Vasonit tablets of prolonged action, p / o 600mg, No. 20

• Violation of peripheral circulation against the background of atherosclerotic, diabetic and inflammatory processes (including with 'intermittent' claudication due to atherosclerosis, diabetic angiopathy, obliterating endarteritis);

• Acute and chronic disorders of cerebral circulation of ischemic origin;

• Symptomatic treatment of the consequences of impaired cerebral circulation of atherosclerotic genesis (impaired concentration, dizziness, memory impairment);

• Atherosclerotic and discirculatory encephalopathy; angiopathy (paresthesia, Raynaud's disease);

• Trophic tissue disorders due to impaired arterial or venous microcirculation (trophic ulcers, post-thrombophlebitic syndrome, frostbite, gangrene);

• Circulatory disorders in the vessels of the eye (acute and chronic circulatory failure in the mesh or in the choroid);

• Dysfunction of the middle ear of vascular origin, accompanied by hearing loss.

VazonitЃ tablets should be taken orally, without chewing, with a sufficient amount of liquid, preferably after meals.
The drug is usually prescribed 1 tablet 600 mg 2 times a day (morning and evening), the maximum daily dose is 1200 mg.
The duration of treatment and dosage regimen with VazonitЃ are set by the doctor individually, depending on the clinical picture of the disease and the therapeutic effect obtained.
In patients with chronic renal failure (creatinine clearance less than 30 ml / min), the daily dose of the drug is reduced to 600 mg.
A dose reduction, taking into account individual tolerance, is necessary in patients with severely impaired liver function.
Treatment can be started with low doses in patients with low blood pressure, as well as in patients at risk due to a possible decrease in blood pressure (patients with severe coronary artery disease or hemodynamically significant cerebral stenosis). In these cases, the dose can only be increased gradually.

One prolonged-release film-coated tablet contains: active substance: pentoxifylline 600 mg;
excipients: hypromellose 15000 cP - 104.0 mg, microcrystalline cellulose - 13.5 mg, crospovidone - 15.0 mg, colloidal silicon dioxide - 3.0 mg, magnesium stearate - 4.5 mg; shell: macrogol 6000 - 3.943 mg, talc - 11.842 mg, titanium dioxide - 3.943 mg, hypromellose 5 cP - 3.286 mg, polyacrylic acid (in the form of 30% dispersion) - 0.986 mg.

• Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other components that make up the drug;

• Acute myocardial infarction;

• Massive bleeding;

• Retinal hemorrhage;

• Acute hemorrhagic stroke;

• Pregnancy;

• Breastfeeding period;

• Age up to 18 years (efficacy and safety have not been established).

Application during pregnancy and during breastfeeding

The use of the drug during pregnancy and lactation is contraindicated.

With care : atherosclerosis of cerebral and / or coronary vessels, especially in cases of arterial hypotension and cardiac arrhythmias; chronic heart failure, liver failure, renal failure (creatinine clearance less than 30 ml / min - risk of cumulation and increased risk of side effects), gastric ulcer and duodenal ulcer, recent surgery (risk of bleeding), increased tendency to bleeding , for example, when using anticoagulants or in violation of the blood coagulation system (risk of more severe bleeding).

Trade name of the drug:

VasoniteЃ

International non-proprietary name:

pentoxifylline

Dosage form:

prolonged-release film-coated tablets

Composition

One prolonged-release film-coated tablet contains: active substance: pentoxifylline 600 mg;
excipients: hypromellose 15000 cP - 104.0 mg, microcrystalline cellulose - 13.5 mg, crospovidone - 15.0 mg, colloidal silicon dioxide - 3.0 mg, magnesium stearate - 4.5 mg; shell: macrogol 6000 - 3.943 mg, talc - 11.842 mg, titanium dioxide - 3.943 mg, hypromellose 5 cP - 3.286 mg, polyacrylic acid (in the form of 30% dispersion) - 0.986 mg.

Description

Oblong biconvex film-coated tablets of white color, scored on both sides. The core of the tablet is white.

Pharmacotherapeutic group

Vasodilator

ATX code - C04AD03

Pharmacological properties

Pharmacodynamics
Xanthine derivative. Improves microcirculation in areas of impaired blood supply. Improves the rheological properties of blood (fluidity) by affecting the pathologically altered deformability of erythrocytes, increases the elasticity of erythrocyte membranes, inhibits the aggregation of erythrocytes and platelets and reduces the increased viscosity of blood. The mechanism of action is associated with the inhibition of phosphodiesterase and the accumulation of cyclic adenosine monophosphate (cAMP) in vascular smooth muscle cells and in blood corpuscles. Pentoxifylline inhibits the aggregation of erythrocytes and platelets, reduces the level of fibrinogen in blood plasma and enhances fibrinolysis, which reduces blood viscosity and improves its rheological properties. Improves the supply of oxygen to tissues in areas of impaired blood circulation, in particular in the extremities, the central nervous system, and, to a lesser extent,in the kidneys. With occlusive lesion of the peripheral arteries ('intermittent' claudication) leads to an increase in walking distance, elimination of nocturnal cramps of the calf muscles, and a decrease in pain at rest. In case of impaired cerebral circulation, it improves symptoms. Providing a weak myotropic vasodilating effect, it somewhat reduces the total peripheral vascular resistance and slightly dilates the coronary vessels.

Pharmacokinetics
After oral administration, pentoxifylline is almost completely absorbed from the gastrointestinal tract. The extended release form provides continuous release and uniform absorption. Pentoxifylline is metabolized in the liver during the 'first pass', resulting in the formation of two pharmacologically active metabolites: 1-5-hydroxyhexyl-3,7-dimethylxanthine (metabolite I) and 1-3-carboxypropyl-3,7-dimethylxanthine (metabolite V ). The concentration of metabolites I and V in plasma, respectively, is 5 and 8 times higher than that of pentoxifylline. When Vazonit tablets are taken orally, the maximum concentration of pentoxifylline and its active metabolites in the blood plasma is achieved after 3-4 hours and remains at a therapeutic level for about 12 hours. The drug is excreted mainly (94%) by the kidneys in the form of metabolites. Excreted in breast milk.In severe renal impairment, excretion of metabolites is slowed down. In case of liver dysfunction, an elongation of the half-life and an increase in bioavailability are noted.

Indications for use

• Violation of peripheral circulation against the background of atherosclerotic, diabetic and inflammatory processes (including with 'intermittent' claudication due to atherosclerosis, diabetic angiopathy, obliterating endarteritis);

• Acute and chronic disorders of cerebral circulation of ischemic origin;

• Symptomatic treatment of the consequences of impaired cerebral circulation of atherosclerotic genesis (impaired concentration, dizziness, memory impairment);

• Atherosclerotic and discirculatory encephalopathy; angiopathy (paresthesia, Raynaud's disease);

• Trophic tissue disorders due to impaired arterial or venous microcirculation (trophic ulcers, post-thrombophlebitic syndrome, frostbite, gangrene);

• Circulatory disorders in the vessels of the eye (acute and chronic circulatory failure in the mesh or in the choroid);

• Dysfunction of the middle ear of vascular origin, accompanied by hearing loss.

Contraindications

• Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other components that make up the drug;

• Acute myocardial infarction;

• Massive bleeding;

• Retinal hemorrhage;

• Acute hemorrhagic stroke;

• Pregnancy;

• Breastfeeding period;

• Age up to 18 years (efficacy and safety have not been established).

Application during pregnancy and during breastfeeding

The use of the drug during pregnancy and lactation is contraindicated.

With care : atherosclerosis of cerebral and / or coronary vessels, especially in cases of arterial hypotension and cardiac arrhythmias; chronic heart failure, liver failure, renal failure (creatinine clearance less than 30 ml / min - risk of cumulation and increased risk of side effects), gastric ulcer and duodenal ulcer, recent surgery (risk of bleeding), increased tendency to bleeding , for example, when using anticoagulants or in violation of the blood coagulation system (risk of more severe bleeding).

Method of administration and dosage

VazonitЃ tablets should be taken orally, without chewing, with a sufficient amount of liquid, preferably after meals.
The drug is usually prescribed 1 tablet 600 mg 2 times a day (morning and evening), the maximum daily dose is 1200 mg.
The duration of treatment and dosage regimen with VazonitЃ are set by the doctor individually, depending on the clinical picture of the disease and the therapeutic effect obtained.
In patients with chronic renal failure (creatinine clearance less than 30 ml / min), the daily dose of the drug is reduced to 600 mg.
A dose reduction, taking into account individual tolerance, is necessary in patients with severely impaired liver function.
Treatment can be started with low doses in patients with low blood pressure, as well as in patients at risk due to a possible decrease in blood pressure (patients with severe coronary artery disease or hemodynamically significant cerebral stenosis). In these cases, the dose can only be increased gradually.

Side effect

From the side of the central nervous system: headache, dizziness, anxiety, sleep disturbances, convulsions, there are cases of aseptic meningitis.
On the part of the skin and subcutaneous fat: hyperemia of the skin of the face, 'hot flushes' of blood to the skin of the face and upper chest, edema, increased fragility of the nails.
From the digestive system: dry mouth, feeling of pressure and fullness in the stomach, decreased appetite, nausea, vomiting, diarrhea, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis. From the side of the organ of vision: visual impairment, scotoma.
From the side of the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina pectoris, decreased blood pressure.
On the part of the hematopoietic and hemostatic system: in rare cases, bleeding may occur (from the mucous membranes, vessels of the skin, stomach, intestines), as well as thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia, aplastic anemia. In this regard, when treating with VazonitЃ, it is necessary to regularly monitor the picture of peripheral blood.
Allergic reactions: pruritus, skin flushing, urticaria, angioedema, anaphylactic shock.
Laboratory indicators: increased activity of 'liver' transaminases: alanine aminotransferase (ALT), aspartate aminotransferase (ACT), as well as lactate dehydrogenase (LDH) and alkaline phosphatase.

Overdose

Symptoms: weakness, dizziness, tachycardia, drowsiness, marked decrease in blood pressure, redness of the skin, loss of consciousness, fever (chills), areflexia, tonic-clonic seizures, signs of gastrointestinal bleeding (vomiting like 'coffee grounds').
Treatment: gastric lavage followed by ingestion of activated charcoal. In case of vomiting with traces of blood, gastric lavage is unacceptable. Further treatment is symptomatic, aimed at maintaining respiratory function and blood pressure. For convulsions, diazepam.

Interaction with other medicinal products

Pentoxifylline can enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandole, cefoperazone, cefotetan), valproic acid. Increases the effectiveness of antihypertensive drugs, insulin and hypoglycemic drugs for oral administration.
Cimetidine increases the plasma concentration of pentoxifylline (risk of side effects).
Combined use with other xanthines can lead to excessive nervous excitement.
In some patients, concomitant use of pentoxifylline and theophylline may lead to an increase in theophylline concentration (risk of side effects associated with theophylline).

special instructions

Patients with severe renal impairment while taking VazonitЃ require particularly careful medical supervision. If during the period of use of the drug in patients there are hemorrhages in the retina of the eye, then the drug is immediately canceled.
Treatment should be carried out under the control of blood pressure. In patients with low and unstable blood pressure, the administered dose should be reduced.
In patients with diabetes mellitus taking hypoglycemic agents, use in large doses can cause hypoglycemia (dose adjustment is required). When used simultaneously with anticoagulants, it is necessary to monitor the indicators of the blood coagulation system, incl. international normalized ratio (MHO).
In patients who have undergone recent surgery, systematic monitoring of hemoglobin and hematocrit is necessary.
In the elderly, dose reduction (increased bioavailability and decreased elimination rate) may be required.
Smoking can reduce the therapeutic efficacy of the drug.

Impact on the ability to drive vehicles and machines

Due to the possible appearance of dizziness, caution is recommended when driving and when servicing complex mechanisms. While taking the drug, the use of alcoholic beverages is not recommended.

Release form

Sustained-release tablets, film-coated, 600 mg each. 10 tablets in PVC / Al blister.
2 blisters with instructions for use in a cardboard box.

Storage conditions

In a dry, dark place at a temperature not exceeding 25 ? C. Keep out of the reach of children.

Shelf life

5 years.
Do not use after the expiration date.

Conditions of dispensing from pharmacies

On prescription.