Rimantadine, tablets 50 mg 20 pcs

Pharmacotherapeutic group: Antiviral drug.
ATX code: J05AC02

Pharmacological properties:

Pharmacodynamics
Rimantadine is an antiviral agent, an adamantane derivative; active against various shiampas of influenza A virus (especially type A2).
A weak base, the drug Rimantadine acts by increasing the pH of endosomes, which have a membrane of vacuoles that surround viral particles after their penetration into the cell. Preventing acidification in these vacuoles blocks the fusion of the viral membrane with the endosome membrane, thus preventing the transfer of viral genetic material into the cell cytoplasm. The drug Rimantadine also inhibits exit of viral particles from the cell, i.e. it interrupts transcription of the viral genome.

Pharmacokinetics
After oral administration, the drug Rimantadine is almost completely absorbed in the intestine.
Absorption is slow. Binding to plasma proteins is about 40%. Distribution volume: adults – 17-25 l/kg, children – 289 l/kg. Concentration in nasal secretion is 50% higher than plasma concentration. Maximal concentration of preparation Rimantadine in plasma (Сmax) when administered by 100 mg once daily – 181 ng/ml, by 100 mg twice daily – 416 ng/ml.
Metabolized in liver. Half-life period (T1/2) – 24-36 hours; excreted by kidneys – 15% unchanged, 75-85% – as metabolites.
The T1/2 in chronic renal insufficiency is increased twice. In patients with renal insufficiency and elderly patients it may accumulate in toxic concentrations if the dose is not corrected in proportion to the decrease of creatinine clearance.

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