II. Indications

  1. Human Immunodeficiency Virus (HIV)
    1. Pneumocystis carinii Pneumonia prophylaxis
    2. Pneumocystis carinii Pneumonia treatment
    3. Patients unable to tolerate Bactrim
  2. Malaria Prophylaxis and Treatment (Malarone)
    1. Third line agent (Mefloquine preferred)
  3. Babesiosis

III. Contraindications

  1. Creatinine Clearance <30 ml/minute/1.73m2
  2. Pregnancy Category C
  3. Breast Feeding of infants under 11 klb (5 kg)

IV. Dosing: Pneumocystis carinii Pneumonia

  1. Prophylaxis: 1500 mg PO qd with food
  2. Treatment: 750 mg PO bid with food for 21 days

V. Dosing: Malaria (Atovaquone/Proguanil or Malarone)

  1. Adults
    1. Prophylaxis: 1 tablet (250 mg/100 mg) orally daily
      1. Start 1-2 days before travel
      2. Stop 7 days after return
    2. Treatment: 4 tablets (1000 mg/400 mg) orally daily for 3 days
  2. Children (over age 1 month)
    1. Weight 5-8 kg
      1. Prophylaxis: 1/2 tablet (62.5 mg /25 mg) orally daily
    2. Weight 9-10 kg
      1. Prophylaxis: 3/4 tablet (62.5 mg /25 mg) orally daily
    3. Weight: 11-20 kg
      1. Prophylaxis: 1 tablet (62.5 mg /25 mg) orally daily
      2. Treatment: 1 tablet (250 mg/100 mg) orally daily
    4. Weight: 21-30 kg
      1. Prophylaxis: 1 tablet (125 mg /50 mg) orally daily
      2. Treatment: 2 tablet (250 mg/100 mg) orally daily
    5. Weight: 31-40 kg
      1. Prophylaxis: 1 tablet (187.5 mg /75 mg) orally daily
      2. Treatment: 3 tablet (250 mg/100 mg) orally daily
    6. Weight: >40 kg (Adult dose)
      1. Prophylaxis: 1 tablet (250 mg /100 mg) orally daily
      2. Treatment: 4 tablet (250 mg/100 mg) orally daily

VI. Precautions: Poor absorption

  1. Take with food (fatty meal) to ensure absorption
  2. Up to 10% of patients still may not absorb Mepron

VII. Efficacy: HIV

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

VIII. 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

IX. Drug Interactions: Reduced plasma levels of Atovaquone

  1. Tetracycline
  2. Metoclopramide (Reglan)
  3. Rifampin

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Cost: Medications

atovaquone (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
ATOVAQUONE 750 MG/5 ML SUSP Generic $2.62 per ml
ATOVAQUONE-PROGUANIL 250-100 MG TABLET Generic $4.14 each
mepron (on 1/1/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
MEPRON 750 MG/5 ML SUSPENSION Generic $2.62 per ml

Ontology: Atovaquone (C0165603)

Definition (NCI) A synthetic hydroxynaphthoquinone with antiprotozoal activity. Atovoquone blocks the mitochondrial electron transport at complex III of the respiratory chain of protozoa, thereby inhibiting pyrimidine synthesis, preventing DNA synthesis and leading to protozoal death.
Definition (CSP) broad-spectrum antiparasitic drug found to be active against Pneumocystis carinii pneumonia in AIDS patients.
Definition (MSH) A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D053626
SnomedCT 391793007, 108718008, 386899002
LNC LP94829-6, MTHU031993
English atovaquone, 2-(4-(4'-chlorophenyl)cyclohexyl)-3-hydroxy-1,4-naphthoquinone, 2-(trans-4-(4-chlorophenyl)cyclohexyl)-3-hydroxy-1,4-naphthoquinone, Atovaquone, 3-(4-(4-chlorophenyl)cyclohexyl)-4-hydroxy-naphthalene-1,2-dione, atovaquone (medication), ATOVAQUONE, Atovaquone [Chemical/Ingredient], Atovaquone - chemical, Atovaquone - chemical (substance), Atovaquone (product), Atovaquone (substance)
Portuguese Atovaquona
Spanish Atovacuona, Atovaquona, atovacuona (producto), atovacuona (sustancia), atovacuona
Russian АТОВАКОН, ATOVAKON
Italian Atovaquone
German Atovaquon, 2-(4-(4'-chlorophenyl)cyclohexyl)-3-hydroxy-1,4-naphthoquinon, 2-(trans-4-(4-chlorophenyl)cyclohexyl)-3-hydroxy-1,4-naphthoquinon
French Atovaquone, 2-(4-(4'-Chlorophényl)cyclohexyl)-3-hydroxy-1,4-naphtoquinone
Czech 2-(trans-4-(4-chlorfenyl)cyklohexyl)-3-hydroxy-1,4-naftochinon, atovachon, 2-(4-(4'-chlorfenyl)cyklohexyl)-3-hydroxy-1,4-naftochinon
Finnish Atovakvoni
Japanese アトバコン
Swedish Atovakvon
Polish Atowakon

Ontology: Mepron (C0378468)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D053626
English Mepron, Wellvone, Glaxo Wellcome brand of atovaquone, GlaxoSmithKline brand of atovaquone, atovaquone GlaxoSmithKline brand, mepron
German Wellvone, Mepron
French Malarone, Wellvone, Mepron
Czech Mepron

Ontology: Malarone (C0595490)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C109496
English Malarone, malarone, GlaxoSmithKline brand of atovaquone-proguanil