Generic name: remdesivir (rem DES i veer) Brand name:Veklury Dosage forms: intravenous powder for injection (100 mg); intravenous solution (5 mg/mL) Drug class: Investigational drugs, Purine nucleosides
Remdesivir (Veklury) is an antiviral drug with activity against SARS-CoV-2 (COVID-19). It has been FDA approved for the treatment of adult and pediatric patients with COVID-19 infection requiring hospitalization.
Remdesivir has got emergency authorization by the FDA in combination with Baricitinib for patients with severe COVID-19 infection who require supplemental oxygen, invasive mechanical ventilation, or ECMO (extracorporeal membrane oxygenation).
Warnings
Remdesivir is for use only in people with COVID-19 who are in a hospital. You must remain under the care of a doctor while receiving remdesivir.
Before taking this medicine
You should not be treated with remdesivir if you are allergic to it.
Tell your doctor if you have ever had:
liver disease; or
kidney disease.
Tell your doctor if you are pregnant or plan to become pregnant, or if you are breastfeeding.
Remdesivir (Veklury) Uses:
It is indicated for the treatment of COVID-19 infection in adults and children who are 12 years of age or more and weighing at least 40 kgs or more requiring hospitalization.
The drug should only be administered in a hospital or a healthcare setting that is capable of providing acute inpatients hospital care.
Update November 19th, 2020:
“FDA Approved Baricitinib (Olumiant) in combination with Remdesivir for COVID-19 infection”
FDA on 19th November approved Remdesivir + Baricitinib (a Janus Kinase inhibitor) for the treatment of patients infected with COVID-19 fulfilling the following criteria [Ref]:
Adult and pediatric patients who are 2 years of age or older,
“WHO recommends against the use of Remdesivir in patients with COVID-19 infection!”
The recent recommendations advising physicians not to use “Remdesivir” in patients with COVID-19 infection were developed by an international guideline development group, which includes 28 clinical care experts, 4 patient-partners, and one ethicist.
Data from WHO Solidarity Trial and three randomized clinical trials that were evaluated did not support the use of remdesivir in patients with COVID-19 infection.
The WHO recommendation states [Ref]:
THE EVIDENCE SUGGESTED NO IMPORTANT EFFECT ON MORTALITY, NEED FOR MECHANICAL VENTILATION, TIME TO CLINICAL IMPROVEMENT, AND OTHER PATIENT-IMPORTANT OUTCOMES.
Remdesivir (Veklury) Dose in Adults and children weighing 40 kgs or more:
Note:
Before treatment initiation, perform renal and liver function testing and calculate estimated GFR.
Monitor prothrombin time prior to treatment initiation and during the treatment in all patients.
Remdesivir (Veklury) Dose in the treatment of COVID-19 infection:
Loading Dose: A single loading dose of 200 mg via intravenous infusion on day 1.
Maintenance Dose: After a loading dose on the first day, initiate maintenance treatment as 100 mg intravenous infusion from day 2 and onwards.
Treatment Duration:
Patients not requiring invasive mechanical ventilation or extracorporeal membrane oxygenation (ECMO):
The recommended duration is a total of 5 days.
The duration of treatment may be extended to a total of 10 days in patients who do not show significant improvement with the five days of treatment.
Patients requiring Invasive mechanical ventilation or ECMO:
The recommended duration of treatment is 10 days.
Remdesivir (Veklury) Dose in Children:
The safety and efficacy of the drug in patients who are 12 years of age or younger and weighing 40 kgs or less have not been established.
For dose in children 12 years of age or older weighing 40 kgs or more, refer to “Dose in Adults”.
Pregnancy Risk Category: C
Clinical trials are currently being conducted.The data available is limited.The data available from published case reports, and compassionate use of Remdesivir in pregnancies are not enough to assess for drug-related adverse maternal or fetal outcomes.
Studies on animal reproduction did not reveal any adverse outcomes for fetal health at 4x the recommended doses.
Patients who are pregnant and are admitted to a hospital are at greater risk for adverse pregnancy outcomes because of COVID-19 infection.
Remdesivir use during breastfeeding:
It is unknown whether the drug can be excreted into breastmilk.The drug was detected in breastmilk from lactating animals in animal studies.
Manufacturers recommend weighing the benefits and risks of drug treatment for the mother against the benefits of breastfeeding.
Remdesivir Dose in Kidney Disease:
The use of remdesivir in patients with kidney disease has not been evaluated.
The intravenous formulation contains betadex sulfobutyl ether sodium that is excreted via the kidneys. The manufacturer recommends avoiding it in patients with an estimated GFR of less than 30 ml/minute.
Renal functions and eGFR should be calculated before treatment initiation and during the treatment.
USE IN PATIENTS WITH EGFR OF LESS THAN 30 ML/MINUTE IS NOT RECOMMENDED
Remdesivir Dose in Liver disease:
There are no dosage adjustments provided in the manufacturer’s labeling. The manufacturer recommends monitoring liver functions before treatment initiation and as clinically indicated during treatment.
Side effects of Remdesivir (Veklury):
Hypersensitivity reactions:
Hypersensitivity reactions including serious anaphylactic reactions may occur.
Urticaria
Itching
Rash
Swelling around the face and eyes.
Difficulty breathing
Hepatotoxicity:
Liver enzyme elevations predominantly ALT and AST may occur.
Extravasation:
Administration site extravasation can occur resulting in vesication
Neurological side effects:
Seizures
Contraindications to Remdesivir (Veklury):
Veklury is not recommended for patients suffering from hypersensitivity reactions to any component or drug.
Warnings and precautions
Hypersensitivity reactions:
Hypersensitivity reactions, including infusion-related allergic reaction, may occur.Itching, nausea, urticaria, itching and other allergic reactions can all occur.Anaphylactoid reactions can be serious and may lead to death. They may manifest as hypotension or shortness of breath, tachycardia or hypoxia, fever and angioedema.
To avoid hypersensitivity reactions, it is best to give the drug by slow intravenous injection for at least two hours.
Patients should be monitored closely during and after the administration of the drug.
Hypersensitivity reactions can be severe and should be stopped immediately.
Patients who have a history of hypersensitivity reactions to the drug should be advised not to take it.
Hepatotoxicity:
It is not uncommon to experience mild or moderate elevations of liver enzymes (ALT, AST), but these usually disappear after discontinuing treatment.
Patients with COVID-19 infection may also experience mild to moderate transaminitis.
As indicated, liver function should be checked at baseline and periodically throughout treatment.
The treatment might need to be stopped if the ALT is higher than 10 times the normal upper limit.
Patients with elevated ALT that is not more than 10 times the normal upper limit may need to be stopped from treatment.
Use Hydroxychloroquine or Chloroquinephosphate in conjunction
Patients who take concomitant hydroxychloroquine and chloroquine may have lower antiviral activity.
Remdesivir is not recommended for use with hydroxychloroquinephosphate or chloroquinephosphate due to its antagonistic activity.Both antimalarial drugs block the intracellular metabolic activation.
Monitoring Parameters:
Observe for hypersensitivity reactions
Monitor liver functions and renal functions at baseline and as clinically indicated during the treatment.
Monitor the oxygenation status of the patient.
How to administer Remdesivir (Veklury)?
The drug is administered via a slow intravenous infusion over 30 – 120 minutes. It should not be administered simultaneously with any other medication. Compatibility with solutions other than 0.9% saline is not known.
The product does not contain any bacteriostatic agent or a preservative. Care should be taken to avoid any inadvertent contamination while preparing the solution. It is best to infuse the prepared solution immediately after preparation.
The injection should be allowed to equilibrate at room temperature before preparing the final solution. Sealed vials can be stored for up to 12 hours at room temperature before dilution.
The injection should be diluted in an infusion bag containing 250 ml of 0.9% saline. The bag should be inverted 20 times to mix the solution bag. Do not shake the bag.
The prepared solution is stable for 24 hours at room temperature or 48 hours at refrigerated temperature.
Mechanism of action of Remdesivir (Veklury):
Remdesivir (Veklury), an antiviral drug, is active against COVID-19.It blocks the SARS-CoV2 essential RNA polymerase, which is critical for viral replication.
After it has been distributed into cells, it is converted to adenosine monophosphate intermediate and metabolized.It is converted to active form depending on the type of cell.
Cellular kinases then phosphorylate it to the pharmacologically active nucleoside triphosphate metabolism.
RDV-TP (Remdesivir Triphosphate) is incorporated by the SARS-2 RNA-dependentRNA polymerase. It acts as an analog to adenosinetriphosphate.This causes delayed chain termination in the replication of viral RNA.
Protein binding:
88 – 93%
Half-life elimination:
One hour
Metabolism:
CES1 (80%)
Cathepsin A (10%)
CYP3A (10%)
Drug elimination:
Major route of drug elimination: 80% of the drug is metabolized, 10 % is excreted in urine, 10% (Not detected)
What happens if I miss a dose?
Because you will receive remdesivir in a clinical setting, you are not likely to miss a dose.
What happens if I overdose?
Since remdesivir is given by a healthcare professional in a medical setting, you will be treated quickly if an overdose occurs.
What should I avoid while receiving remdesivir?
Follow your doctor's instructions about any restrictions on food, beverages, or activity.
What other drugs will affect remdesivir?
Tell your doctor if you also take chloroquine or hydroxychloroquine. Either of these other medicines could make remdesivir less effective.
International Brand Names of Remdesivir:
Veklury (GiLead Sciences)
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