The mechanism of action, pharmacokinetics and pharmacodynamics, clinic
al efficacy, adverse effects, and dosage of atovaquone in the manageme
nt of mild to moderate Pneumocystis carinii pneumonia (PCP) are review
ed. Atovaquone has a novel mechanism of action that has been hypothesi
zed to result in microbicidal rather than microbistatic activity again
st Pnemocystis carinii. Absorption of the drug is significantly enhanc
ed by the presence of food, particularly food with a high fat content.
In comparative trials, atovaquone was slightly less effective than tr
imethoprim-sulfamethoxazole and as effective as pentamidine isethionat
e in treating mild to moderate PCP. Atovaquone is associated with a lo
wer incidence of treatment-limiting adverse reactions than are trimeth
oprim-sulfamethoxazole and pentamidine isethionate. The most commonly
occurring adverse effect in patients receiving atovaquone is rash, and
the drug does not appear to cause bone marrow suppression. The FDA-ap
proved dosage regimen for atovaquone in treating mild to moderate PCP
is 750 mg (three 250-mg tablets) administered orally three times daily
with food for 21 days. Atovaquone may be considered a first-line trea
tment for patients with the acquired immunodeficiency syndrome who hav
e mild to moderate PCP and have demonstrated an intolerance to trimeth
oprim-sulfamethoxazole.