Pharmacotherapeutic group: VASOPROTECTIVES/CAPILLARY STABILIZING AGENTS/BIOFLAVONOIDS. C05CA53: Cardiovascular system.
Pharmacology: Pharmacodynamics: In pharmacology: DAFLON exerts a dual action on the venous return system: at vein and venule level, it increases parietal tone and exerts an anti-stasis action; at the microcirculatory level, it reinforces capillary resistance and normalises capillary permeability.
In clinical pharmacology: Controlled, double-blind studies using methods that allow demonstrating and quantifying the activity on venous haemodynamics have confirmed the pharmacological properties of this medicinal product in humans.
Dose/effect relationship: Statistically significant dose-effect relationships have been demonstrated for the following venous plethysmography parameters: capacitance, distensibility and emptying time.
500-mg: The best dose-effect ratio is obtained with 2 tablets.
1,000-mg: The best dose/effect ratio is obtained with 1 tablet.
Venotonic activity: It increases venous tone: venous occlusion plethysmography with a mercury strain gauge revealed a reduction in venous emptying time.
Microcirculatory activity: Controlled, double-blind studies have demonstrated a statistically-significant difference between this medicinal product and placebo. In patients with signs of capillary fragility, it increases capillary resistance as measured by angiosterrometry.
Efficacy and clinical safety: In clinical practice: Controlled, double-blind clinical studies versus placebo demonstrated the therapeutic activity of the medicinal product in phlebology, in the treatment of chronic venous insufficiency (functional and organic) of the lower limbs.
Pharmacokinetics: In humans, following oral administration of the medicinal product with carbon 14-labelled diosmin: Excretion is essentially faecal and urinary excretion is on average of 14% of the administered quantity.
The elimination half-life is 11 hours.
The product is highly metabolised, this metabolism is revealed by the presence of different phenol acids in the urine.
Toxicology: Preclinical safety data: Non-clinical data reveal no special hazard for humans based on conventional studies of repeated dose toxicity, genotoxicity and toxicity to reproduction.