Пентоксифиллин-ФПО®

General characteristics. Structure:

Active ingredient: 100 mg of a pentoksifillin in 1 tablet.

Excipients: povidone (polyvinylpirrolidone low-molecular), lactose (sugar milk), silicon dioxide colloid (aerosil), potato starch, talc, magnesium stearate.

Excipients for a cover: methacrylic acid and ethyl acrylate copolymer (kollinut MAY 100 P), polyethyleneglycol 4 000 (macrogoal), titanium dioxide, acid red 2 C (an azoruby, E-122), polysorbate (twin 80), talc, a silicone emulsion.

Pharmacological properties:

Pharmacodynamics. Pentoksifillin improves microcirculation and rheological properties of blood, has vasodilating effect, blocks phosphodiesterase and promotes accumulation of cyclic adenosinemonophosphate in cells with simultaneous saturation of energy potential that in turn leads to a vazodilatation, decrease in the general peripheric resistance, increase of shock and minute volumes of blood without considerable change of heart rate.

Pentoksifillin slows down aggregation of thrombocytes and erythrocytes, increases their elasticity, reduces fibrinogen level in plasma and strengthens a fibrinolysis that reduces viscosity of blood and improves its rheological properties. Has weak myotropic, vasodilating effect. Expanding coronary arteries, increases delivery of oxygen to a myocardium (anti-anginal effect), expanding vessels of lungs - improves blood oxygenation.

In general, пентоксифиллин causes improvement of microcirculation and supply of fabrics with oxygen in a brain and in extremities, in a smaller measure – in kidneys.

Pharmacokinetics. After intake пентоксифиллин it is almost completely soaked up from digestive tract. Drug is exposed to "the first passing" through a liver with education of 2 main pharmacological of active metabolites: 1-5-hydroxyhexyl-3,7-dimethylxantine (metabolite of I) and 1-3-carboxypropyl-3,7-dimethylxantine (metabolite of V). Concentration of a metabolite of I and V in a blood plasma, respectively, in 5 and 8 times is higher, than a pentoksifillina. Time of achievement of the maximum concentration – 1 hour.

The elimination half-life – 0,5-1,5 hours Pentoksifillin is removed preferential by kidneys – 94% in the form of metabolites (preferential a metabolite of V), through intestines – 4%, in the first 4 hours are removed to 90% of a dose. It is allocated with breast milk. At a heavy renal failure removal of metabolites is slowed down. At an abnormal liver function lengthening of an elimination half-life and increase in bioavailability is noted.

Indications to use:

· The disturbances of peripheric circulation caused by atherosclerosis, a diabetes mellitus (a diabetic angiopatiya);

· Chronic disturbances of cerebral circulation of ischemic genesis;

· Atherosclerotic and distsirkulyatorny encephalopathies; angiopatiya (paresthesias, Raynaud's disease);

· Trophic disturbances of fabrics owing to disturbance of arterial or venous microcirculation (trophic ulcers, a posttromboflebichesky syndrome, freezing injuries, gangrene);

· Obliterating endarteritis;

· A subacute and chronic circulatory unefficiency in mesh and in an eye choroid;

· Hearing disorder of vascular genesis.

Route of administration and doses:

Пентоксифиллин-ФПО® accept inside after food, swallow entirely and wash down with a small amount of water.

Accept 200 mg (2 tablets) of 3 times a day. After achievement of therapeutic effect (as a rule, 1-2 weeks) the dose is reduced to 100 mg (1 tablet) by 3 times a day. The maximum daily dose – 1 200 mg. Course of treatment 1-3 months.

At patients with a chronic renal failure (clearance of creatinine less than 10 ml/min.) the dose is reduced twice.

Duration of treatment and the mode of dosing of a pentoksifillin is set by the doctor individually, depending on a clinical picture of a disease and the gained therapeutic effect.

Features of use:

Patients with the expressed renal failures at reception of Pentoksifillin-FPO® need especially careful medical observation. If during use of drug for patients there are eye retinal apoplexies, drug is immediately cancelled. Treatment should be carried out under control of arterial pressure. At the patients with a diabetes mellitus accepting hypoglycemic means, appointment in high doses can cause a hypoglycemia (dose adjustment is required). At appointment along with anticoagulants it is necessary to watch indicators of coagulant system of blood carefully.

At the patients who transferred recently an operative measure systematic control of concentration of hemoglobin and a hematocrit is necessary.

At elderly patients reduction of a dose (increase in bioavailability and reduction in the rate of removal) can be required.

Smoking can reduce a therapeutic effectiveness of drug.

The patient with labile arterial pressure, with tendency to arterial hypotension and with the expressed renal failures the dose is increased gradually and selected individually.

In case of a lactose intolerance or insufficiency of the corresponding enzyme it is necessary to consider that 1 tablet Pentoksifillin-FPO® contains 55 mg of lactose in the structure.

Side effects:

From a nervous system: headache, dizziness; uneasiness, sleep disorders; spasms; aseptic meningitis (seldom).

From integuments and a hypodermic fatty tissue: a dermahemia of the person, "inflows" of blood to face skin and an upper part of a thorax, hypostases, the increased fragility of nails.

From the alimentary system: dryness in a mouth, a loss of appetite, an intestines atony, nausea, vomiting, an exacerbation of cholecystitis, cholestatic hepatitis.

From sense bodys: vision disorder, scotoma.

From warmly vascular system: tachycardia, arrhythmia, cardialgia, progressing of stenocardia, lowering of arterial pressure.

From bodies of a hemopoiesis and system of a hemostasis: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; bleedings (including from mucous membranes of a stomach, intestines.

Allergic reactions: skin itch, dermahemia, small tortoiseshell, Quincke's disease, acute anaphylaxis.

Laboratory indicators: increase in activity of "hepatic" transaminases (ALT, nuclear heating plant, LDG) and alkaline phosphatase.

Interaction with other medicines:

Pentoksifillin strengthens effect of heparin, fibrinolitic means, theophylline, anti-hypertensive and hypoglycemic means (both insulin, and hypoglycemic means for intake).

Pentoksifillin can strengthen effect of the medicines influencing coagulant system of blood (indirect and direct anticoagulants, trombolitik), antibiotics (including cephalosporins – a tsefamandol, a tsefoperazon, a tsefotetan), valproic acid.

Cimetidinum increases concentration of a pentoksifillin in a blood plasma (risk of emergence of side effects).

Joint appointment with other xanthines can lead to excessive nervous excitement of patients.

Contraindications:

Hypersensitivity to a pentoksifillin and other derivatives of methylxanthine; acute myocardial infarction; massive bleeding; hemorrhagic stroke, eye retinal apoplexy; pregnancy; lactation period; age up to 18 years (efficiency and safety are not established).

With care drug is appointed at chronic heart failure, a liver and/or renal failure. It is also necessary to be careful at purpose of a pentoksifillin the patient with a peptic ulcer of a stomach and duodenum, to the patient who recently transferred an operative measure (risk of developing of bleedings).

Overdose:

Symptoms: weakness, dizziness, tachycardia, the expressed lowering of arterial pressure, an unconscious condition, drowsiness or excitement, a loss of consciousness, a hyperthermia, an areflexia, toniko-clonic spasms, symptoms of gastrointestinal bleeding (vomiting like "coffee thick").

Treatment: a gastric lavage with the subsequent intake of absorbent carbon, symptomatic therapy (including the measures directed to maintenance of breath and arterial pressure), urgent actions at bleeding.

Storage conditions:

List B. In the dry, protected from light place at a temperature of 25 °C. To store in the place, unavailable to children! A period of validity - 3 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

The tablets covered with a kishechnorastvorimy cover, 100 mg. On 10 or 20 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3 or 6 blister strip packagings with the application instruction in a pack from a cardboard.