Трентал® 400

General characteristics. Structure:

Active agent: пентоксифиллин - 400,00 mg.
Excipients: povidone (polyvinylpirrolidone), gietelloza (hydroxyethylcellulose), talc, magnesium stearate.
Structure of a cover: gipromelloz (gidroksipropilmetiltsellyuloz), benzyl alcohol, titanium dioxide, talc, macrogoal (polyethyleneglycol) 6000.

Description. Oblong biconvex tablets, film coated white color. On the one hand tablets engraving of "ATA".

Pharmacological properties:

Pharmacodynamics. Трентал® 400 improves rheological properties of blood (flowability) due to influence on patholologically the changed deformability of erythrocytes, inhibiting aggregation of thrombocytes and reducing the increased viscosity of blood. Трентал® 400 improves microcirculation in zones of the broken blood circulation.
As active Трентал® 400 active ingredient contains derivative xanthine - пентоксифиллин. The mechanism of its action is connected with inhibition of phosphodiesterase and accumulation of tsAMF in cells of smooth muscles of vessels and uniform elements of blood.
Having weak myotropic sosudorasslablyayushchy effect, пентоксифиллин reduces the general peripheric resistance a little and slightly expands coronary vessels.
Treatment Тренталом® 400 leads to improvement of symptomatology of disturbances of cerebral circulation.
Success of treatment at occlusal damage of peripheral arteries (for example, the alternating lameness) is shown in lengthening of a distance of walking, elimination of night spasms in gastrocnemius muscles and disappearance of pains at rest.

Pharmacokinetics. After oral administration пентоксифиллин quickly and almost it is completely soaked up.
After almost full absorption пентоксифиллин it is metabolized. Absolute bioavailability of a pentoksifillin makes 19±13%. The main active metabolite 1-(5 hydroxyhexyl) - 3,7 dimethylxantine (a metabolite of I) has the concentration in a blood plasma twice exceeding initial concentration of a pentoksifillin.
The elimination half-life of a pentoksifillin after peroral introduction makes 1,6 h.
Pentoksifillin is completely metabolized and more than 90% are removed through kidneys in the form of not conjugated water-soluble metabolites. Removal of metabolites is late at patients with an impaired renal function.
At patients with an abnormal liver function the elimination half-life of a pentoksifillin is extended and absolute bioavailability increases.

Indications to use:

Disturbances of peripheric circulation of atherosclerotic genesis (for example, the alternating lameness), a diabetic angiopatiya, trophic disturbances (for example, trophic ulcers of shins, gangrene).
Disturbances of cerebral circulation (effect of cerebral atherosclerosis, as, for example, disturbance of concentration of attention, dizziness, memory impairment), ischemic and postinsultny states.
Disturbances of blood circulation in a retina and a choroid of an eye, an otosclerosis, degenerative changes against the background of pathology of vessels of an inner ear and decrease in hearing.

Route of administration and doses:

The dosage is established by the doctor according to specific features of the patient.
The usual dose makes: one tablet Трентал® 400 two or three of time a day. The maximum daily dose - 1200 mg. Drug should be swallowed entirely in time or right after meal, washing down with enough water.
At patients with an impaired renal function (the clearance of creatinine is lower than 30 ml/min.) the dosage can be lowered to 1-2 tablets a day.
Reduction of a dose, taking into account individual portability, is necessary at patients with a heavy abnormal liver function.
Treatment can be begun with small doses at patients with low arterial pressure, and also at the persons which are in risk group in view of a possible lowering of arterial pressure (patients with a severe form of an ischemic heart disease or with hemodynamically significant stenoses of vessels of a brain). In these cases the dose can be increased only gradually.

Features of use:

Treatment should be carried out under control of arterial pressure.
At the patients with a diabetes mellitus accepting hypoglycemic means, purpose of high doses can cause the expressed 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 recently transferred an operative measure systematic control of level of hemoglobin and a hematocrit is necessary.
The entered dose has to be reduced at patients with low and unstable arterial pressure.
At elderly people reduction of a dose (increase in bioavailability and reduction in the rate of removal) can be required.
Safety and efficiency of a pentoksifillin at children are studied insufficiently.
Smoking can reduce a therapeutic effectiveness of drug.

Side effects:

In cases when Trental is used in high doses there can be following side effects:
from a nervous system: headache, dizziness, uneasiness, sleep disorders, spasms;
from integuments and podkozhnozhirovy cellulose: 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: a xerostomia, anorexia, an intestines atony, pressure sense and overflow in a stomach, nausea, vomiting, diarrhea;
from a cardiovascular sitema: tachycardia, arrhythmia, cardialgia, progressing of stenocardia, lowering of arterial pressure;
from system of a hemostasis and bodies of a hemopoiesis: a leukopenia, thrombocytopenia, a pancytopenia, bleedings from vessels of skin, mucous membranes, a stomach, intestines, a hypofibrinogenemia;
from sense bodys: vision disorder, scotoma;
allergic reactions: itch, dermahemia, small tortoiseshell, Quincke's disease, acute anaphylaxis.
Very seldom cases of development of aseptic meningitis, an intra hepatic cholestasia and increase in activity of "hepatic" transaminases, an alkaline phosphatase meet.

Interaction with other medicines:

Pentoksifillin is capable to strengthen action of the means reducing the arterial pressure (APF inhibitors, nitrates).
Pentoksifillin can strengthen effect of the medicines influencing coagulant system of blood (indirect and direct anticoagulants, trombolitik), antibiotics (including cephalosporins).
Cimetidinum increases concentration of a pentoksifillin in plasma (risk of emergence of side effects).
Joint appointment with other xanthines can lead to excessive nervous excitement.
Antihyperglycemic effect of insulin or hypoglycemic drugs can be strengthened at reception of a pentoksifillin (the increased risk of development of a hypoglycemia). Strict control of such patients is necessary.
Some patients have a concomitant use of a pentoksifillin and theophylline can lead to increase in level of theophylline. It can lead to increase or strengthening of the side effects connected with theophylline.

Contraindications:

Трентал® 400 it should not be applied at patients:
• with hypersensitivity to a pentoksifillin, other methylxanthines or to any of fillers;
• with massive bleedings;
• with extensive retinal apoplexies of an eye;
• with hematencephalons;
• with an acute myocardial infarction;
• aged up to 18 years;
• at pregnancy, in the period of a lactation.

With care drug should be used at patients with:
• heavy cardiac arrhythmias (risk of deterioration in arrhythmia);
• arterial hypotension (risk of a further lowering of arterial pressure, see the section "Route of Administration and Doses");
• chronic heart failure;
• peptic ulcer of a stomach and duodenum;
• an impaired renal function (the clearance of creatinine is lower than 30 ml/min.) (risk of cumulation and the increased risk of development of side effects, see the section "Route of Administration and Doses");
• heavy abnormal liver functions (risk of accumulation and the increased risk of side effects, see the section "Route of Administration and Doses");
• after recently postponed operative measures;
 
• the increased bent to bleeding, for example, as a result of use of anticoagulants or at disturbances in system of a blood coagulation (risk of development of heavier bleedings).

Overdose:

Clinical picture: dizziness, desires on vomiting, falling of arterial pressure, tachycardia, arrhythmia, reddening of integuments, a loss of consciousness, a fever, an areflexia, toniko-clonic spasms.
In case of the disturbances described above it is necessary to see a doctor urgently.
Symptomatic treatment: the special attention has to be directed to maintenance of arterial pressure and function of breath. Convulsive attacks are removed administration of diazepam.
At emergence of the first signs of overdose (the increased perspiration, nausea, cyanosis) immediately stop administration of drug. Provide lower position of the head and an upper part of a trunk. Watch free passability of respiratory tracts.

Storage conditions:

To store in the dry place at a temperature not above 25 °C. To store in the place, unavailable to children.
List B. Period of validity 4 years. Not to use drug after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of the prolonged action, film coated, 400 mg. On 10 tablets in the blister from PVC / aluminum foil. On 2 blisters together with the application instruction in a cardboard pack.