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Safety and effectiveness concerns of lopinavir/ritonavir in COVID-19 affected patients: a retrospective series.
Lepage, Marc-Antoine; Rozza, Nicholas; Kremer, Richard; Grunbaum, Ami.
  • Lepage MA; McGill University Health Centre, Montreal, Canada.
  • Rozza N; McGill Faculty of Medecine and Health Sciences, Montreal, Canada.
  • Kremer R; McGill Faculty of Medecine and Health Sciences, Montreal, Canada.
  • Grunbaum A; McGill University Health Centre, Montreal, Canada.
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.
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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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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