Pentosan polysulfate sp 54

Pentosan polysulfate sp 54 is an anti-thrombotic drug.

Pentosan polysulfate (Na salt) prevents the appearance of thrombosis, and at the same time lyses the formed thrombi, increasing the internal fibrinolytic potential. It has an effect through fibrinolysis and its AT3-independent inhibitory 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 red blood cells), the use of drugs causes an improvement in perfusion. [2]

Indications Pentosan polysulfate sp 54

It is used for the supportive treatment of disorders of peripheral circulation within the arteries (intermittent claudication or Fontaine phase 2b) to increase the tolerance of physical activity associated with walking.

It is prescribed for therapy with subacute, acute or chronic thromboembolic and thrombotic pathologies.

It can be used to prevent the development of complications of the thromboembolic / thrombotic type.

Release form

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

Pharmacodynamics

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

Pharmacokinetics

Bioavailability indicators of drugs after i / m or s / c injection are almost 100%. The values of biotransformation, distribution, and elimination of the substance correspond to those of heparin. In this case, the medication differs from heparin in that it is also absorbed inside the gastrointestinal tract.

The level of plasma Cmax after oral administration is noted after 1-2 hours, remaining within these limits for a period of at least 4 hours. The half-life is 25+ hours.

Pentosan polysulfate Na salt is excreted through the kidneys; a small amount of the substance is excreted in the feces. Inside the urine, an unchanged active ingredient and its depolymerized and desulfated metabolic elements are recorded.

Dosing and administration

With active phases of the disease of a severe nature.

A) performing s / c injections.

Usually, subcutaneous administration of the 1st ampoule of the drug (0.1 g) is performed 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, on the 1st day of therapy, it is allowed to inject 0.1 g of drugs s / c with at least 8-hour intervals. After weakening the intensity of acute symptoms, the portion is gradually reduced to 1 ampoule (0.1 g) per day. Often, therapy at the indicated dosage is continued for a period of 10 days.

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

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

B) intravenous injection of previously diluted fluids.

During the 1-2 days, it is required to inject 0.3 g of drugs in 24 hours. During 3-6 days - 0.2 g in 24 hours. The drug is dissolved in 5% glucose or 0.9% isotonic fluid.

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

For life-threatening acute disorders, a portion of the drug (0.1 g) is allowed to be administered through an initial bolus.

It is necessary to inject the medicine immediately after its dissolution.

Introduction for chronic or subacute forms of the disease.

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

The injections are carried out over several weeks.

• Application for children

There is no information regarding the use of drugs 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 hepatitis B or pregnancy. The active element of the drug does not cross the placenta. Animal testing did not reveal the development of fetotoxic or embryotoxic activity. The medication can be prescribed to pregnant women only in case of strict indications.

For the period of therapy with the introduction of drugs, it is necessary to refuse breastfeeding.

Lumbar or epidural anesthesia during childbirth should not be performed for women in labor using anticoagulants.

Contraindications

Among the contraindications:

• severe intolerance associated with pentosan polysulfate, Na salt or other elements of the drug;
• a history of type 2 thrombocytopenia associated with the effect of the sodium salt of pentosan polysulfate or heparin;
• bleeding;
• diathesis having a hemorrhagic form;
• conditions of hemophilic origin;
• ulcerative lesions or bleeding inside the gastrointestinal tract;
• recent intracerebral hemorrhage;
• operations in the area of the eyes, spinal cord or brain;
• spinal anesthesia;
• suspicion of the presence of a neoplasm with the likelihood of bleeding;
• having a severe pathology affecting the kidneys, liver or pancreas;
• a subacute form of endocarditis of an infectious nature;
• the threat of abortion or a tendency to develop miscarriages;
• suspicion of placental presentation or the likelihood of its too early detachment;
• other risks associated with pregnancy.

Side effects Pentosan polysulfate sp 54

The main side signs:

• lesions in the area of the blood system and lymph: single hematomas, DVT, prolonged bleeding, thromboembolism and thrombocytopenia appear;
• violations associated with the work of the NA: ischemic stroke is observed singly;
• problems with cardiac function: single cardiac defects, myocardial infarction or heart failure develop;
• disorders of vascular activity: single aortic stenosis or intermittent claudication appears;
• symptoms associated with the gastrointestinal tract: vomiting or nausea is observed singly;
• lesions of the subcutaneous layers and epidermis: signs of allergy or alopecia develop singly;
• systemic disorders and manifestations in the area of the injection: single hematoma and pain in the area of the injection are noted;
• Violations of the activity of the liver and liver: an increase in the indices of intrahepatic enzymes is recorded;
• others: hyperpnea, fever, arthralgia or renal dysfunction appears singly.

Overdose

Among the signs of intoxication is the appearance of hematomas, as well as external or internal bleeding.

Taking into account the severity of the manifestations of an overdose, a portion is reduced or therapy is canceled. The effect of pentosan polysulfate Na salt can be neutralized by using an appropriate volume of protamine sulfate.

Interactions with other drugs

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

Storage conditions

Pentosan polysulfate sp 54 must be kept out of the reach of small children. Temperature readings - maximum 25 ° С.

Shelf life

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

Analogs

An analogue of the medication is the Thrombocid agent.