| Combination of | |
|---|---|
| Atovaquone | Antimalarial medication |
| Proguanil | Antimalarial medication |
| Clinical data | |
| AHFS/Drugs.com | monograph |
| Licence data | US FDA:link |
| Pregnancy cat. | ? |
| Legal status | POM (UK) ℞ Prescription only |
| Routes | Oral |
| Identifiers | |
| ATC code | P01BB51 |
| PubChem | CID 11954242 |
| ChemSpider | 21230364 |
| KEGG | D02472 |
| (what is this?) (verify) |
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The drug combination atovaquone/proguanil (INNs, trade name Malarone) is an antimalarial medication used in both the treatment and prevention of malaria, commercially available from GlaxoSmithKline since 2000. Atovaquone alone is not indicated for treatment or prevention of malaria as monotherapy (i.e. without proguanil).
A "standard" tablet of Malarone contains 100 mg of proguanil hydrochloride and 250 mg of atovaquone. A "pediatric" tablet of Malarone contains 25 mg of proguanil hydrochloride and 62.5 mg of atovaquone.
Contents |
The adult treatment dose is four "standard" tablets once a day for three days. In children, the drug is prescribed by body weight:
Malarone is not licensed for use in children weighing 10 kg or less. The "pediatric" tablets are not used in malaria treatment.
The advice of a specialist should always be sought when starting malaria treatment. Malarone should not be used to treat severe malaria, when an injectable drug (quinine or artesunate in the UK; quinidine in the US) should be 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.
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 7 days after returning from the malarious area.
The child dose is prescribed according to body weight:
The duration of treatment is the same as for adults.
Proguanil acts as a mitochondrial sensitiser and synergizes with atovaquone; also, there is a high natural frequency of cytochrome B mutants which leads to a high failure rate if atovaquone is used on its own to treat malaria. Specific mutations (Y268S, Y268C) have been shown to confer resistance in vivo,[1][2][3] but there are other mechanisms of resistance that remain unknown.[4]
Malarone is notable for having far fewer side effects than other, older malaria drugs. While some people experience side effects, such as cough, diarrhea, dizziness, headache, loss of appetite, mouth sores, nausea, stomach pain, vomiting, and weakness, the majority have none or few of these.[5]
Atovaquone selectively inhibits the parasitic electron transport chain.
Proguanil, via its metabolite cycloguanil, functions as a dihydrofolate reductase inhibitor, halting parasitic deoxythymidilate synthesis.[6]