Pentoxifylline-SZ - instructions for use, dose, side effects, contraindications

Active substance: pentoxifylline in recalculation on 100% a substance - 100 mg. Excipients: calcium stearate - 1.6 mg, starch potato - 7.5 mg, hypromellose (hydroxypropylmethylcellulose) 1.7 mg, lactose monohydrate (milk sugar) 40.0 mg, povidone (low molecular weight polyvinylpyrrolidone) 9.2 mg.

Shell composition: hypromellose (hydroxypropylmethylcellulose) 0.7 mg, polysorbate 80 (tween 80) 0.3 mg, Acryl from (methacrylic acid copolymer with ethyl acrylate 1: 1 (40.0%), titanium dioxide (15.0%), talc (37.25%), triethyl citrate (4.8% %), silicon colloidal oxide anhydrous (1.25%), sodium hydrogen carbonate (1.2%), sodium lauryl sulfate (0.5%)) - 8.998 mg, acid red 2 C or dye azorubin (carmoazine) 0.002 mg.

Description:

The tablets covered with an enteric-insoluble coat of pink color, round biconcave.

Pharmacotherapeutic group:Vasodilator

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

Pentoxifylline improves microcirculation and rheological properties of blood, has a vasodilating effect, block phosphodiesterase and promote the accumulationcAMP in the cells. Pentoxifylline inhibits the aggregation of platelets and erythrocytes, increases their elasticity, reduces the level of fibrinogen in the plasma and strengthens fibrolysis, which reduces the viscosity of blood and improves its rheological properties. Has a weak myotropic, vasodilating action. Pentoxifylline slightly reduces the overall peripheral resistance and slightly dilates the coronary vessels. Generally, Pentoxifylline causes improvement of microcirculation and supply of tissues with oxygen in the brain and in the extremities, to a lesser extent - in the kidneys.

Pharmacokinetics:

After oral administration Pentoxifylline almost completely absorbed from the gastrointestinal tract. The drug undergoes a "first pass" through the liver with the formation of 2 major pharmacologically active metabolites: 1-5-hydroxyhexyl-3,7-dimethylxanthine (metabolite I) and 1-3-carboxypropyl-3,7- W dimethylxanthine (metabolite V). The concentration of metabolite I and V in the blood plasma, respectively, is 5 and 8 times higher than pentoxifillin. The time to reach the maximum concentration is 1 hour. The half-life is 0.5 to 1.5 hours. Pentoxifylline is excreted mainly by the kidneys - 94 % in the form of Metabolites (mainly metabolite V), intestine - 4 %, for the first 4 hours up to 90% of the dose is output. Excreted in breast milk. With severe renal dysfunction, excretion of metabolites is slowed down. When liver function is disrupted, the half-life is prolonged and bioavailability is increased.

Indications:

- violation of peripheral circulation due to atherosclerosis, diabetes mellitus (diabetic angiopathy);

- acute and chronic disorders of cerebral circulation of ischemic genesis;

- atherosclerotic and discirculatory Encephalopathies; angiopathy (paresthesia, bothe Reynaud slaughter);

- trophic tissue disorders due to disturbances in arterial or venous micsrocirculation (trophic ulcers, postgrasm | jeflebic syndrome, frostbite, gangrene);

- obliterating endarteritis;

- acute, subacute and chronic circulatory insufficiency in the retina or in the choroid of the eye;

- hearing loss of vascular genesis

Contraindications:

Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other ingredients of the finished dosage form, porphyria, acute myocardial infarction, massive bleeding, retinal hemorrhage, acute hemorrhagesacute stroke, severe coronary or cerebral atherosclerosis, severe cardiac arrhythmias, pregnancy, breastfeeding, age under 18 (efficacy and safety not establisheds).

Carefully:

Carefully: the drug is prescribed to patients with atherosclerosis of cerebral and / or coronary vessels, especially in cases of arterial hypotension and heart rhythm disorders, heart failure, hepatic insufficiency. Care should also be taken when Pentoxifylline is administered to patients with peptic ulcer and duodenal ulcer,recently underwent surgical intervention (risk of bleeding).

Patients with labile arterial pressure and a tendency to arterial hypotension and patients with severe renal dysfunction increase the dose gradually and select individually.

Pregnancy and lactation:contraindicated

Dosing and Administration:

Pentoxifylline is taken orally after dosing. The tablets are covered with a special shell, soluble in the intestines, so they are swallowed whole, washed down with a small amount of water. Take 200 mg (2 tablets) 3 times a day. If necessary, the dose is gradually increased to 1200 mg per day, divided into 2-3 doses. The maximum daily dose is 1200 mg. The course is treated for 1-3 months.

In patients with chronic renal failure (creatinine clearance less than 10 ml / min), the dose is halved.

The duration of treatment and the dosage regimen of Pentoxifylline are established by the attending physician individually, depending on the clinical picture of the disease and the therapeutic effect obtained.

Side effects:

From the central nervous system: headache, dizziness; anxiety, sleep disturbances; convulsions.

From the skin and subcutaneous fat tissue: facial flushing, "tides" of blood to the face and upper Thurs | £ ti chest, swelling, increased fragility of the nails.

From the digestive system: dry mouth, decreased appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis.

From the sense organs: impaired vision, scotoma.

From the side of the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina, lowering of arterial pressure.

On the part of the organs of hematopoiesis and the system of hemostasis: Thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; bleeding from the vessels of the skin, mucous membranes, stomach, intestines.

Allergic reactions: itching, hyperemia fzhi, urticaria, angioneurotic edema, anaphylactic shock.

Laboratory indicators: increased activity of "liver" transaminases (ALT, ACT, LDH) and alkaline phosphatase.

Overdose:

Symptoms: nausea, dizziness, tachycardia, pronounced decrease in blood pressure, skin redness, fever (chills), agitation, areflexia, tonic-clonic convulsions, vomiting "coffee grounds", arrhythmias,loss of consciousness

If the above described violations occur, the patient should urgently consult a doctor.

Treatment: symptomatic. Particular attention should be directed to maintaining blood pressure and respiratory function, 'Cramps are removed by the introduction of diazepam. Urgent measures in the event of severe anaphylactic reactions (shock):

- when the first signs appear (potlivrst, nausea, cyanosis) immediately stop taking the drug;

- in addition to other necessary measures, provide a lower position of the head and upper body and provide freedom for breathing;

- urgent medical measures: introduces IV epinephrine (adrenalin). If necessary, the introduction of epinephrine can be repeated.

Interaction:

Pentoxifylline enhances the action of heparin, fibrinolytic drugs, theophylline, antihypertensive and hypoglycemic agents (both insulin and oral hypoglycemic agents).

Pentoxifylline may enhance the action of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins cefamandola, cefoperazone, cefotetana),valproic acid.

Cimetidine increases the concentration of pentoxifylline in the blood plasma (risk of side effects).

Co-administration with other xanthines can lead to excessive nervous excitement of patients.

Special instructions:

Patients with severe renal impairment when taking Pentoxifylline require particularly careful medical supervision. In the event that during the period of application of the drug in patients bleeding occurs in the retina of the eye, the drug is immediately canceled. Treatment should be carried out under the control of arterial pressure. In patients with diabetes mellitus, limiting gipoglikemicakie funds, the appointment in large doses can cause hypoglycemia (requires dose adjustment). At appointment simultaneously with anticoagulants it is necessary to watch carefully indicators of a coagulating system of a blood. In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit is necessary. In elderly people, dose reduction may be required (increased bioavailability and reduced rate of excretion). Smoking can reduce the therapeutic effectiveness of the drug.

Form release / dosage:

Intestine-soluble tablets shell, 100 mg.

10 or 30 tablets in a planar cell packaging.

60 tablets in a polymer jar or vial polymer.

6 contour mesh packages for 10 tablets, 2, 4 contour spinal

packs of 30 tablets or each jar or a bottle together with the instructions for

application in a cardboard bundle.

Packaging:(10) - packings, cell planimetric (6) - packs cardboard
(30) - packings cellular planimetric (2) - packs cardboard
(30) - packings cellular planimetric (4) - packs cardboard
(60) - polymer cans (1) - packs cardboard
(60) - polymer bottles (1) - packs cardboard

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004868/07

Date of registration:17.12.2007

The owner of the registration certificate:NORTH STAR, CJSC NORTH STAR, CJSC Russia

Manufacturer: & nbsp

NORTH STAR, CJSC Russia

Information update date: & nbsp26.08.2015

Illustrated instructions

Instructions

Pentoxifylline-SZ (Pentoxifylline-SZ)