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Lopinavir‐Ritonavir: A New Protease Inhibitor
Author(s) -
Mangum Eric M.,
Graham Kathleen K.
Publication year - 2001
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1592/phco.21.17.1352.34419
Subject(s) - ritonavir , lopinavir , lopinavir/ritonavir , medicine , protease inhibitor (pharmacology) , nelfinavir , pharmacology , diarrhea , nausea , virology , gastroenterology , viral load , human immunodeficiency virus (hiv) , antiretroviral therapy
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‐naïve 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.