Drug information of Remdesivir

Remdesivir


Remdesivir is an experimental medicine being studied for use in treating conditions caused by coronaviruses. It is not yet known if remdesivir is a safe and effective treatment for any condition.

Mechanism of effect

Remdesivir is an adenosine nucleotide prodrug that is metabolized to the pharmacologically active nucleoside triphosphate metabolite after being distributed into cells. Remdesivir triphosphate acts as an adenosine triphosphate analog and competes for incorporation into RNA chains by the SARS-CoV-2 RNA-dependent RNA polymerase, resulting in delayed chain termination during viral RNA replication .

Pharmacodynamic

Remdesivir is a nucleoside analog used to inhibit the action of RNA polymerase. The duration of action is moderate, as it is given once daily. Patients should be counselled regarding the risk of infusion related reactions, elevated transaminases, and potential decreased efficacy when combined with hydroxychloroquine or chloroquine.

Pharmacokinetics

Metabolism:Metabolized to remdesivir triphosphate

Excretion: Urine (~74%; 49% as metabolite); feces (18%)

Drug indications

Coronavirus disease 2019 (COVID-19)

Dosage

May 1, 2020: The FDA has granted an emergency use authorization (EUA) for remdesivir to treat hospitalized adults and children with suspected or laboratory-confirmed SARS CoV-2 infection and severe COVID-19 disease.

EUA facilitates broader use of remdesivir, enabling access at additional hospitals across the country.

Severe COVID-19 disease is defined as patients with an oxygen saturation (SpO2) ≤94% on room air or requiring supplemental oxygen or requiring mechanical ventilation or requiring extracorporeal membrane oxygenation (ECMO).

Optimal treatment duration is unknown; for this EUA, dosing is as follows:

Dosage (weight 40 kg or more)

-Requires mechanical ventilation and/or ECMO

Day 1 loading dose: 200 mg IV infused over 30-120 min, THEN

Days 2-10 maintenance dose: 100 mg IV qDay

-Does not require mechanical ventilation and/or ECMO

Day 1 loading dose: 200 mg IV infused over 30-120 min, THEN

Days 2-5 maintenance dose: 100 mg IV qDay

If clinical improvement not demonstrated, treatment may be extended for up to 5 additional days (ie, up to 10 days total)

PEDIATRIC

Dosage (weight 3.5-40 kg)

-Requires mechanical ventilation and/or ECMO

Day 1 loading dose: 5 mg/kg mg IV infused over 30-120 min, THEN

Days 2-10 maintenance dose: 2.5 mg/kg IV qDay

-Does not require mechanical ventilation and/or ECMO

Day 1 loading dose: 5 mg/kg IV infused over 30-120 min, THEN

Days 2-5 maintenance dose: 2.5 mg/kg IV qDay

If clinical improvement not demonstrated, treatment may be extended for up to 5 additional days (ie, up to 10 days total)

 

Drug contraindications

Hypersensitivity to this drug

Hypersensitivity to drug or any ingredient

Side effects

fever , infusion reactions , Decreased creatinine clearance

Hyperglycemia ,Increased serum alanine aminotransferase ,increased serum aspartate aminotransferase ,Acute renal failure ,decreased estimated GFR , increased serum creatinine ,Fever ,ALT/AST Grade 3 ,ALT/AST Grade 4 ,Total bilirubin Grade 4, Decreased creatinine clearance ,Infusion related reaction (including hypotension, nausea, vomiting, diaphoresis, and shivering)

Interactions

atovaquone/proguanil , Divalproex sodium , Atomoxetine , Asparaginase , Amiodarone , Acarbose , Epirubicin , Ethambutol , Brentuximab , pegaspargase , givosiran , Macitentan , lutetium lu 177 dotatate , Kava kava , ethotoin , Daclizumab , Gefitinib , Gemtuzumab , ambrisentan , belinostat , ozanimod , selpercatinib , quinapril , bosutinib , Sulfamethoxazole , tolvaptan , Pasireotide , bedaquiline , etodolac , Blinatumomab , Ceritinib , Nilutamide , rilpivirine , Ipilimumab , Siponimod , Troleandomycin , Meclofenamate , Nabumetone , Oxaprozin , gilteritinib , Carmustine , Cobimetinib , Trovafloxacin , SULFISOXAZOLE , Cerivastatin , Larotrectinib , Crizotinib , Interferon alfa-2a , Rofecoxib , Methylnaltrexone , Bromfenac , Moexipril , lenvatinib , pexidartinib , elagolix , Metaxalone , Fedratinib , Tolcapone , Pralatrexate , Binimetinib , inotersen , Ixazomib , trabectedine , Duvelisib , Fostamatinib , Abacavir , Atovaquone , Aminosalicylic Acid , Ethionamide , Pazopanib , Benazepril , Milnacipran , Maraviroc , Nintedanib , red yeast rice , Troglitazone , Sulindac , Tipranavir , Oxytetracycline , Demeclocycline , Pyrazinamide , Eltrombopag , Pirfenidone , Efavirenz , Bexarotene , EMTRICITABINE , Celecoxib , Chlorzoxazone , Ketoprofen , Fosinopril , fenoprofen , Ramipril , Trandolapril , Perindopril , Tocilizumab , Peginterferon alfa-2b , dehydroepiandrosterone , Clofarabine , Regorafenib , Ponatinib , Inotuzumab‎ , Felbamate , Fosphenytoin , Idelalisib , Ivacaftor , Abiraterone , Tacrine , Panobinostat , Ribociclib , Niacin , Sarilumab , flurbiprofen , Lenalidomide , Telithromycin , Phenylbutazone , vemurafenib , Chloroquine , Rosiglitazone , Zileuton , Dantrolene , Afatinib , alectinib , Valproic acid , carfilzomib , Nefazodone , Axitinib , dronedarone , ritonavir , nevirapine , Aldesleukin , pravastatin , fluvastatin , Lomitapide , Mipomersen , teriflunomide , mercaptopurine , Didanosine , Pioglitazone , Fluoxymesterone , Tamoxifen , Dimethyl Fumarate , Pitavastatin , Febuxostat , Darunavir , Caspofungin , Zalcitabine , Stavudine , Zidovudine , Clarithromycin , Clotrimazole , Interferon beta-1a , Bicalutamide , Disulfiram , Rosuvastatin , orlistat , Voriconazole , Captopril , Carbamazepine , Ketorolac , Ketoconazole , Moxifloxacin , acitretin , Natalizumab , Nitrofurantoin , Nilotinib , Hydroxychloroquine , Minocycline , Methotrexate , Methimazole , Methyldopa , Mefenamic acid , Meloxicam , Lamivudine , Lapatinib , Lomustine , Lovastatin , Levofloxacin , Lisinopril , Fluconazole , Phenazopyridine , Fenofibrate , Phenytoin , Fingolimod , Labetalol , Sulfadiazine , Sulfasalazine , Cytarabine , Simvastatin , Cyclosporine , Flutamide , Diclofenac , Rifampin , Riluzole , Zafirlukast , Sunitinib , Sorafenib , Gemcitabine , Danazol , Dacarbazine , Doxycycline , Deferasirox , Duloxetine , Tretinoin , Testosterone , Temozolomide , Tolmetin , Tizanidine , Thioguanine , Bosentan , Posaconazole , Piroxicam , Tetracycline , Trastuzumab , Terbinafine , Interferon beta-1b , Interferon gamma-1b , Indomethacin , Infliximab , Bupropion , Bortezomib , Ibuprofen , Itraconazole , Isotretinoin , Isoniazid , Imatinib , Interferon alfa 2b , Erlotinib , Erythromycin , Acetaminophen , Oxaliplatin , Oxandrolone , Oxymetholone

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Alerts

-Infusion-related reactions observed during, and/or been temporally associated with, administration.Signs and symptoms may include hypotension, nausea, vomiting, diaphoresis, and shivering.If these symptoms occur, discontinue immediately and implement appropriate treatment

-Increased hepatic transaminases reported in healthy volunteers and patients with COVID-19

-in Hepatic impairment Use only if potential benefit outweighs risk

-Pediatric patients (aged >28 days) with eGFR <30 mL/min: Not recommended unless the potential benefit outweighs potential risk

-Full-term neonates (aged ≥7 days to ≤28 days) with serum creatinine >1 mg/dL: Not recommended unless the potential benefit outweighs potential risk

Points of recommendation

-ALT ≥5 x ULN at baseline: Do not initiate drug

-Discontinue drug if

    ALT ≥5 x ULN during treatment; may resume when ALT <5 X ULN,

    ALT elevation accompanied by signs or symptoms of liver inflammation or increasing conjugated bilirubin, alkaline phosphatase, or INR

-Coadministration of remdesivir is not recommended with chloroquine or hydroxychloroquine.Based on in vitro data, chloroquine demonstrated an antagonistic effect on the intracellular metabolic activation and antiviral activity of remdesivir

-Measure eGFR for all patients before dosing

-Obtain hepatic laboratory testing in all patients before initiating remdesivir and daily while receiving remdesivir

Pregnancy level

Consult a physician before using

No studies have been conducted in pregnant women

Remdesivir should be used during pregnancy only if the potential benefit justifies the potential risk for the mother and fetus

Breast feeding warning

Data are not available regarding the presence of remdesivir in human milk, effects on breastfed infants, or effects on milk production


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