Product Overview
Composition
Active ingredient:
Sulodexide 250 LU *
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, propyl parahydroxybenzoate 0.13 mg, titanium dioxide (E171) 0.29 mg, iron oxide red (E172) 0.86 mg .
* - lipoprotein lipase unit
pharmachologic effect
Wessel Due F (sulodexide) is a biological drug, which is a natural mixture of glycosaminoglycans (GAG): 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 (KGII). 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 the usual coagulation parameters (activated partial thromboplastin time (APTT), thrombin time, activated factor X). Thus, it can be assumed that sulodexide, when administered orally, has no anticoagulation 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 electric charge of the pores of the vascular basement membrane. In addition, the drug normalizes the rheological properties of blood by reducing the level of triglycerides (stimulates the lipolytic enzyme - lipoprotein lipase, hydrolyzing 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 types of action 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 a labeled drug, the first peak of sulodexide in blood plasma is observed after 2 hours, the second from 4 to 6 hours, after which the drug is no longer detected in plasma; the concentration is restored after approximately 12 hours, and then remains constant until approximately the 48th hour. A constant plasma level is detected after 12 hours, probably due to the slow release of the drug by the absorption organs and, in particular, the vascular endothelium. Sulodexide is distributed in the vascular endothelium at a concentration of 20-30 times higher than the concentration in other tissues. It is metabolized in the liver and excreted mainly by the kidneys. In a study of a radiolabelled drug, 55.23% of sulodexide was excreted in the urine during the first 96 hours.
Indications
- angiopathy with an increased risk of thrombosis, including after myocardial infarction;
- cerebrovascular accident, including an acute period of ischemic stroke and a period of early recovery; discirculatory encephalopathy due to atherosclerosis, diabetes mellitus, hypertension; vascular dementia;
- occlusive lesions of the peripheral arteries of both atherosclerotic and diabetic origin;
- phlebopathy, deep vein thrombosis;
- microangiopathies (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, because it does not cause or aggravate it.
Contraindications
- hemorrhagic diathesis and diseases accompanied by decreased blood coagulability;
- pregnancy I trimester.
With caution: When combined with anticoagulants, blood coagulation parameters should be monitored.
Side effects
data on the incidence of adverse drug reactions associated with the use of sulodexide were obtained during clinical trials involving patients treated with standard doses of the drug with the usual duration of treatment.
Adverse reactions associated with the use of sulodexide were classified by the systemic-organ class and distributed by frequency of occurrence in the following order: very often (≥ 1/10), often (≥ 1/100 to <1/10), infrequently (≥ 1 / 1000 to <1/100), rarely (≥ 1/10000 to <1/1000), very rarely (<1/10000).
Nervous system: infrequently - headache, very rarely - loss of consciousness.
Hearing organ: often - dizziness.
Gastrointestinal tract: often - pain in the upper abdomen, diarrhea, nausea, infrequently - a feeling of discomfort in the abdomen, dyspepsia, flatulence, vomiting, very rarely - gastric bleeding.
Allergic reactions: often - a skin rash of various localization, infrequently - eczema, erythema, urticaria.
According to post-registration observations.
During the post-registration use of sulodexide, additional adverse events were recorded. The frequency of these unwanted effects cannot be estimated due to the fact that information about them comes in the form of spontaneous messages. Accordingly, the frequency of these adverse events is classified as “unknown” (cannot be calculated based on available data).
Anemia, disorders of plasma protein metabolism, disorders of the gastrointestinal tract, melena, angioedema, ecchymosis, genital edema, genital erythema, polymenorrhea.
Interaction
How to take, course of administration and dosage
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, at the discretion of the doctor, the dosage regimen can be changed.
Overdose
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 coagulation indicators should be periodically monitored.
Impact on the ability to drive vehicles and mechanisms
Does not affecthe ability to drive vehicles and mechanisms.
