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

lactose (milk sugar), potato starch, povidone (Kollidon 25), methylcellulose or giprolose (hydroxypropyl cellulose Klucel), stearic acid, silicon dioxide colloid (aerosil);

shell:

acryl-from: methacrylic acid copolymer with ethyl acrylate 1: 1, titanium dioxide E 171, talc, triethyl citrate, silicon dioxide colloid, sodium bicarbonate, sodium lauryl sulfate.

Description:tablets, coated with enteric coating of white color, round, biconvex. On the fracture is white or almost white.

Pharmacotherapeutic group:vasodilator

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

Pentoxifylline is a derivative of xanthine. Improves microcirculation and rheological properties of blood. The mechanism of action is associated with the inhibition of phosphodiesterase and an increase in the content of cyclic adenosine monophosphate in platelets and adenosine triphosphate in erythrocytes, while saturating the energy potential, which in turn leads to vasodilation, a decrease in total peripheral vascular resistance, an increase in systolic and minute heart volume without a significant change in the heart rate.

Expanding coronary artery, increasing oxygen delivery to the myocardium (antianginal effect), lung vessels - improves blood oxygenation.

Increases the tone of the respiratory musculature (intercostal muscles and diaphragm). It leads to an increase in the content of adenosine in the brain, a positive effect on the bioelectrical activity of the central nervous system.

Reduces the viscosity of the blood, causes disaggregation of platelets, increases the elasticity of the erythrocyte membrane (due to the effect on the pathologically altered erythrocyte deformity). Improves microcirculation in areas of impaired blood circulation.

In the occlusive lesion of peripheral arteries (intermittent claudication), leads to an elongation of the walking distance, elimination of night cramps of calf muscles and pain at rest.

Pharmacokinetics:

The drug is rapidly metabolized in the liver. In the process of metabolism, several active metabolites are formed, the main ones being metabolite 1 and metabolite 5. Their concentrations in the blood plasma are 5 and 8 times (respectively) higher than the concentration of the starting substance.

Time to reach the maximum concentration in the blood plasma -1h. The half-life is 0,5 - 1,5 hours.

It is excreted by the kidneys in the form of metabolites (94%) and through the intestine (4%), in the first 4 hours up to 90% of the dose is excreted. Unchanged, 2% of the drug is excreted.

Excreted in breast milk.

Pentoxifylline and its metabolites do not bind to blood plasma proteins.

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:

- Violations of peripheral blood circulation caused by atherosclerosis, diabetes mellitus (diabetic angiopathy);

- Chronic disorders of cerebral circulation of ischemic genesis;

- Atherosclerotic and discirculatory encephalopathy; Angiopathy (paresthesia, Raynaud's disease);

- Trophic tissue disorders due to violation of arterial or venous microcirculation (trophic ulcers, postthrombophlebitic syndrome, frostbites, gangrene);

- Obliterating endarteritis;

- Disturbances of blood circulation in the vessels of the eye (acute and chronic circulatory insufficiency in the retina or choroid of the eye);

- Disorders of the function of the middle ear of vascular genesis, accompanied by deafness.

Contraindications:

Hypersensitivity to pentoxifylline and other methylxanthine derivatives; acute myocardial infarction; massive bleeding; acute hemorrhagic stroke, hemorrhage in the retina of the eye; pregnancy; lactation period; age to 18 years (efficacy and safety not established).

Carefully:

Carefully the drug is prescribed for atherosclerosis of cerebral and / or coronary vessels, especially in cases of arterial hypotension and rhythm disturbances; chronic heart failure, hepatic and / or renal failure. Care should also be taken when administering pentoxifylline to patients with gastric ulcer and duodenal ulcer, patients who have recently undergone surgical intervention (risk of bleeding).

Not recommended for lactose intolerance, galactosemia, glucose / galactose absorption disorder.

Pregnancy and lactation:contraindicated

Dosing and Administration:

Inside after eating, without chewing and washing down with enough water.

Duration of treatment and dosing regimen are set individually by the attending physician, depending on the clinical picture of the disease and the therapeutic effect. The drug is taken starting with 200 mg (2 tablets) 3 times a day during the first week; with a sharp arterial hypotension and symptoms of irritation from the gastrointestinal tract or the central nervous system, the initial dose is reduced to 100 mg (1 tablet) 3 times a day.

At course treatment appoint 100 mg (1 tablet) 3 times a day. The maximum daily dose is 1200 mg. The course of treatment is recommended by a doctor.

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

Side effects:

From the central nervous system: headache, dizziness; anxiety, sleep disturbances; convulsions; aseptic meningitis (rarely).

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, nausea, vomiting, 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 (including from the mucous membranes of the stomach, intestines), nosebleeds.

Allergic reactions: skin itching, skin hyperemia, urticaria, angioedema, anaphylactic shock.

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

Overdose:

Symptoms: weakness, dizziness, tachycardia, marked decrease in blood pressure, fainting, drowsiness or arousal, loss of consciousness, hyperthermia, areflexia, tonic-clonic convulsions, signs of gastrointestinal bleeding (vomiting like "coffee grounds").

Treatment: gastric lavage followed by the introduction of activated charcoal, symptomatic therapy (including measures aimed at maintaining respiration and blood pressure), urgent measures for bleeding.

Interaction:

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

Pentoxifylline may enhance the effect of drugs affecting the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandol, cefaperazone, 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 have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit concentration is necessary. In elderly patients a dose reduction may be required (increased bioavailability and reduced elimination rate). Smoking can reduce the therapeutic effectiveness of the drug.

In case of lactose intolerance or insufficiency of the corresponding enzyme, one should take into account that 1 tablet Pentoxifylline contains in its composition 25 mg of lactose.

Form release / dosage:

Intestine-soluble film coated tablets, 100 mg.

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

6 contour mesh packages together with instructions for use are placed in a pack of cardboard.

Packaging:(10) - packings, cell planimetric (6) - packs cardboard

Storage conditions:

In the dark place at a pacenot higher than 25 ° С.

Keep out of the reach of children.

Shelf life:

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

Terms of leave from pharmacies:On prescription

Registration number:P N002791 / 01

Date of registration:22.07.2008

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Representation: & nbspVALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Information update date: & nbsp25.08.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)