Diosmin, 600 mg 30 pcs.

Pharmacodynamics

Diosmin is a benzpyron derivative. It belongs to the group of bioflavonoids. It has phlebotonic action (decreases venous distensibility, increases venous tone (dose-dependent effect), decreases venous congestion), improves lymphatic drainage (increases tone and frequency of contraction of lymph capillaries, increases their functional density, reduces lymphatic pressure), It improves microcirculation (increases capillary resistance (dose-dependent effect), decreases their permeability), reduces leukocyte adhesion to the venous wall and their migration into the paravenous tissue, improves oxygen diffusion and perfusion in the skin tissue, has anti-inflammatory effect.

It enhances vasoconstrictor effect of adrenaline and noradrenaline, blocks production of free radicals, synthesis of prostaglandins and thromboxane. It was shown that diosmin decreases plasma levels of enzymes responsible for metabolism of mucopolysaccharides in the venous wall.

In clinical trials diosmin decreased venous bed capacity and venous stasis volume (according to plethysmography), decreased average pressure in deep and superficial leg veins (according to ultrasound Dopplerography) and increased systolic and diastolic blood pressure in patients with postoperative orthostatic hypotension. Pharmacokinetics Absorption Rapidly absorbed from the gastrointestinal tract, detected in plasma 2 hours after administration. Bioavailability of diosmin after oral administration is approximately 40-57.9%.

Diosmin is transformed by intestinal microflora into diosmetin, hippuric acid and benzoic acid. Distribution Maximum concentration in plasma is reached 5 hours after intake. Diosmin is evenly distributed and accumulated in all layers of the wall of hollow veins and subcutaneous veins of lower limbs, to a lesser extent – in kidneys, liver, lungs and other tissues.

Distribution volume is 62.1 liters. Selective accumulation of diosmin and/or its metabolites in the venous vessels reaches a maximum by the ninth hour after administration and persists for 96 hours. Metabolism Diosmin is metabolized in the liver. The main metabolite is hydroxyphenylpropionic acid.

Metabolites of diosmin are excreted mainly by the kidneys in the form of conjugates with glucuronic acid.

Excretion 79% of ingested diosmin is excreted by kidneys, through the intestine – 11%, in the bile – 2.4%. Enterohepatic circulation of diosmin is observed. After intake of diosmin labeled with a radioactive isotope, about 86% is excreted by the kidneys and intestines within 48 hours.

Indications

As part of complex therapy:
to eliminate symptoms of varicose veins of the lower extremities;
to eliminate symptoms of chronic lymphovenous insufficiency of the lower extremities: a feeling of heaviness or fatigue in the legs, pain;
in case of microcirculation disorders
to eliminate the symptoms of acute hemorrhoids.

Pharmacological effect

Pharmacodynamics

Diosmin is a benzpyrone derivative. Belongs to the group of bioflavonoids. It has a phlebotonic effect (reduces the distensibility of veins, increases the tone of the veins (dose-dependent effect), reduces venous stagnation), improves lymphatic drainage (increases the tone and frequency of contraction of lymphatic capillaries, increases their functional density, reduces lymphatic pressure), improves microcirculation (increases the resistance of capillaries (dose-dependent effect), reduces their permeability), reduces adhesion leukocytes to the venous wall and their migration into paravenous tissues, improves oxygen diffusion and perfusion in the skin tissue, and has an anti-inflammatory effect.

Strengthens the vasoconstrictor effect of adrenaline, norepinephrine, blocks the production of free radicals, the synthesis of prostaglandins and thromboxane. It has been shown that diosmin reduces the plasma levels of enzymes responsible for the metabolism of mucopolysaccharides in the venous wall.

In clinical studies, diosmin reduced venous capacity and venous congestion volume (as measured by plethysmography), decreased mean pressure in the deep and superficial veins of the legs (as measured by Doppler ultrasound), and increased systolic and diastolic blood pressure in patients with postoperative orthostatic hypotension. Pharmacokinetics Absorption Rapidly absorbed from the gastrointestinal tract, detected in blood plasma 2 hours after administration. The bioavailability of diosmin after oral administration is approximately 40-57.9%.

In the intestine, diosmin is transformed by intestinal microflora into diosmetin, hippuric and benzoic acid. Distribution The maximum concentration in blood plasma is achieved 5 hours after administration. Diosmin is evenly distributed and accumulates in all layers of the wall of the vena cava and saphenous veins of the lower extremities, and to a lesser extent in the kidneys, liver, lungs and other tissues.

The distribution volume is 62.1 l. Selective accumulation of diosmin and/or its metabolites in venous vessels reaches a maximum by the ninth hour after administration and persists for 96 hours. Metabolism Diosmin is metabolized in the liver. The main metabolite is hydroxyphenylpropionic acid.

Diosmin metabolites are excreted primarily by the kidneys in the form of conjugates with glucuronic acid.

Removal
79% of taken diosmin is excreted by the kidneys, through the intestines – 11%, with bile – 2.4%.
Enterohepatic circulation of diosmin is noted. After taking radiolabeled diosmin, approximately 86% is excreted by the kidneys and intestines within 48 hours.

Special instructions

Treatment of acute hemorrhoids is carried out in combination with other drugs. If there is no rapid clinical effect, it is necessary to conduct additional examination and adjust the therapy.

In case of venous circulation disorders (varicose veins of the lower extremities, chronic lymphovenous insufficiency of the lower extremities), the maximum treatment effect is ensured by a combination of therapy with lifestyle changes: it is advisable to avoid prolonged stay in an upright position and reduce excess body weight.

In some cases, wearing special stockings (compression stockings) helps improve blood circulation. If there is no improvement or if the symptoms of the disease worsen, consult a doctor.

Do not exceed the maximum duration and recommended doses of the drug without consulting a doctor.

Active ingredient

Diosmin

Composition

One film-coated tablet contains

Pregnancy

Pregnancy Until now, in clinical practice there have been no reports of any side effects when using the drug in pregnant women. However, for safety reasons, it is not recommended to use the drug in the first trimester of pregnancy.

Use during pregnancy in the second and third trimesters is possible only as prescribed by a doctor in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

Experimental studies have not revealed a teratogenic effect of diosmin on the fetus.

Breastfeeding period
It is not recommended to take the drug during breastfeeding, since there is no data on the penetration of diosmin into breast milk.

Contraindications

hypersensitivity to the components of the drug;
I trimester of pregnancy and breastfeeding (experience of use is limited);
age up to 18 years.

Side Effects

Classification of the incidence of side effects according to the recommendations of the World Health Organization (WHO): very often ≥ 1/10; often from ≥ 1/100 to < 1/10; infrequently from ≥ 1/1000 to < 1/100; rarely from ≥ 1/10000 to < 1/1000; very rarely <1/10000, including isolated reports; frequency unknown - based on available data, it is not possible to determine the frequency of occurrence.From the gastrointestinal tract: often – nausea, vomiting, diarrhea, dyspeptic disorders, heartburn, constipation; uncommon – colitis.From the central nervous system: rarely – headache, malaise, dizziness.From the skin and subcutaneous fat: rarely – skin rashes, skin itching.Allergic reactions: rarely – urticaria; frequency unknown – isolated swelling of the face, lips, eyelids; in exceptional cases – angioedema (Quincke’s edema).If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Symptoms Symptoms of overdose are not described.

Given the wide therapeutic range of diosmin, the risk of toxicity in case of overdose appears to be negligible.

Treatment
A specific antidote is unknown.

Recommendations for use

Use the drug only according to the indications, method of administration and in the doses indicated in the instructions. Before using the drug, you should consult your doctor.

Diosmin is intended for oral administration. For varicose veins of the lower extremities and chronic lymphovenous insufficiency, 1 tablet per day is prescribed in the morning on an empty stomach.

The duration of therapy is usually 2 months. In severe forms of chronic lymphovenous insufficiency (swelling, pain, cramps, etc.), treatment may be longer (the total duration of continuous therapy should not exceed 3-4 months). Courses of treatment with Diosmin are repeated after 2-3 months.

For the treatment of chronic lymphovenous insufficiency during the 2nd and 3rd trimester of pregnancy, the drug is used 1 tablet 1 time per day. The duration of therapy is no more than 30 days.

The drug should be stopped 2-3 weeks before birth. In case of exacerbation of hemorrhoids, the drug is prescribed 2-3 tablets per day with meals for 7 days. Then, if necessary, you can continue taking the drug 1 tablet once a day for 1-2 months. For microcirculation disorders

The drug is prescribed 1 tablet per day in the morning on an empty stomach. The duration of therapy is usually 1-2 months.
If one or more doses of the drug are missed, it is necessary to continue using the drug as usual and at the usual dose.

Storage conditions

Store in a place protected from light at a temperature not exceeding 25 °C.

Shelf life

3 years

Manufacturer

Vertex, Russia