Neuraminidase Inhibitors – Action, Use & Side Effects
Neuraminidase inhibitors are antiviral medications that specifically target the influenza virus, reducing its spread within the body and shortening the duration of flu illness.
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Neuraminidase inhibitors are antiviral medications that specifically target the influenza virus, reducing its spread within the body and shortening the duration of flu illness.
What Are Neuraminidase Inhibitors?
Neuraminidase inhibitors are a class of antiviral drugs used specifically against influenza viruses (flu viruses). They work by blocking the enzyme neuraminidase, which is found on the surface of influenza A and B viruses and is essential for the release of newly formed viral particles from infected cells. By inhibiting this enzyme, the spread of the virus throughout the body is significantly reduced.
Mechanism of Action
The enzyme neuraminidase cleaves sialic acid bonds on the surface of host cells. This step is necessary for newly formed viruses to leave the infected cell and infect neighboring cells. Neuraminidase inhibitors bind competitively to the active site of this enzyme, preventing the cleavage of sialic acid. As a result, newly produced viral particles remain attached to the cell surface and cannot spread further. This reduces the viral load in the body and lessens the severity of illness.
Active Substances and Application
Oseltamivir
Oseltamivir (brand name: Tamiflu) is the most well-known neuraminidase inhibitor and is taken orally as a capsule or oral suspension. It is approved for both the treatment and prevention (prophylaxis) of influenza. Treatment should ideally begin within 48 hours of the onset of the first symptoms.
Zanamivir
Zanamivir (brand name: Relenza) is administered by inhalation and is delivered directly to the airways. It is also approved for the treatment and prophylaxis of both influenza A and B.
Peramivir
Peramivir is administered intravenously and is particularly suitable for patients who are unable to take oral or inhaled medications, for example in cases of severe illness.
Laninamivir
Laninamivir is a long-acting neuraminidase inhibitor approved primarily in Japan and administered by inhalation.
Indications
Neuraminidase inhibitors are used for:
- Treatment of seasonal influenza A and B
- Prophylaxis in high-risk groups (e.g., immunocompromised individuals, the elderly, pregnant women)
- Treatment of avian influenza (bird flu) and pandemic influenza strains
- Post-exposure prophylaxis after close contact with an infected person
Dosage
Dosage varies depending on the active substance, route of administration, age, and renal function of the patient. For oseltamivir, the standard adult treatment dose is typically 75 mg twice daily for 5 days. In children, the dose is adjusted according to body weight. A dose reduction is required in patients with impaired kidney function.
Side Effects
Neuraminidase inhibitors are generally well tolerated. The most common side effects include:
- Nausea and vomiting (especially with oseltamivir; taking it with food is recommended)
- Headache
- Dizziness
- Bronchospasm (particularly with zanamivir; caution in patients with asthma or COPD)
- In rare cases: neurological symptoms such as confusion or hallucinations (especially in children and adolescents)
Resistance
As with other antiviral agents, resistance can develop. The H275Y mutation in the neuraminidase gene is particularly well known and can lead to oseltamivir resistance. Regular surveillance programs monitor the emergence of resistant influenza strains worldwide.
Important Notes
Neuraminidase inhibitors are not a substitute for the annual flu vaccination. Vaccination remains the most important measure for preventing influenza. Antiviral therapy complements vaccination but does not replace it. Early initiation of treatment -- ideally within the first 48 hours of symptom onset -- is critical for effectiveness.
References
- World Health Organization (WHO): Influenza (Seasonal). WHO Fact Sheet, 2023. Available at: https://www.who.int/news-room/fact-sheets/detail/influenza-(seasonal)
- Jefferson T, Jones M, Doshi P et al.: Oseltamivir for influenza in adults and children: systematic review of clinical study reports and summary of regulatory comments. BMJ 2014; 348: g2545.
- Hayden FG: Antivirals for influenza: historical perspectives and lessons learned. Antiviral Research 2006; 71(2-3): 372-378.
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