Pentoksifillin of 2,0% 5 ml of N5

General characteristics. Structure:

International and chemical names: pentoxifylline; 3,7-dimetil-1-(5 oxohexyl) - 3,7-dihydro-1H-feather-beds-2,6-dion); main physical and chemical properties: transparent colourless or with slightly yellowish shade liquid;
structure: 1 ml contains a pentoksifillin of 0,02 g; excipients: sodium chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. The means improving microcirculation, a vasoprotective. The mechanism of action is caused by oppression of phosphodiesterase and accumulation of cyclic adenosinemonophosphoric acid with decrease in concentration of intracellular calcium in unstriated muscles of vessels and in uniform elements of blood. Slows down aggregation of thrombocytes and erythrocytes, increases their elasticity, reduces fibrinogen level in plasma and strengthens a fibrinolysis, reducing viscosity of blood and improving its rheological properties. 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.

Pharmacokinetics. It is quickly and completely soaked up. Contacting 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 of dimethylxantine and 1-3-carboxypropyl-3,7-dimethylxantine. It is removed preferential by kidneys, an insignificant part (4%) – through intestines, can be allocated through breast milk.

Indications to use:

Cerebrovascular pathology, in particular atherosclerosis of brain vessels, states after the postponed myocardial infarction; diabetic nefroangiopatiya and other diabetic angiopatiya, disturbance of peripheric circulation (Raynaud's disease, endarteritis, etc.); vascular pathology of eyes (acute and chronic insufficiency of blood supply of a retina and choroid). Functional hearing disorder of vascular genesis.

Route of administration and doses:

Vnutriarterialno, intravenously, intramusculary. At acute disorders brain (an ischemic stroke) and peripheric circulation 0, 1 g of drug intravenously enter into 250-500 ml of 0,9% of solution of sodium of chloride or 5% of solution of glucose (duration of introduction of 90-180 min.); vnutriarterialno at first in a dose of 0,1 g in 20–50 ml of 0,9% of solution of sodium of chloride, then – on 0,2-0,3 g in 30–50 ml of solvent. Rate of administering – 0,1 g (5 ml of 2% of solution of Pentoksifillin) in 10 min. The daily dose at intravenous administration can be raised further on 50–100 mg to achievement of the maximum daily dose 300 mg. In hard cases introduction of 400 mg/days to 2 receptions is admissible.
Intramusculary deeply on 100–200 mg 2-3 times a day. In parallel with parenteral use it is possible to apply inside, in a daily dose of 800-1200 mg in 2-3 receptions. At the expressed disturbances of local blood circulation by the adult and to children 12 years are more senior (with body weight more than 50 kg) drug is appointed on 0,6 g by 2 times a day.

Features of use:

At Pentoksifillin's use the patient has to be in horizontal position. Treatment should be carried out under control of the ABP. At arterial hypotension the dose is raised gradually. Patients with the expressed atherosclerosis cannot vnutriarterialno administer the drug.
At heart failure administration of cardiac glycosides is necessary.
Before Pentoksifillin's introduction it is necessary to reach blood circulation compensation.
At the patients with diabetes accepting hypoglycemic means, purpose of high doses. Pentoksifillina can cause a hypoglycemia (correction of doses is required).
At appointment with anticoagulants it is necessary to watch indicators of coagulant system of blood.
The patients who transferred recently an operative measure need to control the level of hemoglobin and a hematocrit systematically.
With care to use drug to patients with round ulcers of a stomach and duodenum (risk of development of bleeding).
At patients of advanced age and patients with diseases of a liver, kidneys Pentoksifillin's dose decreases. At clearance of creatinine less than 10 ml/min. appoint 50–70% of a dose.

Side effects:

Headache, dizziness, nervousness, drowsiness or sleeplessness. Tachycardia, stenocardia attacks, arrhythmia, hypotonia. Nausea, vomiting, a gastralgia, an intestines atony, an exacerbation of cholecystitis, cholestatic hepatitis, increase in concentration of liver enzymes in blood, change of body weight, hypostases, the dispeptic phenomena. Leukopenia, pancytopenia, thrombocytopenia, hypofibrinogenemia, bleedings. Hyperemia of integuments, seldom rash, itch, urticaria.
At intravenous and intra arterial administration decrease in the ABP.

Interaction with other medicines:

Strengthens effect of hypotensive and antidiabetic medicines (the dose of drug should be lowered). At combined use with sympatholytics, ganglioblokator, vazodilatator lowering of arterial pressure is possible; with ketoloraky, meloksikamy increase in a prothrombin time with risk of development of bleedings; with heparin, fibrinolitic drugs and anticoagulants of indirect action strengthening of anticoagulative action. Cimetidinum considerably increases Pentoksifillin's concentration in blood with increase in probability of development of side effects.

Contraindications:

Hypersensitivity to methylxanthine derivatives, an acute myocardial infarction, plentiful bleedings, the expressed atherosclerosis of coronary and brain vessels (contraindicated intra aortal introduction), a hemorrhagic stroke, eye retinal apoplexies, pregnancy, breastfeeding, children's age up to 12 years.

Overdose:

Symptoms: decrease in the ABP, hyperemia of integuments, hypotonia, drowsiness, agitation, spasms, consciousness disturbance, symptoms of gastrointestinal bleedings (vomiting of color of "a coffee thick"), fever.
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 unavailable to children, protected from light place, at a temperature not above 25 °C.

Period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 2% on 5 ml in ampoules No. 5.