Malarone
| Combination of | |
|---|---|
| Atovaquone | Antimalarial medication |
| Proguanil | Antimalarial medication |
| Clinical data | |
| AHFS/Drugs.com | Monograph |
| License data | |
| Pregnancy category |
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| Routes of administration |
Oral |
| ATC code | |
| Legal status | |
| Legal status |
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| Identifiers | |
| PubChem CID | |
| ChemSpider | |
| KEGG | |
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The drug combination atovaquone/proguanil (INNs, trade names Malarone, Malanil) is an antimalarial medication used in both the treatment and prevention of malaria. Atovaquone alone is not indicated for treatment or prevention of malaria as monotherapy (i.e., without proguanil). Atovaquone/proguanil has been commercially available from GlaxoSmithKline since 2000, and its patent expired in 2013. Malarone has applications for treating chloroquine-resistant malaria.
A standard tablet of Malarone contains 100 mg of proguanil hydrochloride and 250 mg of atovaquone. A pediatric tablet contains 25 mg of proguanil hydrochloride and 62.5 mg of atovaquone.
The adult treatment dose is four standard tablets once a day for three days. In children, the drug is prescribed by body weight:
Atovaquone/proguanil is not licensed for use in children weighing 10 kg or less. The pediatric tablets are not used in malaria treatment, but are used for prophylaxis.
Atovaquone/proguanil is not normally used to treat severe malaria, when an injectable drug such as quinine is used instead.
Medical advice should always be taken before choosing a drug for malaria prevention. Because some strains of malaria are resistant, Malarone is not effective for malaria prevention in all parts of the world. It must be taken with a fatty meal or at least some milk to be absorbed adequately, and to avoid painful stomach irritation which proguanil frequently causes when taken without food. Also, stomach irritation may occur if one lies down within a half hour after taking this medicine.
The adult dose is one standard tablet daily starting one or two days before traveling into a malaria-endemic area, and continuing throughout the stay and then for another seven days after returning from the area.
The child dose is prescribed according to body weight:
The duration of treatment is the same as for adults.
Proguanil acts as a sensitiser and synergizes with atovaquone. When atovaquone is used as a sole agent, a high natural frequency of mutants leads to a high failure rate. This is potentially due to the high lipophilicity and slow uptake of atovaquone, which results in a relatively prolonged period of parasite exposure at ineffective concentrations. Specific mutations (Y268S, Y268C) have been shown to confer resistance in vivo, but the other mechanisms of resistance remain unknown.
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