Pharmacologic properties of Daflon 500 mg.
OBJECTIVE
Some pharmacologic activities of a micronized flavonoid complex consisting of 90% diosmin + 10% hesperidin (Daflon 500 mg*) have been investigated by use of various experimental models: (1) interference with mechanisms of edema (synthesis of arachidonic acid derivatives, microvascular hyperpermeability induced by bradykinin, ischemia, or streptozotocin), (2) interference with lymphatic drainage (thoracic duct fistula in the dog).


RESULTS
Daflon 500 mg inhibited prostaglandin E2 (PGE2) and thromboxane A2 (TxA2) synthesis during a one-month oral daily treatment (100 mg.kg-1.day-1) in the rat, after induction of chronic inflammation by subcutaneous implantation of sponge fragments. Microvascular hyperpermeability induced by bradykinin or ischemia in the rat cremaster muscle was reduced after an oral treatment with Daflon 500 mg (100 mg.kg-1 twice daily). Microvascular hyperpermeability of the streptozotocin-induced diabetic rat was antagonized when Daflon 500 mg (300 mg.kg-1 once daily) was given orally as a preventive treatment. In the anesthetized dog, an increase in lymphatic flow, correlated with administered doses, was observed after IV injection of Daflon 500 mg. Lymphatic flow was maximal twenty minutes after injection of the drug (12.5 mg.kg-1) and was three times higher than the basal flow.


CONCLUSIONS
The protective effect of Daflon 500 mg against the formation of perivascular edema and its therapeutic value in the treatment of venous stasis could be explained by its inhibitory activity on the inflammatory process or ischemia-induced hyperpermeability and by its stimulatory effect on the pulsatile activity of lymphatic vessels.
Labrid
C
C
Institut de Recherches Internationales Servier, Courbevoie, France.
D000818:Animals; D002199:Capillary Permeability / Q000187:drug effects; D003921:Diabetes Mellitus, Experimental / Q000503:physiopathology; D015232:Dinoprostone / Q000096:biosynthesis; D004145:Diosmin / Q000494:pharmacology*; D004285:Dogs; D004338:Drug Combinations; D004487:Edema / Q000517:prevention & control; D005419:Flavonoids / Q000494:pharmacology; D006569:Hesperidin / Q000494:pharmacology*; D007249:Inflammation / Q000378:metabolism; D007678:Kidney Glomerulus / Q000098:blood supply; D008196:Lymph / Q000187:drug effects / Q000502:physiology; D009132:Muscles / Q000098:blood supply; D051381:Rats; D013897:Thoracic Duct / Q000502:physiology; D013929:Thromboxane B2 / Q000096:biosynthesis
D004338:Drug Combinations; D005419:Flavonoids; C080675:S 5682; D013929:Thromboxane B2; D004145:Diosmin; D006569:Hesperidin; D015232:Dinoprostone