| ATOVAQUONE/PROGUANIL HYDROCHLORIDe
Malarone, Malarone Pediatric
Classifications: antimalarial; Therapeutic: antimalarial
Prototype: Chloroquine HCl & Metronidazole
Pregnancy Category: C
Atovaquone 250 mg/proguanil HCl 100 mg, atovaquone 62.5 mg/proguanil HCl 25 mg tablets
Combination of two antimalarial drugs. Atovaquone inhibits electron transport system in mitochondria of the malaria parasite,
thus interfering with nucleic acid and ATP synthesis of the parasite. Proguanil interferes with DNA synthesis of the malaria
This drug combination has synergistic activity toward malarial treatment because each component has a different mode of
Prevention and treatment of malaria due to P. falciparum, even in chloroquine-resistant areas.
Known hypersensitivity to atovaquone or proguanil; pregnancy (category C); severe malaria.
Cerebral malaria, complicated malaria, pulmonary edema; renal failure, renal impairment; hepatic disease; lactation; older
adults; African Americans, Chinese, Japanese; diarrhea, emesis, GI disease; hepatic disease, infection, sunlight (UV) exposure.
Use in children weighing <9 kg is not established.
Route & Dosage
|Prevention of Malaria
Adult: PO 1 tablet q.d. with food starting 12 d before travel to malarial area and continuing for 7 d after return
Child: PO 1120 kg, 1 pediatric tablet q.d.; 2130 kg, 2 pediatric tablets q.d.; 3140 kg, 3 pediatric tablets q.d.; >40 kg, 1 adult tablet q.d. with food starting 12 d before travel to malarial area and continuing for 7 d after return
Treatment of Malaria
Adult: PO 4 tablets as a single daily dose for 3 d
Child: PO 58 kg, 2 pediatric tablets; 910 kg, 3 pediatric tablets; 1120 kg, 1 adult tablet; 2130 kg, 2 adult tablets; 3140 kg, 3 adult tablets; >40 kg, 4 adult tablets as a single daily dose for 3 d
- Give at the same time each day with food or a drink containing milk.
- Give a repeat dose if vomiting occurs within 1 h after dosing.
Adverse Effects (≥1%)Body as a Whole:
back pain, asthenia, anorexia. Digestive: Nausea, abdominal pain, diarrhea,
dyspepsia. CNS: Headache. Respiratory:
Pruritus. Other: Anaphylactic reaction.
InteractionsDrug: Rifampin, rifabutin, tetracycline
may decrease serum
may decrease absorption.
PharmacokineticsAbsorption: Atovaquone (A),
Poor, absorption improved when taken with a fatty meal; Proguanil (P),
Extensively absorbed. Duration: A,
623 wk after a 3-wk course of therapy. Distribution: A,
Penetrates poorly into cerebrospinal fluid; >99.9% protein bound; P,
75% protein bound. Metabolism: A,
Not metabolized; P,
Metabolized by CYP2C19 to cycloguanil. Elimination: A,
>94% in feces over 21 d (enterohepatically cycled); P,
Primarily in urine. Half-Life: A,
23 d; P,
Assessment & Drug Effects
- Lab tests: Monitor AST and ALT periodically, especially with long-term therapy.
- Monitor for S&S of parasitemia in patients receiving tetracycline and in those experiencing diarrhea or vomiting.
- Note: Only use metoclopramide to control vomiting if other antiemetics are not available.
Patient & Family Education
- Take this drug at the same time each day for maximum effectiveness.
- Note: Absorption of this drug may be reduced with diarrhea and vomiting. Consult physician if either of these occurs.