Vazonite - instructions for use, dose, side effects, contraindications

One tablet of prolonged action, film-coated, contains: active substance: pentoxifylline 600 mg; Excipients: hypromellose 15000 cP - 104.0 mg, microcrystalline cellulose - 13.5 mg, crospovidone - 15.0 mg, silicon dioxide colloid - 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 tablets, covered with a film coating of white color, with a risk on both sides.The core of the tablet is white.

Pharmacotherapeutic group:Vasodilator

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

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 is associated with inhibition of phosphodiesterase and the accumulation of cyclic adenosine monophosphate (cAMP) in vascular smooth muscle cells and blood corpuscles elements. Pentoxifylline inhibits the aggregation of red blood cells and platelets reduces the level of fibrinogen in plasma and enhances fibrinolysis, thus reducing blood viscosity and improves its flow characteristics. Improves the supply of oxygen to tissues in areas of impaired blood circulation, in particular, in the limbs, the central nervous system, and, to a lesser extent, in the kidneys. With occlusive lesions of peripheral arteries ("intermittent" lameness) leads to an increase in walking distance,elimination of night cramps calf muscles, reducing pain at rest. When the cerebral circulation is disturbed, it improves the symptoms. Having a weak myotropic vasodilating effect, somewhat reduces the overall peripheral vascular resistance and slightly dilates the coronary vessels.

Pharmacokinetics:

After oral administration pentoxifylline almost completely absorbed from the gastrointestinal tract. The prolonged form provides continuous release 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. When administered to tablets of the Vasonitis, the maximum concentration of pentoxifylline and its active metabolites in blood plasma is reached after 3-4 hours and remains at the therapeutic level for about 12 hours. The drug is excreted primarily (94%) by the kidneys in the form of metabolites.Excreted in breast milk. With severe renal dysfunction, excretion of metabolites is slowed down. When liver function is disrupted, the half-life is prolonged and bioavailability is increased.

Indications:

- Violation of peripheral circulation against the background of atherosclerotic, diabetic and inflammatory processes (including "intermittent" lameness caused by atherosclerosis, diabetic angiopathy, obliterating endarteritis);

- Acute and chronic disorders of cerebral circulation of ischemic genesis;

- Symptomatic treatment of the consequences of cerebral circulation disorders of atherosclerotic origin (violation of concentration, dizziness, memory impairment);

- Atherosclerotic and dyscirculatory encephalopathy; Angiopathy (paresthesia, Raynaud's disease);

- Trophic tissue disorders due to the violation of arterial or venous microcirculation (trophic ulcers, postthrombophlebitic syndrome, frostbite, gangrene);

- Disturbances of blood circulation in the vessels of the eye (acute and chronic circulatory insufficiency in the mesh or in the choroid of the eye);

- Disorders of the function of the middle ear of vascular genesis, accompanied by deafness.

Contraindications:

- Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other components included in the formulation;

- Acute myocardial infarction;

- Massive bleeding;

- Hemorrhage in the retina of the eye;

- Acute hemorrhagic stroke;

- Pregnancy;

- Breastfeeding period;

- Age to 18 years (effectiveness and safety not established).

Carefully:

Atherosclerosis of cerebral and / or coronary vessels, especially in cases of arterial hypotension and violations rhythm of the heart; chronic heart failure, hepatic insufficiency, renal insufficiency (creatinine clearance less than 30 ml / min - risk of cumulation and an increased risk of side effects), peptic ulcer and duodenal ulcer, recent surgery (risk of bleeding), increased tendency to bleeding, for example, when using anticoagulants or when the blood coagulation system is violated (the risk of developing more severe bleeding).

Pregnancy and lactation:The use of the drug during pregnancy and during breast-feeding is contraindicated.

Dosing and Administration:

Tablets Vazonit ® should be taken orally, without chewing, squeezed with enough liquid, preferably after eating.

The drug is usually prescribed for 1 tablet 600 mg 2 times a day (morning and evening), the maximum daily dose of 1200 mg.

Duration of treatment and dosage regimen with the drug Vazonit® are determined 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.

Dose reduction, taking into account individual tolerance, is necessary in patients with severe impairment of liver function.

Treatment can be initiated in small doses in patients with low blood pressure, as well as in patients at risk because of possible lowering of blood pressure (patients with severe ischemic heart disease or hemodynamically significant stenoses of cerebral vessels). In these cases, the dose can be increased only gradually.

Side effects:

From the central nervous system: headache, dizziness, anxiety, sleep disorders, convulsions, there are cases of development of aseptic meningitis.

From the skin and subcutaneous fat: hyperemia of the skin of the face, "tides" of blood to the skin of the face and upper chest, swelling, increased brittleness of the nails.

From the digestive system: dry mouth, 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: impaired vision, scotoma.

From the side of the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina pectoris, lowering of arterial pressure.

On the part of the organs of hematopoiesis and the system of hemostasis: in rare cases canoznakatbleeding (from the mucous membranes, vessels of the skin, stomach, intestines), as well as thrombocytopenia, leukopenia, pancytopenia, hypophybrinogenemia, aplastic anemia. In this regard, when treating the drug Vazonit®, it is necessary to carry out regular monitoring of the pattern of peripheral blood

Allergic reactions: skin itching, skin hyperemia, 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 convulsions, signs of gastrointestinal bleeding ("coffee grounds" vomiting).

Treatment: gastric lavage followed by ingestion of activated charcoal. In the case of vomiting with traces of blood, gastric lavage is unacceptable. Further treatment symptomatic, aimed at maintaining the function of breathing and blood pressure. With convulsions - diazepam.

Interaction:

Pentoxifylline can enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandole, cefoperazone, cefotetana), 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).

Joint application with other xanthines can lead to excessive nervous excitation.

In some patients, simultaneous use of pentoxifylline and theophylline may lead to an increase in theophylline concentration (risk of theophylline side effects).

Special instructions:

Patients with severe renal dysfunction during the admission of Vasonit® need particularly careful medical supervision. In the event that during the period of application of the drug the patients have hemorrhages in the retina of the eye, the drug is immediately canceled.

Treatment should be carried out under the control of arterial pressure. In patients with low and unstable arterial pressure, the dose to be administered 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 parameters of the blood coagulation system, incl. international normalized attitude (INR).

In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit is necessary.

In elderly people, a dose reduction may be required (increased bioavailability and reduced rate of excretion).

Smoking can reduce the therapeutic effectiveness of the drug.

Effect on the ability to drive transp. cf. and fur:

Due to the possible appearance of dizziness, it is recommended to use caution when driving vehicles and when servicing complex mechanisms. During the intake of the drug is not recommended the use of alcoholic beverages.

Form release / dosage:

Tablets of prolonged action, film-coated, for 600 mg.

For 10 tablets in PVC / Al blister.

2 blisters together with instructions for use in a cardboard box.

Packaging:(10) - blisters (2) - packs cardboard

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N013693 / 01

Date of registration:05.07.2010 / 23.08.2013

Expiration Date:Unlimited

The owner of the registration certificate:VALEANT, LLC VALEANT, LLC Russia

Manufacturer: & nbsp

G.L.PHARMA, GmbH Austria

Representation: & nbspVALEANT LLC VALEANT LLC Russia

Information update date: & nbsp11.01.2017

Illustrated instructions

Instructions

Vazonite® (Vasonit®)