ArticleAntimicrobial agents and chemotherapy2011
Pharmacokinetics, pharmacodynamics, and allometric scaling of chloroquine in a murine malaria model.
Article in Antimicrobial agents and chemotherapy, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 51 papers.
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Who cites it
51 citing papers in PubMed.
- Chloroquine is grossly under dosed in young children with malaria: implications for drug resistance.PloS one · 2014Trial
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- Captivating Synergistic, Dose-Dependent Anticancer Effects of Tumor-Regulation Modulators Chloroquine and Ivermectin Completely Abolished by an Opposing Modulator, Deoxycholic Acid, in Hamster Fibrosarcoma: In Vivo, In Vitro, and Literature Review.Pharmaceuticals (Basel, Switzerland) · 2026Article
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- Evaluation of Violacein Metabolic Stability and Metabolite Identification in Human, Mouse, and Rat Liver Microsomes.Pharmaceutics · 2025Article
- The Kir2.1E299V mutation increases atrial fibrillation vulnerability while protecting the ventricles against arrhythmias in a mouse model of short QT syndrome type 3.Cardiovascular research · 2024Article
- Identification of a Dual Autophagy and REV-ERB Inhibitor withJournal of medicinal chemistry · 2024Article
- Antimalarial evaluation of alkyl-linked bis-thiadiazine derivatives in murine model infected with twoADMET & DMPK · 2024Article
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- Macrophage-evading and tumor-specific apoptosis inducing nanoparticles for targeted cancer therapy.Acta pharmaceutica Sinica. B · 2023Article
- Drug Repurposing in Chagas Disease: Chloroquine Potentiates Benznidazole Activity against Trypanosoma cruziAntimicrobial agents and chemotherapy · 2022Article
- Methodology to streamline flow cytometric-based detection of early stage Plasmodium parasitemia in mice.Journal of microbiological methods · 2022Article
- Broad-spectrum Respiratory Virus Entry Inhibitors.Advances in experimental medicine and biology · 2022Article
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- Studies of Potency and Efficacy of an Optimized Artemisinin-Quinoline Hybrid against Multiple Stages of thePharmaceuticals (Basel, Switzerland) · 2021Article
- Pharmacokinetic evaluation of Chalcone derivatives with antimalarial activity in New Zealand White Rabbits.BMC research notes · 2021Article
- A functional outside-in signaling network of proteoglycans and matrix molecules regulating autophagy.Matrix biology : journal of the International Society for Matrix Biology · 2021Article
- Physiologically Based Pharmacokinetics of Lysosomotropic Chloroquine in Rat and Human.The Journal of pharmacology and experimental therapeutics · 2021Article
- Lysosomal Biogenesis and Implications for Hydroxychloroquine Disposition.The Journal of pharmacology and experimental therapeutics · 2021Article
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Chloroquine (CQ) is an important antimalarial drug for the treatment of special patient groups and as a comparator for preclinical testing of new drugs. Pharmacokinetic data for CQ in animal models are limited; thus, we conducted a three-part investigation, comprising (i) pharmacodynamic studies of CQ and CQ plus dihydroartemisinin (DHA) in Plasmodium berghei-infected mice, (ii) pharmacokinetic studies of CQ in healthy and malaria-infected mice, and (iii) interspecies allometric scaling for CQ from 6 animal and 12 human studies. The single-dose pharmacodynamic study (10 to 50 mg CQ/kg of body weight) showed dose-related reduction in parasitemia (5- to >500-fold) and a nadir 2 days after the dose. Multiple-dose regimens (total dose, 50 mg/kg CQ) demonstrated a lower nadir and longer survival time than did the same single dose. The CQ-DHA combination provided an additive effect compared to each drug alone. The elimination half-life (t(1/2)), clearance (CL), and volume of distribution (V) of CQ were 46.6 h, 9.9 liters/h/kg, and 667 liters/kg, respectively, in healthy mice and 99.3 h, 7.9 liters/h/kg, and 1,122 liters/kg, respectively, in malaria-infected mice. The allometric equations for CQ in healthy mammals (CL = 3.86 × W(0.56), V = 230 × W(0.94), and t(1/2) = 123 × W(0.2)) were similar to those for malaria-infected groups. CQ showed a delayed dose-response relationship in the murine malaria model and additive efficacy when combined with DHA. The biphasic pharmacokinetic profiles of CQ are similar across mammalian species, and scaling of specific parameters is plausible for preclinical investigations.
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