Atovaquone

0 comments
Absorption The bioavailability of atovaquone is low and variable and is highly dependent on formulation and diet. Bioavailability of the suspension increases two-fold when administered with meals. When administered with food, bioavailability is approximately 47%. Without food, the bioavailability is 23%.
Volume of distribution
  • 0.60 ± 0.17 L/kg
Protein binding Atovaquone is extensively bound to plasma proteins (99.9%) over the concentration range of 1 to 90 µg/mL.
Metabolism
Some evidence suggests limited metabolism (although no metabolites have been identified).
Route of elimination The half-life of atovaquone is long due to presumed enterohepatic cycling and eventual fecal elimination. There was little or no excretion of atovaquone in the urine (less than 0.6%).
Half life 2.2 to 3.2 days
Clearance
  • 10.4 +/- 5.5 ml/min [HIV-infected patients receiving IV administration]
Toxicity The median lethal dose is higher than the maximum oral dose tested in mice and rats (1825 mg/kg per day). Overdoses up to 31,500 mg of atovaquone have been reported. In one such patient who also took an unspecified dose of dapsone, methemoglobinemia occurred. Rash has also been reported after overdose.
Affected organisms
  • Plasmodium

0 comments:

Post a Comment

Copyright 2011 Pharmacokinetics of Drugs.
Blogger Template by Noct.