Table 2. Characteristics of Antiviral Agents That Are Approved or Under Evaluation for Treatment of COVID-19

Last Updated: November 03, 2020

Table 2. Characteristics of Antiviral Agents That Are Approved or Under Evaluation for Treatment of COVID-19
Drug Name Dosing Regimens
The doses listed here are for approved indications or from reported experiences or clinical trials.
Adverse Effects Monitoring Parameters Drug-Drug Interaction Potential Panel’s Recommendations, Comments, and Links to Clinical Trials
Chloroquine
Dose Previously Suggested in an EUA for Adults and Adolescents Weighing ≥50 kg:
  • CQ 1 g PO once on Day 1, then CQ 500 mg PO once daily for 4–7 days of total treatment. Treatment duration should be based on clinical evaluation.
  • Prolonged QTc interval, Torsades de Pointes, AV block, ventricular arrhythmia
  • Gastrointestinal effects (e.g., nausea, vomiting, diarrhea)
  • Hepatitis
  • Hypoglycemia
  • Hemolysis (especially in patients with G6PD deficiency)
  • Myopathy
  • Rash
  • Given the risk of heart rhythm problems, the FDA cautions against using CQ to treat COVID-19 outside of a hospital or a clinical trial.1
  • CBC, hepatic panel, blood glucose, SCr, potassium, magnesium
  • Baseline ECG
  • Follow-up ECG if CQ is given with QTc-prolonging drugs or if the patient has underlying cardiac disease
  • Additive effect with other drugs that prolong the QTc interval (including AZM) or that cause hypoglycemia
  • CYP2D6 inhibitor (moderate)
  • P-gp inhibitor
  • The Panel recommends against the use of CQ with or without AZM for the treatment of COVID-19 in hospitalized patients (AI).
  • In nonhospitalized patients, the Panel recommends against the use of CQ with or without AZM for the treatment of COVID-19, except in a clinical trial (AI).
  • The Panel recommends against using high-dose CQ (600 mg twice daily for 10 days) for the treatment of COVID-19 (AI).
  • Dose-dependent toxicity
  • A list of clinical trials is available here: Chloroquine
Hydroxychloroquine Adults:
  • Various loading and maintenance doses have been reported in studies or in clinical care.
Dose Previously Suggested in an EUA for Hospitalized Adults and Adolescents Weighing ≥50 kg:
  • HCQ 800 mg PO once on Day 1, then HCQ 400 mg PO once daily for 4–7 days of total treatment. Treatment duration should be based on clinical evaluation.
  • Prolonged QTc interval, Torsades de Pointes, AV block, ventricular arrhythmia
  • Gastrointestinal effects (e.g., nausea, vomiting, diarrhea)
  •  Hepatitis
  • Hypoglycemia
  • Myopathy
  • Anxiety, agitation, hallucinations, psychosis
  • Allergic reaction/rash
  • Given the risk of heart rhythm problems, the FDA cautions against using HCQ for to treat COVID-19 outside the setting of a hospital or a clinical trial.1
  • CBC, hepatic panel, blood glucose, SCr, potassium, magnesium
  • Baseline ECG
  • Follow-up ECG if HCQ is given with QTc-prolonging drugs (e.g., AZM) or if the patient has underlying cardiac disease
  • Additive effect with other drugs that prolong the QTc interval (including AZM) or that cause hypoglycemia
  • CYP2D6 inhibitor (moderate)
  • P-gp inhibitor
  • The Panel recommends against the use of HCQ with or without AZM for the treatment of COVID-19 in hospitalized patients (AI).
  • In nonhospitalized patients, the Panel recommends against the use of HCQ with or without AZM for the treatment of COVID-19, except in a clinical trial (AI).
  • Long elimination; half-life is 40–55 days.
  • Dose-dependent toxicity
  • A list of clinical trials is available here: Hydroxychloroquine
Lopinavir/Ritonavir Adults:
  • LPV 400 mg/RTV 100 mg PO twice daily for 10–14 days
Neonates Aged ≥14 Days with a PMA ≥42 Weeks and Children Aged <18 Years:
  • LPV 300 mg/m2 plus RTV 75 mg/m2 (maximum dose: LPV 400 mg/RTV 100 mg) PO twice daily for a total of 7 days
  • Gastrointestinal effects (e.g., nausea, vomiting, diarrhea)
  • Transaminase elevation
  • QTc interval prolongation and Torsades de Pointes have been reported.
  • PR interval prolongation
  • HIV antigen/antibody testing at baseline
  • Serum transaminase levels
  • Consider monitoring ECG when LPV/RTV is given with other QTc-prolonging medications.
High Drug-Drug Interaction Potential
Lopinavir:
  • CYP3A4 inhibitor and substrate
Ritonavir:
  • CYP3A4 > CYP2D6 substrate
  • Potent CYP3A4 and CYP2D6 inhibitor
  • Inducer of UGT1A1 and CYP1A2, CYP2C8, CYP2C9, and CYP2C19
  • The Panel recommends against using LPV/RTV (AI) or other HIV PIs (AIII) to treat COVID-19, except in a clinical trial.
  • Liquid formulation is commercially available. Crushing LPV/RTV tablets may result in significantly decreased drug exposure (AUC ↓ 45%).2
  • Use with caution in patients with hepatic impairment.
  • A list of clinical trials is available here: Lopinavir/Ritonavir
Remdesivir

Note: RDV is FDA approved for the treatment of COVID-19.

For Hospitalized Adult and Pediatric Patients (Aged ≥12 Years and Weighing ≥40 kg)

For Patients Who Are Not Mechanically Ventilated and/or on ECMO:

  • RDV 200 mg IV over 30–120 minutes on Day 1, followed by RDV 100 mg IV on Day 2 through Day 5
  • In patients who have not shown clinical improvement after 5 days of therapy, treatment may be extended up to 10 days.                 

For Mechanically Ventilated Patients and/or Patients on ECMO:

  • RDV 200 mg IV over 30–120 minutes on Day 1, followed by RDV 100 mg IV on Day 2 through Day 10

Suggested Dose in EUAa for Hospitalized Pediatric Patients Weighing 3.5 kg to <40 kg or Aged <12 Years and Weighing ≥3.5 kg

For Patients Weighing 3.5 kg to <40 kg:

  • RDV 5 mg/kg IV over 30–120 minutes on Day 1, followed by RDV 2.5 mg/kg once daily starting on Day 2
  • For patients who are not mechanically ventilated and/or on ECMO, the recommended treatment duration is 5 days. If patients have not shown clinical improvement after 5 days of therapy, treatment may be extended up to 10 days.
  • For mechanically ventilated patients and/or patients on ECMO, the recommended treatment duration is 10 days.

For Patients Aged <12 Years and Weighing ≥40 kg:

  • Same dose as for adults and children aged >12 years and weighing >40 kg
  • Nausea
  • ALT and AST elevations
  • Hypersensitivity
  • Increases in prothrombin time
  • Drug vehicle is SBECD, which has been associated with renal toxicity. SBECD accumulation may occur in patients with moderate or severe renal impairment.
  • Each 100 mg vial of remdesivir lyophilized powder contains 3g of SBECD and each 100 mg/20 mL vial of remdesivir solution contains 6g of SBECD.
  • Infusion reactions
  • Renal function, hepatic function, and prothrombin time should be monitored before and during treatment as clinically indicated
  • Not recommended if eGFR is <30 mL/min
  • RDV may need to be discontinued if ALT levels increase to >10 times the ULN and should be discontinued if there is an increase in ALT level and signs or symptoms of liver inflammation are observed.3
  • Clinical drug-drug interaction studies of RDV have not been conducted.
  • In vitro, RDV is a substrate of CYP3A4, OATP1B1 and P-gp and an inhibitor of CYP3A4, OATP1B1, OATP1B3, and MATE1.3
  • Minimal to no reduction in RDV exposure is expected when RDV is coadministered with dexamethasone (Gilead Sciences, written communication, July 2020).
  • CQ or HCQ may decrease the antiviral activity of RDV; coadministration of these drugs is not recommended.3
  • No significant interaction is expected between RDV and oseltamivir or baloxavir (Gilead Sciences, personal and written communications, August and September 2020).
Availability:
  • RDV is approved by the FDA for the treatment of COVID-19 in hospitalized adult and pediatric patients (aged ≥12 years and weighing ≥40 kg).
  • An EUAa is available for hospitalized pediatric patients weighing 3.5 kg to <40 kg or aged <12 years and weighing ≥3.5 kg.
  • A list of clinical trials is available here: Remdesivir