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

Spasmolytic agent from the group of purines. Improves microcirculation and rheological properties of blood. The mechanism of action is associated with the inhibition of phosphodiesterase and an increase in the concentration of cyclic AMP in platelets and ATP in erythrocytes with a simultaneous saturation of the energy potential, which in turn leads to vasodilation, a decrease in total peripheral vascular resistance, an increase in the shock and minute volume of blood without a significant change in the heart rate Heart rate).

Expanding the coronary arteries, increases oxygen delivery to the myocardium (anti-anginal effect), lung vessels - improves oxygenation of the blood.

Increases the tone of the respiratory musculature (intercostal muscles and diaphragm).

Reduces the viscosity of the blood, increases the elasticity of the erythrocyte membrane (due to the effect on the pathologically altered erythrocyte deformability).Improves microcirculation in areas of impaired blood circulation. In the occlusive lesion of peripheral arteries ("intermittent" lameness) leads to an elongation of the distance of walking, elimination of night cramps of gastrocnemius muscles and pain at rest.

Pharmacokinetics:

After oral administration pentoxifylline almost completely absorbed from the gastrointestinal tract. The prolonged form ensures continuous release of the active substance and its uniform absorption. 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 metabolites I and V in the blood plasma, respectively, is 5 and 8 times higher than pentoxifylline. The time to reach the maximum concentration for prolonged forms is 2-4 hours. It is distributed evenly. 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%), for the first 4 hour up to 90% of the dose. 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 blood circulation caused by atherosclerosis, diabetes mellitus (diabetic angiopathy); obliterating endarteritis.

- 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);

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

- hearing disorders of vascular genesis.

Contraindications:

- Hypersensitivity to pentoxifylline, other methylxanthines or to any of the components of the drug;

- massive bleeding;

- hemorrhage in the retina of the eye;

- hemorrhage in the brain;

- acute myocardial infarction;

- porphyria;

- severe arrhythmias;

- severe atherosclerotic lesions of the coronary or cerebral arteries;

- acute hemorrhagic stroke;

- uncontrolled arterial hypotension;

- age under 18 years (effectiveness and safety not established);

- pregnancy, lactation.

Carefully:

the drug should be used in patients with arterial hypotension (risk of lowering blood pressure), peptic ulcer and duodenal ulcer, chronic heart failure, impaired renal function (creatinine clearance below 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), increased tendency to bleeding, including as a result of the use of anticoagulants or in the case of disorders in the system coagulated I have the blood (the risk of more severe bleeding), recently transferred after surgical interventions.

Pregnancy and lactation:

The use of pentoxifylline is contraindicated during pregnancy. The issue of stopping breastfeeding or abolishing pentoxifylline therapy should be addressed, given its importance to the mother.

Dosing and Administration:

Inside after eating, not liquid, squeezed with enough water.

The drug is prescribed 400 mg (1 tablet) 2-3 times a day. The maximum daily dose is 1200 mg. The course of treatment is recommended by a doctor.

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.

The clinical effect is achieved within 2-4 weeks, but therapy is recommended to continue for at least 8 weeks to adequately assess the effectiveness.

In patients with chronic renal insufficiency (creatinine clearance less than 10 ml / min.), it is necessary to reduce the dose of the drug in half.

In patients on hemodialysis, it is recommended to begin treatment with a daily dose of 400 mg, followed by a gradual increase in the dose (no earlier than 4 days) until the usual recommended.

Side effects:

From the central and peripheral nervous system: headache, dizziness, anxiety, sleep disorders, 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: xerostomia, anorexia, intestinal atony, nausea, vomiting, diarrhea, increased activity of "liver" enzymes, alkaline phosphatase, cholestatic hepatitis, exacerbation of cholecystitis.

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

From the hemostasis and hematopoiesis system: leukopenia, thrombocytopenia, pancytopenia, bleeding from the vessels of the skin, mucous membranes of the stomach, intestines, hypofibrinogenemia.

From the sense organs: impaired vision, scotoma;

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

Other: hypoglycemia.

Overdose:

Symptoms: weakness, sweating, nausea, cyanosis, dizziness, lowering of arterial pressure, tachycardia, fainting, drowsiness or agitation, arrhythmia, hyperthermia, areflexia, loss of consciousness, tonic-clonic convulsions, signs of gastrointestinal bleeding ("coffee grounds" vomiting).

Treatment: gastric lavage followed by the introduction of activated charcoal.Symptomatic therapy: measures aimed at maintaining the function of breathing and blood pressure; emergency measures for bleeding.

Interaction:

Pentoxifylline may enhance the action of blood pressure lowering agents (angiotensin-converting enzyme (ACE) inhibitors, nitrates).

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.

Ciprofloxacin increases the concentration of pentoxifylline in the blood plasma, so it is recommended to reduce the concentration of pentoxifylline by half.

Ketorolac increases prothrombin time and risk of bleeding. The risk of bleeding also increases with simultaneous reception with meloxicam.

Cimetidine increases the concentration of pentoxifylline in the blood plasma (risk of side effects). Other H2 receptor blockers (famotidine, ranitidine and nisatidine) to a lesser extent affect the metabolism of pentoxifylline.

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

The hypoglycemic effect of insulin or oral hypoglycemic agents can be enhanced by taking pentoxifylline (an increased risk of developing hypoglycemia). Strict monitoring of such patients is necessary.

In some patients, simultaneous administration of pentoxifylline and theophylline may lead to an increase in the level of theophylline. This may lead to an increase or increase in side effects associated with theophylline.

Special instructions:

Treatment should be carried out under the control of arterial pressure.

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

At appointment simultaneously with anticoagulants it is necessary to watch carefully indicators of a coagulating system of a blood.

Patients who have recently undergone surgery need systematic monitoring of hemoglobin and hematocrit.

The administered dose should be reduced in patients with low and unstable blood pressure.

In elderly people, a dose reduction may be required (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.

Effect on the ability to drive transp. cf. and fur:there is no evidence of the effect of pentoxifylline on the ability to drive or other mechanical means.

Form release / dosage:

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

Packaging:10 tablets in a blister pack. 2 blisters per cardboard pack together with instructions for use.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N014830 / 02

Date of registration:24.06.2008

Date of cancellation:2017-04-28

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, dd, Novo mesto, AO Slovenia

Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Information update date: & nbsp28.04.2017

Illustrated instructions

Instructions

Pentylin (Pentilin)