Safety and effectiveness concerns of lopinavir/ritonavir in COVID-19 affected patients: a retrospective series.
Clin Toxicol (Phila)
; 59(7): 644-647, 2021 07.
Article
in English
| MEDLINE | ID: covidwho-1109095
ABSTRACT
CONTEXT Originally developed for treatment of human immunodeficiency virus (HIV), the antiviral combination lopinavir/ritonavir (LPV/r) is being repurposed for treating the novel coronavirus disease (COVID-19) despite minimal experience in this markedly different population and an in-vitro derived EC50 against SARS-CoV-2 several hundred-fold greater than for HIV. We present a case series including a case of severe hyponatremia and a 32-fold overdose raising safety and effectiveness concerns in COVID-19 patients. METHODS:
We measured LPV trough concentrations in 12 patients and reviewed their clinical charts for side effects known to occur in HIV patients.FINDINGS:
Compared to established LPV trough concentrations in HIV patients, concentrations in COVID-19 patients were 3-fold greater (19.37 ± 10.12 mcg/mL versus 6.25 mcg/mL). In addition, cholestasis and dyslipidemia toxicity thresholds were exceeded in 12/12 and 11/12 patients respectively. No patients achieved the presumed therapeutic concentration. Side effects included gastrointestinal symptoms (5/12), electrolyte imbalances (4/12), liver enzyme disturbances (5/12) and triglyceride elevations (2/12).CONCLUSION:
No patients reached presumed therapeutic LPV concentrations despite experiencing side effects and exceeding cholestasis and dyslipidemia toxicity thresholds. This raises concerns for the safety and effectiveness of LPV/r. Clinicians should consider closely monitoring for side effects and not necessarily attribute them to COVID-19.Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Ritonavir
/
Lopinavir
/
SARS-CoV-2
/
COVID-19 Drug Treatment
Type of study:
Diagnostic study
/
Experimental Studies
/
Observational study
/
Prognostic study
Limits:
Adult
/
Aged
/
Female
/
Humans
/
Male
/
Middle aged
Language:
English
Journal:
Clin Toxicol (Phila)
Journal subject:
Toxicology
Year:
2021
Document Type:
Article
Affiliation country:
15563650.2020.1842882
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