Lopinavir cerebrospinal fluid steady-state trough concentrations in HIV-infected adults

The Annals of Pharmacotherapy
Robert DiCenzoGiovanni Schifitto

Abstract

The central nervous system may act as a sanctuary site for viral replication in the setting of low antiretroviral penetration. Data on lopinavir cerebrospinal fluid (CSF) trough concentration (C(trough)) values have yet to be reported. To describe lopinavir CSF C(trough) values and compare them with a measure of HIV susceptibility. In a prospective, open-label design, HIV-infected adults whose regimen included lopinavir/ritonavir 400/100-mg soft-gel capsules twice daily for at least 4 weeks were enrolled. Each subject had 8 plasma lopinavir concentrations determined over a 12-hour dosing interval and 1 CSF lopinavir C(trough) value determined at the end of the study. Linear regression methods tested for associations between CSF or CSF to plasma concentration ratio and covariates including pharmacokinetic parameters and CSF protein. Ten patients (7 male; median [range] +/- SD age 45.3 +/- 2.8 y) completed the study. Median (intraquartile range [IQR]) lopinavir plasma 0- to 12-hour area under the curve (AUC(0-12)) and minimum concentrations were 71.3 h x microg/mL (48.4-87.6) and 3.82 microg/mL (2.76-5.34). Median (IQR) CSF C(trough), paired plasma concentration, and time since last dose were 11,200 pg/mL (6760-16,400), 5.42 micr...Continue Reading

References

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Citations

Feb 12, 2013·Bioanalysis·Robin DiFrancescoGene D Morse
Sep 10, 2014·Clinical Pharmacokinetics·Andrea CalcagnoStefano Bonora
Oct 12, 2011·The Journal of Antimicrobial Chemotherapy·Lucy GarveyAlan Winston
Dec 14, 2011·The Journal of Antimicrobial Chemotherapy·Aylin YilmazMagnus Gisslén
Nov 20, 2012·CNS Drugs·Christine EisfeldIngo Husstedt
Aug 9, 2011·Thérapie·Aurélie Barrail-TranUNKNOWN Groupe Suivi Therapeutique Pharmacologique de la Societe Francaise de Pharmacologie et de Therapeutique
Nov 11, 2017·The Journal of Antimicrobial Chemotherapy·Malon Van den HofDasja Pajkrt
Oct 14, 2020·Current Opinion in Pharmacology·Sean N AvedissianCourtney V Fletcher
Feb 5, 2021·Clinical Pharmacology and Therapeutics·Aaron S Devanathan, Mackenzie L Cottrell

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