Pharmacokinetics and Pharmacodynamics of Nelfinavir Administered Twice or Thrice Daily to Human Immunodeficiency Virus Type 1--Infected Children

Gatti, G.; Castelli-Gattinara, G.; Cruciani, M.; Bernardi, S.; De Pascalis, C.R.; Pontali, E.; Papa, L.; Miletich, F.; Bassetti, D.
June 2003
Clinical Infectious Diseases;6/1/2003, Vol. 36 Issue 11, p1476
Academic Journal
We studied the pharmacokinetics and pharmacodynamics of nelfinavir administered 2 or 3 times per day to human immunodeficiency virus type 1 (HIV-1)-infected children receiving highly active antiretroviral therapy containing nelfinavir. The geometric mean trough concentrations of nelfinavir for the thrice- and twice-daily regimens were 1.55 mg/L and 1.11 mg/L, respectively (P = not significant). Nelfinavir concentrations did not correlate with total daily dose, dose per kilogram of weight, age, weight, previous protease inhibitor (PI) experience, or CD4[sup +] cell percentage. In the 25 PI-naive children, the virus load reductions at 24 weeks of treatment with the twice- and thrice-daily regimens were comparable. A significantly higher percentage of children in the twice-daily group had a trough concentration of nelfinavir of less than the inhibitory concentration of 95% (P = .042). The decrease in the virus load at 24 weeks of treatment was not correlated with the trough concentration of nelfinavir. The variability of trough concentrations was extremely high, particularly among recipients of the twice-daily regimen, resulting in a higher number of patients with subinhibitory concentrations of nelfinavir in this group.


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