Lopinavir-Ritonavir: a new protease inhibitor.
Lopinavir is a new protease inhibitor that is structurally related to ritonavir. It recently was approved by the Food and Drug Administration as a coformulation with ritonavir under the brand name Kaletra. Ritonavir substantially increases lopinavir drug exposure by inhibiting cytochrome P450 isoenzyme 3A4. Based on limited data, lopinavir-ritonavir demonstrates safety and efficacy in both antiretroviral-naive and protease inhibitor-experienced patients. It has the ability to durably suppress human immunodeficiency virus (HIV) RNA for up to 2 years in antiretroviral-naïve patients. Compared with nelfinavir, it had superior virologic control at 48 weeks in antiretroviral-naïve patients. Its side effects include diarrhea, abnormal stools, abdominal pain, nausea, vomiting, and asthenia. A number of patients experienced grade 3-4 laboratory abnormalities in liver function tests, cholesterol, and triglycerides while receiving this drug combination. The exact resistance patterns of lopinavir-ritonavir are unknown, but the Department of Health and Human Services strongly recommends it for the initial treatment of HIV-infected adults and adolescents.
Mangum
E M
EM
Department of Pharmacy Practice, College of Pharmacy, Nova Southeastern University and the North Broward Hospital District, Ft Lauderdale, Florida 33328, USA.
Graham
K K
KK
D017320:HIV Protease Inhibitors / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D061466:Lopinavir; D011744:Pyrimidinones / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D019438:Ritonavir / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*
D017320:HIV Protease Inhibitors; D011744:Pyrimidinones; D061466:Lopinavir; D019438:Ritonavir