Pentoksifillin таб п / about 100 mg No. 60

General characteristics. Structure:

Active agent: пентоксифиллин (in terms of 100% substance) - 100 mg;
excipients: stearic acid, potato starch, methyl cellulose water-soluble, lactose (sugar milk), povidone (polyvinylpirrolidone low-molecular medical).

Structure of a cover: целлацефат (atsetilftaliltsellyuloz), titanium dioxide, castor oil, liquid paraffin (liquid paraffin), azoruby (acid red 2 C), talc, beeswax;
Description: The tablets covered with a kishechnorastvorimy cover of pink color, round biconvex.

Pharmacological properties:

Pharmacodynamics. Pentoksifillin improves microcirculation and rheological properties of blood, has vasodilating effect, blocks phosphodiesterase and promotes accumulation of tsAMF in cells. Pentoksifillin slows down aggregation of thrombocytes and erythrocytes, increases their elasticity, reduces fibrinogen level in plasma and strengthens фибриолиз that reduces viscosity of blood and improves its rheological properties. Has weak myotropic, vasodilating effect, Pentoksifillin reduces the general peripheric resistance a little and slightly expands coronary vessels. In general, Pentoksifillin causes improvement of microcirculation and supply of fabrics with oxygen in a brain and in extremities, in a smaller measure – in kidneys.

Pharmacokinetics. After intake Pentoksifillin is almost completely soaked up from digestive tract. Drug is exposed to "the first passing" through a liver with education of 2 main pharmacological of active metabolites: 1-5-hydroxyhexyl-3,7-dimethylxantine (metabolite of I) and 1-3-carboxypropyl-3,7-dimethylxantine (metabolite of V). Concentration of a metabolite of I and V in a blood plasma, respectively, in 5 and 8 times is higher, than a pentoksifillina. Time of achievement of the maximum concentration – 1 hour. The elimination half-life – 0,5 – 1,5 hours Pentoksifillin is removed preferential by kidneys – 94% in the form of metabolites (preferential a metabolite of V), intestines – 4%, in the first 4 hours are removed to 90% of a dose. It is allocated with breast milk. 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:

Disturbance of the peripheric circulation caused by atherosclerosis, a diabetes mellitus (a diabetic angiopatiya);
- acute and chronic disorders of cerebral circulation of ischemic genesis;
- atherosclerotic and distsirkulyatorny encephalopathies; angiopatiya (paresthesias, Raynaud's disease);
- trophic disturbances of fabrics owing to disturbance of arterial or venous microcirculation (trophic ulcers, a posttromboflebichesky syndrome, frostbites, gangrene);
- obliterating endarteritis;
- an acute, subacute and chronic circulatory unefficiency in a retina or in an eye choroid;
- hearing disorder of vascular genesis.

Route of administration and doses:

Pentoksifillin accept inside after food. Tablets are covered with a special cover, soluble in intestines therefore they are swallowed entirely, washing down with a small amount of water. Accept 200 mg (2 tablets) 3 times a day. If necessary the dose is gradually increased to 1200 mg the day divided into 2-3 receptions. The maximum daily dose - 1200 mg. Course of treatment 1-3 months. At patients with a chronic renal failure (clearance of creatinine less than 10 ml/min.) the dose is reduced twice. Duration of treatment and the mode of dosing by Pentoksifillin are established by the attending physician individually, depending on a clinical picture of a disease and the gained therapeutic effect.

Features of use:

Patients with the expressed renal failures at Pentoksifillin's reception need especially careful medical observation. If during use of drug for patients there are eye retinal apoplexies, then drug is immediately cancelled. Treatment should be carried out under control of arterial pressure. At the patients with a diabetes mellitus accepting hypoglycemic means, appointment in high doses can cause a 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 level of hemoglobin and a hematocrit is necessary. 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.

Side effects:

- from the central nervous system: headache, dizziness; uneasiness, sleep disorders; spasms.
- from integuments and a hypodermic fatty tissue: 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: dryness in a mouth, a loss of appetite, an intestines atony, an exacerbation of cholecystitis, cholestatic hepatitis.
- from sense bodys: vision disorder, scotoma.
- from cardiovascular system: tachycardia, arrhythmia, cardialgia, progressing of stenocardia, lowering of arterial pressure.
- from bodies of a hemopoiesis and system of a hemostasis: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; bleedings from vessels of skin, mucous membranes, a stomach, intestines.
- allergic reactions: itch, dermahemia, small tortoiseshell, Quincke's disease, acute anaphylaxis.
- laboratory indicators: increase in activity of "hepatic" transaminases (ALT, nuclear heating plant, LDG) and alkaline phosphatase.

Interaction with other medicines:

Pentoksifillin strengthens effect of heparin, fibrinolitic drugs, theophylline, anti-hypertensive and hypoglycemic means (both insulin, and peroral hypoglycemic means). 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. 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 of patients.

Contraindications:

Hypersensitivity to a pentoksifillin, other derivatives of methylxanthine or other ingredients of a ready dosage form, a porphyria, an acute myocardial infarction, massive bleedings, an eye retinal apoplexy, an acute hemorrhagic stroke, the expressed coronary or cerebral atherosclerosis, the expressed disturbances of a heart rhythm, pregnancy, the feeding period a breast, age up to 18 years (efficiency and safety are not established).

With care: drug is appointed the patient with atherosclerosis of cerebral and/or coronary vessels, especially in cases of arterial hypotension and disturbances of a heart rhythm, heart failure, liver failure. It is also necessary to be careful at Pentoksifillin's appointment the patient with a peptic ulcer of a stomach and duodenum, to the patient who recently transferred an operative measure (risk of developing of bleedings). The patient with labile arterial pressure and with tendency to arterial hypotension and patients with the expressed renal failures the dose is increased on sedately and selected individually.

Overdose:

Symptoms: nausea, dizziness, tachycardia, the expressed lowering of arterial pressure, reddening of integuments, fervescence (fever), agitation, an areflexia, toniko-clonic spasms, vomiting "a coffee thick", arrhythmias, a loss of consciousness. At emergence of the disturbances of the patient described above has to see a doctor urgently.

Treatment: symptomatic. The special attention has to be directed to maintenance of arterial pressure and function of breath. Spasms are removed administration of diazepam. Urgent actions at emergence of heavy anaphylactic reactions (shock): - at emergence of the first signs (perspiration, nausea, cyanosis) immediately stop administration of drug; - in addition to other necessary actions provide lower position of the head and an upper part of a trunk and provide freedom for breath; - urgent medical actions: enter into Epinephrinum (adrenaline). If necessary introduction of Epinephrinum can be repeated.

Storage conditions:

List B. In the dry place protected from light, at a temperature not above 25 °C. To protect from children. Period of validity 2 years. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

The tablets covered with a kishechnorastvorimy cover, 100 mg. On 10 tablets in a blister strip packaging. On 60 tablets in bank of light-protective glass either in bank polymeric or in a bottle polymeric. 6 blister strip packagings or each can or a bottle together with the application instruction are placed in a pack from a cardboard.