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Atovaquone/Proguanil

    Brands

    DEA Class; Rx

    Common Brand Names; Malarone

    • Antimalarials

    Oral antimalarial combination with potent synergistic antimalarial activity. Atovaquone is structurally and pharmacologically related to the older antimalarials, lapinone and parvaquone. Proguanil is a synthetic biguanide derivative of pyrimidine and a prodrug for cycloguanil. Certain populations are poor metabolizers (e.g., Asian and African populations) of proguanil. In these patients, conversion of proguanil to cycloguanil is inadequate.

    Indicated for the treatment of malaria.

    For malaria prophylaxis.
    For the treatment of refractory or relapsed babesiosis as part of combination therapy.

    Hypersensitivity

    Prophylaxis in severe renal impairment (CrCl <30 mL/min)

    • Abdominal pain (3-31%)
    • Transaminase increases (17-27%)
    • Headache (3-14%)
    • Vomiting (1-13%)
    • Nausea (12%)
    • Asthenia (8%)
    • Diarrhea (1-8%)
    • Pruritus (6%)
    • Anorexia (5%)
    • Dizziness (5%)
    • Dyspepsia (1-4%)
    • Gastritis (0-3%)

    Administration does not provide radical cure, nor does it prevent delayed primary attacks of P vivax and P ovale

    Patients with severe malaria are not candidates for oral therapy; not evaluated in treatment of cerebral malaria or severe manifestations of malaria (eg, hyperparasitemia, pulmonary edema, renal failure)

    Hepatitis and increased transaminase levels reported with prophylactic use; monitor closely; use caution with existing hepatic impairment; hepatic enzyme elevations may persist for four weeks after treatment has ended

    Not for treatment of cerebral malaria or other severe manifestations of complicated malaria

    Absorption may be reduced in patients with diarrhea or vomiting; monitor closely, and consider antiemetic use; if severe, use alternative antimalarial

    Monotherapy may result in parasite relapse of P vivax malaria

    Recrudescent P falciparum infection or chemoprophylactic failure after monotherapy should be treated with different schizonticide

    Prophylaxis should not be prematurely discontinued; delayed cases of P. falciparum malaria may occur

    Complete prophylaxis includes therapy, protective clothing, insect repellents, and bednets

    No chemoprophylactic regimen is 100% effective; patient should seek medical care for any febrile illness that occurs

    Treatment failure reported in patients >100 kg; monitoring and follow up recommended in this patient group

    P falciparum malaria carries higher risk of death and serious complications in pregnant women; patient should discuss risks and benefits of travel, and if travel cannot be avoided, additional prophylaxis, including protective clothing, must be employed

    Pregnancy category: C

    Lactation: Proguanil is excreted into milk in small quantities, but excretion of atovaquone is unknown; use with caution

    Adults

    Total of atovaquone 250 mg/100 mg (1 tablet) proguanil per day PO for prophylaxis; total of atovaquone 1 g/400 mg proguanil (4 tablets) per day PO for treatment (3 days only).

    Elderly

    Total of atovaquone 250 mg/100 mg (1 tablet) proguanil per day PO for prophylaxis; total of atovaquone 1 g/400 mg proguanil (4 tablets) per day PO for treatment (3 days only).

    Adolescents

    See weight-based dosing for each indication.

    Children

    See weight-based dosing for each indication.

    Infants

    >= 5 kg: See weight-based dosing for each indication.
    < 5 kg: Safety and efficacy have not been established.

    Atovaquone/proguanil

    tablet

    • 250mg/100mg