Chemical formula: C₂₀H₂₇N₅O₃ Molecular mass: 385.468 g/mol
Bamifylline is a methylxanthinic derivative with two side chains in position 7 and 8, distinguishing it clearly from theophylline.
Bamifylline carries out a bronchospasmolytic action on the smooth musculature and also blocks the action of the bronchoconstriction mediators.
The intensity of its bronchospasmolytic action is equal to that of theophylline.
Unlike theophylline, bamifylline usually has no exciting effects on the central nervous system.
Its pharmacokinetic characteristics are very interesting. Its absorption, both by oral and rectal route, is rapid, reaching the plasma peak between the first and the second hour. Its diffusion in the extravascular area is high, with a distribution volume equal to 1000 liters.
Bamifylline is rapidly metabolized to give 3 metabolites, also active and marked by high plasma concentrations. The prolonged activity of the drug allows for two daily administrations only.
Bamifylline final elimination half-life is of 17.5 hours. The excretion mostly occurs by urinary route.
Bamifylline shows a high therapeutical index, due to the wide interval between the minimum active and the maximum tolerated plasma levels (0.18 and 20 ug/ml, respectively).
The twice-daily administration of bamifylline leads to plasma levels of steady-state within 3-5 days both for bamifylline and its metabolites.
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