Pentoksifillin

General characteristics. Structure:

Active ingredient: 100 mg of a pentoksifillin.

Excipients: Stearic acid, potato starch, methyl cellulose water-soluble, lactose (sugar milk), povidone (polyvinylpirrolidone low-molecular medical).

Structure of a cover: Tsellatsefat (atsetilftaliltsellyuloza), titanium dioxide, castor oil, liquid paraffin (liquid paraffin), azoruby (acid red 2 C), talc, beeswax.

The medicine improving microblood circulation due to reduction of its viscosity, a vasoprotective.

Pharmacological properties:

Pharmacodynamics. The means improving microcirculation, a vasoprotective derivative dimethylxantine. Pentoksifillin reduces viscosity of blood, causes disaggregation of thrombocytes, increases elasticity of erythrocytes (due to influence on patholologically the changed deformability of erythrocytes), improves microcirculation and increases concentration of oxygen in fabrics. Increases concentration of tsAMF in thrombocytes and ATP in erythrocytes with simultaneous saturation of energy potential that in turn leads to a vazodilatation, decrease in OPSS, increase of a stroke output of blood and minute volume of blood without considerable change of ChSS.

Expanding coronary arteries, increases delivery of oxygen to a myocardium, expanding vessels of lungs, improves blood oxygenation. Raises a tone of respiratory muscles (intercostal muscles and a diaphragm).

In/in introduction, along with the action stated above, leads to strengthening of collateral circulation, increase in volume of the proceeding blood through section unit.

Increases concentration of ATP in a brain, favorably influences bioelectric activity of TsNS. Improves microcirculation in zones of the broken blood supply.

At occlusal damage of peripheral arteries (the "alternating" lameness) leads to lengthening of a distance of walking, elimination of night spasms of gastrocnemius muscles and pains at rest.

Pharmacokinetics. After intake it is well soaked up from a GIT. Insignificant metabolism at "the first passing" through a liver is noted. Contacts membranes of erythrocytes. Is exposed to biotransformation at first in erythrocytes, then in a liver. Some metabolites are active. T1/2 makes 0.4-0.8 h of plasma of not changed substance, metabolites - 1-1.6 h. In 24 h the most part of a dose is removed with urine in the form of metabolites, a smaller part (about 4%) - through intestines.

Removal of a pentoksifillin decreases at patients of advanced age and at liver diseases.

Indications to use:

The disturbances of peripheric circulation (including at the alternating lameness) connected with chronic occlusal circulatory disturbances in arterial vessels of the lower extremities. Ischemic disturbance of cerebral circulation, ischemic stroke and postinsultny states; cerebral atherosclerosis (dizziness, headache, disturbances of memory, sleep disorder), distsirkulyatorny encephalopathy, virus neuroinfection (prevention of possible disturbance of microcirculation). An ischemic heart disease, a state after the postponed myocardial infarction. Diabetic angiopatiya. Acute disorders of blood circulation in a retina and a choroid of an eye, an acute ischemic neuropathy of an optic nerve. An otosclerosis, degenerative changes against the background of pathology of vessels of an inner ear with gradual decrease in hearing. HOBL, bronchial asthma. Impotence of vascular genesis.

Route of administration and doses:

Pentoksifillin accept inside after food.

Tablets are covered with a special cover, soluble in intestines therefore they are swallowed entirely, washing down with a small amount of water.

Accept 200 mg (2 tablets) 3 times a day.

If necessary the dose is gradually increased to 1200 mg the day divided into 2-3 receptions.

The maximum daily dose - 1200 mg.

Course of treatment 1-3 months.

Duration of treatment and the mode of dosing by Pentoksifillin are established by the attending physician individually, depending on a clinical picture of a disease and the gained therapeutic effect.

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

Features of use:

With care to apply at lability of the ABP (tendency to arterial hypotension), chronic heart failure, a peptic ulcer of a stomach and a duodenum (to intake), after recently postponed operative measures, at a liver and/or renal failure, at children and teenagers aged up to 18 years (efficiency and safety are not studied).

At renal failures or heavy abnormal liver functions correction of the mode of dosing of a pentoksifillin is required.

During treatment it is necessary to control the ABP level.

At simultaneous use with anti-hypertensive means, insulin, peroral hypoglycemic drugs reduction of a dose of a pentoksifillin can be required.

At simultaneous use with anticoagulants it is necessary to control blood coagulation indicators carefully.

Adequate and well controlled clinical trials of safety of use of a pentoksifillin at pregnancy are not conducted.

Pentoksifillin and his metabolites are allocated with breast milk. In need of use in the period of a lactation it is necessary to stop breastfeeding.

Side effects:

From TsNS: headache, dizziness; uneasiness, sleep disorders; spasms.

Dermatological reactions: 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, an exacerbation of cholecystitis, cholestatic hepatitis, increase in activity of hepatic transaminases and ShchF.

From an organ of sight: vision disorder, scotoma.

From cardiovascular system: tachycardia, arrhythmia, cardialgia, progressing of stenocardia, decrease in the ABP.

From system of a hemopoiesis: thrombocytopenia, leukopenia, pancytopenia.

From coagulant system of blood: hypofibrinogenemia; bleedings from vessels of skin, mucous membranes, a stomach, intestines.

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

Interaction with other medicines:

Pentoksifillin can exponentiate effect of anti-hypertensive drugs.

Against the background of parenteral use of a pentoksifillin in high doses strengthening of hypoglycemic effect of insulin at patients with a diabetes mellitus is possible.

At simultaneous use with ketorolaky increase in risk of development of bleedings and/or increase in a prothrombin time is possible; with meloksikamy - increase in risk of development of bleedings; with sympatholytics, ganglioblokator and vazodilatator - decrease in the ABP is possible; with heparin, fibrinolitic drugs - strengthening of anticoagulative action.

Cimetidinum considerably increases concentration of a pentoksifillin in a blood plasma, in this regard at simultaneous use the probability of development of side effects can increase.

Contraindications:

Acute myocardial infarction, porphyria, massive bleeding, hemorrhagic stroke, eye retinal apoplexy, pregnancy, lactation period. For in/in introductions (in addition) - arrhythmias, the expressed atherosclerosis of coronary or brain arteries, uncontrollable arterial hypotension.

Hypersensitivity to a pentoksifillin and other derivatives of xanthine.

Overdose:

Symptoms: nausea, dizziness, tachycardia, the expressed lowering of arterial pressure, reddening of integuments, fervescence (fever), agitation, an areflexia, toniko-clonic spasms, vomiting "a coffee thick", arrhythmias, a loss of consciousness. At emergence of the disturbances of the patient described above has to see a doctor urgently.

Treatment: symptomatic. The special attention has to be directed to maintenance of arterial pressure and function of breath. Spasms are removed administration of diazepam. Urgent actions at emergence of heavy anaphylactic reactions (shock). At emergence of the first signs (perspiration, nausea, cyanosis) immediately stop administration of drug.

In addition to other necessary actions provide lower position of the head and an upper part of a trunk and provide freedom for breath. Urgent medical actions: enter into Epinephrinum (adrenaline). If necessary introduction of Epinephrinum can be repeated.

Storage conditions:

To store in dry, protected from light and the place, unavailable to children, at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

60 pieces - bottles polymeric (1) - packs cardboard.
60 pieces - bottles of dark glass (1) - a pack cardboard.
10 pieces - planimetric strip packagings (6) - packs cardboard.