Chemical formula: C₁₂H₁₀CaO₁₀S₂ Molecular mass: 190.174 g/mol
Regulator of capillary functions. Calcium dobesilate acts on the capillary walls by regulating its impaired physiological functions – increased permeability and decreased resistance. It increases erythrocyte flexibility, inhibits platelet hyperaggregation and, in diabetic retinopathy, it reduces plasma and blood hyperviscosity, thus improving blood rheological properties and tissue irrigation. These effects allow to correct capillary dysfunctions either of functional origin or caused by constitutional or acquired metabolic disorders. Calcium dobesilate contributes to reduce oedema.
After oral administration of 500mg of calcium dobesilate, its blood level is above 6 μg/ml between the 3rd and 10th hour, with a maximum (Cmax) of 8 μg/ml on the average after 6 hours (tmax). Twenty four hours after intake blood level is about 3 μg/ml. The rate of protein-binding is 20-25%.
In animals, calcium dobesilate does not cross the haematoencephalic or the placental barrier, but it is not known whether this is also the case in humans.
Calcium dobesilate enters the maternal milk in very low quantities (0,4 μg/ml after intake of 1500mg as observed in one study).
Calcium dobesilate does not enter the enterohepatic cycle and is excreted mainly unchanged with only 10% being excreted as metabolites.
About 50% of the orally administered dose are eliminated in the first 24-hour urine and about 50% in the faeces.
Plasma half-life is around 5 hours.
It is not known to what extent renal function disorders influence the pharmacokinetic properties of calcium dobesilate.
Acute and chronic toxicity studies, foetotoxicity and mutagenicity studies on calcium dobesilate have not revealed any toxic effect.
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