Table 3.
Current drugs used against COVID-19.
| Drug | Mechanism of action | Results of clinical case reports | Adverse effects | Dose | References |
|---|---|---|---|---|---|
| Antiviral drugs | |||||
| Remdesivir | The prodrug, belonging to the group of nucleotide analogs, generates an active metabolite capable of entering cells and inhibits viral RNA polymerase. Inhibitory capacity against SARS-CoV-2 in vitro has been observed*. | Decreased recovery time, disease progression, as well as mortality compared to placebo. | -Infusion-related hypotension - Hepatotoxic - Nephrotoxic - Gastrointestinal symptoms |
-First dose of 200 mg -100 mg/day for 5–9 days. | (166) |
| TMPRSS2 antagonist | |||||
| Camostat | Produces GBPA, that inhibits many of the serine proteases that SARS CoV and SARS-CoV-2 use for virus-to-host cell membrane fusion, like TMPRSS2**. | Reduces the likelihood of serious infection, as well as morbidity and mortality. | -Eruption - Pruritus - Oedema - Urticaria |
It has been used at different doses in humans and other pathologies. e.g., : 200 mg every 8 h | (167) |
| Nafamostat mesylate | Inhibited SARS-CoV-2 S protein-mediated entry into host cells with about 15-fold-higher efficiency than camostat, with a 50% effective concentration. | In combination with Favipiravir has shown a decrease in mortality. | Hyperkalemia | 0.2 mg per kg/hour by continuous IV infusion, for 14 days. | (168, 169) |
| Monoclonal antibodies | |||||
| Tocilizumab | IL-6 receptor antagonist | May reduce the hospital stay, the need for ICU admission, and the need for invasive mechanical ventilation. |
- Increased risk of secondary infections. - Hypersensitivity reactions - Neutropenia and thrombocytopenia - Hepatotoxicity |
>75 kg: 600 mg single dose <75 kg: 400 mg single dose*** | (170) |
| Anakinra | IL-1 receptor antagonist | Reduced both needs for invasive mechanical ventilation and mortality in severe COVID-19 patients. |
- Elevation of liver enzymes three times higher than their reference value. - Possible thromboembolic events. |
100 mg every 6 h for a maximum of 15 days. | (171, 172) |
| Mavrilimumab | Binds to GM-CSFRα**** and disrupts downstream signaling. | Fast clinical improvement, decrease both the need for mechanical ventilation and mortality. | No adverse reactions to the infusion were observed. | 6 mg/kg single dose. | (173) |
| Steroids | |||||
| Dexamethasone |
- Anti-inflammatory action. - Inhibits phospholipase A2 and, consequently, prostaglandin, thromboxane, and leukotriene synthesis - Suppresses leukocyte migration - Recovers the BBB by upregulation of ZO-1 tight junction protein |
Decreased mortality in patients requiring oxygen therapy and mechanical ventilatory support when treatment is initiated 7 days after symptom onset. |
- Hyperglycemia - Increased risk of bacterial and fungal infections. |
6 mg/day for 10 days. | (174) |
GBPA, 4-[4-guanidinobenzoyl-oxy] phenylacetic acid; GM-CSF, Granulocyte-macrophage colony-stimulating factor (GM-CSF); TMPRSS2, Transmembrane serine protease 2.
*
Inhibitory activity against SARS-CoV-1 and MERS-CoV has been demonstrated.
**
The high expression of TMPRSS2 in different brain areas could be a potential therapeutic target for neurological manifestations and complications.
***
According to safety criteria and clinical trial data.
****
GM-CSF is a cytokine with a cardinal role in inflammation modulation. Ligand binding to the GM-CSF receptor-α (GM-CSFRα) activates multiple pro-inflammatory pathways and, in macrophages and neutrophils, results in increased secretion of pro-inflammatory cytokines.