Vazonit retard coated tablets 600 mg No. 20

Instructions for use Vazonit retard coated tablets 600 mg No. 20

Composition

active ingredient: pentoxifylline;

1 tablet contains 600 mg of pentoxifylline;

excipients: hypromellose 15000, hypromellose 5, crospovidone, microcrystalline cellulose, colloidal anhydrous silica, magnesium stearate, macrogol 6000, talc, titanium dioxide (E 171), polyacrylate dispersion.

Dosage form

Retard tablets, coated.

Main physicochemical properties: oblong, biconvex tablets, film-coated, white, with a breakline on both sides.

Pharmacotherapeutic group

Peripheral vasodilators. ATX code C04A D03.

Pharmacological properties

Pharmacodynamics

The drug improves microcirculation and rheological properties of blood, has a vasodilating effect. The active substance - pentoxifylline - is a xanthine derivative. The mechanism of action is associated with the inhibition of phosphodiesterase and the accumulation of cAMP in vascular smooth muscle cells, blood cells, other tissues and organs. Pentoxifylline inhibits platelet and erythrocyte aggregation, increases their elasticity, reduces the level of fibrinogen in blood plasma and enhances fibrinolysis, which reduces blood viscosity and improves its rheological properties. The drug improves the supply of tissues with oxygen in areas of impaired blood circulation, primarily in the extremities, central nervous system, to a lesser extent - in the kidneys. It slightly dilates coronary vessels.

The special prolonged-release form of the tablet ensures constant and long-lasting maintenance of the effect, which allows for use at longer intervals.

Pharmacokinetics

The properties of the tablet ensure continuous release of the active substance and its uniform absorption from the gastrointestinal tract. The drug undergoes "first-pass" metabolism in the liver, resulting in the formation of a number of pharmacologically active metabolites. The absolute bioavailability of the drug is on average 19.4%. Vasonite does not bind to plasma proteins. The maximum concentration of pentoxifylline and its active metabolites in the blood plasma is reached after 3-4 hours and remains at a therapeutic level for about 12 hours. The drug is excreted mainly in the urine, in the form of metabolites - 90% is excreted by the kidneys.

In patients with renal insufficiency (creatinine clearance < 30 ml/min), the elimination of Vasonite and its metabolites is delayed.

In patients with hepatic insufficiency, the half-life is prolonged and absolute bioavailability is increased.

Indication

To extend pain-free walking distance in patients with chronic peripheral arterial occlusive disease in Fontan stage IIb (intermittent claudication) when other interventions such as gait training, angioplasty and/or reconstructive procedures cannot be performed or are not indicated.

Inner ear dysfunction caused by circulatory disorders (including hearing loss and sudden hearing loss).

Contraindication

Vasonite is contraindicated:

patients with hypersensitivity to pentoxifylline, other methylxanthines or any of the excipients of the drug;

patients with extensive retinal hemorrhage, with cerebral hemorrhage (risk of increased bleeding). If retinal hemorrhage occurs during treatment with pentoxifylline, the drug should be discontinued immediately;

patients with cerebral hemorrhage or other clinically significant bleeding;

patients in the acute period of myocardial infarction;

patients with gastric and/or intestinal ulcers;

patients with hemorrhagic diathesis.

Interaction with other medicinal products and other types of interactions

When co-administered with the drugs listed below, the possibility of drug interactions should be considered.

Drugs that lower blood pressure.

Pentoxifylline may enhance the effect of antihypertensive agents, and the decrease in blood pressure may be more pronounced.

Anticoagulants.

Pentoxifylline may potentiate the effects of anticoagulants. Patients with an increased tendency to bleed, such as those receiving concomitant anticoagulant treatment, require close monitoring (including regular monitoring of the INR (international normalized ratio)) as there is a risk of more severe bleeding.

Oral antidiabetic drugs, insulin.

A more significant decrease in blood sugar levels and the development of hypoglycemic reactions are possible. It is necessary to monitor blood sugar levels at intervals that are set individually for each patient.

Theophylline.

The concentration of theophylline in the blood may increase, and as a result, side effects may be exacerbated during the treatment of respiratory tract diseases.

Cimetidine.

Possible increase in plasma pentoxifylline levels and enhanced effects of pentoxifylline.

Ciprofloxacin.

Potential additive effect with platelet aggregation inhibitors: Due to the increased risk of bleeding, concomitant use of platelet aggregation inhibitors (e.g. clopidogrel, eptifibatide, tirofiban, epoprostenol, iloprost, abciximab, anagrelide, NSAIDs (nonsteroidal anti-inflammatory drugs) other than selective COX-2 inhibitors, acetylsalicylates [ASA/LAS], ticlopidine, dipyridamole) with pentoxifylline should be done with caution.

With simultaneous use with antiadrenergic drugs and ganglioblockers, a significant decrease in blood pressure may be observed. Simultaneous use of adrenergic substances and xanthines leads to stimulation of the central nervous system.

Application features

At the first signs of an anaphylactic/anaphylactoid reaction, treatment with Vazonit should be discontinued and medical attention should be sought.

When using the drug Vazonit in patients with chronic heart failure, the phase of circulatory compensation should first be achieved.

In patients with diabetes mellitus and receiving treatment with insulin or oral antidiabetic agents, when using high doses of the drug Vazonit, the effect of these drugs on blood sugar levels may be increased (see section "Interaction with other medicinal products and other types of interactions"). In these cases, the dose of insulin or oral antidiabetic agents should be reduced and the patient should be especially carefully monitored.

Patients with systemic lupus erythematosus (SLE) or other connective tissue diseases should be prescribed pentoxifylline only after a thorough analysis of the possible risks and benefits.

Since there is a risk of developing aplastic anemia during treatment with pentoxifylline, regular complete blood counts should be performed.

In patients with renal insufficiency (creatinine clearance less than 30 ml/min) or severe liver dysfunction, the elimination of pentoxifylline may be delayed. Appropriate monitoring is required.

Particularly careful observation is necessary for:

patients with severe cardiac arrhythmias;

patients with myocardial infarction;

patients with arterial hypotension;

Patients with severe atherosclerosis of the cerebral and coronary vessels, especially with concomitant arterial hypertension and heart rhythm disturbances. These patients may experience angina attacks, arrhythmias and arterial hypertension when taking the drug.

patients with renal insufficiency (creatinine clearance below 30 ml/min);

patients with severe hepatic insufficiency;

patients with a high tendency to bleed, for example due to anticoagulant treatment or blood clotting disorders. For bleeding, see section "Contraindications";

patients who have recently undergone surgical treatment (increased risk of bleeding, which requires systematic monitoring of hemoglobin and hematocrit levels);

patients receiving concomitant treatment with pentoxifylline and vitamin K antagonists or platelet aggregation inhibitors (see section "Interaction with other medicinal products and other types of interactions");

patients receiving concomitant treatment with pentoxifylline and antidiabetic drugs (see section "Interaction with other medicinal products and other types of interactions");

patients receiving concomitant treatment with pentoxifylline and ciprofloxacin (see section “Interaction with other medicinal products and other types of interactions”).

patients receiving concomitant treatment with pentoxifylline and theophylline (see section "Interaction with other medicinal products and other types of interactions").

Use during pregnancy or breastfeeding

Pregnancy

There is insufficient experience with the use of the drug in pregnant women. Therefore, it is recommended not to use the drug Vazonit during pregnancy.

Breast-feeding

Pentoxifylline passes into breast milk in small amounts. If treatment with Vazonit is prescribed, breastfeeding should be discontinued.

Ability to influence reaction speed when driving vehicles or other mechanisms

Does not affect.

Method of administration and doses

The dosage is determined by the doctor individually, depending on the nature and course of the disease.

Chronic peripheral arterial occlusive disease in Fontan stage IIb (intermittent claudication).

Unless otherwise prescribed, 1 tablet of 600 mg is used 1-2 times a day (600-1200 mg of pentoxifylline per day).

Dose adjustment is necessary for patients with low or unstable blood pressure.

Dosage for patients with renal insufficiency (creatinine clearance less than 30 ml/min) should be selected taking into account individual tolerability.

For patients with severe liver dysfunction, a dose reduction is required. The decision to reduce the dose is made by the physician, who in each individual case must take into account the severity of the disease and the tolerability of the drug.

Inner ear dysfunction caused by circulatory disorders (including hearing loss and sudden hearing loss).

In cases of severe circulatory disorders, the onset of action can be accelerated by prescribing tablets in combination with parenteral administration of pentoxifylline. The total daily dose (parenteral + oral) should not exceed 1200 mg of pentoxifylline.

Depending on the severity of symptoms, treatment may be either oral only, or a combination of oral and parenteral (intravenous infusion), or parenteral only (intravenous infusion).

Dose adjustment may be necessary for patients with low or unstable blood pressure.

In patients with renal insufficiency (creatinine clearance less than 30 ml/min), the dose should be titrated to 50-70% of the standard dose, taking into account individual tolerability.

The decision to reduce the dose in patients with severe liver dysfunction should be made by the physician, taking into account the severity of the disease and the tolerability of the drug in each individual patient.

Method and duration of application.

The tablet should be swallowed whole (without chewing) with sufficient water. The duration of use should be determined by the doctor depending on the clinical condition of each individual patient.

Note.

In case of accelerated passage through the gastrointestinal tract (laxatives, diarrhea, surgical shortening of the intestine), in some cases, undissolved tablet residues are excreted from the body. If premature excretion occurs only from time to time, this should not be given much attention.

Children

Due to the lack of sufficient clinical experience, Vazonit should not be prescribed to children (under 18 years of age).

Overdose

Symptoms: Dizziness, nausea, decreased blood pressure, tachycardia, hot flashes, fainting, fever, agitation, areflexia, tonic-clonic seizures, arrhythmias, vomitus resembling coffee grounds as a sign of gastrointestinal bleeding, areflexia and tonic-clonic seizures.

Treatment: If the overdose has occurred recently, gastric lavage or activated charcoal may be used to prevent further absorption.

Treatment should be symptomatic, as there is no specific antidote. Intensive care unit observation may be necessary to prevent complications.

Emergency measures in case of severe hypersensitivity reactions (shock). At the first signs of severe reactions (e.g. skin reactions (urticaria), flushing, restlessness, headache, sudden sweating, nausea), a venous catheter should be inserted. In addition to standard emergency measures such as placing the patient in a supine position with the legs elevated, ensuring a patent airway and administering oxygen, emergency medical treatment is indicated, including intravenous fluid replacement, intravenous epinephrine (adrenaline), glucocorticoids (e.g. methylprednisolone 250-1000 mg intravenously), and histamine receptor antagonists.

Depending on the severity of clinical symptoms, artificial respiration may be necessary, and in case of circulatory arrest, restoration of vital functions according to usual recommendations.

Side effects

The following adverse reactions have been reported during clinical trials and post-marketing experience. The frequency of occurrence is unknown.

Expiration date

5 years.

Storage conditions

Store in a dry, dark place out of reach of children at a temperature not exceeding 25°C.

Packaging

10 tablets in a blister, 2 blisters in a box.

Vacation category

According to the recipe.

Producer

H.L. Pharma GmbH/GL Pharma GmbH.

Address

Schlossplatz 1, 8502 Lannach, Austria/Schlossplatz 1, 8502 Lannach, Austria