Single-Dose Pharmacokinetics of Indinavir and the Effect of Food

Prediction of Nonlinear Intestinal Absorption of CYP3A4 and P-Glycoprotein Substrates from their In Vitro Km Values

“…Indinavir has a high LIN 3A4 value but was predicted to be linear because of a high FaFg value close to 1 ( Table I). The plasma unbound Cmax of indinavir is higher than the Ki value (33), and the saturation of hepatic CYP3A4 may be the cause of the false-negative prediction for indinavir. For predicting nonlinear pharmacokinetics caused by both saturation of intestinal CYP3A4/P-gp and hepatic CYP3A4, this decision tree needs to be used in combination with the reported prediction method for nonlinear pharmacokinetics caused by saturation (inhibition) of hepatic metabolism (34,35).…”

Therapeutic Drug Monitoring of Indinavir in HIV-Infected Patients Undergoing HAART

“…Although IDV is widely used, the optimal range of IDV trough plasma level still remains controversial [3][4][5]11].The results of a retrospective analysis of IDV plasma concentrations from HIV-infected patients at different clinical stages treated with IDV are reported here. Plasma drug concentrations of IDV were determined in patients undergoing therapy with nucleoside reverse-transcriptase inhibitors (NRTI) and IDV alone, or in combination with IDV+RTV.…”

“…Due to limited bioavailability IDV should be taken without food three times a day (t.i.d.). This leads to adherence problems in patients treated with IDV [5]. Loss of viral suppression may be due to suboptimal antiviral potency and selection of an IDV-resistant virus population [6].…”

HIV–TB Drug Interactions

“…Indinavir is extensively (80%) absorbed from an empty stomach, and its bioavailability is decreased when administered with a fatty meal [106]. The addition of ritonavir to indinavir increases bioavailability, regardless of the stomach content [107].…”