Atovaquone/Proguanil

Aka: Atovaquone/Proguanil, Malarone

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II. Indications

  1. Malaria Prophylaxis and Treatment (Malarone)
    1. Uncomplicated Plasmodium FalciparumMalaria infection
    2. Regions with artemisinin resistance (Chloroquine or Mefloquine resistance)

III. Contraindications

  1. Creatinine Clearance <30 ml/min
    1. Avoid for Malaria Prophylaxis (and Exercise caution in Malaria treatment)

IV. Mechanism

  1. See Atovaquone
  2. Proguanil is a Biguanide compound that is metabolized to cycloguanil (anti-Malaria agent)

V. Medications

  1. Adult Tablet: Atovaquone 250 mg Proguanil 100 mg
  2. Child Tablet: Atovaquone 62.5 mg Proguanil 25 mg
  3. Administration
    1. Take with food or milk at same time daily
    2. Repeat dose if Vomiting within 1 hour of dose

VI. Dosing: Malaria Prophylaxis

  1. General
    1. Start 1-2 days before travel
    2. Stop 7 days after return
  2. Adult
    1. Take 1 tablet (250 mg/100 mg) orally daily
  3. Children (over age 1 month; weight >5 kg)
    1. Weight 5-8 kg: 1/2 children's tablet orally daily
    2. Weight 9-10 kg: 3/4 tablet orally daily
    3. Weight: 11-20 kg: 1 childrens tablet (62.5/25 mg) orally daily
    4. Weight: 21-30 kg: 2 childrens tablets orally daily
    5. Weight: 31-40 kg: 3 childrens tablets orally daily
    6. Weight: >40 kg (Adult dose): 1 adult tablet (250 mg /100 mg) orally daily

VII. Dosing: Malaria Treatment

  1. Adults
    1. Take 4 tablets (1000 mg/400 mg) orally daily for 3 days
  2. Children (over age 1 month; weight >5 kg)
    1. Weight 5-8 kg: 2 childrens tablets orally daily
    2. Weight 9-10 kg: 3 childrens tablets orally daily
    3. Weight: 11-20 kg: 1 adult tablet (250 mg/100 mg) orally daily
    4. Weight: 21-30 kg: 2 adult tablets orally daily
    5. Weight: 31-40 kg: 3 adult tablets orally daily
    6. Weight: >40 kg (Adult dose): 4 adult tablets orally daily

VIII. Adverse Effects

  1. Common
    1. Headache
    2. Abdominal Pain
    3. Nausea and Vomiting
      1. Consider Antiemetic before dose
  2. Other adverse effects
    1. Nightmares
    2. Insomnia
    3. Oral Ulcers

IX. Safety

  1. Considered safe in Lactation
    1. Avoid in Breast Feeding infants <5 kg
  2. Pregnancy Category C
    1. Lack of safety data (but no reported major birth defects)
    2. Not recommended for Malaria Prophylaxis by CDC

X. Drug Interactions

  1. Atovaquone levels are decreased by other drugs
    1. Efavirenz
    2. Tetracycline
    3. Metoclopramide
  2. Warfarin
    1. INR increased

XI. Resources

  1. Atovaquone Proguanil (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=57d74d71-8cf8-4b10-9420-22954fae623c

XII. References

  1. (2000) Med Lett Drugs Ther 42(1093):109-12 [PubMed]
  2. (2019) Drugs for Malaria Prophylaxis, Med Lett Drugs Ther, p. e104-5
  3. (2023) Presc Lett, Malaria Prophylaxis, Resource #350806

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