proguanil การใช้

• Prophylaxis with mefloquine was compared to prophylaxis with atovaquone-proguanil.
• Proguanil displays synergism when used in combination with the antimalarial atovaquone.
• It is proposed that drugs such as proguanil act to disrupt retinoid homeostasis.
• Atovaquone-proguanil is an effective alternative in patients unable to tolerate chloroquine.
• This mechanism of action differs from when proguanil was used as a singular agent.
• 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.
• Atovaquone / proguanil has been commercially available from GlaxoSmithKline since 2000, and its patent expired in 2013.
• Proguanil, via its metabolite cycloguanil, functions as a dihydrofolate reductase inhibitor, halting parasitic deoxythymidilate synthesis.
• The combination atovaquone-proguanil may be used in those patients who are unable to take chloroquine for whatever reason.
• Recent research has suggested a role for retinoids in cutaneous adverse effects for a variety of drugs including the antimalarial drug proguanil.
• Atovaquone alone is not indicated for treatment or prevention of malaria as monotherapy ( i . e ., without proguanil ).
• The addition of proguanil has shown to reduce resistance to atovaquone and increase the ability of atovaquone to trigger a mitochondrial apoptotic cascade.
• Some such as proguanil, pyrimethamine and trimethoprim selectively inhibit folate's actions in microbial organisms such as bacteria, protozoa and fungi.
• The combination of atovaquone and proguanil to treat malaria was patented by Glaxo Wellcome in 1999, and its patent protection expired in 2013.
• It combines two medications : atovaquone, used to treat lung infections in immune-compromised patients, and proguanil, an old malaria therapy.
• Roughly 67 % of participants in the mefloquine arm reported greater than or equal to one adverse event, vs 71 % in the atovaquone-proguanil arm.
• In the mefloquine arm, 5 % of the users reported severe events requiring medical attention, vs 1.2 % in the atovaquone-proguanil arm.
• This is commonly referred to as  collapse of the mitochondrial membrane potential .  Proguanil lowers the effective concentration of atovaquone needed to increase permeability of the mitochondrial membrane.
• Lastly, some drugs, such as furazolidone, furoxone, benomyl, fumagillin, proguanil and clamoxyquine, have been shown to impede spore development, which reduces infection rates.