体外抗病毒研究 COVID-19疫情发生后, 中国的科学家为寻找有效 的抗病毒药物, 做了大量的体外细胞筛选试验。2020 Chloroquine phosphate: therapeutic drug for COVID-19
, 以及安全性等作一综述。, 磷酸氯喹治疗 Covid-19 的现状, M O Liqian, Ping Zheng
doi:10.12122/j.issn.1673-4254.2020.04.22
Since the outbreak of coronavirus disease 2019 (COVID-19) in the late 2019, a variety of antiviral drugs have been used in the first-line clinical trial. The Diagnostic and Treatment Protocol for COVID-19 (Trial Version 6) in China recommends chloroquine phosphate for the first time as an anti-coronavirus trial drug. As a classic drug for treatment of malaria and rheumatism, chloroquine phosphate has been used clinically for more than 80 years, and has also shown good results in the treatment of various viral infections. As the plasma drug concentration varies greatly among different races and individuals and due to its narrow treatment window, chloroquine in likely to accumulate in the body to cause toxicity. Among the treatment regimens recommended for COVID-19, reports concerning the safety of a short-term high-dose chloroquine regimen remain scarce. In this review, the authors summarize the current research findings of chloroquine phosphate in the treatment of COVID-19, and examine the pharmacokinetic characteristics, antiviral therapy, the therapeutic mechanism and safety of chloroquine.
References
Cortegiani, Ingoglia, Ippolito, A systematic review on the efficacy and safety of chloroquine for the treatment of COVID-19 [J], J Crit Care,
doi:10.1016/j.jcrc.2020.03.005
Moussavi, Ruengweerayut, Population pharmacokinetics of a three-day chloroquine treatment in patients with Plasmodium vivax infection on the Thai-Myanmar border [J], J Mal
Mégarbane, Bloch, Hirt, Blood concentrations are better predictors of chioroquine poisoning severity than plasma concentrations: a prospective study with modeling of the concentration/effect relationships [J], Clin Toxicol
Pb, Panchal, Warren, Evaluation of Ebola Virus Inhibitors for Drug Repurposing [J], ACS Infect Dis
Riou, Barriot, Rimailho, Treatment of Severe Chloroquine Poisoning [J], New Engl J Med
Vincent, Bergeron, Benjannet, Chloroquine is a potent inhibitor of SARS coronavirus infection and spread[J], J Virol
Wang, Cheng, Increasing Host Cellular Receptor-Angiotensin-Converting Enzyme 2 (ACE2) Expression by Coronavirus may Facilitate 2019-nCoV Infection [J], bioRxiv,
doi:10.1101/2020.02.24.963348
[12 ; ]梁晓竟, 氯喹抗疟研究概况 [J], 预防医学情报杂志
[17 ; Al-Bari, Chloroquine analogues in drug discovery: new directions of uses, mechanisms of actions and toxic manifestations from malaria to multifarious diseases[J], J Antimicrob Chemoth
[19 ; ]routy, Angel, Patel, Assessment of chloroquine as a modulator of immune activation to improve CD4 recovery in immune nonresponding HIV-infected patients receiving antiretroviral therapy [J], HIV Med
[20 ; ]al-Bari, Targeting endosomal acidification by chloroquine analogs as a promising strategy for the treatment of emerging viral diseases [J], Pharmacol Res Perspect
[21 ; ]savarino, Shytaj, Chloroquine and beyond: exploring antirheumatic drugs to reduce immune hyperactivation in HIV/AIDS [J], Retrovirology
[26 ; Schrezenmeier, Dörner, Mechanisms of action of hydroxychloroquine and chloroquine: implications for rheumatology[J], Nat Rev Rheumatol
[28 ; ]li R, Qiao, Zhang, Analysis of angiotensin-converting enzyme 2 (ACE2) from different species sheds some light on cross-species receptor usage of a novel coronavirus 2019-nCoV [J], J Infect,
doi:10.1016/j.jinf.2020.02.013
[3 ; Wang, Cao, Zhang, Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro [J], Cell Res
[32 ; Ducharme, Farinotti, Clinical pharmacokinetics and metabolism of chloroquine. Focus on recent advancements [J], Clin Pharmacokinet
[4 ; Mackenzie, Dose refinements in long-term therapy of rheumatoid arthritis with antimalarials[J], Am J Med
[41 ; ]olafuyi, Badhan, Dose Optimization of Chloroquine by Pharmacokinetic Modeling During Pregnancy for the Treatment of Zika Virus Infection [J], J Pharm Sci
[42 ; ]taylor Wr, White, Antimalarial drug toxicity: a review[J], Drug Safety
[44 ; ]kiel, Chloroquine Suicide [J], JAMA
[49 ; ]luzzi, Peto, Adverse Effects of Antimalarials[J], Drug Safety
[5 ; Gao, Tian, Yang, Breakthrough: Chloroquine phosphate has shown apparent efficacy in treatment of COVID-19 associated pneumonia in clinical studies [J], Bio Sci Trends
[8 ; Gbinigie, Frie, Should chloroquine and hydroxychloroquine be used to treat COVID-19? A rapid review [J], BJGP Open,
doi:10.3399/bjgpopen20X101069
]augustijns, Geusens, Verbeke, Chloroquine levels in blood during chronic treatment of patients with rheumatoid arthritis[J], Eur J Clin Pharmacol
]augustijns, Verbeke, Stereos elective Pharmacokinetic Properties of Chloroquine and De-Ethyl-Chloroquine in Humans[J], clin pharmacokinet
]chattopadhyay, Mahajan, Kumar, Assessment of safety of the major antimalarial drugs [J], Expert Opin Drug Saf
]clemessy, Angel, Borron, Therapeutic trial of diazepam versus placebo in acute chloroquine intoxications of moderate gravity [J], Intensive Care Med
]de Wilde, Jochmans, Posthuma, Screening of an FDA-Approved Compound Library Identifies Four Small-Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Replication in Cell Culture [J], Antimicrob Agents Chem
]fantini, Scala, Chahinian, Structural and molecular modeling studies reveal a new mechanism of action of chloroquine and hydroxychloroquine against SARS-CoV-2 infection[J], Int J Antimicrob Agents
]frisk-Holmberg, Bergqvist, Termond, The single dose kinetics of chloroquine and its major metabolite desethylchloroquine in healthy subjects [J], Eur J Clin Pharmacol
]kaewkhao, Chotivanich, Winterberg, High sensitivity methods to quantify chloroquine and its metabolite in human blood samples using LC-MS/MS [J], Bioanalysis
]keyaerts, Vijgen, Maes, In vitro inhibition of severe acute respiratory syndrome coronavirus by chloroquine[J], Biochem Biophys Res Commun
]looareesuwan, White, Chanthavanich, Cardiovascular toxicity and distribution kinetics of intravenous chloroquine [J], Br J Clin Pharmacol
]mullié, Jonet, Desgrouas, Differences in anti-malarial activity of 4-aminoalcohol quinoline enantiomers and investigation of the presumed underlying mechanism of action[J], Malaria J
]murray, Down, Boulware, Reduction of Immune Activation with Chloroquine Therapy during Chronic HIV Infection [J], JVirol
]mzayek, Deng, Mather, Randomized dose-ranging controlled trial of AQ-13, a candidate antimalarial, and chloroquine in healthy volunteers [J], PLoS Clin Trials
]ooi, Chew, Loh, In vitro inhibition of human influenza A virus replication by chloroquine[J], J Virol
]parson, Koeniger, Johnson, Analysis of chloroquine and metabolites directly from whole-body animal tissue sections by liquid extraction surface analysis (LESA) and tandem mass spectrometry[J], J Mass Spectrom
]salata, Calistri, Parolin, Antiviral activity of cationic amphiphilic drugs [J], Expert Rev Anti-infe
]thomé, Lopes, Tm, Chloroquine: Modes of action of an undervalued drug [J], Immunol Lett
]walker, Salako, Alvan, The disposition of chloroquine in healthy Nigerians after single intravenous and oral doses [J], Brit J Clin Pharmaco
]中华人民共和国国家卫生与计划生育委员会, 抗疟药使用规范: WS/ T485-2016 [S]