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Vessel Due F
Sulodexide

Antithrombotic drugs
Vessel Due F ampoules: Each ampoule contains: Sulodexide 600 LSU Excipients: sodium chloride, water for injection.
Vessel Due F capsules: Each capsule contains: Sulodexide 250 LSU

Excipients: Sodium lauryl sarcosinate, Precipitated silica, Triglycerides, gelatine, glycerol, sodium ethyl p-oxybenzoate, sodium propyl p-oxybenzoate, titanium dioxide E171 and red iron oxide E172.

Mechanisms of action
Sulodexide has a relevant antithrombotic activity both in rats and rabbits. In the case of rats, Sulodexide is able to prevent the formation of venous and arterial thrombus; it is also effective in reducing the weight of pre-formed thrombi both by parenteral and oral administration.

The antithrombotic activity is related to:
a) A block of thrombin and cathepsin G platelet aggregation;
b) Inhibitory effect on platelet adhesives;
c) A block in platelet function;
d) Anticoagulant and pro-fibrinolytic activity shown both in vivo and in vitro in animals and in humans.

The mechanism of action of the antithrombotic activity is due to the simultaneous inhibition of circulating thrombin through its affinity for anti-thrombin III and the thrombin bound to surfaces, such as the surface of the thrombus, as well as through affinity for heparin cofactor II. This simultaneous action which catalyses the thrombin inhibition reaction seems to be better than that observed with heparin and increases the antithrombotic potential of Sulodexide. Furthermore, Sulodexide causes less bleeding than conventional heparin at doses which are active on thrombosis. Affinity for fibrin both in vitro and in vivo, both after intravenous and oral administration has been shown; in fact, Sulodexide labeled with fluorescent binds to the fibrin of the thrombus and it is found to be still bound even several hours after administration. This observation could mean that Sulodexide is able to carry out its antithrombotic action locally on the thrombus. Sulodexide shows an anti-atherosclerotic activity in experimental models in rabbits.

The pharmacological profile of Sulodexide described up to now is completed by normalisation of altered lipid levels which occurs through the activation of lipoprotein lipase.

Pharmacology
Sulodexide carries out a marked antithrombotic action both on arteries and veins.

Several clinical studies carried out by administering the product parenterally and orally, demonstrated that the antithrombotic activity of Sulodexide is due to the dose-dependent inhibition of some coagulation factors, especially activated factor X; interference with thrombin remains instead at levels of low significance and the consequences of an anticoagulative action are generally avoided. Antithrombotic action is sustained even by the inhibition of platelet aggregation and by the activation of circulatory and wall fibrinolytic system.

Sulodexide also normalises the viscosity parameters which are usually altered in patients with vascular pathologies with thrombotic risk; this action mainly takes place through the reduction of fibrinogen levels. Sulodexide pharmacological profile described so far is completed with the normalization of altered lipidic values by the activation of lipoprotein lipase.

Studies carried out to show other possible effects in addition to the above mentioned, primary to therapeutic efficacy, confirmed that the administration of VESSEL DUE F has no anticoagulant effects.

Pharmacokinetics
Sulodexide is characterised by absorption through the gastrointestinal barrier which may be demonstrated based on pharmacodynamic effects of the drug after oral, intraduodenal, intraileal and rectal administration in rats of Sulodexide labeled with fluoresceine. Dose-effect and dose-time correlations in rats and rabbits have been shown following administration by the routes indicated above. The labeled substance is initially accumulated in the intestinal cells and then is released by the serum pole in the systemic circulation.

The concentration of radioactive substance significantly increases in time at the level of brain, kidney, heart, liver, lung, testicle and plasma. Pharmacological tests carried out on man with i.m. and i.v. administration of the product revealed linear dose-effect relationship. The metabolism was mainly hepatic and the excretion mainly urinary.

Absorption after oral administration in man studied with labeled product, showed that a first blood level peak occurred after 2 hours and a second between the 4th and the 6th hour, after which the drug is no longer detectable in plasma; it reappears at about the 12th hour and then remains constant until about the 48th hour. The constant blood level found after the 12th hour is probably due to slow release of the drug by the uptake organs and in particular vessel endothelia. Urinary excretion: using the labeled product, 55.23% of the administered radioactivity is excreted through urine during the first 96 hours. This elimination shows a peak after about 12 hours, and an average urinary value of 17.6% of the administered dose in 0-24 hour interval; a second peak at around the 36th hour and urinary elimination of 22% from the 24th to the 48th hour and a third peak at around the 78th hour and a urinary elimination of about 14.9% in the 48-96 hour period. After 96 hours, radioactivity is no longer detectable in the collected samples.

Faecal excretion: the total radioactivity recuperated from the faeces is 23% in the first 48 hours, after which no labeled substance can be detected.

Indications
Vascular pathologies with thrombotic risk.

Contraindications
Individual hypersensitivity towards the product, heparin, or heparin-like drugs. Diathesis and haemorrhagic diseases.

Undesirable effects
Occasionally occur.
Capsules: disturbances of the gastroenteric system with nausea, vomiting and epigastralgia.

Ampoules: pain, burning sensation and haematoma at the site of the injection. Also, in rare case, sensitization may occur with cutaneous reactions or reactions on other sites.

Precautions/Warnings
Given the low toxicity of the substance, there are no particular precautions for use. However, when treatment with anticoagulants is under way, haemocoagulative parameters should be monitored periodically.

Drug interactions
As Sulodexide is a heparin-like molecule, it may increase the anticoagulant effects of heparin itself and of oral anticoagulants if administered at the same time.

Use in pregnancy
As a precaution, the use of the substance is not advisable during pregnancy even though studies on fetal toxicity have not revealed any embryo-fetotoxic effects.

Pharmaceutical precautions
As Sulodexide is an acid polysaccharide, if administered in extemporaneous association, it may react by forming complexes with all the base substances. The incompatible substances commonly used for extemporaneous associations for phleboclysis are: vitamin K, vitamins of the B complex, hydrocortisone, jaluronidase, calcium gluconate, quaternary ammonium salts, chloramphenicol, tetracycline, streptomycin.

Dosage
Capsules: 1 capsule twice a day, far from meals.
Ampoules: 1 ampoule a day, i.m. or i.v.

Generally it is advisable to start the therapy with the ampoules and after 15-20 days, continue the treatment with capsules for 30-40 days. The complete therapeutic cycle should be repeated at least twice a year. The posology may be varied in quantity and frequency at the discretion of the doctor.

Symptoms and treatment for overdosage
Haemorrhage is the only effect which may occur with an overdosage. In the case of a haemorrhage, it is necessary to inject 1% protamine sulphate (3 ml i.v. = 30 mg) as it is used in "heparin haemorrhages".

Packing
Ampoules: Type I yellow glass weak-point 2 ml ampoule containing a clear light-yellow to yellow liquid. Each cardboard box containing a polystyrene tray with 10 dark glass ampoules with injectable solution.
Capsules: 50 capsules (cardboard box containing 2 blisters of 25 soft capsules each).

Storage conditions

Store below 30 C.


Expiry period

5 years from the date of manufacture.

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