Remdesivir is an antiviral drug that inhibits the RNA polymerase of SARS-CoV-2, blocking viral replication. It is administered intravenously as a prodrug that is metabolized to the active nucleoside triphosphate form inside cells. For COVID-19 treatment in adults and children over 12 weighing over 40kg, it is given as a 200mg loading dose on day 1 followed by 100mg daily for 5-10 days, depending on clinical improvement and need for ventilation support. Common side effects include increased creatinine, decreased hemoglobin and lymphocytes, and increased glucose and liver enzymes.

1. Remdesivir
Dr Imtiaz Ahmad PGR-MD

2. Mechanism of Action
• Inhibits SARS-CoV-2 RNA-dependent RNA polymerase (RdRp), which is essential for viral
replication
• Adenosine nucleotide prodrug that distributes into cells, where it is metabolized to form the
pharmacologically active nucleoside triphosphate metabolite
• Metabolism of remdesivir to remdesivir triphosphate (RDV-TP) demonstrated in multiple cell
types
• RDV-TP acts as an analog of adenosine triphosphate (ATP) and competes with the natural ATP
substrate for incorporation into nascent RNA chains by the SARS-CoV-2 RNA-dependent RNA
polymerase, which results in delayed chain termination during replication of the viral RNA
• Remdesivir triphosphate is a weak inhibitor of mammalian DNA and RNA polymerases with low
potential for mitochondrial toxicity

3. Dosage Forms & Strengths
Injection, lyophilized powder for reconstitution
• 100mg/vial
Injection, concentrated solution
• 100mg/20mL (5mg/mL)

4. Coronavirus Disease 2019 (COVID-19)
• Indicated for adults and pediatric patients aged ≥12 years who weigh
≥40 kg for treatment of COVID-19 requiring hospitalization
• Day 1 loading dose: 200 mg IV infused over 30-120 min, THEN
• Day 2 and thereafter: 100 mg IV qDay
• Treatment duration
• Not requiring invasive mechanical ventilation and/or extracorporeal
membrane oxygenation (ECMO): 5 days; if clinical improvement not
demonstrated, treatment may be extended up to 10 days total
• Requires invasive mechanical ventilation and/or ECMO: 10 days

5. Dosage Modifications
• Renal impairment
• Pharmacokinetics have not been evaluated in patients with renal
impairment
• eGFR ≥30 mL/min: No dose adjustment
• eGFR <30 mL/min: Not recommended; sulfobutylether-beta-
cyclodextrin sodium salt (SBECD) excipient in the concentrated
solution is renally cleared and accumulates in patients with decreased
renal function
• Hepatic impairment
• Not evaluated; unknown if dosage adjustment required

6. Dosing Considerations
• Laboratory tests
• Obtain before initiating in all patients and while receiving as clinically
appropriate
• Determine eGFR
• Perform hepatic laboratory testing
• Determine prothrombin time

7. COVID-19 in Younger Children (Investigational)
Emergency Use Authorization (EUA) issued for hospitalized pediatric patients
weighing 3.5 kg to <40 kg or children aged <12 years who weigh at least 3.5 kg
Weight 3.5-40 kg
Day 1 loading dose: 5 mg/kg mg IV infused over 30-120 min, THEN
Day 2 and thereafter: 2.5 mg/kg IV qDay
Age <12 years and weight 40 kg or more
Day 1 loading dose: 200 mg IV infused over 30-120 min, THEN
Day 2 and thereafter: 100 mg IV qDay

8. Interactions
Serious - Use Alternative
• chloroquine
• hydroxychloroquine sulfate
Pregnancy
• Available data from published case reports and compassionate use of
remdesivir in pregnant women are insufficient to evaluate for a drug-
associated risk of major birth defects, miscarriage, or adverse
maternal or fetal outcomes

9. Elimination & Excretion
• Half-life
• 1 hr
• Major route
• Metabolism
• Urine
• 10%
• Feces
• Not detected

10. Adverse Effects
• Adverse Effects
• >10%
• Creatinine increased* (5-15%)
• Hemoglobin decreased* (6-15%)
• Glucose increased* (11-12%)
• Lymphocytes decreased* (11%)
• Prothrombin time increased (9%)
• ALT increased* (3-8%)
• AST increased* (6-7%)
• Nausea (3-5%)
• Bilirubin increased* (2%)
• Hypersensitivity reactions (<2%)
• Generalized seizure (<2%)
• Rash (<2%)