zanamivir

Brand: Relenza

Prototype: oseltamivir
Drug Class: neuraminidase inhibitor antiviral
Drug Family: antiviral
Subclass: inhaled neuraminidase inhibitor (influenza)
Organ Systems: infectious-diseaserespiratory

Mechanism of Action

Competitively inhibits influenza A and B neuraminidase, preventing cleavage of sialic acid from cell surface receptors; blocks viral release and spread from infected cells; inhaled formulation delivers drug directly to respiratory tract.

influenza neuraminidase (NA)

Indications

  • treatment of influenza A and B (initiated within 48 hours of symptom onset)
  • prophylaxis of influenza A and B in household contacts

Contraindications

  • zanamivir hypersensitivity
  • severe asthma or COPD (risk of bronchospasm)

Adverse Effects

Common

  • cough (from inhalation)
  • bronchospasm (particularly in reactive airway disease)
  • sinusitis

Serious

  • severe bronchospasm (with or without asthma/COPD — can be fatal)
  • anaphylaxis
  • neuropsychiatric events (particularly in pediatric patients)

Pharmacokinetics (ADME)

Absorption 4–17% systemic absorption (inhaled); rest deposited in oropharynx
Distribution minimal systemic distribution from inhaled route
Metabolism not metabolized (unchanged drug systemically available)
Excretion renal (unchanged, absorbed fraction)
Half-life 2.5–5.1 hours (systemic)
Onset rapid (local respiratory tract)
Peak 1–2 hours
Duration 12 hours (twice-daily dosing for treatment)
Protein Binding <10%
Vd low (systemic)

Drug Interactions

Drug / Agent Mechanism Severity
live attenuated influenza vaccine antiviral activity may reduce vaccine replication; do not administer 2 weeks before or 48 hours after zanamivir moderate

Nursing Considerations

  1. Teach inhaler technique: zanamivir is delivered via Diskhaler device; proper inhalation is essential for lung deposition.
  2. Assess for reactive airway disease before prescribing; contraindicated in severe asthma or COPD — have a bronchodilator available if zanamivir is used.
  3. Initiate within 48 hours of symptom onset for meaningful clinical benefit in influenza treatment.
  4. Counsel patients that zanamivir is not a substitute for annual influenza vaccination.

Clinical Pearls

  • Zanamivir's inhaled route delivers very high concentrations directly to the respiratory epithelium, potentially advantageous for severe influenza pneumonia, while minimizing systemic exposure — though this also limits its role when systemic antiviral activity is needed.
  • Resistance to zanamivir can develop but is less common than with oseltamivir; zanamivir retains activity against many oseltamivir-resistant H275Y strains.

Safety Profile

Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Not required
TDM Not required