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. 2020 Jul 2;9(7):2084. doi: 10.3390/jcm9072084

Table 2.

Brief description of COVID-19 therapeutic options recommended by World Health Organization (WHO) guidelines [117,118,119,120].

Drug Name Pharmacological Class Clinical Phase EC50 (half maximal effective concentration) Dose Mechanism of Action Adverse Effects
Remdesivir—(RDV) nucleoside analogue Severe 0.77 µM 200 mg—day 1; 100 mg/day—9 days inhibitor of the CoVs RNA-dependent RNA polymerase (RdRp)
  • incompletely characterized toxicological profile: phlebitis, constipation, headache, ecchymosis, nausea, pain in the extremities

  • elevation of hepatic enzymes values

Chloroquine (CQ) 4-aminoquinoline Mild-to-moderate and severe—depending on the guideline applied 23.90 µM (24 h)
5.47 µM (48 h)
CQ base (600 mg/diagnosis; 300 mg—12 h later and 300 mg up to 5 days) or CQ phosphate (1000 mg/diagnosis; 500 mg—12 h later and 300 mg up to 5 days) weak base able to elevate the pH of acidic intracellular organelles, such as endosomes and lysosomes
  • retinopathy

  • hypotension

  • ECG changes

  • irreversible cardiomyopathy—long-term users

  • direct myocardial toxicity

  • exacerbate the existent myocardial dysfunction

  • QT prolongation

  • risk of Torsade de Pointes (TdP) even at therapeutic doses

  • interaction with antiarrhythmics

* in the case of HCQ, the adverse effects have a lower intensity, but are not absent
Hydroxychloroquine (HCQ) 4-aminoquinoline Mild-to-moderate and severe—depending on the guideline applied 6.14 µM (24 h)
0.72 µM (48 h)
HCQ—400 mg at suspicion/diagnosis; 400 mg—12 h later and 200 mg—until day 5 weak bases able to elevate the pH of acidic intracellular organelles, such as endosomes and lysosomes
Liponavir/ritonavir (LPv/r) Protease inhibitor Mild-to-moderate - 400 mg/100 mg/day—14 days peptidomimetic inhibitor of HIV protease enzyme
  • hypercholesterolemia and increased serum triglycerides

  • increased gamma-glutamyl transferase

  • increased serum ALT

  • upper respiratory tract infection

  • diarrhea

  • nausea

  • headache

  • skin rush

  • neutropenia

  • anxiety

  • QT prolongation