Latren solution for inf. 0.5mg/ml quarrystone. 200 ml

Pharmacological properties

Pharmacodynamics. pentoksifillin — derivative methylxanthine. the mechanism of action of a pentoksifillin is connected with oppression fde and accumulation 3.5-amf in cells of unstriated muscles of vessels, blood cells and also in other fabrics and bodies. pentoksifillin slows down aggregation of thrombocytes and erythrocytes, increases their flexibility, reduces the increased concentration of fibrinogen in blood plasma and strengthens a fibrinolysis that reduces viscosity of blood and improves its rheological properties. besides, pentoksifillin has weak myotropic vasodilating effect, reduces the general peripheric vascular resistance a little and shows positive inotropic effect. owing to use of a pentoksifillin the microcirculation and supply of fabrics with oxygen, most of all improve — in extremities, central nervous system, it is moderate — in kidneys. medicament slightly expands coronary vessels.

Pharmacokinetics. The active metabolite main pharmacological 1-(5 hydroxyhexyl) - 3.7 dimethylxantine (metabolite of I) is defined in blood plasma in the concentration twice exceeding those of not changed substance and is with it in a condition of the return biochemical balance. In this regard pentoksifillin and its metabolite it is necessary to consider as active whole. T _½ pentoksifillina makes 1.6 h

Pentoksifillin is metabolized completely, 90% are allocated with kidneys in the form of not conjugated water-soluble polar metabolites. 4% of the entered dose are removed with a stake. At patients with heavy renal failures the excretion of metabolites is slowed down. At patients with an abnormal liver function the lengthening of T _½ a pentoksifillin is noted.

Indication

Atherosclerotic encephalopathy; ischemic cerebral stroke; distsirkulyatorny encephalopathy; the disturbances of peripheric circulation caused by atherosclerosis, diabetes (including a diabetic angiopatiya), inflammation; the trophic disturbances in fabrics connected with damage of veins or disturbance of microcirculation (posttromboflebitichesky syndrome, trophic ulcers, gangrene, freezing injury); obliterating endarteritis; angioneyropatiya (Raynaud's disease); disturbance of blood circulation of an eye (an acute, subacute, chronic circulatory unefficiency in a retina and a choroid of an eye); dysfunction of an inner ear of vascular genesis which is followed by decrease in hearing.

Use

In/in infusion are the most effective way of parenteral administration of medicament which are better transferred. the mode of dosing is defined by the doctor and depends on severity of circulator disturbances, body weight and shipping of treatment. infusion can be carried out only if solution transparent.

Adult recommend such schemes of treatment:

1. In/in infusion of 100-600 mg of a pentoksifillin 1–2 times a day. Duration in in drop infusion is 60–360 min., that is introduction of 100 mg of a pentoksifillin has to last at least 60 min.;

2. At serious condition of the patient (especially in constant pain, gangrene or trophic ulcers) performing infusion of a pentoksifillin for 24 h is possible. At such scheme of introduction the dose is defined at the rate of 0.6 mg/kg/h. The daily dose calculated thus for the patient with the body weight of 70 kg makes 1000 mg, for the patient with the body weight of 80 kg — 1150 mg. Irrespective of the body weight of the patient the maximum daily dose makes 1200 mg. The volume of infusional solution is calculated individually taking into account associated diseases, a condition of the patient and averages 1-1.5 l/days

Duration of a parenteral course of treatment is defined by the doctor who carries out treatment.

Contraindication

Hypersensitivity to components of medicament and derivatives of xanthine. acute myocardial infarction. porphyria. massive bleedings at the time of prescribing of medicament or its appointments diagnosed the day before. hemorrhagic diathesis, extensive retinal apoplexies of an eye (it is necessary to stop immediately medicament use). arrhythmia, heavy atherosclerosis of coronary or brain vessels, uncontrollable arterial hypotension. liver and/or renal failure. stomach ulcer and/or intestinal ulcers. cerebral hemorrhage (risk of strengthening of bleeding).

Side effects

Laboratory indicators: increase in level of transaminases, increase in level shchf.

from heart: arrhythmia, tachycardia, stenocardia, a cardialgia, fluctuation of the ABP, feeling of compression behind a breast.

from the haematogenic and lymphatic system: thrombocytopenia with a Werlhof's disease and aplastic anemia (partial or complete cessation of formation of all blood cells, a pancytopenia) that the lethal outcome, a hypofibrinogenemia can cause.

from nervous system: dizziness, headache, aseptic meningitis, tremor, paresthesia, spasms.

from skin and hypodermic fabrics: an itching, erubescence and urticaria, a toxic epidermal necrolysis and Stephens's syndrome — Johnson, the increased fragility of nails.

from vessels: feeling of heat (inflows), bleedings, peripheral hypostasis.

from the immune system: anaphylactic reactions, anaphylactoid reactions, Quincke's disease, bronchospasm and acute anaphylaxis.

from the system of digestion: nausea, vomiting, anorexia, intestines atony, exacerbation of cholecystitis, cholestatic hepatitis.

from a liver and biliary tract: intra hepatic cholestasia.

Mental disturbances: excitement and sleep disorder, hallucinations, uneasiness, sleep disorder.

from an organ of sight: disorder of vision, conjunctivitis, retinal apoplexies, peeling of a retina, scotoma.

Others: it was reported about cases of emergence of a hypoglycemia, the increased sweating, fervescences, a fever.

Special instructions

At the first signs of development of anaphylactic/anaphylactoid reaction should stop immediately infusion and to ask for the help the doctor. in case of use of medicament for patients with chronic heart failure it is previously necessary to reach a blood circulation compensation phase.

(see INTERACTIONS). In these cases it is necessary to lower a dose of insulin or oral anti-diabetic means and to watch especially carefully a condition of the patient. Patients with a system lupus erythematosus or other diseases of connective tissue pentoksifillin can appoint only after the thorough analysis of possible risks and advantage. As during treatment pentoksifilliny there is a risk of developing aplastic anemia, regular control of the general blood test is necessary. At patients with a renal failure (clearance of creatinine of 30 ml/min.) or heavy dysfunction of a liver the removal of a pentoksifillin can be slowed down. Appropriate monitoring is necessary.

needs Especially attentive observation for patients with:

• heavy cardiac arrhythmia;
• myocardial infarction;
• arterial hypotension;
• profound atherosclerosis of cerebral and coronary vessels, especially at the accompanying AG and disturbances of a warm rhythm. At these patients at administration of medicament attacks of stenocardia, arrhythmia and AG are possible;
• renal failure (clearance of creatinine of 30 ml/min.);
• heavy liver failure;
• high tendency to bleedings caused, for example, by treatment by anticoagulants or disturbances of fibrillation. Concerning bleedings see. CONTRAINDICATIONS;
• patients for which decrease in the ABP causes high risk (for example patients with a heavy ischemic heart disease or a stenosis of vessels, krovosnabzhayushchy a brain);
• patients who at the same time receive treatment pentoksifilliny and antivitamins K (see INTERACTIONS);
• patients who at the same time receive treatment pentoksifilliny and antidiabetic means (see INTERACTIONS).

Use during pregnancy and feeding by a breast contraindicated.

Children. There is no experience of use of medicament for children.

Ability to influence speed of response at control of vehicles or work with other mechanisms. As medicament is used in the conditions of a hospital, there are no data on such influence.

Interaction

Effect of decrease in level of glucose in blood, inherent in insulin or oral antidiabetic means, can amplify. therefore patients who receive medicament treatment in diabetes have to be under careful observation.

During the post-marketing period it was reported about cases of increase in anticoagulating activity at the patients who were at the same time receiving treatment pentoksifilliny and antivitamins K. When dosing of a pentoksifillin is appointed or changes, it is recommended to carry out control of anticoagulating activity at this group of patients. Pentoksifillin can strengthen hypotensive effect of antihypertensive medicaments and other medicaments which can cause decrease in the ABP.

to increase in level of theophylline in blood. Therefore increase in frequency and increase in expressiveness of side reactions of theophylline is possible.

Incompatibility. Drug should not be mixed with other medicines in one capacity.

Overdose

Symptoms: weakness, dizziness, decrease hell, unconscious state, tachycardia, drowsiness or excitement, loss of consciousness, hyperthermia, areflexia, spasms, gastrointestinal bleedings, nausea, inflows.

Treatment: symptomatic. Holding special urgent events for prevention of bleeding can be required.

to Store

at a temperature not above 25 °C. not to freeze.