MALARONE

AbsorptionAtovaquone is a highly lipophilic compound with low aqueous solubility. The bioavailability of atovaquone shows considerable inter‑individual variability.

Effect of FoodMALARONE should be taken with food or a milky drink. Dietary fat taken with atovaquone increases the rate and extent of absorption, increasing AUC 2 to 3 times and C max 5 times over fasting. The absolute bioavailability of the tablet formulation of atovaquone when taken with food is 23%.

DistributionAtovaquone is h...

14.1 Prevention of P. falciparum Malaria MALARONE was evaluated for prophylaxis of P. falciparum malaria in 5 clinical trials in malaria‑endemic areas and in 3 active‑controlled trials in non‑immune travelers to malaria‑endemic areas. Three placebo‑controlled trials of 10 to 12 weeks’ duration were conducted among residents of malaria‑endemic areas in Kenya, Zambia, and Gabon. The mean age of subjects was 30 (range: 17 to 55), 32 (range: 16 to 64), and 10 (range: 5 to 16) years, respectively. Of a total of 669 randomized patients (including 264 pediatric patients aged 5 to 16 years), 103 were ...

• Prophylaxis: Common adverse reactions (≥4%) in adults were diarrhea, dreams, oral ulcers, and headache; these events occurred in a similar or lower proportion of subjects receiving MALARONE than an active comparator. Common adverse reactions (≥5%) in pediatric patients included abdominal pain, headache, cough, and vomiting. ( 6.1 )
• Treatment: Common adverse reactions (≥5%) in adolescents and adults were abdominal pain, nausea, vomiting, headache, diarrhea, asthenia, anorexia, and dizziness. ...

• MALARONE is contraindicated in individuals with known hypersensitivity reactions (e.g., anaphylaxis, erythema multiforme or Stevens-Johnson syndrome, angioedema, vasculitis) to atovaquone or proguanil hydrochloride or any component of the formulation.
• MALARONE is contraindicated for prophylaxis of P. falciparum malaria in patients with severe renal impairment (creatinine clearance <30 mL/min) ...

• Atovaquone absorption may be reduced in patients with diarrhea or vomiting. If used in patients who are vomiting, parasitemia should be closely monitored and the use of an antiemetic considered. In patients with severe or persistent diarrhea or vomiting, alternative antimalarial therapy may be required. ( 5.1 )
• In mixed P. falciparum and Plasmodium vivax infection, P. vivax relapse occurred commonly when patients were treated with MALARONE alone. ( 5.2 )
• In the event of recrudescent P. fal...

7 DRUG INTERACTIONS

• Administration with rifampin or rifabutin is known to reduce atovaquone concentrations; concomitant use with MALARONE is not recommended. ( 7.1 )
• Proguanil may potentiate anticoagulant effect of warfarin and other coumarin-based anticoagulants. Caution advised when initiating or withdrawing MALARONE in patients on anticoagulants; coagulation tests should be closely monitore...