Contraindicated in:
Use Cautiously in:
CNS: headache, insomnia, weakness.
CV: TORSADES DE POINTES, ↑ PR interval, heart block, QT interval prolongation.
Derm: ERYTHEMA MULTIFORME, STEVENS JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS, rash.
Endo: hyperglycemia.
GI: HEPATOTOXICITY, PANCREATITIS, diarrhea (↑ in children), abdominal pain, nausea, taste aversion (in children), vomiting (↑ in children).
Misc: immune reconstitution syndrome.
Drug-Drug:
Drug-Natural Products:
(Generic available)
Without Concurrent Efavirenz, Nevirapine, or Nelfinavir
With Concurrent Efavirenz, Nevirapine, or Nelfinavir
Therapeutic Classification: antiretrovirals
Pharmacologic Classification: protease inhibitors, metabolic inhibitors
Absorption: Well absorbed following oral administration; food enhances absorption.
Distribution: Ritonavir poor CNS penetration.
Protein Binding: Lopinavir 9899% bound to plasma proteins.
Metabolism/Excretion: Lopinavir completely metabolized in the liver by the CYP3A isoenzyme. Ritonavir highly metabolized by the liver (by CYP3A and CYP2D6 isoenzymes); one metabolite has antiretroviral activity; 3.5% excreted unchanged in urine.
Half-life: Lopinavir 56 hr Ritonavir 35 hr.