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Eszopiclone and Kaletra Oral Solution

Determining the interaction of Eszopiclone and Kaletra Oral Solution and the possibility of their joint administration.

Check result:
Eszopiclone <> Kaletra Oral Solution
Relevance: 01.10.2022 Reviewer: Shkutko P.M., M.D., in

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:

Ritonavir may significantly increase the blood levels of eszopiclone. This can increase the risk of side effects including daytime drowsiness, motor impairment, amnesia, anxiety, abnormal thinking, hallucinations, behavioral changes, and breathing difficulties (especially if you have a respiratory disorder such as asthma or obstructive sleep apnea). You may need a dose adjustment or more frequent monitoring by your doctor to safely use both medications. Talk to your doctor if you have any questions or concerns. Your doctor may already be aware of the interaction, but has determined that this is the best course of treatment for you and has taken appropriate precautions and is monitoring you closely for any potential complications. You should avoid the use of alcohol while being treated with eszopiclone. Avoid driving or operating hazardous machinery until you know how the medication affects you, and do not exceed the dosage or frequency of use prescribed by your doctor. Because there may be some residual effects of eszopiclone the day after you take it, it may be advisable to wait at least 12 hours after dosing to drive or operate machinery, even when you may feel fully awake. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Professional:

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.
Eszopiclone

Generic Name: eszopiclone

Brand name: Lunesta

Synonyms: n.a.

Kaletra Oral Solution

Generic Name: lopinavir / ritonavir

Brand name: Kaletra

Synonyms: Kaletra

In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.

Interaction with food and lifestyle
Disease interaction