Lopinavir

Lopinavir is a protease inhibitor with high specificity for HIV-I protease. Ritonavir strongly inhibits lopinavir metabolism coadministration of lopin avir and ritonavir in healthy volunteers increased the area under the lopin avir plasma concentration-time curve >100-fold. Trough plasma concentration :antiviral 50% effective concentration ratio fo r 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 protea se inhibitors. Coformulated lopinavir and ritonavir (lopinavir/ritonavir) 400/100mg twice daily for 48 weeks suppressed HIV replication in significantly more antiret roviral-naive patients than nelfinavir 750mg 3 times daily tall patients al so received stavudine and lamivudine). Suppression of viral replication was observed in most protease inhibitor-ex perienced 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 t o2 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 patien ts (aged 6 months to 12 years), Diarrhoea, nausea and asthenia were the most frequently reported adverse ef fects in patients receiving lopinavir/ritonavir-based regimens. Elevated to tal cholesterol, triglyceride and hepatic enzyme levels were also reported.