Lopinavir

Lopinavir is a protease inhibitor with high specificity for HIV-I protease. Ritonavir strongly inhibits lopinavir metabolism coadministration of lopinavir and ritonavir in healthy volunteers increased the area under the lopinavir plasma concentration-time curve >100-fold. Trough plasma concentration :antiviral 50% effective concentration ratio for lopinavir was >75 for wild-type HIV at the dose used in clinical trials, compared to values of less than or equal to4 for other commonly used protease inhibitors. Coformulated lopinavir and ritonavir (lopinavir/ritonavir) 400/100mg twice daily for 48 weeks suppressed HIV replication in significantly more antiretroviral-naive patients than nelfinavir 750mg 3 times daily tall patients also received stavudine and lamivudine). Suppression of viral replication was observed in most protease inhibitor-experienced patients with lopinavir/ritonavir (400/100, 400/200 or 533/133mg twice daily for 48 or 96 weeks) in combination with greater than or equal to2 nucleoside reverse transcriptase inhibitors (NRTIs) and either efavirenz or nevirapine. 48 weeks of treatment with twice daily lopinavir/ritonavir (230/57.5 or 300/75 mg/m(2) for the first 12 weeks and then 300/75 mg/m(2)) in combination with 1 or 2 NRTIs, with Or without nevirapine, suppressed viral replication in the majority of antiretroviral-naive and -experienced paediatric patients (aged 6 months to 12 years), Diarrhoea, nausea and asthenia were the most frequently reported adverse effects in patients receiving lopinavir/ritonavir-based regimens. Elevated total cholesterol, triglyceride and hepatic enzyme levels were also reported.