Plasma Concentrations of the HIV-Protease Inhibitor Lopinavir are Suboptimal in Children Aged 2 Years and Below

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Abstract
Background: Lopinavir/ritonavir (LPV/r) has been licensed for the treatment of HIV-infected children >6 months in the US and >2 years in the EU. Limited LPV paediatric pharmacokinetic data are available. We studied LPV pharmacokinetics to determine whether the recommended dose (230/57.5 mg/m 2 twice daily) results in optimal LPV exposure in all age groups. Virological efficacy was a secondary objective. Methods: HIV-1-infected children who started treatment with LPV/r and two nucleoside reverse transcriptase inhibitors underwent a 12-h pharmacokinetic curve. LPV plasma concentrations were determined with a validated HPLC method with UV detection. If C min was 0–12h , C max and C min of LPV were 75.3 (±33.7) mg/l.h, 9.33 (±3.27) mg/l and 3.68 (±2.48) mg/l, respectively, which is similar to previously published data. Interindividual variability was large. C min was inadequate in 7/23 children. Significantly more children 2 years. Dose increase to ±300/75 mg/m 2 LPV/r led to C min >1.0 mg/l. The studied regimen provided excellent viral suppression for naive and pretreated patients. Conclusions: Mean LPV pharmacokinetic parameters in these HIV-infected children are similar to published data, but exposure is significantly reduced in children 2 LPV/r in this age population are urgently warranted.

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