Pentoksifillin of 0,2%

General characteristics. Structure:

Active agent: 2 g of a pentoksifillin, 9 g of sodium of chloride.

Excipient: water for injections to 1 l.

The drug rendering the anti-aggregation, improving microcirculation, angioprotektivny, vasodilating action.

Pharmacological properties:

Pharmacodynamics. Pentoksifillin is the main representative of new pharmacological group of drugs – haemo rheological means. It increases plasticity (deformability) of erythrocytes that allows them to get into vessels with the changed gleam (diameter) and to improve blood supply of fabrics, especially against the background of a hypoxia. It lowers their ability to aggregation, facilitates penetration and into an extravasated bed that also promotes oxygenation of fabrics. Pentoksifillin oppresses biosynthesis of fibrinogen and lowers viscosity of blood. Under the influence of drug formation of pseudopodiums at thrombocytes decreases. It is characteristic that at such multidimensional intervention of a pentoksifillin in the processes providing a hemostasis, the risk of bleedings does not increase.

At an inflammation пентоксифиллин has ability to reduce adhesion and aggregation of polymorphonuclear leukocytes, to inhibit "metabolic explosion" and to prevent their damaging action on endothelium cells. It inhibits activity of phosphodiesterase, slows down destruction of tsAMF, reduces concentration of intracellular calcium and strengthens effects of adenosine. Pentoksifillin has subtle vasodilating effect and prevents reduction of vessels under the influence of vasopressor incentives. In recent years it is established what пентоксифиллин has ability to oppress products of pro-inflammatory cytokines (first of all, a factor of a necrosis of a tumor and interleykinov-1,-2,-6).

Pharmacokinetics. At intravenous administration пентоксифиллин gets to fabrics, well gets through a blood-brain barrier. The elimination half-life of a pentoksifillin varies within 0,4-0,8 h. Is exposed to biotransformation in a liver with formation of two main metabolites: 1-(5 hydroxyhexyl) - 3,7 dimethylxantines (metabolite-1) and 1-(3 carboxypropyl) - 3,7 dimethylxantines (metabolite-5) which have similar activity and have an elimination half-life from 1 to 1,6 hours. In 1,5-2 h after infusion concentration of metabolites exceeds the content of initial connection by 5-8 times. By the 8th o'clock concentration of a pentoksifillin and its metabolites in blood considerably decreases (to 10% of initial).

It is excreted preferential by kidneys (to 95%), generally in the form of a metabolite-5. With excrements less than 4% of drug are removed. At the nursing women it is allocated with the lactating glands. Owing to the large volume of distribution and strong linkng with erythrocytes the pharmacokinetics of a pentoksifillin at a hemodialysis practically does not change.

Indications to use:

Ischemic disturbances at patients with atherosclerotic damages of arteries of the lower extremities, at coronary atherosclerosis, atherosclerotic defeats of other localizations. Ischemic disturbances of cerebral circulation, a state after an ischemic stroke, distsirkulyatorny encephalopathy, angioneyropatiya (paresthesias, a Crocq's disease, Reynaud's syndrome). Prevention of disturbances of microcirculation at a diabetes mellitus, a diabetic angiopatiya. Disturbances of blood circulation in an eye retina (both acute, and chronic). After operations of shunting of arteries and prosthetics of valves of heart. The trophic disturbances of fabrics and bodies connected with thrombosis of arteries or veins. In recent years пентоксифиллин as effective antitsitokinovy drug is used at treatment of sepsis, and also for prevention of "a rejection syndrome" of transplanted organs at the recipient.

Route of administration and doses:

The drug is administered intravenously kapelno by 3 times a day on 100-200 mg (50-100 ml of 0,2% of solution) within 20-30 minutes to the patient in a prone position. At heavy patients it is possible to increase a daily dose to 800 mg a day. If necessary пентоксифиллин it can be entered vnutriarterialno. At the expressed atherosclerosis of vessels of a brain the drug cannot be administered in a carotid artery. At treatment of chronic atherosclerotic or diabetic defeats appoint a course of intravenous infusions of drug daily or every other day.

Features of use:

At purpose of a pentoksifillin along with anticoagulants it is necessary to watch indicators of coagulant system of blood carefully. At purpose of drug it is necessary to control the level of arterial pressure also.

Patients with chronic heart failure before purpose of a pentoksifillin should carry out treatment by cardiac glycosides to provide optimal effect of a pentoksifillin.

With extra care it is necessary to appoint пентоксифиллин to patients who have a hypersensitivity to methylxanthines (caffeine, theophylline, theobromine). Safety of use of a pentoksifillin at pregnancy is not established in this connection it is not recommended to appoint drug. Pentoksifillin is allocated with breast milk therefore for the period of treatment it is necessary to stop breastfeeding.

Side effects:

At vvedeniivozmozhno short-term decrease in the ABP, dizziness, a headache, feeling of inflow of heat to the person, heartbeat, tachycardia, stenocardia attacks. At prolonged use of a pentoksifillin in high doses the intestines atony, cholestatic hepatitis, the increased content in blood of enzymes (an aspartataminotrasferaza, alaninaminotranspherase, an alkaline phosphatase, a lactate dehydrogenase), a leukopenia, a pancytopenia, a hypofibrinogenemia is possible. Sometimes at patients the allergy to a pentoksifillin develops.

Interaction with other medicines:

Pentoksifillin strengthens effect of hypotensive drugs, insulin, peroral gipoglikemiziruyushchy drugs.

Simultaneous use of a ketolorak increases risk of bleeding.

Co-administration of a pentoksifillin and theophylline can lead to increase in plasma concentration and increase in an elimination half-life of theophylline.

At joint purpose of a pentoksifillin with NPVS increase in risk of bleeding is possible.

Contraindications:

Acute myocardial infarction, massive bleeding, acute hemorrhagic stroke, amotio of a retina and retinal apoplexy of an eye. Relative contraindications are crushing atherosclerotic defeat of vessels of a brain and heart, heavy disturbances of a cordial rhythm.

Overdose:

Symptoms: hyperemia of the person, arterial hypotonia, klonikotonichesky spasms, loss of consciousness, vomiting "a coffee thick", fever.

Treatment: use anticonvulsant drugs, pressor amines, symptomatic therapy (including the measures directed to maintenance of breath and arterial pressure).

Storage conditions:

List B. In the place protected from moisture and light at a temperature not above + 25 °C. Period of validity 2 years.

Issue conditions:

According to the recipe

Packaging:

On 100, 250 or 500 ml in polymeric containers.