Composition
One film-coated tablet contains: Active ingredient: diosmin – 600,00 mg; excipients:  microcrystalline cellulose – 241.50 mg; talc – 18.00 mg; hyprolose (hydroxypropylcellulose) – 13.50 mg; croscarmellose sodium – 13.50 mg;magnesium stearate – 9.00 mg; colloidal hydrophobic silicon dioxide – 4.50 mg; film coating: [hypromellose – 16.20 mg, talc – 5.40 mg, titanium dioxide – 2.79 mg, macrogol 4000 (polyethylene glycol 4000) – 2.43 mg, iron oxide red dye (iron oxide) – 0.18 mg] or [dry mixture for film coating containing hypromellose (60%), talc (20%), titanium dioxide (10.33%), macrogol 4000 (polyethylene glycol 4000) (9%), iron oxide red dye (iron oxide) (0.67%)]- 27.00 mg
Pharmacological action
Pharmacodynamicadiosmin is a benzpyron derivative. It belongs to the group of bioflavonoids. It has a phlebotonizing effect (reduces the extensibility of veins, increases the tone of veins (dose-dependent effect), reduces venous congestion), improves lymphatic drainage (increases the tone and frequency of contraction of lymphatic capillaries, increases their functional density, reduces lymphatic pressure), improves microcirculation (increases capillary resistance (dose-dependent effect), reduces their permeability), reduces the adhesion of leukocytes to the venous wall and their migration to the paravenous tissues, improves oxygen diffusion and perfusion in the skin tissue, has an anti-inflammatory effect. Increases the vasoconstrictive effect of epinephrine, norepinephrine, blocks the production of free radicals, the synthesis of prostaglandins and thromboxane. Diosmin has been shown to reduce plasma levels of enzymes responsible for the metabolism of mucopolysaccharides in the venous wall. In clinical studies, diosmin reduced the capacity of the venous bed and the volume of venous congestion (according to plethysmography), reduced the average pressure in the deep and superficial veins of the legs (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 blood plasma 2 hours after use. The bioavailability of diosmin after oral use is approximately 40-57.9%. In the intestine, diosmin is transformed by the intestinal microflora into diosmetin, hippuric acid and benzoic acid. Distribution The maximum concentration in blood plasma is reached 5 hours after use. Diosmin is evenly distributed and accumulates in all layers of the wall of the vena cava and subcutaneous veins of the lower extremities, to a lesser extent-in the kidneys, liver, lungs and other tissues. The volume of distribution is 62.1 l. Selective accumulation of diosmin and / or its metabolites in venous vessels reaches a maximum by the ninth hour after ingestion and persists for 96 hours. Diosmin is metabolized in the liver. The main metabolite is hydroxyphenylpropionic acid. Diosmin metabolites are mainly excreted by the kidneys in the form of conjugates with glucuronic acid. Excretion 79% of diosmin taken is excreted by the kidneys,11% by the intestines, and 2.4% by bile. Enterohepatic circulation of diosmin is noted. After ingestion of diosmin labeled with a radioactive isotope, approximately 86% is excreted by the kidneys and intestines within 48 hours.
Indications
As part of complex therapy: to eliminate the symptoms of varicose veins of the lower extremities;to eliminate the symptoms of chronic lymphovenous insufficiency of the lower extremities: a feeling of heaviness or fatigue in the legs, pain; when microcirculation is disturbed to eliminate the symptoms of acute hemorrhoids.
Use during pregnancy and lactation
Pregnancy So far 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 exceeds the potential risk to the fetus. In experimental studies, no teratogenic effect of diosmin on the fetus was detected. Breast-feedingthe drug is not recommended during breastfeeding, as there are no data on the penetration of diosmin into breast milk.
Recommendations for use
Use the drug only according to the indications, the method of use and in the doses indicated in the instructions. Before using the drug, you should consult your doctor. The drug Diosmin is intended for oral use. With varicose veins of the lower extremities and chronic lymphovenous insufficiency,1 tablet is prescribed per day in the morning on an empty stomach. The duration of therapy is usually 2 months. In severe forms of chronic lymphovenous insufficiency (swelling, pain, convulsions, etc. ) treatment may be longer (the total duration of continuous therapy should not exceed 3-4 months). Courses of treatment with Diosmin are repeated in 2-3 months. For the treatment of chronic lymphovenous insufficiency during the II and III trimester of pregnancy, the drug is used 1 tablet 1 time a day. The duration of therapy is not more than 30 days. The drug should be discontinued 2-3 weeks before delivery. In case of exacerbation of hemorrhoids, the drug is prescribed 2-3 tablets a day with meals for 7 days. Further, if necessary, you can continue taking the drug 1 tablet 1 time a day for 1-2 months. In case of 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 in the usual mode and in the usual dose.
Contraindications
hypersensitivity to the components of the drug; I trimester of pregnancy and lactation (limited experience); age up to 18 years.
Side effects
Classification of the frequency of side effects according to the recommendations of the World Health Organization (WHO): very common ≥ 1/10; often from ≥ 1/100 to < 1/10; infrequently from ≥ 1/1000 to < 1/100; rarely from ≥ 1/10000 to < 1/1000; very rare From the gastrointestinal tract: often – nausea, vomiting, diarrhea, dyspeptic disorders, heartburn, constipation; infrequently-colitis. From the central nervous system: rarely-headache, malaise, dizziness. From the skin and subcutaneous fat: rarely-skin rashes, itching. Allergic reactions: rarely-urticaria; frequency unknown-isolated swelling of the face, lips, eyelids; in exceptional cases-angioedema (angioedema). If any of the side effects listed in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.
Overdose
Symptoms of overdose are not described. Given the wide therapeutic range of diosmin, the risk of intoxication in overdose is insignificant. Treatment-specific antidote unknown.
Special instructions
Treatment of acute hemorrhoids is carried out in combination with other drugs. In the absence of a rapid clinical effect, it is necessary to conduct an additional examination and adjust the therapy. In case of violation of venous circulation (varicose veins of the lower extremities, chronic lymphovenous insufficiency of the lower extremities), the maximum effect of treatment is provided by combining therapy with lifestyle changes: it is advisable to avoid prolonged stay in an upright position, reduce excess body weight. In some cases, the wearing of special stockings (compression knitwear) helps to improve blood circulation. If there is no reduction or if the symptoms of the disease become more severe, consult your doctor. Do not exceed the maximum time and recommended doses of the drug without consulting a doctor.
Storage conditions
Store in a dark place at a temperature not exceeding 25 °C. Keep out of reach of children.
Shelf life
3 years
Active ingredient
Diosmin
Dosage form
Tablets
Description
For pregnant women as prescribed by a doctor, For adults as prescribed by a doctor
Indications
Hemorrhoids, Varicose veins, Vascular eye diseases, Trophic ulcers
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