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Pharmacology: PHARMACODYNAMICS: Diosmin and Hesperidin act on: Venous tone: by inhibiting the breakdown of norepinephrine (noradrenaline) by COMT (catechol-O-methyltransferase).
Noradrenergic activity is thereby prolonged and venous tone increased. The degree of this effect varies in linear relation to the dose administered.
The microcirculation: protection of microvascular permeability via inhibition of adhesion of leukocytes, their intratissue migration, the release of inflammatory mediators and the expression of certain leukocyte (L-selectin) and endothelial (ICAM-1, VCAM-1) adhesion substances initiating the inflammatory events leading to raised microcirculatory venous pressure.
PHARMACOKINETICS: Absorption: After oral administration, Diosmin is well absorbed. Hesperidin is converted to hesperetin by the microflora of the colon, and then, it is absorbed by colonocytes.
Metabolism: The product is highly metabolised, this metabolism is revealed by the presence of different phenol acids in the urine.
Excretion: Excretion is essentially faecal and urinary excretion is on average 14% of the administered quantity.
Elimination Half-life: 11 hours.
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