TY - JOUR
T1 - Decreased exposure to saquinavir in HIV-1-infected patients after long-term antiretroviral therapy including ritonavir and saquinavir
AU - Gisolf, Elisabeth H.
AU - Van Heeswijk, Rolf P.G.
AU - Hoetelmans, Richard W.M.
AU - Danner, Sven A.
PY - 2000
Y1 - 2000
N2 - Objective: To explore whether steady-state plasma pharmacokinetics of ritonavir and saquinavir change during long-term treatment in HIV-1-infected patients on antiretroviral treatment including ritonavir and saquinavir. Methods: The pharmacokinetics of ritonavir and saquinavir were assessed during an 8-h period on two occasions in six HIV-1 infected patients on stable twice daily treatment with ritonavir 400 mg, saquinavir 400 mg and stavudine 40 mg with or without lamivudine 150 mg twice daily. Results: The first study day was 4-12 months (median 7 months) after the start of the current regimen. The second study day was 9-15 months (median 10 months) later. No significant differences were observed for the ritonavir pharmacokinetics between the first and second study day. However, median change in plasma trough level of saquinavir between the two study days was -30% (range -79 to +11%; P = 0.06). Median change in maximum plasma concentration was -40% (range -62 to +34%; P = 0.09). The median change in area under the plasma concentration versus time curve over 0-8 h was -33% (range 53 to +21%; P = 0.06). Conclusion: The exposure to saquinavir decreased over time in HIV-infected patients on stable antiretroviral therapy. These data suggest that regular monitoring of plasma drug concentrations should become part of routine patient care even in apparently compliant patients. (C) 2000 Lippincott Williams and Wilkins.
AB - Objective: To explore whether steady-state plasma pharmacokinetics of ritonavir and saquinavir change during long-term treatment in HIV-1-infected patients on antiretroviral treatment including ritonavir and saquinavir. Methods: The pharmacokinetics of ritonavir and saquinavir were assessed during an 8-h period on two occasions in six HIV-1 infected patients on stable twice daily treatment with ritonavir 400 mg, saquinavir 400 mg and stavudine 40 mg with or without lamivudine 150 mg twice daily. Results: The first study day was 4-12 months (median 7 months) after the start of the current regimen. The second study day was 9-15 months (median 10 months) later. No significant differences were observed for the ritonavir pharmacokinetics between the first and second study day. However, median change in plasma trough level of saquinavir between the two study days was -30% (range -79 to +11%; P = 0.06). Median change in maximum plasma concentration was -40% (range -62 to +34%; P = 0.09). The median change in area under the plasma concentration versus time curve over 0-8 h was -33% (range 53 to +21%; P = 0.06). Conclusion: The exposure to saquinavir decreased over time in HIV-infected patients on stable antiretroviral therapy. These data suggest that regular monitoring of plasma drug concentrations should become part of routine patient care even in apparently compliant patients. (C) 2000 Lippincott Williams and Wilkins.
KW - Antiretroviral therapy
KW - Pharmacokinetic profile
KW - Ritonavir
KW - Saquinavir
UR - http://www.scopus.com/inward/record.url?scp=0034073929&partnerID=8YFLogxK
U2 - https://doi.org/10.1097/00002030-200005050-00005
DO - https://doi.org/10.1097/00002030-200005050-00005
M3 - Article
C2 - 10839587
SN - 0269-9370
VL - 14
SP - 801
EP - 805
JO - AIDS
JF - AIDS
IS - 7
ER -