and CYP2E1.

Does not appear to inhibit CYP isoenzymes 1A2, 2A6, 2C9, 2C19, 2D6, 2E1, or 3A4.

Drugs Affecting Hepatic Microsomal Enzymes

Inhibitors of CYP3A4: potential pharmacokinetic interaction (increased plasma eszopiclone concentrations). In patients receiving a potent CYP3A4 inhibitor, initial eszopiclone dosage should not exceed 1 mg; dosage may be increased to 2 mg if clinically indicated.

Inducers of CYP3A4: potential pharmacokinetic interaction (decreased plasma eszopiclone concentrations).

Protein-bound Drugs

Pharmacokinetic interaction unlikely; not highly bound to plasma proteins.

Specific Drugs

Drug Interaction Comments
Antifungals, azoles (itraconazole, ketoconazole) Increased plasma eszopiclone concentrations; 2.2-fold increase in eszopiclone exposure reported following concomitant use of eszopiclone 3 mg and ketoconazole 400 mg Initial eszopiclone dosage should not exceed 1 mg; may increase dosage to 2 mg if clinically indicated
CNS depressants (e.g., psychotropic drugs, anticonvulsants, antihistamines, alcohol) Possible additive CNS-depressant effects Do not use with alcohol; consider dosage reduction if eszopiclone is used concomitantly with other CNS depressants
Digoxin Pharmacokinetic or pharmacodynamic interactions unlikely
HIV protease inhibitors (nelfinavir, ritonavir) Increased plasma eszopiclone concentrations Initial eszopiclone dosage should not exceed 1 mg; may increase dosage to 2 mg if clinically indicated
Lorazepam No clinically important pharmacokinetic or pharmacodynamic interactions observed following single-dose administration of eszopiclone 3 mg with lorazepam 2 mg
Macrolide antibiotics (clarithromycin, troleandomycin) Increased plasma eszopiclone concentrations Initial eszopiclone dosage should not exceed 1 mg; may increase dosage to 2 mg if clinically indicated
Nefazodone Increased plasma eszopiclone concentrations Initial eszopiclone dosage should not exceed 1 mg; may increase dosage to 2 mg if clinically indicated
Olanzapine Decreased psychomotor performance noted following single-dose administration of eszopiclone 3 mg with olanzapine 10 mg; pharmacokinetic interaction unlikely
Paroxetine Pharmacokinetic or pharmacodynamic interactions unlikely; concomitant use (eszopiclone 3 mg and paroxetine 20 mg daily for 7 days) did not alter relevant parameters
Rifampin Decreased plasma eszopiclone concentrations
Warfarin Pharmacokinetic or pharmacodynamic (PT) interactions unlikely

Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed following oral administration, with peak plasma concentration attained in about 1 hour.

Food

High-fat meal decreases peak plasma concentration by 21% and prolongs the time to peak plasma concentration by about 1 hour; effect on sleep onset may be decreased.

Special Populations

In geriatric patients, AUC is increased by 41% compared with younger adults.

In patients with severe hepatic impairment, systemic exposure is 2 times higher than in healthy individuals.

Distribution

Plasma Protein Binding

Approximately 52–59%.

Elimination

Metabolism

Extensively metabolized via oxidation and demethylation, principally by CYP3A4 and CYP2E1 to 2 major metabolites; (S)-N-desmethyl zopiclone is considerably less active than the parent drug, and (S)-zopiclone-N-oxide is inactive.

Elimination Route

Racemic zopiclone excreted principally in urine (75%), mainly as metabolites. Similar excretion profile expected for eszopiclone, the S-isomer of racemic zopiclone; <10% of eszopiclone dose excreted unchanged in urine.

Half-life

Approximately 6 hours.

Special Populations

In geriatric patients, half-life is approximately 9 hours.

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).

Actions

  • Interacts with the CNS GABAA-receptor complex at binding domains located close to or allosterically coupled to benzodiazepine receptors.
  • Pharmacologically similar to zaleplon and zolpidem.
  • Structurally unrelated to benzodiazepines and other sedative and hypnotic agents that are commercially available in the US, including barbiturates, imidazopyridines (e.g., zolpidem), and pyrazolopyrimidines (e.g., zaleplon).
  • S-enantiomer of zopiclone (a hypnotic agent not commercially available in the US).
  • Binding affinity (in vitro) for benzodiazepine receptors is about 50 times that of the R-enantiomer of racemic zopiclone.

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Uses Dosage and Administration Cautions Drug Interactions Pharmacokinetics Stability Actions Advice to Patients Preparations
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