Lopinavir and Ritonavir

1 Indications and usage kaletra: is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients 14 days and older. Limitations of Use: Genotypic or phenotypic testing and/or treatment history should guide the use of KALETRA. The number of baseline lopinavir resistance-associated substitutions affects the virologic response to KALETRA . KALETRA is an HIV-1 protease inhibitor indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients (14 days and older). ( 1 )

12.1 Mechanism of Action KALETRA is a fixed-dose combination of HIV-1 antiviral drugs lopinavir and ritonavir. As co-formulated in KALETRA, ritonavir inhibits the CYP3A-mediated metabolism of lopinavir, thereby providing increased plasma levels of lopinavir.

Clinical clearance of Lopinavir and Ritonavir (Protease Inhibitor) relies on phase i/ii hepatic conjugation of lopinavir and ritonavir coupled with glomerular and tubular renal excretion with a Approximately 9–15 hours terminal plasma half-life for Lopinavir and Ritonavir half-life; patients absorbing at Estimated 56%–68% oral systemic absorption for Lopinavir and Ritonavir bioavailability typically observe target onset around peak plasma concentration (tmax) reached 1–3 hours post-dose for lopinavir and ritonavir.

FDA clinical labeling for Lopinavir and Ritonavir restricts administration in known hypersensitivity to lopinavir and ritonavir or structurally related protease inhibitor compounds; concomitant contra-labeled cyp/transporter therapies during active lopinavir and ritonavir administration across 100 mg/1 / 25 mg/1 Tablet, Film Coated, 200 mg/1 / 50 mg/1 Tablet, Film Coated, 80 mg/mL / 20 mg/mL Solution, with self-reported patient tracking dominated by nausea (11.4% of reports), diarrhea (8.7% of reports), headache (7.2% of reports).