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Atovaquone-Proguanil HCl
Atovaquone-Proguanil HCl is a combination antimalarial medication used for the prevention and treatment of malaria, a parasitic infection transmitted by mosquito bites. The medication combines two active ingredients: atovaquone, which inhibits the parasite's mitochondrial electron transport chain, and proguanil, which inhibits dihydrofolate reductase, an enzyme critical for DNA synthesis in the malaria parasite. This dual-action approach effectively targets the malaria parasite during its liver and blood stages. Atovaquone-Proguanil HCl is commonly used for travelers to malaria-endemic areas and for treating uncomplicated malaria.
Drug Availability and Controlled Substance Status
Atovaquone-Proguanil HCl is available by prescription only. It is not classified as a controlled substance. The medication is typically supplied in tablet form, with different strengths available for both adult and pediatric patients.
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Frequently Asked Questions
How long should I take Atovaquone-Proguanil HCl for malaria prevention?
Start taking Atovaquone-Proguanil HCl 1-2 days before entering a malaria-endemic area, continue taking it daily during your stay, and for 7 days after leaving the area.
Can I take Atovaquone-Proguanil HCl with other medications?
Atovaquone-Proguanil HCl may interact with other medications, especially those affecting the liver or kidneys. Inform your healthcare provider about all medications and supplements you are taking to avoid potential interactions.
What should I do if I miss a dose of Atovaquone-Proguanil HCl?
If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not double the dose to make up for a missed one.
Is Atovaquone-Proguanil HCl safe to use during pregnancy?
Atovaquone-Proguanil HCl should be used during pregnancy only if the potential benefits outweigh the risks. Pregnant women should consult their healthcare provider before using this medication.
Can I stop taking Atovaquone-Proguanil HCl if I feel better?
No, it is important to complete the full course of Atovaquone-Proguanil HCl to ensure the malaria infection is fully treated and to prevent a recurrence. Stopping the medication early can lead to treatment failure.
Comprehensive Drug Guide
How Does Atovaquone-Proguanil HCl Work?
Atovaquone-Proguanil HCl works through a synergistic mechanism:
- Atovaquone: Interferes with the electron transport chain in the mitochondria of the malaria parasite, leading to the collapse of mitochondrial function and ultimately parasite death.
- Proguanil: Inhibits dihydrofolate reductase, an enzyme necessary for the synthesis of folate and, consequently, DNA and RNA. This inhibition disrupts the replication of the parasite’s DNA, preventing its growth and multiplication.
By targeting different aspects of the parasite's lifecycle, this combination effectively reduces the parasite load in the body.
What is Atovaquone-Proguanil HCl Used For?
Atovaquone-Proguanil HCl is FDA-approved for the following uses:
- Prevention of Malaria: It is used to prevent malaria in travelers and others who are at risk of exposure to malaria in endemic areas.
- Treatment of Uncomplicated Malaria: It is used to treat uncomplicated malaria caused by Plasmodium falciparum, including strains resistant to other antimalarial drugs.
Common Dosages
The dosage of Atovaquone-Proguanil HCl depends on whether it is being used for prevention or treatment:
- For Malaria Prevention: Adults typically take one tablet (250 mg atovaquone/100 mg proguanil) daily, starting 1-2 days before entering a malaria-endemic area and continuing for 7 days after leaving the area.
- For Malaria Treatment: Adults typically take four tablets (1,000 mg atovaquone/400 mg proguanil) as a single dose daily for three consecutive days.
For children, the dosage is weight-based, and pediatric tablets (containing lower doses of atovaquone and proguanil) are available.
Typical Dosing
- Prevention of Malaria: One tablet once daily, starting 1-2 days before entering the endemic area, continuing daily during the stay, and for 7 days after leaving the area.
- Treatment of Malaria: Four tablets once daily for three consecutive days.
It is important to take the medication with food or a milky drink to enhance absorption. Tablets should be swallowed whole and not crushed or chewed.
Typical Dosing
Who Shouldn't Take Atovaquone-Proguanil HCl?
Atovaquone-Proguanil HCl is contraindicated in patients with known hypersensitivity to atovaquone, proguanil, or any component of the formulation. It should not be used in patients with severe renal impairment (creatinine clearance <30 mL/min) due to the risk of accumulation and toxicity. Caution is also advised in pregnant or breastfeeding women, as safety data is limited.
Advice From The Pharmacist
Patients taking Atovaquone-Proguanil HCl for malaria prevention should be advised to start the medication 1-2 days before traveling to a malaria-endemic area and continue for the entire duration of their stay, plus 7 days after leaving the area. It is crucial to take the medication with food or a milky drink to improve absorption. Patients should be reminded that no antimalarial is 100% effective, so they should also use protective measures, such as insect repellent, bed nets, and wearing long sleeves and pants. For treatment, patients should complete the full course of medication even if they start feeling better, to ensure the infection is fully cleared.
Side Effects of Atovaquone-Proguanil HCl
Common Side Effects
Common side effects of Atovaquone-Proguanil HCl include nausea, vomiting, abdominal pain, headache, dizziness, and diarrhea. Some patients may experience a mild skin rash or itching. Serious side effects, though rare, can include severe allergic reactions, liver dysfunction, and pancytopenia (a decrease in blood cells). Patients should seek medical attention if they experience signs of an allergic reaction, such as rash, itching, swelling, or difficulty breathing, or if they develop jaundice, dark urine, or unexplained bleeding or bruising.
Risks and Warnings of Atovaquone-Proguanil HCl
Patients with renal impairment should use Atovaquone-Proguanil HCl with caution, as the medication is partially excreted by the kidneys. Liver function should be monitored in patients with pre-existing liver disease. The medication should be used cautiously in pregnant or breastfeeding women, and only if the potential benefits outweigh the risks. As no antimalarial drug provides complete protection, patients should be advised to follow additional preventive measures against mosquito bites.
Interactions with Atovaquone-Proguanil HCl
Common Drug Interactions
Atovaquone-Proguanil HCl may interact with other medications, particularly those that affect kidney function or liver enzymes. Rifampin and rifabutin, which induce liver enzymes, can reduce the levels of atovaquone in the blood, decreasing its effectiveness. Warfarin and other anticoagulants may have increased effects when used with proguanil, leading to a higher risk of bleeding. Patients should inform their healthcare provider of all medications and supplements they are taking to avoid potential interactions.
Alternatives to Atovaquone-Proguanil HCl
Alternative antimalarial medications include:
- Chloroquine: Effective in areas without chloroquine-resistant malaria.
- Doxycycline: Another option for malaria prevention, often used in areas with chloroquine-resistant malaria.
- Mefloquine: Used for both prevention and treatment of malaria, though it has a higher incidence of neuropsychiatric side effects.
- Primaquine: Used for prevention and treatment, particularly for preventing relapses of malaria caused by Plasmodium vivax and Plasmodium ovale.
The choice of antimalarial depends on the specific region of travel, the resistance patterns of the malaria parasite, and the patient’s medical history.