Which antiviral medications are used for chemoprophylaxis and treatment of influenza?

Updated: Apr 23, 2019
  • Author: Hien H Nguyen, MD, MS; Chief Editor: Michael Stuart Bronze, MD  more...
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Answer

In the United States, the following antiviral drugs are recommended for chemoprophylaxis and/or treatment of influenza:

  • Baloxavir marboxil
  • Oseltamivir
  • Peramivir
  • Zanamivir

The CDC and IDSA have issue guidelines regarding antiviral treatment and prophylaxis. [83, 84]

The neuraminidase inhibitors (oseltamivir, peramivir, and zanamivir) and cap-dependent endonuclease inhibitors (baloxavir marboxil) have activity against influenza A and B viruses (including H1N1), whereas the adamantanes (amantadine and rimantadine) have activity against influenza A viruses only. Since 2006, only the neuraminidase inhibitors have been recommended, because of widespread resistance to the adamantanes among influenza A (H3N2) virus strains. Oseltamivir resistance emerged in the United States during the 2008-2009 influenza season.

Baloxavir marboxil was approved by the FDA in October 2018 for use in adults and adolescents aged 12 years or older as a single weight-based oral dose for use within 48 hours of symptom onset. It is a prodrug that inhibits cap-dependent endonuclease, an enzyme specific to influenza, resulting in inhibition of viral replication. In clinical trials, single-dose baloxavir was safe and effective in treating patients with uncomplicated influenza. It is active against influenza A and B, including strains resistant to neuraminidase inhibitors.

Oseltamivir, peramivir, and zanamivir work by inhibiting influenza virus neuraminidase, a glycoprotein spike that protrudes from the virus envelope; this spike is needed for successful cellular release of virus and transmission within the body.

Peramivir (Rapivab) was approved by the FDA in December 2014 for use in adults as a single 600-mg IV dose. In clinical trials, a single intravenous dose of peramivir, a sialic acid analogue and a selective inhibitor of neuraminidases produced by influenza A and B viruses, is effective and well tolerated in subjects with uncomplicated seasonal influenza virus infection. At both 300 mg and 600 mg, peramivir significantly reduced the time to alleviation of symptoms in comparison with placebo. [85] Additional data from over 2,700 subjects treated with peramivir in 27 clinical trials also supported its approval. It was available in the United States by emergency protocol during the 2009 H1N1 influenza pandemic.


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