pharmachologic effect
Pharmacological action - angioprotective, antiaggregation, vasodilator.
Improves microcirculation and rheological properties of blood. Inhibits phosphodiesterase, promoting the accumulation of cAMP in tissues and organs, incl. in the cells of smooth muscle of blood vessels, in the formed elements of blood. Inhibits the aggregation of platelets and erythrocytes, increases the elasticity of their membranes, reduces the concentration of fibrinogen in plasma and enhances fibrinolysis. Improves oxygen supply to tissues, most notably in the extremities, central nervous system and, to a lesser extent, in the kidneys. Slightly dilates coronary vessels.
Vazonite
Vazonit (active ingredient - pentoxifylline) is a drug that improves microcirculation, a vasodilator and an angioprotector all in one. Some readers may think that this is ordinary pentoxifylline. But it's not that simple. Pentoxifylline has been used in the treatment of patients with peripheral vascular diseases since the early 70s of the last century. At first, the drug was used at a dose of 300 - 400 mg per day. By increasing the daily dose to 1200 mg, clinicians were able to significantly increase its effectiveness. For this reason, long-acting dosage forms of pentoxifylline have gained clear promise in the eyes of specialists. Vazonit from the Austrian pharmaceutical company is one of these drugs, encased in a “retard” matrix, which provides for the gradual release of the active substance. The mechanism of action of vasonite is due to the suppression of the activity of the phosphodiesterase enzyme and the accumulation of cyclic AMP in vascular smooth muscle cells, red blood cells, platelets and leukocytes. The drug improves blood rheology (we are talking, first of all, about fluidity), reduces its viscosity (thinning effect), increases the elasticity of erythrocyte membranes, and inhibits the process of aggregation (sticking together) of erythrocytes and platelets. Vasonite facilitates the delivery of oxygen to tissues with poor circulation (for example, to the limbs or central nervous system). In patients suffering from intermittent claudication, taking the drug increases walking distance, prevents the development of night cramps in the lower leg muscles, and reduces pain at rest. In case of impaired cerebral circulation, vasonite relieves pathological symptoms (weakened memory and attention, dizziness). It has a mild myotropic vasodilator effect, reduces total peripheral vascular resistance to a certain extent and slightly increases the lumen of the blood vessels surrounding the heart.
Vazonit is available in tablets. According to general recommendations, the drug is prescribed 600 mg (1 tablet) 2 times a day, optimally in the morning and evening. The maximum daily dose should not exceed 2 tablets. The duration of pharmacotherapy and dosage regimen are determined by the doctor personally for each patient, depending on the severity of the disease and the observed therapeutic effect. The tablets are best taken after meals with water. Patients suffering from chronic renal failure are limited to a maximum daily dose of 600 mg. Such persons must be under constant medical supervision throughout the entire medication course. If retinal hemorrhage occurs, the drug should be discontinued. Pharmacotherapy with vasonite should be carried out against the background of regular monitoring of blood pressure. In patients with low and/or unstable blood pressure, the dose of the drug should be reduced. In diabetic patients taking antihyperglycemic drugs, the use of Vasonit in high doses can provoke hypoglycemia (in such cases, the dose must be adjusted). If vasonite is used simultaneously with drugs that prevent blood clotting, it is necessary to monitor coagulation parameters. In elderly patients, due to increased bioavailability of the drug and inhibition of the rate of its elimination from the body, a dose adjustment may be required downward. Smokers experience a decrease in the effectiveness of the drug. Another “generator” of human vices—alcohol—must be completely excluded during treatment with vasonite.
Indications of the drug Vazonit®
Peripheral circulation disorders (obliterating endarteritis, diabetic angiopathy, Raynaud's disease).
Ischemic cerebrovascular accidents (ischemic cerebral stroke).
Atherosclerotic and discirculatory encephalopathy, angioneuropathy.
Trophic changes in tissue due to impaired arterial or venous microcirculation (postthrombophlebitic syndrome, varicose veins, trophic ulcers, gangrene, frostbite).
Circulatory disorders of the eye (acute, subacute and chronic circulatory failure in the retina or choroid).
Hearing impairment of vascular origin, accompanied by hearing loss.
Vazonit 600 mg No. 20 tablet p.p.o.retard
Instructions for medical use of the drug Vazonit® retard Trade name Vazonit® retard International nonproprietary name Pentoxifylline Dosage form Film-coated tablets 600 mg Composition One tablet contains the active substance - pentoxifylline 600 mg, excipients: hypromellose, crospovidone, microcrystalline cellulose, colloidal dioxide anhydrous silicon, magnesium stearate, macrogol 6000, talc, titanium dioxide, polyacrylate dispersion. Description Oblong-shaped tablets, white film-coated, with a dividing line on both sides Pharmacotherapeutic group Peripheral vasodilators ATC code C04AD03 Pharmacological properties Pharmacokinetics Taking Vasonit retard tablets orally ensures 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 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 in the urine in the form of metabolites. Pharmacodynamics Vasonit improves microcirculation and rheological properties of blood, and has a vasodilating effect. The active substance contains pentoxifylline, a xanthine derivative. The mechanism of action is associated with inhibition of phosphodiesterase and accumulation of cAMP in vascular smooth muscle cells, blood cells, and other tissues and organs. Pentoxifylline inhibits the aggregation of platelets and erythrocytes, increases their elasticity, reduces the level of fibrinogen in the 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, and, to a lesser extent, in the kidneys, and also reduces the phenomena of cerebral hypoxia. Slightly dilates coronary vessels. Indications for use - peripheral circulatory disorders (obliterating endarteritis, diabetic angiopathy, Raynaud's disease) - ischemic cerebral circulation disorders (ischemic cerebral stroke) - atherosclerotic and dyscirculatory encephalopathy, angioneuropathy - trophic tissue changes due to impaired arterial or venous microcirculation (postthrombophlebitic syndrome, varicose veins) new varicose veins, trophic ulcers, gangrene, frostbite) - circulatory disorders of the eye (acute, subacute and chronic circulatory failure in the retina or choroid) - hearing impairment of vascular origin, accompanied by hearing loss. Method of administration and dosage The duration of treatment and dosage regimen are set by the doctor individually, depending on the clinical picture of the disease and the resulting therapeutic effect. The average duration of treatment is 2-3 weeks. Vazonit retard tablets should be taken orally after meals, without chewing and with a sufficient amount of liquid. The drug is usually prescribed 1 tablet 2 times a day (morning and evening). Side effects - nausea, loss of appetite, vomiting, diarrhea, feeling of fullness in the abdomen and epigastric pain - headache, dizziness, anxiety, sleep disturbances - decreased blood pressure, tachycardia, angina pectoris, heart rhythm disturbances, facial flushing when using high doses - itching, skin rash, urticaria, angioedema, rarely: anaphylactic shock. - in rare cases: bleeding (in the gastrointestinal tract, in the skin, in the mucous membranes), as well as thrombocytopenia, aplastic anemia - visual disturbances, scotoma, convulsions. Contraindications - acute myocardial infarction - massive bleeding - acute hemorrhagic stroke - retinal hemorrhage - increased sensitivity to pentoxifylline and other methylxanthine derivatives (caffeine, theophylline, theobromine) - pregnancy and lactation - children under 18 years of age Drug interactions Pentoxifylline enhances the effect of antihypertensive drugs agents, anticoagulants, insulin, oral hypoglycemic drugs. Special instructions Caution should be exercised when prescribing Vasonit to patients with severe arterial hypotension, with a tendency to orthostatic hypotension, with severe coronary sclerosis and cerebral atherosclerosis with arterial hypertension, patients with heart failure, cardiac arrhythmias, with ulcerative lesions of the gastrointestinal tract, patients who have had surgical intervention (risk of bleeding), in case of impaired renal function. Regular monitoring of blood pressure levels and blood patterns is recommended. Pregnancy and lactation If it is necessary to use the drug during lactation, breastfeeding should be stopped. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms Considering the side effects of the drug, care must be taken when driving vehicles. Overdose Symptoms: nausea, dizziness, decreased blood pressure, increased body temperature (chills), loss of consciousness, possible tonic-clonic convulsions, vomiting “coffee grounds,” arrhythmias, areflexia. Treatment: gastric lavage, symptomatic therapy, no specific antidote. Release form and packaging Retard tablets, film-coated, 600 mg, 20 pieces per package, along with instructions for use. Storage conditions Store at a temperature not exceeding 250C, in a dry place, protected from light. Store out of the reach of children! Shelf life: 60 months Do not use the drug after the expiration date. Conditions for dispensing from pharmacies By prescription, Lannach, Austria
Side effects
Gastrointestinal tract: possible nausea, loss of appetite, vomiting, diarrhea, feeling of fullness in the abdomen and epigastric pain.
CNS: rarely - headache, dizziness, anxiety, sleep disturbance.
Cardiovascular system: when using high doses - decreased blood pressure, tachycardia, angina pectoris, cardiac arrhythmia, facial flushing.
Allergic reactions: possible - itching, skin rash, urticaria, Quincke's edema; rarely - anaphylactic shock.
Hematopoietic system and blood coagulation system: rarely - bleeding (in the gastrointestinal tract, skin, mucous membranes), thrombocytopenia, aplastic anemia.
Precautionary measures
Caution should be exercised when prescribing to patients with severe arterial hypotension, with a tendency to orthostatic hypotension, with severe coronary sclerosis and cerebral atherosclerosis with arterial hypertension, with heart failure, cardiac arrhythmias, with ulcerative lesions of the gastrointestinal tract, with impaired renal function; patients who have undergone surgery (risk of bleeding).
Regular monitoring of blood pressure levels and blood patterns is recommended.
