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Results for “Diosmin”

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At least 19 recordsLinked to original sources
PubMed1986

Comparative effect of tropolone and diosmin on venous COMT and sympathetic activity in rat.

The ability of diosmin to inhibit venous catechol-O-methyltransferase (COMT) activity was studied comparing it with tropolone in rat superior mesenteric vein (MV), inferior vena cava (IVC) and saphenous vein (SV). Diosmin inhibited COMT activity in the mesenteric vein after 200 and 400 mg/kg i.p., but only at 400 mg/kg in IVC. The COMT inhibitory effect of diosmin (400 mg/kg) was smaller than that of tropolone (50 mg/kg). Furthermore, diosmin, but not tropolone, increased urinary normetanephrine (NMN) excretion (+56%) at 400 mg/kg and that of 3-methoxy 4-hydroxyphenylglycol (MHPG) in a dose-dependent way, thus suggesting that diosmin may exert an activating effect on sympathetic activity. Both mechanism--local inhibition of COMT and enhanced sympathetic activity--may contribute to increase NE levels in the synaptic clefts of the vascular wall and explain the venoconstrictor effect of this drug.

Animals↗
PubMed1992

Clinical trial of oral diosmin (Daflon) in the treatment of hemorrhoids.

A double-blind, comparative, controlled study on the effectiveness of the addition of oral diosmin (Daflon; Lab. Servier, Orléans, France) and placebo to a conservative regimen of bulk laxative in the treatment of acute symptoms of first-degree and second-degree internal hemorrhoids was undertaken in 100 patients. The diosmin and placebo groups, with 50 patients each, were comparable in age, sex, symptoms, and the severity of the underlying hemorrhoids. During the first four days, the patients received 12 tablets in three divided doses, and then they received two tablets twice daily for another 10 days. Subjective and objective changes were assessed at the 4th and 14th days of treatment. The diosmin group showed statistically significant objective improvement (P < 0.01) without accompanying subjective improvement on the fourth day. However, at day 14, there was no significant difference in either subjective or objective improvement between the two groups. Two cases in the placebo group were taken out of the trial on the fourth day owing to clinical deterioration. No side effect of diosmin was detected in this study.

Acute Disease↗
PubMed1985

The effects of diosmin (a benzo-pyrone) upon some high-protein oedemas: lung contusion, and burn and lymphoedema of rat legs.

Oral diosmin (a benzo-pyrone) was used to treat rats with contused lungs, in doses of 50 or 200 mg/kg/day. The contusion was produced by direct trauma. The lungs were examined with the electron microscope, both qualitatively and quantitatively, at 1, 2 and 4 days. It was found that diosmin considerably reduced interstitial oedema and tissue disorganization. The concentration of protein, both in the interstitial tissue and in the air spaces, was also much reduced. There was a greater effect at the higher dosage than at the lower one. In two other experiments, this drug was used in the usual models of burn oedema of the rat foot and acute lymphoedema of the rat leg - estimating the amount of oedema by weighing the parts. A low dose (50 mg/kg) reduced the burn oedema; a high dose (200 mg/kg) did not. Both doses reduced the acute lymphoedema of the whole leg, or thigh. The high dose did not do this in the foot, but the low one did. At high doses, diosmin has the usual benzo-pyrone property of releasing mediators in the rat-foot. In other tissues (and, no doubt, species) this drug reduces many forms of high-protein oedema, like the other benzo-pyrones.

Acute Disease↗
PubMed1991

Diosmin therapy alters the in vitro metabolism of noradrenaline by the varicose human saphenous vein.

We have previously shown that diosmin 30-100 mumol/l reduces the metabolism of noradrenaline (NA) in fragments of varicose saphenous veins obtained at surgery. Since diosmin is widely used in patients with chronic venous insufficiency we decided to test if the drug, administered in therapeutic doses to patients, would affect NA metabolism in the veins of the individuals so treated. Sex- and age-matched patients in which surgery was indicated were allocated in the order of admission to control (n = 5) or treated groups (n = 6; 600 mg twice a day, orally, during 10 days). Fragments of saphenous vein were incubated with [3H]NA 0.2 mumol/l during 60 min; the interval between operation and incubation was less than 30 min. Column chromatography and liquid scintillation counting were used to measure [3H]NA and its metabolites. In the treated group, accumulation of [3H]NA was significantly reduced and the formation of metabolites approximately halved. The present results show that oral administration of diosmin has evident effects on the in vitro metabolism of noradrenaline by the varicose tissue.

Administration, Oral↗
PubMed1992

Amine uptake inhibition by diosmin and diosmetin in human neuronal and neuroendocrine cell lines.

Human neuroblastoma cells of sympathetic origin have been used for studying the effects of diosmin and its metabolite diosmetin (vasotonic agent) on amine reuptake systems. Neuroblastoma cells take up 3H-dopamine in a specific and time-dependent manner. 3H-dopamine uptake was dose-dependently inhibited by the known antagonist desipramine. Diosmin did not affect 3H-dopamine uptake at concentrations as high as 1 mM. On the other hand the aglycone metabolite of diosmin, diosmetin, inhibited 3H-dopamine uptake in a dose-dependent manner (IC50 = 4 microM). Diosmetin inhibited 3H-dopamine uptake in control and differentiated neuroblastoma cells, as well as in small-cell lung carcinoma cells. Furthermore diosmetin also inhibited 3H-serotonin uptake in both cell types. These results demonstrate that some flavonoids act as antagonists of plasma membrane amine transporters at the molecular level and suggest that inhibition of amine reuptake at the level of peripheral sympathetic nerve terminals could be responsible for the increased vascular tone observed in vivo after treatment with these drugs.

Biogenic Monoamines↗
PubMed1992

Pharmacokinetics and metabolism of oral diosmin in healthy volunteers.

Pharmacokinetic studies of diosmin were performed after an oral administration to healthy volunteers. Diosmin and its aglycone, diosmetin, were determined by HPLC and LC-MS techniques. At least, at the level of sensitivity of our method, no parent compound was present in the plasma but only its aglycone, diosmetin. Analysis of the pharmacokinetic parameters showed that the drug was rapidly absorbed. Diosmetin presents a long plasma elimination half-life ranging from 26 to 43 hours. Our data show the total absence of urinary elimination for both diosmin and its aglycone diosmetin, while its minor metabolites are eliminated in the urine, mainly as glucuronic acid conjugates. The presence of degradation products such as alkyl-phenolic acids confirms a metabolic pattern similar to other flavonoids.

Absorption↗
PubMedDate not supplied

[A double-blind study comparing the clinical efficacy of the preparation F-117 (hidrosmin) versus diosmin in the treatment of patients with peripheral venous disorders].

A controlled double-blind clinical trial was performed comparing therapeutic efficacy of hidrosmin versus diosmin in patients suffering from chronic venous insufficiency with varicose symptomatology in the inferior limbs. Ten patients were treated with hidrosmin and other 10 with diosmin randomly. The controls carried out during the trial were as follows; basal control before the beginning of the trial and therapeutic controls on days 15, 30, 60 and 90 of the study. With that aim clinical examinations and different explorations were performed: physical exam, phlebography, electrocardiogram, ophthalmological examination and biochemical analyses (hemogram, globular sedimentation rate, platelet counts, etc.). The clinical therapeutic efficacy of hidrosmin in the treatment of chronic venous insufficiency of inferior limbs was superior to the diosmin in most of the studied parameters even though a lower posology was employed. From a clinical point of view the clinical improvement in the subjective symptomatology (heaviness, local tenderness, cramps, paresthesias, etc.) was very superior to the one obtained with the objective signs (phlebography, skin trophism, evolution of the edema, etc.). No significative adverse reactions appeared.

Adult↗
PubMed1988

Effect of diosmin upon red blood cell deformability and osmotic fragility. Relationship with lipid content.

Rats were treated by ingesting forcibly 2 ml of a suspension of four different doses (100, 200, 300 and 400 mg/kg) of diosmin in carboxymethylcellulose (CMC) and were killed immediately or after 3 or 6 hours of fasting. Animals treated by CMC only in a similar way (gavage) exhibited a fall in red blood cell (RBC) membrane cholesterol and an increase in RBC rigidity at the third hour while osmotic fragility remained stable. Diosmin treatment opposed the rise in RBC rigidity evoked by the gavage and induced a dose-dependent decrease of the RBC membrane cholesterol over phospholipid ratio.

Animals↗
PubMedDate not supplied

Synthesis of [ring B-13C6] diosmin.

End products of flavone metabolism are phenolic acids, originating from rings B and C2 and/or C3 of ring C. Several of them are also endogenous products. Synthesis of uniformly labeled ring B-13C-diosmin [5] was performed for the unambiguous distinction, by ms, between endogenous and exogenous phenolic acids.

Carbon Isotopes↗
PubMed1990

[Randomized study of the use of synthetic diosmin in premenstrual and vascular dysplastic mastodynia].

The antalgic effect of synthetic diosmin in 120 patients suffering from vascular and premenstrual mastodynia is studied compared to the same number of non-treated cases. The therapy has been carried out for one consecutive year. For the same period the course of the painful symptomatology, both in the cases treated and in the controls, has been checked. For the treated cases a significant decrease of the painful symptomatology has been obtained and this decrease was maintained.

Adolescent↗
PubMed1977

A pharmacokinetic study of 3H-diosmine.

A pharmacokinetic study of 3H-labelled 7-rhamnoglycoside of 5,7,3'-trihydroxy-4'-methoxyflavone (3H-diosmine) administered both i.v. and orally, shows the great ease with which it is absorbed in digestion. A very sharp difference in elimination between the two modes of treatment must be associated with a difference in metabolism. A study of fixation confirms this conclusion. In particular the fixation on the tunica vascularis, perhaps due to a metabolite, appears relatively late. Furthermore the existence of an enterohepatic cycle assures a permanent hepatic binding.

Animals↗
PubMed1988

[Results of the use of topical diosmin (venosmine) in the treatment of acute hemorrhoid pathology].

There is still much discussion about the pharmacological treatment of certain symptoms caused by haemorrhoids and their complications. In 1986 topical treatment with Diosmina ointment was used on 50 patients (33 males, 17 females) with grade 1, 2, 3 or 4 haemorrhoids featuring strangulation and thrombosis. Patients who had previously been given other treatment were excluded from the study. The efficacy of the treatment was assessed by a simple method previously used by others which involves scoring (0-3) the major symptoms of the condition (bleeding, oedema, erythema, pain, itching) according to severity. The drug was most effective on oedema and erythema, producing 75% and 73% improvements as assessed in three consecutive weekly visits. These results confirm the value of Diosmina in the topical treatment of acute haemorrhoids. In particular the treatment is very well tolerated and produces no unwanted side effects if properly used.

Administration, Topical↗