The pharmacokinetic properties of emtricitabine are summarized in Table 8. Following
oral administration of EMTRIVA, emtricitabine is rapidly absorbed with peak plasma concentrations
occurring at 1−2 hours post-dose. In vitro binding of emtricitabine to human plasma proteins is <4% and
is independent of concentration over the range of 0.02−200 μg/mL. Following administration of
radiolabelled emtricitabine approximately 86% is recovered in the urine and 13% is recovered as
metabolites. The metabolites of emtricitabine include 3′-sulfoxide diastereomers and their glucuronic acid
conjugate. Emtricitabine is eliminated by a combination of glomerular filtration and active tubular
secretion. Following a single oral dose of EMTRIVA, the plasma emtricitabine half-life is approximately
10 hours.
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