Influence of antiretroviral drugs on the pharmacokinetics of prednisolone in HIV-infected individuals.
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Study Design
Authors investigated the influence of antiretroviral (ARV) medications on prednisolone pharmacokinetics in 3 groups of 10 human immunodeficiency virus–infected subjects. One group received lopinavir/ritonavir, and another efavirenz, as part of their ARV regimen; a third group did not receive ARV medications. Each subject received a single 20-mg prednisone dose followed by serial blood sampling for prednisolone. Prednisolone pharmacokinetics were compared among the groups.
Study Results
Area under the concentration–time curve was significantly lower in efavirenz recipients versus subjects receiving lopinavir/ritonavir (geometric mean ratio = 0.60, P = 0.01). Average prednisolone area under the concentration–time curve was higher in subjects taking lopinavir/ritonavir versus subjects not on ARVs; however, this difference was not significant (P > 0.05). Ritonavir increased prednisolone AUC by 30-40% after co-administration in 8 healthy volunteers of RTV 200mg BID and prednisone 20mg
Study Conclusions
These data indicate that prednisolone concentrations may fluctuate widely when human immunodeficiency virus–positive individuals established on efavirenz therapy change to lopinavir/ritonavir or vice versa. No dose adjustments are recommended, but careful monitoring for safety and efficacy is warranted.
References
Busse KH, Formentini E, Alfaro RM, Kovacs JA, Penzac SR. ). influence of antiretroviral drugs on the pharmacokinetics of prednisolone in hiv-infected individuals. Jaids: Journal Of The Acquired Immunodeficiency Syndromes. 2008; 5: 561.
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