Pentosan polysulfate sp 54

Pentosan polysulfate sp 54 is an antithrombotic drug.

Pentosan polysulfate (Na salt) prevents the occurrence of thrombosis, and at the same time lyses formed thrombi, increasing the internal fibrinolytic potential. It has an effect through fibrinolysis and its AT3-independent slowing properties. [ 1 ]

Due to the fact that as a result of these processes, blood viscosity is weakened (probably due to an increase in the elasticity of erythrocytes), the use of drugs causes an improvement in perfusion. [ 2 ]

Indications Pentosan polysulfate sp 54

It is used for the supportive treatment of peripheral circulatory disorders within the arteries (intermittent claudication or Fontaine phase 2b) to improve tolerance to walking-related physical activity.

It is prescribed for the treatment of subacute, acute or chronic thromboembolic and thrombotic pathologies.

Can be used to prevent the development of thromboembolic/thrombotic complications.

Release form

The release of the therapeutic substance is realized in the form of injection liquid - inside ampoules with a capacity of 1 ml. Inside the cellular pack there are 5 such ampoules. Inside the package - 2 such packs.

Pharmacodynamics

The active component of the drug releases lipoprotein lipase, which leads to a decrease in the indicators of total lipids with cholesterol and triglycerides in the blood. There is a movement of lipoprotein fractions towards HDL, due to which the likelihood of atherosclerosis is reduced.

Pharmacokinetics

The bioavailability of the drug after an intramuscular or subcutaneous injection is almost 100%. The values of biotransformation, distribution, and elimination of the substance correspond to similar indicators of heparin. At the same time, the drug differs from heparin in that it is also absorbed within the gastrointestinal tract.

Plasma Cmax level after oral administration is observed after 1-2 hours, remaining within these limits for at least 4 hours. The half-life is 25+ hours.

Pentosan polysulphate Na salt is excreted via the kidneys; a small amount of the substance is excreted with feces. In the urine, unchanged active ingredient and its depolymerized and desulphated metabolic elements are recorded.

Dosing and administration

During active phases of severe diseases.

A) performing subcutaneous injections.

Usually, 1 ampoule of the drug (0.1 g) is administered subcutaneously at 12-hour intervals. In critical conditions, especially in the case of an active phase of embolism or life-threatening acute circulatory disorders inside the arteries, 0.1 g of the drug may be administered subcutaneously on the first day of therapy at minimum 8-hour intervals. After the intensity of acute symptoms has subsided, the dose is gradually reduced to 1 ampoule (0.1 g) per day. Often, therapy at the specified dosage is continued for 10 days.

The needle is inserted at a right angle into the skin fold on the lateral or anterior wall of the peritoneum (the fold is formed between the index finger and thumb). In addition, injections can be made into the thigh or shoulder area. The injection should be done at low speed.

The duration of therapy is selected in accordance with the severity of the disease and its origin. In complex pathologies occurring in the active phase, infusions or injections of the above dosages are used (the therapy lasts a maximum of 10 days).

B) intravenous injections of pre-diluted liquids.

During days 1-2, 0.3 g of the drug should be administered per 24 hours. During days 3-6, 0.2 g per 24 hours. The drug is dissolved in 5% glucose or 0.9% isotonic liquid.

The dosage can be changed taking into account the individual characteristics of the patient.

In life-threatening acute disorders, a dose of the drug (0.1 g) may be administered through an initial bolus injection.

The medicine must be administered immediately after it has dissolved.

Introduction in chronic or subacute forms of the disease.

Often 1 ampoule (0.1 g) is used 3 times a week during the period of 21-28 days. Then injections are performed at longer intervals, especially if the therapy is carried out together with oral administration of the drug tablets.

Injections are carried out over several weeks.

• Application for children

There is no information regarding the use of the drug in pediatrics, which is why it is not prescribed to this subgroup.

Use Pentosan polysulfate sp 54 during pregnancy

There is no information regarding the introduction of Pentosan polysulfate SP 54 during breastfeeding or pregnancy. The active element of the drug does not cross the placenta. Animal testing has not revealed the development of fetotoxic or embryotoxic activity. The drug can be prescribed to pregnant women only in case of strict indications.

During the period of therapy with the introduction of the drug, it is necessary to stop breastfeeding.

Lumbar or epidural anesthesia during childbirth cannot be performed on women who are using anticoagulants.

Contraindications

Among the contraindications:

• severe intolerance associated with pentosan polysulfate sodium salt or other components of the drug;
• history of type 2 thrombocytopenia associated with the effects of pentosan polysulfate sodium salt or heparin;
• bleeding;
• diathesis that has a hemorrhagic form;
• conditions of hemophilic origin;
• ulcerative lesions or bleeding inside the gastrointestinal tract;
• recent intracerebral hemorrhage;
• operations in the eye, spinal cord or brain area;
• spinal anesthesia;
• suspicion of the presence of a neoplasm with the possibility of bleeding;
• having severe pathologies affecting the kidneys, liver or pancreas;
• subacute form of endocarditis of infectious origin;
• threat of abortion or tendency to miscarriage;
• suspicion of placenta previa or the possibility of its premature detachment;
• other risks associated with pregnancy.

Side effects Pentosan polysulfate sp 54

Main side effects:

• lesions in the blood and lymphatic system: hematomas, deep vein thrombosis, prolonged bleeding, thromboembolism and thrombocytopenia appear sporadically;
• disorders associated with the functioning of the nervous system: ischemic stroke is observed sporadically;
• problems with cardiac function: cardiac defects, myocardial infarction or heart failure develop occasionally;
• vascular disorders: aortic stenosis or intermittent claudication may occasionally occur;
• symptoms associated with the gastrointestinal tract: vomiting or nausea are observed occasionally;
• lesions of the subcutaneous layers and epidermis: signs of allergy or alopecia develop occasionally;
• systemic disorders and manifestations in the injection area: isolated hematoma and pain in the injection area;
• disorders of the biliary tract and liver: an increase in intrahepatic enzyme levels is occasionally recorded;
• Others: hyperpnea, fever, arthralgia or renal dysfunction may occur sporadically.

Overdose

Signs of intoxication include the appearance of hematomas, as well as external or internal bleeding.

Taking into account the severity of overdose manifestations, the dose is reduced or therapy is discontinued. The effect of pentosan polysulfate sodium salt can be neutralized by using the appropriate volume of protamine sulfate.

Interactions with other drugs

In case of combined use of the drug with heparin or another anticoagulant, potentiation of anticoagulant properties may occur.

Storage conditions

Pentosan polysulphate sp 54 must be stored in a place closed to small children. Temperature indicators - maximum 25°C.

Shelf life

Pentosan polysulphate sp 54 can be used within a 4-year period from the date of production of the therapeutic substance.

Analogues

An analogue of the drug is Thrombocid.