其他抗病毒药物如何工作?

Reviewed on1/31/2022

How do other antivirals work?

Antivirals are medications used in the treatment and prevention of various types of viral infections. Other antivirals are medications that are not categorized into any specific classes of antivirals. Most of the other antivirals block viral replication by interfering with DNA polymerase, an enzyme vital for DNA synthesis and viral replication.

Some of the other antivirals are active drugs that directly take effect, while some are prodrugs, which release the active form of the drug after being metabolized. Other antivirals include the following:

  • Acyclovir: Acyclovir is an active drug effective againstherpessimplex virus 1 and 2 (HSV-1 and HSV-2) that causegenitaland oral herpes, andvaricella带状疱疹病毒(带状疱疹)which causeschickenpoxandshingles. Acyclovir gets incorporated into the viral DNA, inhibits DNA polymerase, and terminates the DNA chain to prevent viral replication.
  • Brincidofovir: Brincidofovir is aprodrugapproved for treating human smallpox, a disease caused by the variola virus. Although smallpox has been eradicated withvaccination, concerns that the variola virus can be used as a bioweapon remain.
    • Brincidofovir penetrates cells and releases cidofovir which is metabolized to produce cidofovir diphosphate, the active drug that selectively inhibits orthopoxvirus DNA polymerase-mediated viral DNA synthesis and reduces the rate of viral DNA synthesis.
  • Famciclovir: Famciclovir is a prodrug of penciclovir and is used to treat shingles, and suppressrecurrentepisodes of HSV-1 and HSV-2 inimmunocompetentadults as well as human immunodeficiency virus (HIV)-infected adults. Famciclovir blocks viral replication by inhibiting viral DNA polymerase.
  • Foscarnet: Foscarnet (phosphonoformic acid) is used to treatcytomegalovirus(CMV) infection and HSV inimmunocompromisedadults with resistance to acyclovir. Foscarnet works by inhibiting the activity of the pyrophosphate binding site on viral DNA polymerase and prevents viral replication.
  • Remdesivir: Remdesivir is used to treat COVID-19, caused by SARS-CoV-2, anRNA virus. Remdesivir is a prodrug that is metabolized into remdesivir triphosphate (RDV-TP), which inhibits SARS-CoV-2 RNA-dependent RNA polymerase, the enzymeessentialfor viral replication.
  • Tecovirimat: Tecovirimat is anantiviraldrug approved for the treatment of human smallpox disease. Tecovirimat inhibits the activity of orthopoxvirus VP37 protein, preventing the formation of enveloped viral particles (virions) which can get out of the infected cells and infect other healthy cells.
  • Valacyclovir: Valacyclovir is a prodrug and is metabolized by the liver into acyclovir and has similar effects against HSV infections.
  • Valganciclovir: Valganciclovir is a prodrug ofganciclovir, used in the prevention and treatment of CMV infection. Valganciclovir inhibits viral DNA polymerase and prevents DNA synthesis and chain elongation. The drug gets incorporated into the viral DNA and prevents the incorporation of deoxyguanosine triphosphate, an essential compound required for DNA synthesis.

What are the uses of other antivirals?

Other antivirals may be administered through the following routes:

  • Oral tablets, capsules, solutions, or suspensions
  • Intravenous (IV) infusions
  • Intravenous injections

The FDA-approved uses of other antivirals include:

  • Acyclovir:
    • Treatment and suppression of genital herpes
    • Herpes simplex virus (HSV)encephalitis(brain inflammation)
    • Treatment of mucocutaneous HSV infection in immunocompromised adults
    • NeonatalHSV infection
    • Varicella-zoster infection (chickenpox)
    • Herpes zosterinfection (shingles), which is caused by reactivation of VZV
    • Herpetickeratitis(corneal inflammation from herpes) - Orphan
  • Brincidofovir:
    • Human smallpox disease, caused by the variola virus
  • Famciclovir:
    • Acute herpes zoster infection (shingles)
    • Herpes labialis (cold sores that primarily affect the lips)
    • Genital herpes
    • Prevention of HSV reactivation and treatment of recurrent episodes in adults infected with human immunodeficiency virus (HIV)
  • Foscarnet:
    • Cytomegalovirus (CMV) retinitis (inflammation of theretina) in adults withacquiredimmunodeficiency syndrome (AIDS)
    • HSV in immunocompromised adults with resistance to acyclovir
    • Remdesivir:
    • Treatment ofcoronavirusdisease 2019 (COVID-19) in hospitalized patients aged 12 years or older
  • Tecovirimat:
    • Human smallpox disease
  • Valacyclovir:
    • Herpes labialis
    • Herpes zoster
    • Genital herpes
    • Chickenpox
  • Valganciclovir:
    • Treatment of CMV retinitis in adults with AIDS
    • CMV prevention in solid organ (heart/kidney/pancreas) transplant
    • CMVcolitisoresophagitisin HIV-infected adults (off-label)
    • Lymphoproliferative disorder (orphan designation)

What are side effects of other antivirals?

Side effects of other antivirals vary with each type of drug. A few of the most common side effects may include:

  • Acyclovir:
    • Malaise
    • 炎症或phlebitis(vein inflammation) at the injection site
    • Nausea and vomiting
    • Diarrhea
    • Rash or hives
    • Headache
  • Brincidofovir:
    • Diarrhea
    • Nausea and vomiting
    • Abdominal pain
    • Elevated serum creatinine
    • Elevated liver enzymes ALT and AST
    • Elevated total bilirubin
  • Famciclovir:
  • Foscarnet:
    • Fever and headache
    • Nausea and vomiting
    • Anemia
    • Diarrhea
    • Abnormal kidney function
    • Seizures
  • Remdesivir:
    • Abnormal kidney function with reduced eGFR and elevated creatinine level
    • Decrease inhemoglobin
    • Increase inblood glucoselevels
    • Decrease in lymphocytes
    • Increase inprothrombin time(blood clotting time)
    • An increase in liver enzymes ALT and AST
  • Tecovirimat:
    • Headache
    • Nausea and vomiting
    • Abdominal pain
    • Dry mouthand oropharyngeal pain
    • Skin and subcutaneous reactions
    • Abnormal electroencephalogram (EEG)
  • Valacyclovir:
    • Headache
    • Neutropenia(lowneutrophilcount in the blood)
    • Elevated liver enzymes ALT and AST
    • Nasopharyngitis (inflammation of nose and throat)
    • Nausea
    • Abdominal pain
  • Valganciclovir:
    • Diarrhea and abdominal pain
    • Anemia andgranulocytopenia(low count ofgranulocytes, type of immune cells)
    • Fever and headache
    • Insomnia
    • Nausea and vomiting
    • Retinal detachment

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

What are names of some of the other antivirals?

Genericand brand names of some of the other antivirals include:

References
https://reference.medscape.com/drugs/antivirals-other

https://www.fda.gov/drugs/news-events-human-drugs/fda-approves-drug-treat-smallpox

https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214460s000,214461s000lbl.pdf

https://www.uptodate.com/contents/ganciclovir-and-valganciclovir-an-overview

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