Wessel due f 250 units 50 pcs. capsules

Composition and release form

in ampoules of 2 ml; There are 10 ampoules in a box.

25 pcs in blister; There are 2 blisters in a box.

Compound

The soft capsule in a gelatin shell contains 250 LE of the active substance sulodexide .
Additional components are: silicon dioxide (colloidal form), sodium lauryl sarcosinate, triglycerides.

The shell consists of titanium dioxide, gelatin, red iron oxide, sodium propyl parahydroxybenzoate, sodium ethyl parahydroxybenzoate and glycerol .

1 ampoule with a clear solution contains 600 LE of the active ingredient sulodexide. The auxiliary components are water and sodium chloride.

Pharmacodynamics

The fast-flowing heparin-like fraction has an affinity for antithrombin III, and the dermatan fraction has an affinity for heparin cofactor II. The anticoagulant effect is due to the affinity for heparin cofactor II, which inactivates thrombin.

The mechanism of antithrombotic action is associated with the suppression of activated factor X, with increased synthesis and secretion of prostacyclin (PGI2), with a decrease in the level of fibrinogen in the blood plasma, etc.

The profibrinolytic effect is due to an increase in the blood level of tissue plasminogen activator and a decrease in the content of its inhibitor.

The angioprotective effect is associated with the restoration of the structural and functional integrity of vascular endothelial cells, with the restoration of the normal density of the negative electrical charge of the pores of the vascular basement membrane. In addition, the drug normalizes the rheological properties of the blood by reducing the level of triglycerides (stimulates the lipolytic enzyme - lipoprotein lipase, which hydrolyzes triglycerides that are part of LDL).

Reduces blood viscosity, inhibits the proliferation of mesangial cells, and reduces the thickness of the basement membrane.

pharmachologic effect

Direct anticoagulant. The active ingredient is the natural component Sulodexide, isolated and extracted from the mucous membrane of the small intestine of pigs.

The active component consists of two glycosaminoglycans: dermatan sulfate and heparin-like fraction.

The drug has the following effects:

• angioprotective;
• anticoagulant;
• profibrinolytic;
• antithrombotic.

The anticoagulant effect is manifested due to the affinity of heparin for cofactor-2, under the influence of which the blood clot is inactivated.

The antithrombotic effect is ensured by an increase in the secretion and synthesis of prostacyclin, suppression of the active X factor, and a decrease in fibrinogen in the blood.

The profibrinolytic effect is achieved by reducing the level of tissue plasminogen activator inhibitor and increasing the level of the activator itself in the blood.

The angioprotective effect is associated with the restoration of adequate density of the minus electric charge of the pores in the vascular basement membranes. Additionally, the effect is ensured by restoring the integrity of vascular endothelial cells (functional and structural integrity).

Wessel Due F reduces triglyceride , normalizing blood rheological parameters. The active component is able to stimulate lipoprotease (a specific lipolytic enzyme), which hydrolyzes triglycerides, which are part of the “bad” cholesterol .

In diabetic nephropathy, the active substance Sulodexide reduces the production of extracellular matrix by suppressing the proliferation of mesangium cells; reduces the thickness of the basement membrane.

Pharmacokinetics

90% is absorbed in the vascular endothelium (creating a concentration in it that is 20–30 times higher than its concentration in the tissues of other organs) and is absorbed in the small intestine. Metabolized in the liver and kidneys. Unlike unfractionated heparin and low molecular weight heparins, sulodexide is not subject to desulfation, which leads to a decrease in antithrombotic activity and significantly accelerates elimination from the body. Dose distribution across organs showed that the drug undergoes extracellular diffusion in the liver and kidneys 4 hours after administration.

24 hours after intravenous administration, urinary excretion is 50% of the drug, and after 48 hours - 67%.

Pharmacodynamics and pharmacokinetics

The drug is metabolized in the renal system and liver. The active substance does not undergo desulfation, unlike low molecular weight forms of heparin and unfractionated heparin.

Desulfation suppresses antithrombotic activity and significantly accelerates the process of elimination from the body.

The active component is absorbed in the lumen of the small intestine. 90% of the active substance is absorbed by the vascular endothelium. 4 hours after admission, Sulodexide is excreted from the body through the renal system.

Indications for the drug Wessel Due F

angiopathy with an increased risk of thrombosis, incl. after myocardial infarction;

cerebrovascular accidents, including the acute period of ischemic stroke and the period of early recovery;

discirculatory encephalopathy caused by atherosclerosis, diabetes mellitus, hypertension;

vascular dementia;

occlusive lesions of peripheral arteries of atherosclerotic and diabetic origin;

phlebopathy, deep vein thrombosis;

microangiopathy (nephropathy, retinopathy, neuropathy) and macroangiopathy (diabetic foot syndrome, encephalopathy, cardiopathy) in diabetes mellitus;

thrombophilic conditions, antiphospholipid syndrome (together with acetylsalicylic acid, as well as following low molecular weight heparins);

Treatment of heparin-induced thrombotic thrombocytopenia (HTT), since the drug does not cause or worsen HTT.

Indications for use

• thrombosis , phlebopathy;
• pathology of cerebral circulation (acute period of stroke and recovery period);
• angiopathy with a high risk of thromboformation (after myocardial infarction );
• dementia of vascular origin;
• discirculatory form of encephalopathy caused by diabetes mellitus, total atherosclerosis , arterial hypertension ;
• microangiopathy (retinopathy, nephropathy, neuropathy);
• occlusive lesions of peripherally located arteries (against the background of diabetes mellitus and atherosclerosis);
• antiphospholipid syndrome , thrombolytic conditions (can be prescribed after low molecular weight heparin or together with acetylsalicylic acid);
• macroangiopathic changes in patients with diagnosed diabetes mellitus (encephalopathy, diabetic foot syndrome, cardiopathy );
• therapy for heparin-induced thrombotic thrombocytopenia

special instructions

If necessary, it is recommended to use the drug under the control of a coagulogram. At the beginning and end of treatment, it is advisable to determine the following indicators: aPTT (normally - 30–40 s, depending on the type and concentration of the activator used, it can be 25–30 or 35–50 s), antithrombin III content (normally - 210–300 mg/l), bleeding time (normal according to Duques - 2-4 minutes), clotting time of unstabilized blood (normal according to the Milian method as modified by Morawitz - 6-8 minutes). Wessel Due F increases normal values ​​by approximately one and a half times.

Vesel Due, instructions for use (Method and dosage)

In the first 15-20 days, the medication is administered parenterally. Intravenous and intramuscular injections are allowed. Intravenous administration can be drip or bolus.

Scheme: 2 ml (600 LE - 1 ml) of the contents of the ampoule are dissolved in a physiological solution with a volume of 200 ml. Upon completion of injection therapy, they switch to taking the drug in capsule form for 30-40 days. Twice a day, 1 capsule. The preferred time is between meals.

It is recommended to take 2 courses annually. The instructions for Vesel Due F contain an indication of the possibility of changing the above-described treatment regimen, taking into account individual characteristics, tolerance, and other concomitant diseases.

Wessel Due F during pregnancy (and lactation)

The drug should not be prescribed in the first trimester of pregnancy. The medical literature describes the positive experience of treating pregnant women with diagnosed type I diabetes mellitus with sulodexide late toxicosis during pregnancy.

The medication can be used in the 2nd and 3rd trimesters under the supervision of the attending physician and with the consent of an obstetrician-gynecologist or vascular surgeon.

Data on the safety of Wessel Due F during lactation are not found in the relevant literature.

Wessel due f 250 units 50 pcs. capsules

pharmachologic effect

Anticoagulants - heparin and its derivatives.

Composition and release form Wessel Due f 250 units 50 pcs. capsules

Capsules - 1 capsule:

• Active ingredient: sulodexide 250 LE*;
• Excipients: sodium lauryl sarcosinate 3.30 mg, colloidal silicon dioxide 2.00 mg, triacetin 83.87 mg. Capsule shell components: gelatin 53.15 mg, glycerol 22.07 mg, sodium ethyl parahydroxybenzoate 0.26 mg, sodium propyl parahydroxybenzoate 0.13 mg, titanium dioxide (E171) 0.29 mg, red iron oxide (E172) 0.86 mg .

* — lipoprotein lipase unit.

20 or 25 capsules in blisters made of PVC/PVDC base and aluminum film with a transparent PVDC coating layer; 3 blisters of 20 capsules each or 2 or 4 blisters of 25 capsules each, along with instructions for use, are placed in a cardboard pack.

Description of the dosage form

Oval soft gelatin capsules of brick-red color containing a white-gray suspension. A pinkish or pinkish-cream tint to the contents of the capsules is allowed.

Characteristic

A natural product isolated from the mucous membrane of the small intestine of pigs. It is a natural mixture of glycosaminoglycans: heparin-like fraction with a molecular weight of 8,000 daltons (80%) and dermatan sulfate (20%).

Directions for use and doses

1-2 capsules 2 times a day before meals for 30-40 days. Typically, treatment begins with the use of the drug in the dosage form “solution for intravenous and intramuscular use”, 1 ampoule per day, intramuscularly or intravenously, for 15-20 days.

The full course of treatment should be repeated at least 2 times a year.

Depending on the results of the clinical diagnostic examination of the patient, the dosage regimen may be changed at the discretion of the physician.

Pharmacodynamics

Wessel® Due F (sulodexide) is a biological medicinal product that is a natural mixture of glycosaminoglycans (GAGs): a heparin-like fraction with a molecular weight of 8000 daltons (80%) and dermatan sulfate (20%).

The mechanism of action of sulodexide is due to two main properties: the fast-acting heparin-like fraction has an affinity for antithrombin III (ATIII), and the dermatan fraction has an affinity for heparin cofactor II (CHII). After oral administration at the recommended dosage, the amount of sulodexide and its derivatives after the first pass effect is sufficient to induce antithrombin action without affecting conventional coagulation parameters (activated partial thromboplastin time (aPTT), thrombin time, activated factor X). Thus, it can be assumed that sulodexide, when administered orally, does not have an anticoagulant effect.

Pharmacological action: angioprotective, profibrinolytic, antithrombotic.

Pharmacodynamics

The angioprotective effect is associated with the restoration of the structural and functional integrity of vascular endothelial cells, with the restoration of the normal density of the negative electrical charge of the pores of the vascular basement membrane. In addition, the drug normalizes the rheological properties of the blood by reducing the level of triglycerides (stimulates the lipolytic enzyme - lipoprotein lipase, which hydrolyzes triglycerides that are part of LDL).

The effectiveness of the drug in diabetic nephropathy is determined by the ability of sulodexide to reduce the thickness of the basement membrane and the production of extracellular matrix by reducing the proliferation of mesangium cells.

The profibrinolytic effect is due to an increase in the blood level of tissue plasminogen activator and a decrease in the content of its inhibitor. The antithrombotic activity of sulodexide administered orally is mainly the result of all the actions that sulodexide has on the vascular wall (angioprotective effect), fibrinolysis (profibrinolytic effect) and inhibition of platelet adhesion.

Pharmacokinetics

Sulodexide is absorbed in the small intestine. After ingestion of the labeled drug, the first peak of sulodexide in the blood plasma is observed after 2 hours, the second - from 4 to 6 hours, after which the drug is no longer detectable in the plasma; the concentration is restored after approximately 12 hours and then remains constant until approximately the 48th hour. A constant level in the blood plasma is detected after 12 hours, probably due to the slow release of the drug by the absorption organs and, in particular, by the vascular endothelium. Sulodexide is distributed in the vascular endothelium in a concentration 20-30 times higher than the concentration in other tissues. Metabolized in the liver and excreted mainly by the kidneys. In a radiolabeled study, 55.23% of sulodexide was excreted in urine during the first 96 hours.

Indications for use Wessel Due f 250 units 50 pcs. capsules

• Angiopathy with an increased risk of thrombosis, including after myocardial infarction;
• cerebrovascular accident, including the acute period of ischemic stroke and the period of early recovery; discirculatory encephalopathy caused by atherosclerosis, diabetes mellitus, hypertension; vascular dementia;
• occlusive lesions of peripheral arteries of both atherosclerotic and diabetic origin;
• phlebopathy, deep vein thrombosis;
• microangiopathy (nephropathy, retinopathy, neuropathy) and macroangiopathy in diabetes mellitus (diabetic foot syndrome, encephalopathy, cardiopathy);
• thrombophilic conditions, antiphospholipid syndrome (prescribed together with acetylsalicylic acid, as well as after low molecular weight heparins);
• treatment of heparin-induced thrombotic thrombocytopenia, since it does not cause or aggravate it.

Contraindications

• Hypersensitivity;
• hemorrhagic diathesis and diseases accompanied by decreased blood clotting;
• pregnancy first trimester.

With caution: when used together with anticoagulants, blood clotting parameters should be monitored.

Application Wessel due f 250 units 50 pcs. capsules during pregnancy and breastfeeding

During pregnancy, it is prescribed under the strict supervision of a doctor. There is positive experience in using the drug for the treatment and prevention of vascular complications in patients with type I diabetes in the second and third trimesters of pregnancy, with the development of late toxicosis of pregnancy.

special instructions

Due to the pharmacotoxicological properties of sulodexide, the use of the drug does not require special precautions. However, when used together with other anticoagulants, blood clotting parameters should be periodically monitored.

Impact on the ability to drive vehicles and operate machinery

Wessel Due F does not affect the ability to drive vehicles and machinery.

Overdose

Bleeding is the only phenomenon that can occur with an overdose. If bleeding develops, it is necessary to administer protamine sulfate (1% solution), which is used for bleeding caused by heparin.

Side effects of Vessel Due f 250 units 50 pcs. capsules

According to clinical studies

Data on the incidence of adverse drug reactions associated with the use of sulodexide were obtained from clinical studies involving patients treated with standard doses of the drug for the usual duration of therapy.

Adverse reactions associated with the use of sulodexide were classified by system-organ class and distributed according to frequency of occurrence in the following order: very often (≥ 1/10), often (≥ 1/100 to

Nervous system: infrequently - headache, very rarely - loss of consciousness.

Hearing organ: often - dizziness.

Gastrointestinal tract: often - pain in the upper abdomen, diarrhea, nausea; infrequently - abdominal discomfort, dyspepsia, flatulence, vomiting; very rarely - gastric bleeding.

Allergic reactions: often - skin rash of various localizations, infrequently - eczema, erythema, urticaria.

According to post-registration observations.

Additional adverse events have been reported during post-marketing use of sulodexide. The frequency of these undesirable effects cannot be assessed due to the fact that information about them comes in the form of spontaneous reports. Accordingly, the frequency of these adverse events is classified as “unknown” (cannot be calculated based on available data).

Anemia, disorders of plasma protein metabolism, gastrointestinal disorders, melena, angioedema, ecchymosis, genital edema, genital erythema, polymenorrhea.

Drug interactions

No significant interaction of Wessel® Due F with other drugs has been established. When using sulodexide, it is not recommended to simultaneously use drugs that affect the hemostasis system as anticoagulants (direct and indirect).