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Ketoconazole (Systemic) and Mefloquine Hydrochloride

Determining the interaction of Ketoconazole (Systemic) and Mefloquine Hydrochloride and the possibility of their joint administration.

Check result:

Ketoconazole (Systemic) <> Mefloquine Hydrochloride

Relevance: 10.08.2023 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:

Using ketoconazole together with mefloquine is not recommended. Ketoconazole may increase the blood levels and effects of mefloquine. High blood levels of mefloquine can cause an irregular heart rhythm that may be serious. Do not take ketoconazole with mefloquine or within 15 weeks of your last dose of mefloquine. You should seek immediate medical attention if you develop sudden dizziness, lightheadedness, fainting, or fast or pounding heartbeats during treatment with mefloquine. 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:

GENERALLY AVOID: Coadministration with ketoconazole may significantly increase the plasma concentrations of mefloquine. The proposed mechanism is ketoconazole inhibition of mefloquine metabolism via hepatic CYP450 3A4. Because mefloquine prolongs the QT interval in a dose-dependent manner, high plasma levels of mefloquine may increase the risk of ventricular arrhythmias such as ventricular tachycardia, ventricular fibrillation, and torsade de pointes. In eight healthy, nonsmoking volunteers, coadministration of mefloquine (500 mg single oral dose on day 6) with ketoconazole (400 mg orally once daily on days 1 to 10) resulted in a 64% increase in the mean mefloquine peak plasma concentration (Cmax) and a 79% increase in systemic exposure (AUC) compared to mefloquine administered alone. The elimination half-life of mefloquine also increased from 322 to 448 hours. The Cmax, AUC, and half-life of mefloquine carboxylic acid metabolite were decreased by 31%, 28%, and 15%, respectively, with ketoconazole. No side effects were reported after mefloquine alone. However, two subjects reported mild headache during ketoconazole coadministration.

MANAGEMENT: Ketoconazole should not be administered with mefloquine or within 15 weeks of the last dose of mefloquine due to increased risk of potentially fatal prolongation of the QTc interval.

References

Ridtitid W, Wongnawa M, Mahatthanatrakul W, Raungsri N, Sunbhanich M "Ketoconazole increases plasma concentrations of antimalarial mefloquine in healthy human volunteers." J Clin Pharm Ther 30 (2005): 285-90
"Product Information. Lariam (mefloquine)." Roche Laboratories, Nutley, NJ.

Ketoconazole (Systemic)

Generic Name: ketoconazole

Brand name: Nizoral

Synonyms: Ketoconazole

What is Ketoconazole (Systemic)?

Mefloquine Hydrochloride

Generic Name: mefloquine

Brand name: Lariam

Synonyms: Mefloquine

What is Mefloquine Hydrochloride?

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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.

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