Composition, form of production and packaging
Tablets of prolonged action, covered with a film coating of white color, oblong, biconcave, with risk from both sides.
pentoxifylline 600 mg
Excipients: hypromellose 15000 cP - 104 mg, microcrystalline cellulose - 13.5 mg, crospovidone - 15 mg, silicon dioxide colloid - 3 mg, magnesium stearate - 4.5 mg.
The composition of the shell: macrogol 6000 - 3.943 mg, talc - 11.842 mg, titanium dioxide - 3.943 mg, hypromellose 5 cp - 3.286 mg, polyacrylic acid (as a 30% dispersion) - 0.986 mg.
10 pieces. - blisters (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
The xanthine derivative. Improves microcirculation in areas of impaired blood flow. Improves the rheological properties of blood (fluidity) due to the impact on the pathologically changed erythrocyte deformability, increases the elasticity of erythrocyte membranes, inhibits the aggregation of erythrocytes and platelets and reduces the increased viscosity of the blood. The mechanism of action of the drug is associated with the inhibition of phosphodiesterase and the accumulation of cAMP in the cells of the smooth muscles of the vessels and in the blood elements. Pentoxifylline inhibits the aggregation of platelets and erythrocytes, reduces the level of fibrinogen in the blood plasma and strengthens fibrinolysis, which leads to a decrease in blood viscosity and improvement of its rheological properties. Improves the supply of oxygen to tissues in areas of the circulatory system (including the extremities, the central nervous system, and to a lesser extent - in the kidneys). In the occlusive lesion of peripheral arteries (intermittent claudication) leads to an increase in walking distance, elimination of night cramps of gastrocnemius muscles, and reduction of pain at rest. When the cerebral circulation is disturbed, it improves the symptoms. Has a weak myotropic vasodilating effect, somewhat reduces the OPSS and slightly dilates the coronary vessels.
Absorption and Metabolism
When taking pills, pentoxifylline is almost completely absorbed from the digestive tract. The prolonged form ensures continuous release of the active substance and its uniform absorption.
Pentoxifylline is metabolized in the liver at 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 the plasma, respectively, is 5 and 8 times higher than that of pentoxifylline.
C max of pentoxifylline and its active metabolites is achieved after 3-4 hours and remains at the therapeutic level for about 12 hours.
The drug is excreted mainly (94%) by the kidneys in the form of metabolites. Excreted in breast milk.
Pharmacokinetics in special clinical cases
With severe renal dysfunction, excretion of metabolites is slowed down.
If liver function is impaired, lengthening T 1/2 and increasing bioavailability are noted.
- violations of peripheral circulation against atherosclerotic, diabetic and inflammatory processes (including intermittent claudication caused by atherosclerosis, obliterating endarteritis, diabetic angiopathy);
- acute and chronic disorders of cerebral circulation of ischemic genesis;
- symptomatic treatment of the consequences of cerebrovascular accident of atherosclerotic origin (attention deficit disorder, dizziness, memory impairment);
- Atherosclerotic and discirculatory encephalopathy, angioedema (paresthesia, Raynaud's disease);
- trophic tissue disorders due to violation of arterial or venous microcirculation (postthrombophlebitic syndrome, trophic ulcers, gangrene, frostbites);
- impaired blood circulation of the eye (acute and chronic circulatory insufficiency in the mesh or choroid of the eye);
- Dysfunction of the middle ear of vascular genesis, accompanied by deafness.
The drug is usually prescribed to 1 tab. (600 mg) 2 times / day (morning and evening). The maximum dose is 1.2 g.
Duration of treatment and dosing regimen is set by the doctor individually depending on the clinical picture of the disease and the therapeutic effect obtained.
Tablets should be taken orally, without chewing and drinking with a sufficient amount of liquid, preferably after eating.
In patients with chronic renal failure (CC less than 30 ml / min), the daily dose is reduced to 600 mg.
In patients with severe impairment of liver function, a dose reduction with regard to individual tolerability is necessary.
In patients with low blood pressure, as well as in patients at risk for possible reduction in blood pressure (patients with severe coronary artery disease or with hemodynamically significant stenoses of the cerebral vessels), treatment can be initiated in small doses. In these cases, the dose can be increased only gradually.
From the side of the central nervous system: headache, dizziness, anxiety, sleep disturbances, convulsions, there were cases of development of aseptic meningitis.
From the skin and subcutaneous fat: hyperemia of the skin of the face, flushes of blood to the skin of the face and upper chest, swelling, increased brittleness of the nails.
On the part of the digestive system: nausea, vomiting, diarrhea, dry mouth, feeling of pressure and overflow in the stomach, decreased appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis, epigastric pain, increased activity of liver enzymes (ALT, AST, LDH) and AF.
From the side of the organ of vision: scotoma, visual impairment.
From the cardiovascular system: a decrease in blood pressure, tachycardia, the progression of angina pectoris, arrhythmia, cardialgia.
Allergic reactions: skin itching, skin hyperemia, urticaria, angioedema angioedema, anaphylactic shock.
From the hemopoietic system and hemostasis: rarely - bleeding (from the vessels of the stomach, intestines, skin and mucous membranes), thrombocytopenia, leukopenia, pancytopenia, hypophybrinogenemia, aplastic anemia. In this regard, it is necessary to carry out regular monitoring of the picture of peripheral blood.
acute myocardial infarction;
- massive bleeding;
- acute hemorrhagic stroke;
- hemorrhage in the retina of the eye;
- the period of lactation (breastfeeding);
- age under 18 years (effectiveness and safety not established);
- hypersensitivity to the components of the drug;
- Hypersensitivity to other methylxanthine derivatives.
Caution should be given to the preparation for atherosclerosis of cerebral and / or coronary vessels, arterial hypotension, cardiac arrhythmia, chronic heart failure, liver failure, renal insufficiency (CC less than 30 ml / min - risk of cumulation and an increased risk of side effects), peptic ulcer disease stomach and duodenal ulcers, condition after recently transferred surgical interventions (risk of bleeding), increased tendency to bleeding, for example, with ant coagulants, or in violation of blood coagulation (risk of more severe bleeding).
PREGNANCY AND LACTATION
The use of the drug Vazonit В® during pregnancy and during breastfeeding is contraindicated.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be exercised when prescribing Vazonitis for renal dysfunction (KC less than 30 ml / min - risk of cumulation and an increased risk of side effects).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug for liver failure, renal failure (QC less than 30 ml / min - the risk of cumulation and an increased risk of side effects).
APPLICATION FOR CHILDREN
Contraindicated: age under 18 years (efficacy and safety not established).
APPLICATION IN ELDERLY PATIENTS
Older patients may need a dose reduction (increased bioavailability and reduced elimination rate).
Patients with severe renal impairment in the treatment of Vasonitis should be under close medical supervision. In case of a hemorrhage in the retina of the eye during treatment with Vasonitis, the drug should be immediately discontinued.
Treatment should be carried out under the control of blood pressure. In patients with a low and unstable blood pressure, the dose should be reduced.
In patients with diabetes mellitus, who take hypoglycemic drugs, the use of vasonitis in large doses can cause the development of hypoglycemia (dose adjustment is required).
In case of simultaneous application of Vasonitis and anticoagulants, it is necessary to monitor the parameters of the blood coagulation system (including MNO).
For patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit is necessary.
Older patients may need a dose reduction (increased bioavailability and reduced elimination rate).
Smoking can reduce the therapeutic effectiveness of the drug.
During the intake of the drug is not recommended the use of alcoholic beverages.
Impact on the ability to drive vehicles and manage mechanisms
Due to the possible appearance of dizziness, it is recommended to use caution when driving vehicles and servicing complex mechanisms.
Symptoms: weakness, dizziness, marked decrease in blood pressure, tachycardia, drowsiness, redness of the skin, loss of consciousness, fever, chills, tonic-clonic seizures, "coffee grounds" vomiting (as a sign of gastrointestinal bleeding) .
Treatment: gastric lavage followed by activated charcoal. In the case of vomiting with traces of blood, gastric lavage is unacceptable. In the future, symptomatic therapy aimed at maintaining the function of respiration and blood pressure is carried out. When cramps are prescribed diazepam.
Pentoxifylline may enhance the effect of drugs affecting the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandole, cefotetan, cefoperazone), valproic acid.
Increases the effectiveness of antihypertensive drugs, insulin and hypoglycemic agents for oral administration.
Cimetidine increases the concentration of pentoxifylline in the blood plasma (risk of side effects).
Co-administration with other xanthines can lead to excessive nervous excitement of patients.
In some patients, simultaneous use of pentoxifylline and theophylline may lead to an increase in theophylline concentration (risk of theophylline side effects).
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 5 years.