Pentoksifillin

General characteristics. Structure:

Active ingredient: 20 mg of a pentoksifillin in 1 ml of solution.

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

Pharmacological properties:

Pharmacodynamics. Inhibits phosphodiesterase, stabilizes tsAMF and reduces concentration of intracellular calcium. Blocks adenosine receptors. Slows down aggregation of thrombocytes; increases their resistance to deformation, improves rheological properties of blood, suppresses a thrombogenesis and normalizes microcirculation.

The anti-anginal effect (increase in delivery of oxygen to a myocardium) is caused by expansion of coronary arteries. Dilatiruyet vessels of lungs also improves blood oxygenation. Raises a tone of respiratory muscles (intercostal muscles and a diaphragm).

Pharmacokinetics. After intake it is quickly and completely soaked up. Intensively it biotransformirutsya at "the first passing" through a liver with formation of two main metabolites: 1-(5 hydroxyhexyl) −3,7-диметилксантина (метаболит−1) and 1-(3 carboxypropyl) −3,7-диметилксантина (метаболит−5).

Cmax  of a pentoksifillin and key products of its biodegradation is reached during 1 h (for the prolonged forms — later 2–4 h), at the same time concentration of metabolites exceeds the content of initial connection by 5–8 times. T1/2  varies within 0,5–1,5 h. At patients with an abnormal liver function of T1/2pentoksifillina it is extended, and bioavailability increases. It is excreted preferential by kidneys (in a look метаболита−5) and with excrements (less than 4%).

Indications to use:

Disturbance of peripheric circulation (including obliterating endarteritis, diabetic angiopatiya, Raynaud's disease); atherosclerotic and distsirkulyatorny angiopatiya, angioneyropatiya; trophic disturbances of fabrics (including varicosity, trophic ulcers of a shin, gangrene, frostbite, posttrombotichesky syndrome); disturbance of cerebral circulation (effect of cerebral atherosclerosis, for example decrease in concentration of attention, dizziness, memory impairment), ischemic and postinsultny states; disturbance 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:

Inside, initial dose: 600 mg/days in 2–3 receptions; in process of improvement of a state pass to maintenance doses: on 100 mg 3 times a day; course of treatment of 2-3 weeks and more.

In/in, in / and, in oil. Doses and the scheme of treatment are established individually.

Features of use:

Use at pregnancy and feeding by a breast. Contraindicated at pregnancy. Category of action on a fruit on FDA — C. For the period of treatment it is necessary to stop breastfeeding (gets into breast milk).

Treatment should be carried out under control of the ABP.

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 the low and unstable ABP.

At elderly people 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.

Compatibility of solution of a pentoksifillin with infusion solution should be checked in each case. When carrying out in/in infusions of the patient has to be in a prone position.

Side effects:

From a nervous system and sense bodys: headache, dizziness, uneasiness, sleep disorder, spasms, visual disturbances, scotoma; very seldom — aseptic meningitis.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): tachycardia, cardialgia, arrhythmia, progressing of stenocardia, decrease in the ABP, leukopenia, pancytopenia, thrombocytopenia, hypofibrinogenemia.

From bodies of a GIT: dryness in a mouth, a loss of appetite, an intestines atony, an exacerbation of cholecystitis, cholestatic hepatitis, increase in activity of liver enzymes (nuclear heating plant, ALT, ShchF, LDG).

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

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

For tablets in addition: pressure sense and overflow in a stomach, nausea, vomiting, diarrhea.

Interaction with other medicines:

Pentoksifillin is capable to strengthen action of means, the reducing ABP (APF inhibitors, nitrates).

Can strengthen action of the HP influencing coagulant system of blood (indirect and direct anticoagulants, trombolitik), antibiotics (including cephalosporins).

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.

Antihyperglycemic effect of insulin or peroral antidiabetic means can be strengthened at reception of a pentoksifillin (the increased risk of development of a hypoglycemia, strict control of a condition of such patients is necessary).

Some patients have a concomitant use of a pentoksifillin and theophylline can lead to increase in level of theophylline in blood and to strengthening of side effect of theophylline.

Contraindications:

Hypersensitivity, including to other derivatives of methylxanthine (caffeine, theophylline, theobromine), a hemorrhagic stroke, massive bleeding, an extensive retinal apoplexy of an eye, an acute myocardial infarction, pregnancy, feeding by a breast.

For in/in introductions (in addition): arrhythmia, the expressed atherosclerosis of coronary or brain arteries, uncontrollable arterial hypotension.

Restrictions to use. Lability of the ABP (tendency to arterial hypotension), chronic heart failure, peptic ulcer of a stomach and duodenum, renal failure (clearance

Overdose:

Symptoms: weakness, dizziness, decrease in the ABP, feeling of inflows, drowsiness or excitement, disturbance of consciousness, spasm.

Treatment: gastric lavage, purpose of absorbent carbon, anticonvulsant drugs, maintenance of the vital functions.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 100 mg / 5 ml, in an ampoule. On 5 or on 10 ampoules in cardboard packaging.