Hydroxyethylrutosides

Abstract

Hydroxyethylrutosides is a standardised mixture of semisynthetic flavonoids, mainly mono-, di-, tri-, and tetrahydroxyethylrutosides, which acts primarily on the microvascular endothelium to reduce hyperpermeability and oedema. In patients with chronic venous insufficiency or diabetes, hydroxyethylrutosides improves microvascular perfusion and microcirculation, and reduces erythrocyte aggregation. The preparation also has a possible protective effect on the vascular endothelium. In short to medium term placebo-controlled studies (up to 6 months) hydroxyethylrutosides therapy improved signs and symptoms of chronic venous insufficiency, including venous insufficiency associated with pregnancy and lymphoedema, and was well tolerated. However, the long term effects of hydroxyethylrutosides administration have yet to be demonstrated. The preparation also alleviated symptoms in patients with severe haemorrhoids, although there were no corresponding objective improvements. Hydroxyethylrutosides administration has been associated with reductions in retinal vascular permeability in patients with diabetic retinopathy but has no apparent effect on signs of retinal haemorrhage, although a reduction in oedema and haemorrhage has been reported in other patients receiving oral hydroxyethylrutosides in the acute phase of central retinal vein occlusion. There are only limited effective pharmacological treatment options for patients with chronic venous insufficiency or lymphoedema, and hydroxyethylrutosides clearly improves signs and symptoms of these disorders. While its role in diabetic retinopathy and haemorrhoids requires some clarification, hydroxyethylrutosides therapy shows promise as a useful additional option for the management of oedema and other symptoms of chronic venous insufficiency.

Chronic Venous Insufficiency and Venous Ulceration

“…Hydroxyethylrutosides have been used in Europe for more than 30 years to treat various types of dependent edema, and have been reviewed by Wadworth and Faulds. 110 They are a standard mixture of semisynthetic flavinoids that act mainly on the microvascular endothelium to reduce permeability and edema. In most placebo-controlled trials, patients receiving hydroxyethylrutosides had reduced leg volume and circumference, and greater relief of pain, night cramps, and restless legs, which persisted up to 4 weeks following discontinuation of treatment.…”

Quercetin microspheres by solvent evaporation: Preparation, characterization and release behavior

“…Quercetin (Q, 3,5,7,3′,4′‐pentahydroxyflavone) (Scheme ), is a common dietary component occurring in various edible plant and herbal medicines marketed in Europe 1–3. This flavonoid has shown antioxidant and anti‐inflammatory properties in numerous mammalian cell systems, in vitro as well in vivo 4–7; moreover, some of its derivatives are employed to treat cardiovascular chronic pathologies such as venous insufficiency, capillary fragility and permeability, hemorrhoids, and perivascular edema 8. Although the variety of its biological effects, the Q bioavailability is an important unsolved problem.…”

Liquid chromatography/tandem mass spectrometry assay for the quantification of troxerutin in human plasma

“…Troxerutin, {2‐[3,4‐bis(2‐hydroxyethoxy)phenyl]‐3‐[(6‐deoxy‐α‐L‐manno‐pyranosyl)‐β(‐D‐glucopyranosyl)‐oxy]‐5‐hydroxy‐7‐(2‐hydroxyethoxy)‐4 H ‐1‐benzopyran‐4‐one}, a trihydroxyethyl derivative of the flavanoid rutin,1, 2 has been used therapeutically to treat chronic venous insufficiency,3–10 varicosity, capillary fragility,11–13 and abnormal leakage, and it has anti‐erythrocytic, anti‐thrombotic, fibrinolytic,4 odema‐protective,14 and rheological activity 5, 8. Low plasma concentration is achieved following administration of troxerutin; thus a quantification method for the drug in pharmacokinetic studies and monitoring of its efficacy need to be sensitive and specific.…”