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

The xanthine derivative. Improves rheological properties of blood (fluidity) due to the impact on pathologically altered erythrocyte deformability, inhibiting platelet aggregation and decreasing the increased blood viscosity. Improves microcirculation in areas of impaired blood flow. The mechanism of action is associated with the inhibition of phosphodiesterase and the accumulation of cyclic adenosine monophosphate (cAMP) in the cells of the smooth muscles of the vessels and in the shaped elements of the blood.

Having a weak myotropic vasodilating effect, somewhat reduces the overall peripheral resistance and slightly dilates the coronary vessels.

With occlusive lesions of peripheral arteries contributes to the elongation of the distance of walking, the elimination of night cramps in the gastrocnemius muscles, the reduction of pain at rest.

When the cerebral circulation is disturbed, it improves the symptoms.

Pharmacokinetics:

After oral administration pentoxifylline almost completely absorbed from the gastrointestinal tract. The prolonged form provides continuous release and its uniform absorption.Bioavailability is 6-32%.

At oral reception undergoes "the first passage" through a liver with formation of two basic pharmacologically active metabolites: 1-5-hydroxyhexyl-3,7-dimethylxanthine (metabolite I) and 1-3-carboxypropyl-3,7-dimethylxanthine (metabolite V). The concentration of metabolites I and V in the plasma, respectively, is 5 and 8 times higher than pentoxifylline.

The intake of food increases the maximum concentration (Cmax) and the area under the "concentration-time" curve (AUC) pentoxifylline by 28% and 13%, respectively; The metabolite I rate is increased by 20%. The time to reach the maximum concentration (TCam) for prolonged forms is 2-4 hours. The half-life (T1 / 2) after oral administration is 0.4-0.8 hours, metabolites 1-1.6 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 slowed down. When liver function is disrupted, the half-life is prolonged and bioavailability is increased.

Indications:

- violations of peripheral circulation against the background of atherosclerotic and diabetic processes (including "intermittent" lameness caused by atherosclerosis, diabetic angiopathy);

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

- symptomatic treatment of the consequences of an ischemic and hemorrhagic stroke;

- symptomatic treatment of atherosclerotic and dyscirculatory encephalopathy (dizziness, memory impairment, sleep disorders, headache);

- symptomatic treatment of circulatory disorders in the vessels of the eye (acute and chronic circulatory insufficiency in the retina or in the choroid of the eye);

- symptomatic treatment of disturbance of the function of the middle ear of vascular genesis, accompanied by hearing loss.

Contraindications:

- hypersensitivity to the components of the drug;

- hypersensitivity to other xanthine derivatives;

- acute myocardial infarction;

- massive bleeding;

- acute phase of hemorrhagic stroke;

- hemorrhage in the retina of the eye;

- pregnancy;

- lactation period;

- age to 18 years.

Carefully:

FROM caution should be used in patients with severe arrhythmias (risk of worsening of arrhythmia); arterial hypotension (riskfurther lowering of blood pressure (BP)); chronic heart failure; peptic ulcer of the stomach and duodenum; impaired renal function (creatinine clearance (CK) less than 30 ml / min) (risk of cumulation and an increased risk of side effects); severe impairment of liver function (risk of cumulation and an increased risk of side effects); after recently transferred surgical interventions; with a tendency to bleeding, for example, as a result of the use of anticoagulants or with violations from the coagulation system (the risk of developing more severe bleeding).

Pregnancy and lactation:The drug is contraindicated for use during pregnancy. Penetrates into breast milk, during the treatment should stop breastfeeding.

Dosing and Administration:

Inside during or immediately after eating, without chewing, squeezed with enough water.

The drug is prescribed 400 mg 2-3 times a day. The maximum daily dose is 1200 mg. 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 obtained.

In patients with severe renal dysfunction (CC less than 30 ml / min), the dose of the drug should be reduced to 400-800 mg / day.

In patients with hepatic insufficiency, the dose of the drug is reduced taking into account individual tolerance.

In patients with arterial hypotension, as well as in people at risk for possible reduction in blood pressure (patients with severe ischemic heart disease (CHD) or with hemodynamically significant stenoses of cerebral vessels), treatment can be initiated in small doses, followed by a gradual increasing the dose.

Side effects:

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

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: nausea, vomiting, diarrhea, dryness of the oral mucosa, anorexia, intestinal atony, sensation of pressure and overfilling of the stomach, intrahepatic cholestasis.

From the sense organs: impaired vision, scotoma.

From the side of the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina, reduction of blood pressure.

On the part of the organs of hematopoiesis and the system of hemostasis: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia, bleeding (including from the vessels of the skin, mucus. shiny shells, stomach, intestines).

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

Laboratory indicators: increased activity of "hepatic" transaminases: alanine-minotransferase (ALT), aspartateamotransferase (ACT), lactate dehydrogenase (LDH) and alkaline phosphatase.

Overdose:

Symptoms: dizziness, nausea, marked decrease in blood pressure, chills, skin flushing, signs of gastrointestinal bleeding (vomiting like "coffee grounds"), tachycardia, arrhythmia, loss of consciousness, areflexia, clonic convulsions. Treatment: drug cancellation, gastric lavage, taking activated charcoal, giving the patient a horizontal position with raised legs, symptomatic treatment (measures aimed at maintaining respiration and blood pressure), with cramps injected diazepam.

Interaction:

Pentoxifylia can enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandol, cefapperazone, cefotetana).

Strengthens the hypotensive effect of angiotensin-converting enzyme (ACE) inhibitors and nitrates, insulin and oral hypoglycemic drugs (risk of hypoglycemia).

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

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

With the simultaneous use of pentoksifillina and theophylline, it is possible to increase the concentration of theophylline in the blood plasma and increase its side effect.

Special instructions:

Treatment should be carried out under the control of blood pressure. The administered dose should be reduced in patients with low and unstable pressure.

In patients with diabetes mellitus, taking hypoglycemic drugs, the appointment in large doses can cause severe hypoglycemia (dose adjustment is required).

When used concomitantly with anticoagulants, care should be taken to closely monitor blood coagulation system performance.

In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit is necessary.

Elderly people may need to reduce the dose (increased bioavailability and reduced rate of excretion).

The safety and efficacy of pentoxifylline in children have not been adequately studied.

Smoking can reduce the therapeutic effectiveness of the drug.

Taking into account possible side effects of the drug, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

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

Form release / dosage:

Tablets of prolonged action, film-coated, 400 mg.

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered. For 30 or 60 tablets in cans of polymeric. Each jar, 3 or 6 contour squares together with instructions for use in a pack of cardboard.

Packaging:(10) - Contoured Cell Pack (3) / 3 Contour Cell Packs of 10 tablets each - Instructions for use - Cardboard package / - Cardboard package
(10) - Contoured Cell Pack (6) / 6 Contour Cell Packs of 10 tablets - instructions for use - cardboard package / - Cardboard package

Storage conditions:

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

Keep out of the reach of children.

Shelf life:2 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LS-001538

Date of registration:17.08.2011

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

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Information update date: & nbsp23.08.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)