Atovaquone

Aka: Atovaquone, Mepron

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II. Indications

  1. Human Immunodeficiency Virus (HIV)
    1. Pneumocystis carinii Pneumonia prophylaxis
    2. Pneumocystis carinii Pneumonia treatment
      1. Patients unable to tolerate Bactrim
  2. Babesiosis (off-label)
  3. Toxoplasmosis in HIV Infection (off-label)

III. Contraindications

  1. Creatinine Clearance <30 ml/minute/1.73m2
  2. Breast Feeding of infants under 11 lb (5 kg)

IV. Mechanism

  1. Synthetic hydroxynaphthoquinone with Antiprotozoal activity
  2. Atovaquone blocks mitochondrial electron transport at complex 3 of the respiratory chain of Protozoa
    1. Inhibits Pyrimidine synthesis (and therefore Protozoal DNA synthesis)

V. Dosing: Pneumocystis carinii Pneumonia

  1. Adults (and children age >13 years)
    1. Prophylaxis: 1500 mg orally daily with food
    2. Treatment: 750 mg orally twice daily with food for 21 days

VI. Dosing: Toxoplasmosis in comorbid HIV Infection

  1. Atovaquone is taken in combination with either Sulfadiazine or pyrimethanine-leucovorin
  2. Adults (off-label)
    1. Acute: 1500 mg orally twice daily with food for 6 weeks or more
    2. Chronic: 750 to 1500 mg orally with food twice daily

VII. Dosing: Babesiosis (Mild to Moderate Disease, Off-Label Use)

  1. Taken in combination with Azithromycin (high dose Azithromycin if Immunocompromised)
  2. Adult: 750 mg orally every 12 hours with food
  3. Child: 20 mg/kg (up to 750 mg) orally every 12 hours with food for 7 to 10 days

VIII. Dosing: Malaria

  1. See Atovaquone/Proguanil (Malarone)

IX. Precautions: Poor absorption

  1. Take with food (fatty meal) to ensure absorption
  2. Up to 10% of patients still may not absorb Mepron
  3. Repeat dose if Vomiting occurs within one hour of treatment in adults (within 30 minutes for children)
  4. Tablets may be crushed and mixed with 10 ml water if unable to swallow tablets

X. Efficacy: HIV

  1. Not as clinically active as Bactrim
  2. Pneumocystis Pneumonia treatment Failure rate: 17%
    1. Contrast with 6% for Bactrim

XI. Adverse Effects

  1. Less dose-limiting adverse reactions than Bactrim
    1. Atovaquone: 7%
    2. Bactrim: 20%
  2. Rash
  3. Abdominal Pain
  4. Nausea or Vomiting
  5. Diarrhea
  6. Headache
  7. Mild Liver Function Test abnormalities

XII. Safety

  1. Pregnancy Category C
  2. Unknown safety in Lactation
    1. Contraindicated in Breast Feeding of infants under 11 lb (5 kg)

XIII. Drug Interactions

  1. Reduced plasma levels of Atovaquone (and decreased efficacy)
    1. Efavirenz (avoid)
    2. Rifampin (avoid)
    3. Rifabutin
    4. Rifapentine
    5. Tetracycline
    6. Metoclopramide (Reglan)

XIV. Resources

  1. Atovaquone Suspension (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2445304e-4b4e-4358-b098-31f3c49c52ef

XV. References

  1. (2000) Med Lett Drugs Ther 42(1093):109-12 [PubMed]

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Cost: Medications

atovaquone (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
ATOVAQUONE 750 MG/5 ML SUSP Generic $1.22 per ml
ATOVAQUONE-PROGUANIL 250-100 MG TABLET Generic $2.03 each
ATOVAQUONE-PROGUANIL 62.5-25 Generic $0.63 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

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