Vessel Due F, capsules 250 le 60 pcs

Vessel® Due F (sulodexide) is a biological drug which is a natural mixture of glycosaminoglycans (GAGs): a heparin-like fraction with a molecular weight of 8000 dalton (80%) and dermatansulfate (20%).

The mechanism of action of sulodexide is due to two main properties: the fast acting heparin-like fraction has an affinity to antithrombin III (ATIII), and dermatan – to cofactor II heparin (KGII). After oral administration at the recommended dosage, the amount of sulodexide and its derivatives after first-pass effects is sufficient to induce antithrombin action without affecting normal coagulation parameters (activated partial thromboplastin time (APTB), thrombin time, activated factor X). Thus, we can assume that sulodexide when administered orally has no anticoagulation.

Pharmacological action: angioprotective, profibrinolytic, antithrombotic.

Pharmacodynamics

Angioprotective effect is associated with the restoration of structural and functional integrity of vascular endothelial cells, with the restoration of the normal density of the negative electric charge of the basal membrane pores of blood vessels. Besides, the preparation normalizes rheological blood properties due to reduction of triglycerides level (it stimulates lipolytic enzyme – lipoprotein lipase – that hydrolyzes triglycerides being a part of LDL).

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

Profibrinolytic effect is due to the increase in blood levels of tissue plasminogen activator and reduction of its inhibitor.

The antithrombotic activity of oral sulodexide is mainly the result of all the effects 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 plasma is observed in 2 hours, the second in 4 to 6 hours, after which the drug is no longer detectable in plasma; concentrations recover after about 12 hours and then remain constant until about the 48th hour. Permanent plasma levels are detected after 12 hours, probably due to the slow release of the drug by the absorptive organs and in particular by the vascular endothelium. Sulodexide is distributed in the vascular endothelium at a concentration 20-30 times higher than in other tissues. It is metabolized in the liver and excreted mainly by the kidneys. In a study of radioactive labeled drug 55.23% of sulodexide was excreted with urine during the first 96 hours.

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Indications

Thrombophlebitis, Vascular lesions in diabetes, Diabetic nephropathy, Stroke sequelae, Impaired cerebral circulation, Diabetic retinopathy, Thrombosis prevention

• angiopathies with increased risk of thrombosis, including after myocardial infarction;
• cerebral circulatory disorders, including the acute period of ischemic stroke and early recovery period; discirculatory encephalopathy due to atherosclerosis, diabetes, hypertension; vascular dementia;
• phlebopathies, deep vein thrombosis;
microangiopathies (nephropathy, retinopathy, neuropathy) and macroangiopathies in diabetes (diabetic foot syndrome, encephalopathy, cardiopathy);
• thrombophilic conditions, antiphospholipid syndrome (administered in conjunction with acetylsalicylic acid, and following low molecular weight heparin);
• treatment of heparin-induced thrombotic thrombocytopenia because it does not cause or aggravate it.

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Active ingredient

Sulodexide

Composition

Each capsule contains:

Active ingredient:

sulodexide 250 LE*

Excipients: sodium lauryl sarcosinate 3.30 mg, colloidal silica 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.

* – lipoproteinlipase unit

How to take, the dosage

Take 1-2 capsules 2 times a day before meals for 30-40 days. Usually the treatment starts with the preparation in a dosage form “solution for intravenous and intramuscular application” 1 ampoule a day, intramuscularly or intravenously, for 15-20 days.

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

Depending on the results of clinical and diagnostic examination of the patient the dosing regime may be changed at the discretion of the doctor.

Interaction

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

Special Instructions

Due to the pharmaco-toxicological properties of sulodexide, the use of the drug does not require special precautions. However, when combined with other anticoagulants, blood clotting parameters should be periodically monitored.

Effect on the ability to drive and operate vehicles

Vessel® Due F has no effect on the ability to drive and operate vehicles.

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Contraindications

– Hypersensitivity;
– hemorrhagic diathesis and diseases accompanied by reduced blood clotting;
– pregnancy I trimester.

With caution: When combined with anticoagulants the parameters of blood clotting should be monitored.

Side effects

According to clinical studies

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

The adverse reactions associated with the use of sulodexide were classified in the system-organ class and categorized by frequency of occurrence in the following order: Very common (≥ 1/10), common (≥ 1/100 to < 1/10), infrequent (≥ 1/1000 to < 1/100), rare (≥ 1/10000 to < 1/1000), very rare (< 1/10000).

Nervous system: infrequent – headache, very rare – loss of consciousness.

Hearing organ: frequent – dizziness.

Gastrointestinal tract: frequently – upper abdominal pain, diarrhea, nausea, infrequently – a feeling of discomfort in the abdomen, dyspepsia, flatulence, vomiting, very rarely – stomach bleeding.

Allergic reactions: frequent – skin rash of various localizations, infrequent – eczema, erythema, urticaria.

According to post-registration observations.

During post-registration use of sulodexide additional adverse events were registered. The frequency of these adverse events cannot be estimated due to the fact that they are reported spontaneously. Accordingly, the frequency of these adverse events is classified as “unknown” (cannot be calculated on the basis of available data).

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

Overdose

Bleeding is the only phenomenon that may occur in case of overdose. In case of bleeding it is necessary to administer protamine sulfate (1 % solution) used for heparin-induced bleeding.