Instructions for Vasonit
Dosage form Vasonit:
Oblong biconvex tablets, film-coated white, with a risk on both sides. The core of the tablet is white. Vasonit
Composition Vasonit:
One sustained-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 (as a 30% dispersion) - 0.986 mg. Vasonit
Pharmacodynamics Vasonit:
Xanthine derivative. Improves microcirculation in areas of impaired blood supply. It improves the rheological properties of blood (fluidity) due to the effect on the pathologically altered deformability of red blood cells, increases the elasticity of erythrocyte membranes, inhibits the aggregation of red blood cells and platelets and reduces the increased viscosity of blood. Vasonit
The mechanism of action is associated with inhibition of phosphodiesterase and the accumulation of cyclic adenosine monophosphate (cAMP) in the smooth muscle cells of blood vessels and in the formed elements of the blood.Vasonit
Pentoxifylline inhibits the aggregation of red blood cells and platelets, reduces the level of fibrinogen in the blood plasma and enhances fibrinolysis, which reduces the viscosity of the blood and improves its rheological properties.
It improves the supply of oxygen to tissues in areas of impaired circulation, in particular in the limbs, central nervous system, and, to a lesser extent, in the kidneys. In case of occlusive lesion of the peripheral arteries ("intermittent" claudication), it leads to an increase in walking distance, elimination of night cramps of the calf muscles, and reduction of pain at rest.
With a violation of cerebral circulation improves symptoms. Having a weak myotropic vasodilating effect, it slightly reduces the total peripheral vascular resistance and slightly dilates the coronary vessels.
Pharmacokinetics Vasonit:
After oral administration, pentoxifylline is almost completely absorbed from the gastrointestinal tract. A prolonged form provides continuous release and uniform absorption. Pentoxifylline (Vasonit) undergoes metabolism 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 pentoxifylline.
When oral administration of Wazonit tablets, the maximum concentration of pentoxifylline and its active metabolites in the blood plasma is reached after 3-4 hours and remains at the therapeutic level for about 12 hours. The drug Vasonit is excreted mainly (94%) by the kidneys as metabolites. Excreted in breast milk.
In severe renal impairment, excretion of metabolites is slowed down. In case of impaired liver function, an elimination half-life and increased bioavailability are noted.
Side effects Vasonit:
From the central nervous system: headache, dizziness, anxiety, sleep disturbances, cramps, there are cases of the development of aseptic meningitis.
On the part of the skin and subcutaneous fat: hyperemia of the skin, "flushing" of blood to the skin of the face and upper chest, swelling, increased fragility of the nails. From the digestive system: dry mouth, a feeling of pressure and overflow 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 cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina pectoris, lowering blood pressure. Vasonit
Hematopoietic organs and hemostasis: in rare cases, bleeding (from mucous membranes, blood vessels of the skin, stomach, intestines), as well as thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia, aplastic anemia can occur. In this regard, in the treatment with Wazonit®, it is necessary to regularly monitor the picture of peripheral blood
Allergic reactions: skin itching, flushing of the skin, urticaria, angioedema, anaphylactic shock. Laboratory indicators: increased activity of hepatic transaminases: alanine aminotransferase (ALT), aspartate aminotransferase (ACT), as well as lactate dehydrogenase (LDH) and alkaline phosphatase. Vasonit
Special conditions Vasonit:
Patients with severe renal impairment when taking Wazonit® need especially careful medical supervision. If during the period of use of the drug in patients there are hemorrhages in the retina of the eye, the drug Vasonit 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 taking hypoglycemic agents, the use in large doses can cause hypoglycemia (dose adjustment is required). Vasonit
When used simultaneously with anticoagulants, it is necessary to monitor the indicators of the blood coagulation system, including international normalized ratio (INR). In patients undergoing recent surgery, a systematic monitoring of hemoglobin and hematocrit is necessary. In older people, a dose reduction (increased bioavailability and decreased excretion rate) may be required.
Smoking can reduce the therapeutic effectiveness of the drug. The effect of the drug on the ability to drive vehicles and mechanisms: Due to the possible appearance of dizziness, caution is advised when driving vehicles and when servicing complex mechanisms. The use of alcohol is not recommended while taking the drug.
Indications Vasonit:
- Violation of peripheral circulation against the background of atherosclerotic, diabetic and inflammatory processes (including with "intermittent" lameness due to atherosclerosis, diabetic angiopathy, obliterating endarteritis);
- Acute and chronic cerebrovascular disorders of ischemic origin;
- Symptomatic treatment of the consequences of cerebrovascular accident of atherosclerotic origin (impaired attention, dizziness, memory impairment);
- Atherosclerotic and dyscirculatory encephalopathy; angiopathy (paresthesia, Raynaud's disease);
- Trophic tissue disorders due to violations of arterial or venous microcirculation (trophic ulcers, post-thrombophlebitis syndrome, frostbite, gangrene);
- Circulatory disorders in the vessels of the eye (acute and chronic circulatory failure in the retina or choroid of the eye);
- Disorders of the middle ear function of vascular origin, accompanied by hearing loss. Vasonit
Contraindications Vasonit:
- Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other components that make up the drug Vasonit
Acute myocardial infarction
Massive bleeding
Retinal hemorrhage
Acute hemorrhagic stroke
Pregnancy
The period of breastfeeding;
- Age up to 18 years (efficacy and safety not established). With caution: 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. - the risk of cumulation and an increased risk of side effects), peptic ulcer of the stomach and duodenum, recent surgery (risk of bleeding), increased tendency to bleeding , for example, with the use of anticoagulants or in violation of the blood coagulation system (risk of more severe bleeding).
Pregnancy and lactation: The use of the drug Vasonit during pregnancy and during lactation is contraindicated.
Drug Interactions Vasonit:
Pentoxifylline (Vasonit) can enhance the effect of drugs Vasonit that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandol, cefoperazone, cefotetan), valproic acid.
Increases the effectiveness of antihypertensive drugs, insulin and hypoglycemic agents for oral administration. Cimetidine increases the concentration of pentoxifylline in blood plasma (risk of side effects).
Joint use with other xanthines can lead to excessive nervous excitement. In some patients, the simultaneous use of pentoxifylline and theophylline can lead to an increase in theophylline concentration (the risk of side effects associated with theophylline). Vasonit
Dosage Vasonit:
Vasonit ® tablets should be taken orally, without chewing, with a sufficient amount of liquid, preferably after a meal.
The drug is usually prescribed 1 tablet 600 mg 2 times a day (morning and evening), the maximum daily dose of 1200 mg. The duration of treatment and the dosage regimen of the drug Vasonit® are set by the doctor individually, depending on the clinical picture of the disease and the resulting therapeutic effect.
In patients with chronic renal failure (creatinine clearance less than 30 ml / min), the daily dose is reduced to 600 mg. Dose reduction, taking into account individual tolerance, is necessary in patients with severe hepatic impairment. Vasonit
Treatment can be started in small 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 heart disease or with hemodynamically significant stenosis of cerebral vessels). In these cases, the dose can be increased only gradually.
Overdose Vasonit:
Symptoms Vasonit: 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 such as "coffee grounds").
Treatment: gastric lavage followed by ingestion of activated charcoal. In case of vomiting with traces of blood, gastric lavage is unacceptable. Further symptomatic treatment aimed at maintaining respiratory function and blood pressure. With convulsions - diazepam. Vasonit
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