Saquinavir Suboptimal in HIV-Positive Children Unless Combined With Other PIs -- HIV/AIDS INFO AND UPDATES

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Date Posted: 12:09:16 05/16/02 Thu
Author: Anonymous
Subject: Saquinavir Suboptimal in HIV-Positive Children Unless Combined With Other PIs

Saquinavir Suboptimal in HIV-Positive Children Unless Combined With Other PIs

Reuters Health Information 2002. � 2002 Reuters Ltd
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Introduction
NEW YORK (Reuters Health) Apr 19 - In HIV-infected children, saquinavir alone does not maintain consistently efficacious plasma levels. Combination therapy with other protease inhibitors (PIs) that inhibit saquinavir metabolism is necessary, researchers report.

Dr. Sibylle Grub from F. Hoffmann-La Roche Ltd., Basel, Switzerland, and colleagues examined the pharmacokinetics of saquinavir 50 mg/kg given alone three times a day in 14 children and saquinavir 33 mg/kg plus nelfinavir given three times a day in 13 children. The researchers assessed the results after single dose administration and after short- and long-term use.

They also examined the pharmacokinetics of saquinavir given as a fixed single dose of 1200 mg compared with unrestricted weight-adjusted dosing of 50 mg/kg, according to the report in the March issue of Clinical Pharmacology and Therapeutics.

When saquinavir was used alone it resulted in a lower exposure in children and in adolescents compared with adults who were treated with saquinavir 1200 mg three times daily. This appeared to result from increased systemic clearance and lower oral bioavailability, the researchers note.

Saquinavir combined with nelfinavir reduced the clearance of saquinavir and increased the drugs' exposure in the children to levels that were similar to the levels found in adults, Dr. Grub's team reports.

The investigators found that among the children there was a significant correlation between the average trough concentration of saquinavir and sustained suppression of viral load. "The apparent threshold for maintaining viral load suppression was a mean trough saquinavir concentration of above 200 ng/mL," they add.

Clin Pharmacol Ther 2002;71:122-130.

http://www.medscape.com/viewarticle/432287_print

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