Eszopiclone: profile and news

Sleeping pill war will keep you awake  Mar 2, 2006
Two upstarts, however, have appeared on the battlefield: Lunesta, (eszopiclone) marketed by Sepracor and Sonata (zaleplon), produced by King Pharmaceuticals. ... - Common Ground.ca,

DATAMONITOR: Insomnia: Costing Sufferers Sleep & Economies Money  Feb 22, 2006
The market growth will be driven primarily by the launch and continued up-take of Sepracor's Lunesta (eszopiclone), Takeda's non-scheduled, melatonin drug ... - PharmaLive.com (press release),

RECORD SALES OF SLEEPING PILLS ARE CAUSING WORRIES  Feb 7, 2006
...class are frequently referred to as "Z" drugs, a play on both their effect and the Z's in their generic names, like zolpidem (Ambien) and eszopiclone (Lunesta ... - Amherst Times.com,

Heart-Warming Stories of Success  Feb 13, 2006
Their current success story, Lunesta (eszopiclone) is the S enantiomer (the left-handed form) of an older Aventis drug, zopiclone (note the generic name: S ... - Corante,

CNS-Active Drugs

Ethanol

An additive effect on psychomotor performance was seen with coadministration of eszopiclone and ethanol 0.70 g/kg for up to 4 hours after ethanol administration.

Paroxetine

Coadministration of single doses of eszopiclone 3 mg and paroxetine 20 mg daily for 7 days produced no pharmacokinetic or pharmacodynamic interaction.

Lorazepam

Coadministration of single doses of eszopiclone 3 mg and lorazepam 2 mg did not have clinically relevant effects on the pharmacodynamics or pharmacokinetics of either drug.

Olanzapine

Coadministration of eszopiclone 3 mg and olanzapine 10 mg produced a decrease in DSST scores. The interaction was pharmacodynamic; there was no alteration in the pharmacokinetics of either drug.

Drugs That Inhibit CYP3A4 (Ketoconazole)

CYP3A4 is a major metabolic pathway for elimination of eszopiclone. The AUC of eszopiclone was increased 2.2-fold by coadministration of ketoconazole, a potent inhibitor of CYP3A4, 400 mg daily for 5 days. C_max and t_1/2 were increased 1.4-fold and 1.3-fold, respectively. Other strong inhibitors of CYP3A4 (e.g., itraconazole, clarithromycin, nefazodone, troleandomycin, ritonavir, nelfinavir) would be expected to behave similarly.

Drugs That Induce CYP3A4 (Rifampicin)

Racemic zopiclone exposure was decreased 80% by concomitant useof rifampicin, a potent inducer of CYP3A4. A similar effect would be expected with eszopiclone.

Drugs Highly Bound To Plasma Protein

Eszopiclone is not highly bound to plasma proteins (52-59% bound); therefore, the disposition of eszopiclone is not expected to be sensitive to alterations in protein binding. Administration of eszopiclone 3 mg to a patient taking another drug that is highly protein-bound would not be expected to cause an alteration in the free concentration of either drug.

Drugs With A Narrow Therapeutic Index

Digoxin

A single dose of eszopiclone 3 mg did not affect the pharmacokinetics of digoxin measured at steady state following dosing of 0.5 mg twice daily for one day and 0.25 mg daily for the next 6 days.

Warfarin

Eszopiclone 3 mg administered daily for 5 days did not affect the pharmacokinetics of (R)- or (S)-warfarin, nor were there any changes in the pharmacodynamic profile (prothrombin time) following a single 25 mg oral dose of warfarin.