Eszopiclone and Zykadia

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Consumer information for this interaction is not currently available.ADJUST DOSE: Coadministration with potent inhibitors of CYP450 3A4 may increase the plasma concentrations of both zopiclone and its pharmacologically active S(-) enantiomer, eszopiclone. Zopiclone has been shown in vitro to be metabolized by CYP450 3A4 and CYP450 2C8, while eszopiclone is primarily metabolized by CYP450 3A4 and 2E1 via demethylation and oxidation. In 18 healthy subjects, administration of a single 3 mg dose of eszopiclone with the potent CYP450 3A4 inhibitor ketoconazole (400 mg daily for 5 days) increased eszopiclone half-life, peak plasma concentration (Cmax) and systemic exposure (AUC) by 1.3-, 1.4- and 2.2-fold, respectively. In 10 healthy young subjects, itraconazole 200 mg daily given for 4 days increased the Cmax and AUC of a single 7.5 mg dose of zopiclone by 29% and 73%, respectively, and prolonged its half-life by 40%. The pharmacokinetics of eszopiclone were not reported in this study. A case report describes an 86-year-old woman who experienced morning drowsiness during coadministration of zopiclone and nefazodone, a known potent CYP450 3A4 inhibitor. Zopiclone plasma concentrations were measured both during and after withdrawal of nefazodone therapy. Following discontinuation of nefazodone due to lack of therapeutic effect, the plasma concentration of S(-) zopiclone decreased from 107 to 16.9 ng/mL, and that of R(+) zopiclone decreased from 20.6 to 1.45 ng/mL. MANAGEMENT: Due to increased risk of next-day psychomotor impairment, the dosages of eszopiclone and zopiclone should be reduced when used with potent CYP450 3A4 inhibitors. The manufacturers recommend that total dose of eszopiclone not exceed 2 mg. An initial dose of 3.75 mg is recommended for zopiclone, which may be increased up to 5 mg if clinically indicated. Patients should be advised to avoid driving or operating hazardous machinery until they know how these medications affect them, preferably at least 12 hours after administration of the hypnotic. References "Product Information. Imovane (zopiclone)." Rhone-Poulenc Rorer Canada Inc, Laval, IN. Dresser GK, Spence JD, Bailey DG "Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition." Clin Pharmacokinet 38 (2000): 41-57 Alderman CP, Gebauer MG, Gilbert AL, Condon JT "Possible interaction of zopiclone and nefazodone." Ann Pharmacother 35 (2001): 1378-80 Becquemont L, Mouajjah S, Escaffre O, Beaune P, Funck-Bretano C, Jaillon P "Cytochrome P-450 3A4 and 2C8 are involved in zopiclone metabolism." Drug Metab Dispos 27 (1999): 1068-73 "Product Information. Lunesta (eszopiclone)." Sepracor Inc, Marlborough, MA. View all 5 references

ADJUST DOSE: Coadministration with potent inhibitors of CYP450 3A4 may increase the plasma concentrations of both zopiclone and its pharmacologically active S(-) enantiomer, eszopiclone. Zopiclone has been shown in vitro to be metabolized by CYP450 3A4 and CYP450 2C8, while eszopiclone is primarily metabolized by CYP450 3A4 and 2E1 via demethylation and oxidation. In 18 healthy subjects, administration of a single 3 mg dose of eszopiclone with the potent CYP450 3A4 inhibitor ketoconazole (400 mg daily for 5 days) increased eszopiclone half-life, peak plasma concentration (Cmax) and systemic exposure (AUC) by 1.3-, 1.4- and 2.2-fold, respectively. In 10 healthy young subjects, itraconazole 200 mg daily given for 4 days increased the Cmax and AUC of a single 7.5 mg dose of zopiclone by 29% and 73%, respectively, and prolonged its half-life by 40%. The pharmacokinetics of eszopiclone were not reported in this study. A case report describes an 86-year-old woman who experienced morning drowsiness during coadministration of zopiclone and nefazodone, a known potent CYP450 3A4 inhibitor. Zopiclone plasma concentrations were measured both during and after withdrawal of nefazodone therapy. Following discontinuation of nefazodone due to lack of therapeutic effect, the plasma concentration of S(-) zopiclone decreased from 107 to 16.9 ng/mL, and that of R(+) zopiclone decreased from 20.6 to 1.45 ng/mL.

MANAGEMENT: Due to increased risk of next-day psychomotor impairment, the dosages of eszopiclone and zopiclone should be reduced when used with potent CYP450 3A4 inhibitors. The manufacturers recommend that total dose of eszopiclone not exceed 2 mg. An initial dose of 3.75 mg is recommended for zopiclone, which may be increased up to 5 mg if clinically indicated. Patients should be advised to avoid driving or operating hazardous machinery until they know how these medications affect them, preferably at least 12 hours after administration of the hypnotic.

Eszopiclone

Generic Name: eszopiclone

Brand name: Lunesta

Synonyms: n.a.

What is Eszopiclone?

Zykadia

Generic Name: ceritinib

Brand name: Zykadia

Synonyms: n.a.

What is Zykadia?