Atovaquone
Pronunciation: uh-TOE-vuh-KWONE
Class: Antiprotozoal
Trade Names
Mepron
- Suspension 750 mg/5 mL
Pharmacology
Inhibits mitochondrial electron transport in metabolic enzymes of microorganisms. This may cause inhibition of nucleic acid and adenosine triphosphate synthesis.
Pharmacokinetics
Absorption
Bioavailability is approximately 47%. Food increases absorption approximately 2-fold. AUC is approximately 280 h•mcg/mL (fed) and approximately 169 h•mcg/mL (fasting). C max is approximately 15.1 mcg/mL (fed) and 8.8 mcg/mL (fasting).
Distribution
Highly lipophilic. May undergo enterohepatic recycling. Vd is 0.6 L/kg. 99.9% protein bound.
Elimination
T 1/2 is 67 to 77.6 h. More than 94% is excreted unchanged in the feces; less than 0.6% is excreted in the urine.
Indications and Usage
Treatment of mild to moderate Pneumocystis carinii pneumonia (PCP) in patients who are intolerant of trimethoprim-sulfamethoxazole and acute oral treatment of mild to moderate PCP in patients who are intolerant to trimethoprim-sulfamethoxazole.
Contraindications
Standard considerations.
Dosage and Administration
Prevention of PCPAdults and children 13 to 16 yr of age
PO 1,500 mg once daily with a meal.
Treatment of Mild to Moderate PCPAdults and children 13 to 16 yr of age
PO 750 mg administered with food twice daily for 21 days (total daily dose, 1500 mg).
Storage/Stability
Do not freeze.
Drug Interactions
FoodFood, particularly fats, increases absorption 3-fold.
Highly protein-bound drugsAtovaquone is highly protein bound; interactions may occur because of competition for binding sites.
RifamycinsDecreases steady-state plasma concentrations of atovaquone and increases steady-state plasma concentrations of rifampin.
Laboratory Test Interactions
None well documented.
Adverse Reactions
CNS
Headache; insomnia; dizziness; anxiety.
Dermatologic
Rash; pruritus.
EENT
Sinusitis; rhinitis; altered taste.
GI
Nausea; diarrhea; vomiting; abdominal pain; constipation; oral monilia; anorexia; dyspepsia.
Genitourinary
Elevated creatinine; elevated BUN.
Hematologic
Anemia; neutropenia.
Hepatic
Elevated liver enzymes.
Respiratory
Increased cough.
Miscellaneous
Fever; sweating; weakness; decreased sodium concentration; elevated amylase; allergic reaction; rhinitis; asthenia; infection; dyspnea.
Precautions
Pregnancy
Category C .
Lactation
Undetermined.
Children
Safety and efficacy not established.
Elderly
Atovaquone has not been systematically evaluated in patients older than 65 yr of age.
Hepatic Function
Use caution and closely monitor administration.
Severe PCP
Treatment of severe episodes of PCP has not been evaluated. Efficacy in patients not responding to trimethoprim-sulfamethoxazole has not been established. Atovaquone has not been evaluated for prophylaxis of PCP.
Patient Information
- Inform patient that medication is most effective when taken with food (particularly fatty foods), and to notify health care provider if unable to eat.
- Inform patient that slight rash may develop while taking medication.
- Teach patient to recognize signs of oral fungal infections.
Copyright © 2009 Wolters Kluwer Health.
More Atovaquone resources
- Atovaquone Monograph (AHFS DI)
- atovaquone Advanced Consumer (Micromedex) - Includes Dosage Information
- atovaquone MedFacts Consumer Leaflet (Wolters Kluwer)
- atovaquone Concise Consumer Information (Cerner Multum)
- Atovaquone and Proguanil Hydrochloride Monograph (AHFS DI)
- Mepron Prescribing Information (FDA)
