Pentoksifillin

General characteristics. Structure:

Active agent - пентоксифиллин (in terms of 100% substance) 100.0 mg.

Excipients: sodium chloride, water for injections.

Pharmacological properties:

Pharmacokinetics. Pentoksifillin contacts membranes of erythrocytes. Is exposed to biotransformation at first in erythrocytes, then in a liver with formation of two main metabolites: 1-5-hydroxyhexyl-3,7-dimethylxantine and 1-3-carboxypropyl-3,7-dimethylxantine. Bioavailability – 6-32%. The maximum concentration is reached within 1 hour. The elimination half-life makes about 1 hour. In 24 h the most part of a dose is removed with urine in the form of metabolites, a smaller part through intestines, can be allocated through breast milk.

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

At heavy renal failures removal of metabolites is slowed down.

Pharmacodynamics. Pentoksifillin - the means which is improving microcirculation, having angioprotektivny effect. Derivative dimethylxantine. Pentoksifillin reduces viscosity of blood and increases elasticity of erythrocytes, improves microcirculation and increases concentration of oxygen in fabrics. Increase in elasticity of erythrocytes, apparently, is caused by inhibition of phosphodiesterase and increase as a result of this content of cyclic adenosinemonophosphoric acid in erythrocytes with decrease in concentration of intracellular calcium in unstriated muscles of vessels and in uniform elements of blood. Decrease in viscosity of blood can be a consequence of reduction of concentration of fibrinogen in plasma and suppression of aggregation of erythrocytes and thrombocytes.

Has weak myotropic vasodilating effect, reduces the general peripheric resistance of vessels a little and has moderate positive inotropic effect. Slightly expands coronary vessels. Promotes improvement of supply of fabrics with oxygen, most - in extremities and in the central nervous system. At occlusion of the affected peripheral arteries (the alternating lameness) leads to lengthening of distances of walking, elimination of night spasms of gastrocnemius muscles and pains at rest.

At disturbance of cerebral circulation improves symptomatology.

Indications to use:

- disturbances of peripheric circulation

- ischemic cerebral stroke

- disturbances of blood supply of a brain owing to atherosclerosis

- distsirkulyatorny encephalopathy

- the trophic disturbances of fabrics and bodies connected with thrombosis of arteries and veins, a varicosity, freezing injury

- diabetic angiopatiya

- acute impassability of the central artery of a retina

- acute ischemic neuropathy of an optic nerve

Route of administration and doses:

Vnutriarterialno and intravenously (the patient has to be in a prone position).

Intravenously enter 100 mg (5 ml of solution) into 250-500 ml of 0,9% of isotonic solution of sodium of chloride or 5% of solution of glucose (within 90-180 min.); in case of need the daily dose can be increased to 200-300 mg (10-15 ml).

Vnutriarterialno - at first in a dose of 100 mg (5 ml of solution) in 20-50 ml of 0,9% of isotonic solution of sodium of chloride, and in the next days on 200-300 mg (10-15 ml) in 30-50 ml of solvent (rate of administering of 10 mg/min.).

Duration of a course of treatment is determined by the attending physician.

Introduction of a pentoksifillin in the form of intravenous infusion since it is the most effective and easily transferable form of parenteral administration of drug is recommended.

Features of use:

The patient with heart failure and abnormal liver functions and kidneys drug is appointed with care. Patients with heart failure have to receive medical treatment previously for cardiac glycosides for ensuring full action of a pentoksifillin.

With care to appoint to the patients with a peptic ulcer of a stomach and duodenum who recently transferred an operative measure (risk of developing of bleedings).

Treatment should be carried out under regular control of arterial pressure, a blood picture. If during treatment there are hemorrhages in a mesh cover of an eye, drug is immediately cancelled.

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

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

Smoking can reduce therapeutic effect of drug.

When performing intravenous infusion of the patient has to be in a prone position.

Use for children. Researches about safety and efficiency of drug for treatment of patients up to 18 years are absent.

Considering side effects of drug it is necessary to be careful at control of motor transport or potentially dangerous mechanisms.

Side effects:

- nausea, vomiting, dryness of a mucous membrane of an oral cavity, diarrhea, pains and feeling of weight in epigastriums, the dispeptic phenomena, an intestines atony

- exacerbation of cholecystitis, cholestatic hepatitis

- increase in concentration of liver enzymes in blood

- vision disorders, scotoma

- headache, dizziness, uneasiness, sleep disorders, spasms, aseptic meningitis

- dermahemia, skin rash, itch, small tortoiseshell, Quincke's disease, acute anaphylaxis

- tachycardia, palpitation, pains behind a breast, arrhythmia, a lowering of arterial pressure

- leukopenia, pancytopenia, thrombocytopenia, hypofibrinogenemia, bleedings

- a dermahemia of the person, rushes of blood to face skin and an upper part of a thorax, hypostases, the increased fragility of nails

Interaction with other medicines:

At a concomitant use of a pentoksifillin and anti-hypertensive drugs effect of anti-hypertensive drugs amplifies. In this case the dose of a pentoksifillin needs to be reduced.

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.

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. meloksikamy increase in risk of development of bleedings and/or increase in a prothrombin time is possible; with sympatholytics, ganglioblokator and vazodilatator – the lowering of arterial pressure is possible; with heparin, fibrinolitic drugs and anticoagulants of indirect action – strengthening of anticoagulative action and increase in risk of bleedings.

Contraindications:

- hypersensitivity to methylxanthine derivatives

- acute myocardial infarction

- hemorrhagic stroke

- heavy disturbances of a cordial rhythm

- massive bleeding

- eye retinal apoplexies

- hematencephalon

- the expressed atherosclerosis of coronary and brain vessels (contraindicated intra aortal introduction)

- simple diabetic and proliferating diabetic retinopathy

- children's and teenage age up to 18 years

- pregnancy, lactation period

Overdose:

Symptoms: weakness, dizziness, a hyperemia of integuments, a lowering of arterial pressure, an unconscious condition, tachycardia, drowsiness or excitement, a loss of consciousness, a hyperthermia, an areflexia, tonikoklonichesky spasms, symptoms of gastrointestinal bleeding (vomiting like "coffee thick").

Treatment: general resuscitation actions for recovery of cardiovascular activity (including normalization of the ABP) and breath functions; use of diazepam at a convulsive syndrome. There is no specific antidote.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

On 5.0 ml of drug in ampoules of neutral glass or import.

On each ampoule paste the label from paper label or apply the text directly on an ampoule with paint of an intaglio printing for glass products.

On 5 ampoules pack into a blister strip packaging from a film polyvinyl chloride and a foil aluminum or import. Put the scarificator in each planimetric packaging ampoule.

When packaging ampoules with notches, rings and points scarificators do not invest.

Blister strip packagings together with the approved instructions on a medical use in the state and Russian languages on number of packagings place in boxes from a cardboard or corrugated fibreboard.