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1、 Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19.The COVID-19 resource centre is hosted on Elsevier Connect,the companys public news and information website.Elsevier hereby grants permission to make al
2、l its COVID-19-related research that is available on the COVID-19 resource centre-including this research content-immediately available in PubMed Central and other publicly funded repositories,such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by
3、any means with acknowledgement of the original source.These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.ARTICLE IN PRESS JID:ANTAGE m5G;March 31,2020;9:30 International Journal of Antimicrobial Agents xxx(xxxx)xxx Contents lists available a
4、t ScienceDirect International Journal of Antimicrobial Agents journal homepage: Aminoquinolines against coronavirus disease 2019(COVID-19):chloroquine or hydroxychloroquine Zahra Sahraei a,b,Minoosh Shabani c,d,Shervin Shokouhi c,d,Ali Saffaei e,a Department of Clinical Pharmacy,School of Pharmacy,S
5、hahid Beheshti University of Medical Sciences,Tehran,Iran b Loghman Hakim Hospital,Shahid Beheshti University of Medical Sciences,Tehran,Iran c Department of Infectious Diseases and Tropical Medicine,Loghman Hakim Hospital,Shahid Beheshti University of Medical Sciences,Tehran,Iran d Infectious Disea
6、ses and Tropical Medicine Research Center,Shahid Beheshti University of Medical Sciences,Tehran,Iran e Student Research Committee,Department of Clinical Pharmacy,School of Pharmacy,Shahid Beheshti University of Medical Sciences,Tehran,Iran a r t i c l e i n f o Article history:Received 26 February 2
7、020 Accepted 9 March 2020 Available online xxx Keywords:COVID-19 Chloroquine Hydroxychloroquine Coronavirus Coronavirus disease 2019(COVID-19),caused by severe acute respiratory syndrome coronavirus 2(SARS-CoV-2),continues to spread rapidly across China.As of 7 March 2020,the infection was reported
8、from 97 countries globally.To date,103 882 patients have been confirmed to have COVID-19,of whom 3522 have died 1.Recently,many trials have been designed to determine an ef-fective therapeutic regimen for COVID-19.Of the target regimens,chloroquine therapy is being considered 2.Several clinical tria
9、ls in China have shown chloroquine phosphate,an aminoquinoline used in malaria treatment,to be effective against COVID-19 at a dose of 500 mg/day 3.Chloroquine phosphate also played a promising role in the management of the Zika virus and SARS-CoV outbreaks.Chloroquine acts by increasing the pH of i
10、ntracellular vacuoles and altering protein degradation pathways through acidic hydrolases in the lysosomes,macromolecule synthesis in the en-dosomes,and post-translational protein modification in the Golgi apparatus.In macrophages and other antigen-presenting cells,chloroquine interferes with antige
11、n processing,thereby achieving an antirheumatic response 4.Studies have demonstrated that chloroquine also confers its considerable broad-spectrum antiviral Corresponding author.Student Research Committee,Department of Clinical Pharmacy,School of Pharmacy,Shahid Beheshti University of Medical Scienc
12、es,Niyayesh Highway,Valiasr St,Tehran,1991953381,Iran.E-mail addresses:(Z.Sahraei),(M.Shabani),(S.Shokouhi),(A.Saffaei).effects via interfering with the fusion process of these viruses by decreasing the pH.In addition,chloroquine alters the glycosylation of the cellular receptors of coronaviruses 5.
13、Hydroxychloroquine(Fig.1),a less toxic aminoquinoline,has an N-hydroxyethyl side chain in place of the N-diethyl group of chloroquine.This modifi-cation makes hydroxychloroquine more soluble than chloroquine.Similar to chloroquine,hydroxychloroquine increases the pH and confers antiviral effects.In
14、addition,hydroxychloroquine has a modulating effect on activated immune cells,downregulates the expression of Toll-like receptors(TLRs)and TLR-mediated sig-nal transduction,and decreases the production of interleukin-6 6.Although the antimalarial activity of hydroxychloroquine is equivalent to that
15、of chloroquine,hydroxychloroquine is preferred over chloroquine owing to its lower ocular toxicity 7.Retinopa-thy is a dose-limiting adverse effect of hydroxychloroquine,and a safe daily dose appears to correspond to 6.5 mg/kg of ideal body weight and 5.0 mg/kg of actual body weight 8.Although there
16、 are more clinical data on the anti-coronaviral activity of chloroquine than that of hydroxychloroquine,both of these agents are theoretically similar in their antiviral activity 9.Moreover,chloroquine is not as widely available as hydroxychloroquine in some countries.In addition,chloroquine is asso
17、ciated with greater adverse effects than hydroxychloroquine.For example,in patients with COVID-19,chloroquine can interact with lopinavir/ritonavir,resulting in prolongation of the QT interval.Hence,it is necessary to consider hydroxychloroquine instead of chloroquine when the https:/doi.org/10.1016
18、/j.ijantimicag.2020.105945 0924-8579/2020 Elsevier B.V.and International Society of Chemotherapy.All rights reserved.Please cite this article as:Z.Sahraei,M.Shabani and S.Shokouhi et al.,Aminoquinolines against coronavirus disease 2019(COVID-19):chloroquine or hydroxychloroquine,International Journa
19、l of Antimicrobial Agents,https:/doi.org/10.1016/j.ijantimicag.2020.105945 2 Z.Sahraei,M.Shabani and S.Shokouhi et al./International Journal of Antimicrobial Agents xxx(xxxx)xxx ARTICLE IN PRESS JID:ANTAGE m5G;March 31,2020;9:30 Fig.1.Chemical structure of(a)hydroxychloroquine and(b)chloroquine.latt
20、er is not available for treating patients with COVID-19.For example,in Iran,there is a serious shortage of chloroquine and hydroxychloroquine can be recommended instead.Other thera-peutic agents for COVID-19,such as antiviral agents(oseltamivir,lopinavir/ritonavir,ribavirin,etc.),interferons and int
21、ravenous immunoglobulins that do not interfere with hydroxychloroquine,are currently under investigation.Declarations Funding:None.Competing Interests:None declared.Ethical Approval:Not required.References 1 Xu B,Kraemer MUGOpen COVID-19 Data Curation Group.Open access epidemi-ological data from the
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23、roquine phosphate has shown appar-ent efficacy in treatment of COVID-19 associated pneumonia in clinical studies.Biosci Trends 2020 Feb 19 Epub ahead of print.doi:10.5582/bst.2020.01047.2 Rainsford KD,Parke AL,Clifford-Rashotte M,Kean WF.Therapy and pharmaco-logical properties of hydroxychloroquine
24、and chloroquine in treatment of sys-temic lupus erythematosus,rheumatoid arthritis and related diseases.Inflam-mopharmacology 2015;23:23169.doi:10.1007/s10787-015-0239-y.3 Savarino A,Boelaert JR,Cassone A,Majori G,Cauda R.Effects of chloroquine on viral infections:an old drug against today s disease
25、s?Lancet Infect Dis 2003;3:7227.doi:10.1016/s1473-3099(03)00806-5.4 Plantone D,Koudriavtseva T.Current and future use of chloroquine and hydroxychloroquine in infectious,immune,neoplastic,and neurological dis-eases:a mini-review.Clin Drug Investig 2018;38:65371.doi:10.1007/s40261-018-0656-y.5 Lim H-
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27、H,et al.Hydroxychloroquine prescription trends and predictors for excess dosing per recent ophthalmology guidelines.Arthritis Res Ther 2018;20:133.doi:10.1186/s13075-018-1634-8.7 Tan YW,Yam WK,Sun J,Chu JJH.An evaluation of chloroquine as a broad-acting antiviral against hand,foot and mouth disease.
28、Antiviral Res 2018;149:1439.doi:10.1016/j.antiviral.2017.11.017.Please cite this article as:Z.Sahraei,M.Shabani and S.Shokouhi et al.,Aminoquinolines against coronavirus disease 2019(COVID-19):chloroquine or hydroxychloroquine,International Journal of Antimicrobial Agents,https:/doi.org/10.1016/j.ijantimicag.2020.105945