Pentoksifillin

General characteristics. Structure:

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

Excipients: sodium chloride, dihydrophosphate sodium a dihydrate, hydroxide sodium solution of 1 M, water for injections.

Pharmacological properties:

Pharmacodynamics. Pentoksifillin is derivative xanthine. Improves microcirculation and rheological properties of blood. The mechanism of action is connected with oppression of phosphodiesterase and increase in contents cyclic 3,5 adenosinemonophosphates (3,5-AMF) in thrombocytes and adenosinetriphosphate (ATP) in erythrocytes with simultaneous saturation of energy potential that in turn leads to a vazodilatation, decrease in the general peripheric vascular resistance, increase of systolic and minute volume of heart without considerable change of heart rate.

Expanding coronary arteries, increases delivery of oxygen to a myocardium (antiangi-nalny effect), vessels of lungs - improves blood oxygenation.

Raises a tone of respiratory muscles (intercostal muscles and a diaphragm). At intravenous administration leads to strengthening of collateral circulation, increase in volume of the proceeding blood through section unit. Leads to increase of content of ATP in a brain, favorably influences bioelectric activity of the central nervous system.

Snizhyaet viscosity of blood, causes disaggregation of thrombocytes, increases elasticity of a membrane of erythrocytes (due to influence on patholologically the changed deformirovannost of erythrocytes). Improves microcirculation in zones of the broken blood circulation.

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

Pharmacokinetics. It is metabolized by a liver. In the course of metabolism several active metabolites are formed, basic of which are a metabolite 1 and a metabolite 5. Their concentration in a blood plasma in 5 and 8 times is (respectively) higher than concentration of initial substance. It is allocated preferential in the form of metabolites (94%) with kidneys and through intestines (4%). It is allocated with breast milk. In the first 4 hours about 90% of a dose are removed. In not changed look 2% of drug are removed. Pentoksifillin and his metabolites do not contact proteins of a blood plasma.

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:

- disturbances of peripheric circulation against the background of atherosclerotic, diabetic and inflammatory processes (including at the "alternating" lameness caused by atherosclerosis, a diabetic angiopatiya, an obliterating endarteritis);

- trophic disturbances of fabrics owing to disturbance of arterial and venous microcirculation (varicose ulcers, gangrene, freezing injuries);

- angioneyropatiya (paresthesias, Crocq's disease, Raynaud's disease);

- acute and chronic disorders of cerebral circulation of ischemic type (including at cerebral atherosclerosis);

- states after a hemorrhagic and ischemic stroke;

- disturbances of blood circulation in eye vessels (acute and chronic insufficiency of blood supply of mesh and vascular covers of an eye);

- the disturbances of functions of a middle ear of vascular genesis which are followed by relative deafness.

Route of administration and doses:

The drug is administered intravenously. When performing infusions of the patient has to be in situation "lying".

Intravenously kapelno it is entered slowly in a dose of 100 mg into 250-500 ml of 0,9% of solution of sodium of chloride or into 5% solution of a dextrose (glucose) (introduction duration - 90-180 minutes).

With a chronic renal failure (clearance of creatinine less than 10 ml/min.) 50-70% of a usual dose appoint sick.

Features of use:

Pregnancy and lactation: contraindicated.

Treatment should be carried out under control of arterial pressure.

At patients with chronic heart failure it is necessary to reach blood circulation compensation.

At the patients with a diabetes mellitus accepting hypoglycemic means, purpose of high doses of Pentoksifillin 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 transferred recently an operative measure systematic control of hemoglobin and a hematocrit is necessary.

The entered dose has to be reduced at patients with low and unstable arterial pressure. 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.

Compatibility of solution of a pentoksifillin with infusion solution should be checked in each case.

Influence on ability to manage vehicles and mechanisms. Influence of drug on ability to manage vehicles at an intravenous way of introduction is not studied.

Side effects:

From the central nervous siyetema: headache, dizziness; uneasiness, sleep disorders, spasms.

From cardiovascular system: tachycardia, arrhythmia, cardialgias, it is rare - progressing of symptoms of stenocardia, lowering of arterial pressure.

From integuments: 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: nausea, vomiting, dryness of a mucous membrane of an oral cavity, feeling of weight in a stomach, a loss of appetite, an exacerbation of cholecystitis, cholestatic hepatitis, an atony of intestines, bleeding from mucous membranes of a stomach, intestines.

From sense bodys: vision disorder, scotoma.

From system of a hemostasis and bodies of a hemopoiesis: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; nasal bleedings.

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

Laboratory indicators: increase in activity of "hepatic" transaminases - alaninaminotranspherases (ALT), aspartate aminotransferases (ACT), lactate dehydrogenases (LDG) and an alkaline phosphatase.

Others: aseptic meningitis (seldom).

Interaction with other medicines:

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.

Increases efficiency of hypotensive drugs, insulin and hypoglycemic means for intake.

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.

Contraindications:

- hypersensitivity to the pentoksifillin, other derivatives of xanthine or other components which are a part of drug;

- the expressed coronary or cerebral atherosclerosis;

- acute myocardial infarction;

- the expressed disturbances of a heart rhythm;

- uncontrollable arterial hypotension;

- massive bleeding;

- eye retinal apoplexy;

- hemorrhagic stroke;

- pregnancy, lactation period;

- age up to 18 years (efficiency and safety are not established).

With care. the patient with the labile arterial pressure, tendency to arterial hypotension, chronic heart failure, tendency to hemorrhages, a state after recently postponed operative measures, a liver and/or renal failure.

Overdose:

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

Treatment: symptomatic, directed to maintenance of the vital functions of an organism.

Storage conditions:

List B. To store in the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous administration of 20 mg/ml in ampoules on 5 ml. On 5 ampoules in a blister strip packaging from a film polyvinyl chloride. 1 or 2 blister strip packagings with the scarificator ampoule ceramic or a knife for opening of ampoules and the application instruction in a pack from a cardboard. When using ampoules with a ring of a break or a point of a break the knife or the scarificator do not put.

Packaging: (5) - an ampoule (2)/2 blister strip packagings with the scarificator ampoule ceramic or a knife for opening of ampoules and the instruction on a primeniye in a pack from a cardboard. When using ampoules with a ring of a break or a point of a break a knife or the scarificator not vkladyvayut./-the Cardboard pack. (5) - an ampoule (5)/1 blister strip packaging with the scarificator ampoule ceramic or a knife for opening of ampoules and the instruction on a primeniye in a pack from a cardboard. When using ampoules with a ring of a break or a point of a break a knife or the scarificator not vkladyvayut./-the Cardboard pack