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

Excipients: lactose (milk sugar), methylcellulose, water soluble MC 16, calcium stearate, povidone (low molecular weight polyvinylpyrrolidone 12600 ± 2700), potato starch.

Shell accessories: cellulose (acetylphthalyl cellulose), titanium dioxide, vaseline oil, talc, castor oil, beeswax, azorubin (acid red 2 C).

Description:The tablets covered with a cover, pink color, round, biconcave.

Pharmacotherapeutic group:Vasodilator

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

Pentoxifylline improves microcirculation and blood rheology, has a vasodilating effect, blocks the phosphodiesterase and promotes the accumulation of cAMP in cells. Pentoxifylline inhibits the aggregation of platelets and erythrocytes, increases their elasticity, reduces the level of fibrinogen in the plasma and enhances fibrinolysis, which reduces the viscosity of the blood and improves its rheological properties. Has a weak myotropic, vasodilating action, Pentoxifylline several. reduces overall peripheral resistance and slightly dilates coronary vessels.

Generally, Pentoxifylline causes improvement of microcirculation and supply of tissues with oxygen in the brain and limbs, 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-dimethylxanthine (metabolite V). The concentration of metabolite I and V in the blood plasma, respectively, is 5 and 8 times higher than

Pentoxifylline. The time to reach the maximum concentration is 1 hour. The half-life is 0.5 - 1.5 hours. Pentoxifylline is excreted primarily by the kidneys - 94% in the form of metabolites (mainly metabolite V), intestine - 4%, in the first 4 hours up to 90% of the dose is excreted. Excreted in breast milk. With severe renal dysfunction, excretion of metabolites is slow. 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);

- chronic disorders of cerebral circulation of ischemic genesis;

- atherosclerotic and dyscirculatory encephalopathies; Angiopathy (paresthesia, Raynaud's disease);

- trophic disorders of tissues due to violation of the arterial or venous microcirculation (trophic ulcers, post-trombophlebitic syndrome, chilblain, 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 hemorrhagic stroke, severe coronary or cerebral atherosclerosis, severe heart rhythm disturbances, pregnancy, lactating period, age to 18 years (efficacy and safety not established).

Carefully:

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

Patients with labile arterial blood pressure and co, 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 taken inside after eating, swallowed whole, washed down with a small amount of water. Take 200 mg (2 tablets) 3 times a day. After reaching the therapeutic effect (usually 1 to 2 weeks), the dose is reduced to 100 mg (1 tablet) 3 times a day.

The maximum daily dose is 1200 mg. The course of treatment 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 dosing 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: hyperemia of the skin of the face, "tides" of blood to the skin of the face and upper chest, swelling, increased brittleness 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 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, skin hyperemia, urticaria, angioedema, anaphylactic shock.

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

Overdose:

Symptoms: weakness, dizziness, decreased blood pressure, fainting, tachycardia, drowsiness or agitation, loss of consciousness, hyperthermia, areflexia, TO- Nico-clonic seizures, signs of gastrointestinal bleeding (vomiting-type "coffee grounds").

Treatment: gastric lavage followed by the injection of activated charcoal, symptomatic therapy (incl.measures to maintain breathing and blood pressure), emergency measures for bleeding.

Interaction:

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

Pentoxifylline can enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandol, cefoperaZona, 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 with hemorrhages 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, taking hypoglycemic agents, the appointment in large doses can cause hypoglycemia (dose adjustment is required). At appointment simultaneously with anticoagulants it is necessary to watch carefully indicators of a coagulating system of a blood. In patients who had recently undergone surgery,

a systematic control of hemoglobin and hematocrit. In elderly people, a dose reduction may be required (increased bioavailability and reduced rate of excretion). Smoking can reduce the therapeutic effectiveness of the drug.

Effect on the ability to drive transp. cf. and fur:

Intestine-soluble film coated tablets, 100 mg.

For 10 tablets in a planar cell package.

At 20.30, 60 tablets in a can of orange glass or in a polymer can.

One bank or 2, 3, 6 contour squares, together with instructions for use, are placed in a cardboard box.

Packaging:(10) - packings, cellular, outline (2) - packs, cardboard
(10) - packings, cellular, outline (3) - packs, cardboard
(10) - packings, cell planimetric (6) - packs cardboard
(20) - polymer cans (1) - cardboard packs
(20) - cans of dark glass (1) - packs of cardboard
(30) - polymer cans (1) - packs of cardboard
(30) - cans of dark glass (1) - packs of cardboard
(60) - polymer cans (1) - packs cardboard
(60) - cans of dark glass (1) - packs of cardboard

Storage conditions:

List B. In a dry place inaccessible to children, at a temperature of no higher than 25 ° C.

Shelf life:2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005034/08

Date of registration:30.06.2008

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp25.08.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)