Atovaquone and Proquanil

The Basics

What is Atovaquone and Proquanil?

Used to prevent and treat malaria caused by mosquito bites in countries where malaria is common.

Brand names for Atovaquone and Proquanil

Malarone

How Atovaquone and Proquanil is classified

Anti-infective Agents, Antiparasitic Agents, Antimalarials, Antiprotozoal Agents

Atovaquone and Proquanil During Pregnancy

Atovaquone and Proquanil pregnancy category

Category CNote that the FDA has deprecated the use of pregnancy categories, so for some medications, this information isn’t available. We still think it’s useful to list historical info, however, given what a common proxy this has been in the past.

What we know about taking Atovaquone and Proquanil while pregnant

Atovaquone Atovaquone was not teratogenic and did not cause reproductive toxicity in rats at doses up to 1,000 mg/kg/day corresponding to maternal plasma concentrations up to 7.3 times the estimated human exposure during treatment of malaria based on AUC. In rabbits, atovaquone caused adverse fetal effects and maternal toxicity at a dose of 1,200 mg/kg/day corresponding to plasma concentrations that were approximately 1.3 times the estimated human exposure during treatment of malaria based on AUC. Adverse fetal effects in rabbits, including decreased fetal body lengths and increased early resorptions and post-implantation losses, were observed only in the presence of maternal toxicity. In a pre- and post-natal study in rats, atovaquone did not produce adverse effects in offspring at doses up to 1,000 mg/kg/day corresponding to AUC exposures of approximately 7.3 times the estimated human exposure during treatment of malaria. Proguanil A pre- and post-natal study in Sprague-Dawley rats revealed no adverse effects at doses up to 16 mg/kg/day of proguanil hydrochloride (up to 0.04-times the average human exposure based on AUC). Pre- and post-natal studies of proguanil in animals at exposures similar to or greater than those observed in humans have not been conducted. Atovaquone and Proguanil The combination of atovaquone and proguanil hydrochloride was not teratogenic in pregnant rats at atovaquone:proguanil hydrochloride (50:20 mg/kg/day) corresponding to plasma concentrations up to 1.7 and 0.1 times, respectively, the estimated human exposure during treatment of malaria based on AUC. In pregnant rabbits, the combination of atovaquone and proguanil hydrochloride was not teratogenic or embryotoxic to rabbit fetuses at atovaquone:proguanil hydrochloride (100:40 mg/kg/day) corresponding to plasma concentrations of approximately 0.3 and 0.5 times, respectively, the estimated human exposure during treatment of malaria based on AUC. There are no adequate and well-controlled studies of atovaquone and/or proguanil hydrochloride in pregnant women. MALARONE should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Falciparum malaria carries a higher risk of morbidity and mortality in pregnant women than in the general population. Maternal death and fetal loss are both known complications of falciparum malaria in pregnancy. In pregnant women who must travel to malaria-endemic areas, personal protection against mosquito bites should always be employed in addition to antimalarials. [See PATIENT INFORMATION.] The proguanil component of MALARONE acts by inhibiting the parasitic dihydrofolate reductase [see CLINICAL PHARMACOLOGY]. However, there are no clinical data indicating that folate supplementation diminishes drug efficacy. For women of childbearing age receiving folate supplements to prevent neural tube birth defects, such supplements may be continued while taking MALARONE.

Taking Atovaquone and Proquanil While Breastfeeding

What are recommendations for lactation if you're taking Atovaquone and Proquanil?

No information is available on the use of atovaquone and proguanil during breastfeeding. The Centers for Disease Control and Prevention does not currently recommend it for the prevention of malaria in women breastfeeding infants weighing less than 5 kg (11 pounds). However, it can be used for treatment of women who are breastfeeding infants of any weight when the potential benefit outweighs the potential risk to the infant (e.g., treating a breastfeeding woman who has acquired P. falciparum malaria in an area of multidrug-resistant strains and who cannot tolerate other treatment options).[1] In general, very small amounts of antimalarial drugs are excreted in the breast milk of lactating women. Because the quantity of antimalarial drugs transferred in breast milk is insufficient to provide adequate protection against malaria, infants who require chemoprophylaxis must also receive the recommended dosages of antimalarial drugs.[1]

Maternal / infant drug levels

No information is available on the use of atovaquone and proguanil during breastfeeding. The Centers for Disease Control and Prevention does not currently recommend it for the prevention of malaria in women breastfeeding infants weighing less than 5 kg (11 pounds). However, it can be used for treatment of women who are breastfeeding infants of any weight when the potential benefit outweighs the potential risk to the infant (e.g., treating a breastfeeding woman who has acquired P. falciparum malaria in an area of multidrug-resistant strains and who cannot tolerate other treatment options).[1] In general, very small amounts of antimalarial drugs are excreted in the breast milk of lactating women. Because the quantity of antimalarial drugs transferred in breast milk is insufficient to provide adequate protection against malaria, infants who require chemoprophylaxis must also receive the recommended dosages of antimalarial drugs.[1]

Possible effects of Atovaquone and Proquanil on milk supply

Relevant published information was not found as of the revision date.

Possible alternatives to Atovaquone and Proquanil

None listed