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Chloroquine for SARS-CoV-2: Implications of Its Unique Pharmacokinetic and Safety Properties.


ABSTRACT: Since in vitro studies and a preliminary clinical report suggested the efficacy of chloroquine for COVID-19-associated pneumonia, there is increasing interest in this old antimalarial drug. In this article, we discuss the pharmacokinetics and safety of chloroquine that should be considered in light of use in SARS-CoV-2 infections. Chloroquine is well absorbed and distributes extensively resulting in a large volume of distribution with an apparent and terminal half-life of 1.6 days and 2 weeks, respectively. Chloroquine is metabolized by cytochrome P450 and renal clearance is responsible for one third of total clearance. The lack of reliable information on target concentrations or doses for COVID-19 implies that for both adults and children, doses that proved effective and safe in malaria should be considered, such as 'loading doses' in adults (30 mg/kg over 48 h) and children (70 mg/kg over 5 days), which reported good tolerability. Here, plasma concentrations were?

SUBMITTER: Smit C 

PROVIDER: S-EPMC7165255 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature

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Chloroquine for SARS-CoV-2: Implications of Its Unique Pharmacokinetic and Safety Properties.

Smit Cornelis C   Peeters Mariska Y M MYM   van den Anker John N JN   Knibbe Catherijne A J CAJ  

Clinical pharmacokinetics 20200601 6


Since in vitro studies and a preliminary clinical report suggested the efficacy of chloroquine for COVID-19-associated pneumonia, there is increasing interest in this old antimalarial drug. In this article, we discuss the pharmacokinetics and safety of chloroquine that should be considered in light of use in SARS-CoV-2 infections. Chloroquine is well absorbed and distributes extensively resulting in a large volume of distribution with an apparent and terminal half-life of 1.6 days and 2 weeks, r  ...[more]

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