Lopinavir/ Ritonavir
Lopinavir and ritonavir are protease inhibitors approved for use in
human immunodeficiency virus (HIV) 1. They are among the drugs being
trialled for possible repurposing in COVID-19 treatment.
Lopinavir/ritonavir is usually given as a combination therapy as
ritonavir is said to increase the half-life of lopinavir by inhibiting
the cytochrome P450 that metabolises it. Protease inhibitors generally
prevent maturation of the viral particles by binding to the HIV-1
protease enzyme and preventing the cleavage of Gag-pol polyproteins
(group-specific antigen-polymerase). This leads to the production of
nascent immature, defective viral particles that are non-infectious (Yan
et al, 2020; Dionne, 2019; Sheahan et al., 2020; Painstil & Cheng,
2019; Tobaiqy et al., 2020).
The adverse effects that have been reported with lopinavir/ritonavir
include nausea and vomiting, diarrhea, anemia, hyperlipidaemia, alanine
transaminase elevation, impaired cognition or memory, insomnia and skin
toxicity (Su et al, 2019; Jespersen et al., 2018; Dionne, 2019; Silva et
al., 2020). It is therefore instructive to be cautious in administering
lopinavir/ritonavir to patients that have impaired liver functions,
dyslipidaemia and psychiatric disposition.