Zanamivir

When ATH:
J05AH01

Pharmacological action

Powerful and highly selective inhibitor of neyroaminidazy, influenza virus surface enzyme, which provides a release of virus particles from infected cells and accelerates the penetration of the virus through the mucosal barrier to the surface of epithelial cells, thereby infecting etc.. cells of the respiratory tract. Replication of influenza virus limited surface epithelial cells of the respiratory tract. Zanamivir is active in the extracellular space, reducing the reproduction of both types of influenza virus (A and B) and preventing release of virus particles from cell surface of airway epithelium.

Pharmacokinetics

After inhalation of 10-20% of the absorbed dose administered, serum concentrations determined in 1-2 hours. The low systemic absorption (preserved and repeated inhalation) It leads to the low systemic concentrations and AUC. The absolute bioavailability after oral administration - 2%. In elderly patients and in patients with chronic renal failure bioavailability after administration 20 10-20 mg%. After oral inhalation, zanamivir is deposited in the respiratory tract in high concentrations. After inhalation 10 mg zanamivir in airway epithelial layer higher than the average concentration 1/2 inhibitory concentration for neyroaminidazy in 340 just across the 12 h after inhalation and 52 times through 24 no. Deposited in the oropharynx and lung (about 77,6% and 13,2% respectively). Do not metabolized. T1/2 после пероральной ингаляциии — 2,6–5,05 ч. Total clearance - 2,510,9 l /. Excreted by the kidneys in an unmodified form for 24 no.

Testimony

Influenza types A and B in adults and children older than 5 years (Treatment and Prevention).

Contraindications

Hypersensitivity, pregnancy (I trimester), lactation, childhood (to 5 years).

Dosage regimen

Inhalation.

Treatment: 2 inhalation 2 twice a day for 5 days. The total daily dose - 20 mg.

Prevention: 2 inhalation 1 once a day for 10 days. The total daily dose - 10 mg. Duration of reception can be increased to 1 Months, if the risk of infection persists for more than 10 days.

Side effect

Very often - more 1/10, often - more 1/100 less 1/10, sometimes - more 1/1000 less 1/100, rarely - more 1/10 000 less 1/1000, very rare - less 1/10000, including individual cases.

The respiratory system: very rarely - bronchospasm, difficulty breathing.

For the skin: very rarely - rash, hives.

Allergic reactions: very rare - swelling of the face, larynx.

Drug Interactions

Do not combine with other. inhalants (incl. ʙronxodilatatorami).

Cautions

For optimal effect, treatment should be started when the first symptoms of the disease. Patients with respiratory problems should have as a means of emergency short-bronchodilators for the treatment of zanamivir.