Atovaquone/proguanil
Atovaquone/proguanil is a combination medication used for the treatment and prevention of malaria. It consists of two active ingredients: atovaquone and proguanil. This combination is marketed under the brand name Malarone among others.
Medical Uses[edit]
Atovaquone/proguanil is primarily used for:
- Malaria prophylaxis: It is taken to prevent malaria, especially in travelers to areas where malaria is prevalent.
- Malaria treatment: It is used to treat uncomplicated malaria caused by Plasmodium falciparum, a parasite known for its resistance to other antimalarial drugs.
Mechanism of Action[edit]
The two components of atovaquone/proguanil work synergistically to inhibit the growth of the malaria parasite:
- Atovaquone interferes with the parasite's mitochondrial electron transport chain, which is essential for energy production.
- Proguanil is a prodrug that is converted into its active form, cycloguanil, which inhibits the enzyme dihydrofolate reductase (DHFR), disrupting the parasite's ability to synthesize DNA and replicate.
Dosage and Administration[edit]
The dosage of atovaquone/proguanil varies depending on whether it is being used for prevention or treatment:
- For malaria prophylaxis, it is typically taken once daily, starting 1-2 days before entering a malaria-endemic area, continuing throughout the stay, and for 7 days after leaving the area.
- For malaria treatment, it is usually taken as a three-day course, with one dose taken daily.
Side Effects[edit]
Common side effects of atovaquone/proguanil include:
Serious side effects are rare but can include:
- Severe allergic reactions
- Hepatotoxicity
- Anemia
Contraindications[edit]
Atovaquone/proguanil should not be used in individuals with:
- Severe renal impairment
- Known hypersensitivity to atovaquone, proguanil, or any component of the formulation
Interactions[edit]
Atovaquone/proguanil may interact with other medications, including:
- Rifampin and rifabutin, which can reduce the effectiveness of atovaquone.
- Tetracycline, which can also reduce the effectiveness of atovaquone.
- Metoclopramide, which can decrease the absorption of atovaquone.
Pharmacokinetics[edit]
- Atovaquone has a half-life of approximately 2-3 days and is primarily excreted unchanged in the feces.
- Proguanil has a half-life of about 12-21 hours and is metabolized in the liver to its active form, cycloguanil.
History[edit]
Atovaquone/proguanil was approved for medical use in the late 1990s and has since become a widely used option for both the prevention and treatment of malaria.
See Also[edit]
References[edit]
External Links[edit]
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