A Model Based Assessment of Redistribution Dependent Elimination and Bioavailability of Rifabutin

Effects of Fluconazole and Clarithromycin on Rifabutin and 25- O -Desacetylrifabutin Pharmacokinetics

“…A Bayesian approach was applied to simulate a 24-h dosing interval, using a model with parameters for rifabutin from a previous study. Using this model and the previous data (6) as Bayesian priors, we could achieve excellent fits of our data and accurately estimate a 24-h AUC. Rifabutin disposition was well described by a two-compartment model with a lag time for absorption.…”

“…Data were fit by a two-compartment model that included a lag time for oral absorption. Prior literature was used to aid in model construction and parameter estimation (6). Due to the limited number of concentration-time points and short duration of sampling, the data were fit using Bayesian estimation with the ADAPT II pharmacokinetic program (3).…”

Clinical Evaluation of the Nelfinavir‐Rifabutin Interaction in Patients with Tuberculosis and Human Immunodeficiency Virus Infection

“…The AUC for the desacetylrifabutin metabolite is normally about 10% that of the parent compound, with similar antimycobacterial activity. [17][18][19] However, its contribution to toxicity is not well understood. Whereas CYP3A4 only partially metabolizes rifabutin, it predominantly metabolizes desacetyl metabolite; therefore, CYP3A inhibition increases levels of this metabolite more than it raises levels of rifabutin.…”

The effect of grapefruit juice on the time-dependent decline of artemether plasma levels in healthy subjects*1

“…It is unknown which enzymes are involved in this autoinduction, although it was recently found that artemisinin induced omeprazole metabolism in human beings that was associated with increased hydroxylation by CYP 2C19 7 . Autoinduction of drug‐metabolizing enzymes has also been described for rifampin (INN, rifampicin), rifabutin, and carbamazepine and is generally associated with increased CYP3A4 activity 8 , 9 , 10 …”