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chloroquine [chloroquine phosphate] (Aralen, Atabrine, Artrichin, Nivaquine, Cisplaquin, Quingamine, Avoclor, Chingaminum)
Tradename: Aralen, Atabrine. (chloroquine phosphate).
Indications:
1) prophylaxis for malaria
2) treatment of uncomplicated, mild to moderate malaria
3) extraintestinal amebiasis
4) rheumatoid arthritis Contrandications:
- appears to have activity against SARS CoV2 (COVID-19) in vitro [4] but is associated with higher in hospital mortality, QT prolongation & ventricular arrhythmias in patients with COVID-19
- FDA rescinded emergency use authorization of chloroquine to treat COVID-19 patients [7]
Dosage:
1) malarial prophylaxis:
a) 8 mg/kg up to 500 mg PO weekly
b) 300 mg weekly [2]
c) from 1 week before exposure to 4 weeks post exposure
2) malarial treatment:
a) adults:
1] loading dose: 1000 mg chloroquine phosphate, 600 mg (base)
2] 500 mg chloroquine phosphate, 300 mg (base) after 6 hours
3] 500 mg chloroquine phosphate. 300 mg (base) QD for 2 days
b) children
1] loading dose: 10 mg/kg up to 600 mg (base)
2] 5 mg/kg up to 300 mg after 6 hours
3] 5 mg/kg up to 300 mg QD for 2 days
3) rheumatoid arthritis: 250 mg (150 mg base) mg PO QD
4) extraintestinal amebiasis
a) adults:
1] loading dose: 1000 mg chloroquine phosphate, 600 mg (base)
2] 500 mg chloroquine phosphate, 300 mg (base) PO QD for 2-3 weeks
b) children: 10 mg/kg (base) up to 300 mg PO QD for 2-3 weeks
5) 500 mg choroquine phosphate (300 mg base)
- EC90 value of chloroquine against SARS CoV2 is 6.90 uM, achievable with oral dose of 500 mg chloroquine phosphate (300 mg base) [4], but contraindicated for treatment of COVID-19
Tabs: chloroquine phosphate 250 chloroquine phosphate (150 mg base) & 500 mg (300 mg base).
Monitor:
1) ophthalmologic examination recommended prior to therapy & every 6 months with continued therapy
2) liver function tests (LFTs)
Adverse effects:
1) not common (1-10%)
- nausea/vomiting, dizziness, diarrhea
2) uncommon (< 1%)
- hypotension, fatigue, personality changes, headache, pruritus, anorexia, stomatitis, blood dyscrasia, retinopathy, blurred vision,lightening of hair
3) EKG changes (QT prolongation)
- ventricular arrhythmias in 4.3% of patients hospitalized for COVID-19 vs 0.3% of controls [6]
Drug interactions:
1) cimetidine, kaolin, magnesium trisalicylate,
2) rabies vaccine
Interactions
drug interactions
drug adverse effects of antimalarials
Related
amebiasis
chloroquine/hydroxychloroquine for COVID-19
malaria
General
amebicide
antimalarial
quinoline; leucoline; chinoleine; 1-benazazine; benzo[b]pyridine
Properties
MISC-INFO: elimination route LIVER
KIDNEY
pregnancy-category -
safety in lactation -
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Deprecated Reference
- Wang M, Cao R, Zhang L et al
Remdesivir and chloroquine effectively inhibit the recently emerged
novel coronavirus (2019-nCoV) in vitro.
Cell Res. 2020 Mar;30(3):269-271.
PMID: 32020029 Free PMC Article
- Prescriber's Digital Referenc
Chloroquine phosphate - Drug Summary
https://www.pdr.net/drug-summary/Chloroquine-Phosphate-chloroquine-phosphate-3418
- Mehra MR, Desai SS, Ruschitzka F, Patel AN
Hydroxychloroquine or chloroquine with or without a macrolide for
treatment of COVID-19: a multinational registry analysis.
Lancet. May 22, 2020
PMID: 32450107 Free PMC article
https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(20)31180-6/fulltext
* authors associated with Surgisphere implicated in false data *
- FDA News Release June 15, 2020
Coronavirus (COVID-19) Update: FDA Revokes Emergency Use
Authorization for Chloroquine and Hydroxychloroquine.
https://www.fda.gov/news-events/press-announcements/coronavirus-covid-19-update-fda-revokes-emergency-use-authorization-chloroquine-and