Pharmacotherapeutic Class: Vasculoprotectives/Capillary stabilizing agents/Bioflavonoids. ATC Code: C05CA53.
Pharmacology: Pharmacodynamics: 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.
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. The best dose/effect ratio is obtained when 1000mg tablets daily are taken.
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.
Clinical practice: Double-blind placebo-controlled trials have demonstrated the therapeutic effect of the drug in phlebology, in the treatment of chronic venous insufficiency of the lower limbs, both functional and organic.
Pharmacokinetics: In man, following oral administration of the substance containing 14C Diosmin: Excretion is mainly faecal and a mean of 14% of the dose administered is excreted in the urine.
The elimination half-life is 11 hours.
The drug is extensively metabolised as evidenced by the presence of various phenol acids in the urine.
Toxicology: Preclinical safety data: Preclinical data from conventional toxicology studies of repeated dose toxicity, genotoxicity and reproductive function did not reveal any particular risk to humans.