Pentoksifillin

Pentoksifillin – the medicine with vasodilating, anti-aggregation, angioprotektivny action promoting microcirculation improvement.

Form of release and structure

Dosage forms of production of drug Pentoksifillin:

• Solution for intravenous and intra arterial administration of 20 mg/ml: transparent, colourless or slightly yellowish (in ampoules on 5 ml, on 5 or 10 ampoules in planimetric strip or plastic packagings (pallets), on 1 or 2 packagings (pallet) in a cardboard pack);
• Solution for injections of 20 mg/ml (in ampoules on 5 ml, on 3, 5 or 10 ampoules in planimetric strip or plastic packagings (pallets), on 1-4 packagings (pallet) in a cardboard pack or on 5 or 10 ampoules in a cardboard pack);
• Solution for infusions of 0,04%, 0,08%, 0,2%: transparent, colourless (in polymeric containers on 100, 250 or 500 ml);
• Concentrate for preparation of solution for infusions of 20 mg/ml (in ampoules on 5 ml, on 5 ampoules in blisters or blister strip packagings, on 1 or 2 blisters or packagings in a cardboard pack, an ampoule knife in a set);
• Concentrate for preparation of solution for intravenous and intra arterial administration of 20 mg/ml: slightly yellowish or colourless, transparent (in ampoules on 5 ml, on 5 or 10 ampoules complete with an ampoule knife in a cardboard pack or on 5 or 10 ampoules in planimetric strip or plastic packagings (pallets), on 1 or 2 packagings (pallet) in a cardboard pack complete with an ampoule knife);
• Tablets ретард, film coated: pink, a kapsulovidny form, on one party – the line of a break (in blister strip packagings on 10 or 20 pieces, on 1-6 or 10 packagings in a cardboard pack);
• The tablets covered with a kishechnorastvorimy cover: biconvex, pink, on cross section two layers are visible (in blister strip packagings on 10 or 20 pieces, on 1-6 or 10 packagings in a cardboard pack; in dark polymeric or glass jars on 10, 20, 30, 40, 50 or 60 pieces, after 1 bank in a cardboard pack).

Structure of 1 ml of solution for intravenous and intra arterial administration:

• Active agent: пентоксифиллин – 20 mg;
• Additional components: monosubstituted sodium phosphate, sodium chloride, water for injections.

Structure of 1 ml of solution for injections:

• Active agent: Pentoksifillin – 20 mg;
• Additional components: sodium chloride, water for injections.

Structure of 1 ml of solution for infusions:

• Active agent: пентоксифиллин – 0,4, 0,8 or 2 mg;
• Additional components: sodium chloride, water for injections.

Structure of 1 ml of a concentrate for preparation of solution for infusions:

• Active agent: пентоксифиллин – 20 mg;
• Additional components: water for injections.

Structure of 1 ml of a concentrate for preparation of solution for intravenous and intra arterial administration:

• Active agent: пентоксифиллин – 20 mg;
• Additional components: dihydrosodium phosphate, sodium chloride, solution of sodium of hydroxide of 0,1 M, water for injections.

Structure of 1 tablet ретард, film coated:

• Active agent: пентоксифиллин – 400 mg;
• Additional components and cover: ethyl cellulose, magnesium stearate, double-base calcium phosphate, talc, gidroksipropilmetiltsellyuloza, diethyl phthalate, titanium dioxide, karmoizinovy varnish.

Structure of 1 tablet covered with a kishechnorastvorimy cover:

• Active agent: пентоксифиллин – 100 mg;
• Additional components: talc, lactose (milk sugar), carmoisin (azoruby), povidone (polyvinylpirrolidone), potato starch, stearic acid, copolymer of methacrylic acid and ethyl acrylate 1:1 (kollinut MAE-100 R), poly(ethylene oxide)-4000 (macrogoal-4000), titanium dioxide (pigmental dioxide of titanium).

Indications to use

• Angioneyropatiya (paresthesias, Raynaud's disease);
• Disturbances of peripheric circulation which are caused by inflammatory processes, a diabetes mellitus, atherosclerosis;
• Disturbances of cerebral circulation of ischemic type (acute and chronic current);
• Obliterating endarteritis;
• Chronic, acute and subacute circulatory unefficiency in a retina or a choroid of an eye;
• The trophic disturbances of fabrics connected with disturbances of venous or arterial microcirculation (freezing injuries, trophic ulcers, gangrene, a posttromboflebitichesky syndrome);
• The hearing disorder having a vascular etiology;
• Encephalopathies of an atherosclerotic and distsirkulyatorny etiology.

Contraindications

Absolute:

• Myocardial infarction (acute current);
• Eye retinal apoplexies;
• The expressed atherosclerosis (coronary or cerebral);
• Massive bleedings;
• Hemorrhagic stroke (acute current);
• The expressed disturbances of a heart rhythm;
• Age up to 18 years;
• Period of pregnancy and lactation;
• Hypersensitivity to the components which are a part of drug, and also other methylxanthines.

Relative (drug Pentoksifillin it is necessary to appoint with care in the presence of the following states / diseases):

• Tendency to arterial hypotension and labile arterial pressure (the doctor sets the dosing mode individually, increase in a dose needs to be carried out gradually);
• Peptic ulcer of a stomach and duodenum;
• The expressed functional disturbances of kidneys (the doctor sets the dosing mode individually, increase in a dose needs to be carried out gradually);
• The operative measure postponed in recent time (there is a high probability of development of bleedings).

Route of administration and dosage

Solution for infusions and solution for intravenous and intra arterial administration
Intra arterial introduction: speed – 10 mg a minute; an initial dose – 100 mg of drug (in 0,9% solution of sodium chloride of 20-50 ml), increase further a dose to 200-300 mg (in 0,9% solution of sodium chloride of 30-50 ml).

Intravenously Pentoksifillin enter slowly kapelno for 90-180 minutes:

• Solution for infusions: a dose – 50-100 mg, in case of need – 200 mg (as much as possible in day – 300 mg). During introduction of the patient has to be in a prone position;
• Solution for intravenous and intra arterial administration: a dose – 100 mg of drug in 0,9% solution of sodium chloride or 5% solution of glucose (dextrose) of 250-500 ml. At the expressed atherosclerosis of vessels of a brain administration of drug in a carotid artery is forbidden.

Patients with a chronic renal failure (the clearance of creatinine is less than 30 ml in a minute) need a dose decline for 30-50%.

For treatment of diabetic or atherosclerotic defeats in a chronic form conduct a course of intravenous infusions every other day or daily.

Tablets
Pentoksifillin accept inside, without chewing and without breaking (entirely), washing down with water, it is desirable – after food.

As a rule, the tablets covered with a kishechnorastvorimy cover appoint 2 pieces 3 times a day. An average daily dose – 600 mg, maximum – 1200 mg. Most often in 1-2 weeks the single dose is reduced to 1 tablet, at the same time frequency rate of reception of Pentoksifillin remains invariable.

The doctor determines duration of a therapeutic course individually, as a rule, it makes 1-3 months.

At a chronic renal failure (the clearance of creatine is less than 10 ml in a minute) the dose decline is necessary twice.

Pentoksifillin in the prolonged dosage forms usually appoint with frequency rate of reception 2 times a day, duration of a therapeutic course – of 2-3 weeks and more.

Side effects

• Central nervous system: condition of uneasiness, dizziness, spasms, sleep disorders, headache;
• Alimentary system: loss of a tone (atony) of intestines, dryness in a mouth, a loss of appetite, the hepatitis proceeding with an intra hepatic cholestasia, an exacerbation of cholecystitis;
• Cardiovascular system: arrhythmia, tachycardia, lowering of arterial pressure, cardialgia, progressing of stenocardia;
• System of a hemostasis and bodies of a hemopoiesis: thrombocytopenia, a pancytopenia, a hypofibrinogenemia, a leukopenia, bleedings from vessels of skin, mucous membranes of intestines and/or stomach;
• Sense bodys: a vision disorder, the defect of a field of vision which is not reaching its borders (scotoma);
• Integuments and hypodermic fatty tissue: hypostases, increase in fragility of nails, a dermahemia of the person, rushes of blood to face skin and an upper part of a thorax;
• Allergic reactions: dermahemia, Quincke's disease, small tortoiseshell, itch, acute anaphylaxis;
• Laboratory indicators: increase in indicators of activity of hepatic transaminases (lactate dehydrogenase, alaninaminotranspherase, aspartate aminotransferase) and alkaline phosphatase;
• Others: aseptic meningitis (seldom).

In case of development of the first symptoms of hypersensitivity reaction it is necessary to cancel drug use urgently.

During therapy it is regularly necessary to carry out control of a picture of blood that is connected with messages on developing of bleedings (in mucous membranes, skin, digestive tract), thrombocytopenia and aplastic anemia.

Special instructions

At combined use with anticoagulants it is necessary to control indicators of coagulant system of blood carefully.

Pentoksifillin's compatibility with infusion solutions needs to be checked in an individual order.

Patients with the expressed renal failures need careful control of a state.

In hemorrhage cases in a mesh cover of an eye treatment is immediately cancelled.

After the postponed operative measures in recent time it is necessary to exercise systematically control of level of hemoglobin and a hematocrit.

Therapy, in particular intra arterial and intravenous administration of Pentoksifillin, it is necessary to carry out under control of arterial pressure. Sick with unstable or low arterial pressure the entered dose is reduced.

At chronic heart failure before a course it is necessary to reach blood circulation compensation.

Pentoksifillin's appointment in high doses the patient with the diabetes mellitus undergoing therapy by hypoglycemic drugs can lead to a hypoglycemia (such patients need dose adjustment).

At the smoking patients the therapeutic effectiveness of Pentoksifillin can be lowered.

The patient at advanced age in certain cases drug is appointed in reduced doses (it is connected with reduction of speed of removal of active agent and increase in its bioavailability).

Medicinal interaction

The combined use of Pentoksifillin with some drugs / substances can lead to development of the following effects:

• Cimetidinum: concentration of a pentoksifillin in a blood plasma and, as a result, probability of development of side reactions increases;
• Valproic acid, heparin, theophylline, fibrinolitic drugs, anti-hypertensive and hypoglycemic means (insulin, peroral hypoglycemic means), drugs exerting impact on coagulant system of blood (anticoagulants, trombolitik), antibiotic medicines (including cephalosporins): their action amplifies;
• Other xanthines: excessive nervous excitement develops.

Terms and storage conditions

To store in dry, protected from light, the place, unavailable to children.

Period of validity:

• Tablets ретард – 3 years at a temperature up to 25 °C;
• The tablets covered with a kishechnorastvorimy cover – 2 years at a temperature up to 30 °C;
• Concentrate for preparation of solution for intravenous and intra arterial administration, solutions for injections, infusions, intravenous and intra arterial administration – 2 years at a temperature up to 25 °C.