Instructions Pentoxifylline enteric-coated tablets 100 mg No. 50
Composition
active ingredient: pentoxifylline;
1 tablet contains 100 mg of pentoxifylline;
Excipients: lactose monohydrate, potato starch, magnesium stearate, hypromellose (hydroxypropylmethylcellulose), povidone, methacrylate copolymer dispersion, propylene glycol, talc, titanium dioxide (E 171), carmoisine (E 122).
Dosage form
Enteric-coated tablets.
Main physicochemical properties: round, film-coated tablets of pink color, convex on the upper and lower surfaces. When broken, when viewed under a magnifying glass, a core surrounded by a single solid layer is visible.
Pharmacotherapeutic group
Peripheral vasodilators. Pentoxifylline.
ATX code C04A D03.
Pharmacological properties
Pharmacodynamics
Pentoxifylline is a methylxanthine derivative. The mechanism of action of pentoxifylline is associated with the inhibition of phosphodiesterase and the accumulation of cAMP in vascular smooth muscle cells, blood cells, and other tissues and organs. Pentoxifylline inhibits platelet and erythrocyte aggregation, increases their flexibility, reduces the increased concentration of fibrinogen in blood plasma and enhances fibrinolysis, which reduces blood viscosity and improves its rheological properties. In addition, pentoxifylline causes a weak myotropic vasodilator effect, slightly reduces total peripheral vascular resistance and has a positive inotropic effect. As a result of the use of pentoxifylline, microcirculation and tissue oxygen supply improve, most of all in the extremities, central nervous system, moderately in the kidneys. The drug slightly dilates coronary vessels.
Pharmacokinetics
The main pharmacologically active metabolite 1-(5-hydroxyhexyl)-3,7-dimethylxanthine (metabolite I) is determined in blood plasma at a concentration exceeding the concentration of the unchanged substance by 2 times and is in a state of reverse biochemical equilibrium with it. In this regard, pentoxifylline and its metabolite should be considered as an active whole. The half-life of pentoxifylline is 1.6 hours.
Pentoxifylline is completely metabolized, more than 90% is excreted by the kidneys in the form of
unconjugated water-soluble polar metabolites. Less than 4% of the administered dose is excreted in the feces. In patients with severe renal impairment, excretion of metabolites is slowed. In patients with impaired liver function, a prolongation of the half-life of pentoxifylline is noted.
Indication
Atherosclerotic encephalopathy; ischemic cerebral stroke; dyscirculatory encephalopathy; peripheral circulatory disorders caused by atherosclerosis, diabetes mellitus (including diabetic angiopathy), inflammation; trophic disorders in tissues associated with venous damage or impaired microcirculation (postthrombophlebitic
syndrome, trophic ulcers, gangrene, frostbite); obliterating endarteritis; angioneuropathy (Raynaud's disease); circulatory disorders of the eye (acute, subacute, chronic circulatory insufficiency in the retina and choroid of the eye); disorders of the inner ear of vascular origin, which are accompanied by hearing loss.
Contraindication
Pentoxifylline is contraindicated:
patients with hypersensitivity to pentoxifylline, other methylxanthines or any of the excipients of the drug; patients with massive bleeding (risk of increased bleeding); patients with extensive retinal hemorrhage, with cerebral hemorrhage (risk of increased bleeding). If retinal hemorrhage occurs during treatment with pentoxifylline, the drug should be discontinued immediately; patients in the acute period of myocardial infarction; patients with gastric and/or intestinal ulcers; patients with hemorrhagic diathesis.
Interaction with other medicinal products and other types of interactions
The blood sugar-lowering effect of insulin or oral antidiabetic agents may be potentiated. Therefore, patients receiving drug treatment for diabetes should be closely monitored.
In the post-marketing period, cases of increased anticoagulant activity have been reported in patients receiving concomitant treatment with pentoxifylline and
Vitamin K antagonists. When prescribing or changing the dosage of pentoxifylline, it is recommended to monitor anticoagulant activity in this group of patients.
Pentoxifylline may enhance the hypotensive effect of antihypertensive agents and other drugs that may cause a decrease in blood pressure.
Concomitant use of pentoxifylline and theophylline may lead to increased blood levels of theophylline in some patients. Therefore, an increase in the frequency and severity of adverse reactions to theophylline is possible.
Potential additive effect with platelet aggregation inhibitors: Due to the increased risk of bleeding, concomitant use of platelet aggregation inhibitors (e.g. clopidogrel, eptifibatide, tirofiban, epoprostenol, iloprost, abciximab, anagrelide, NSAIDs other than selective COX-2 inhibitors, acetylsalicylates [ASA/LAS], ticlopidine, dipyridamole) with pentoxifylline should be done with caution.
Concomitant use with cimetidine may increase the concentration of pentoxifylline and metabolite I in blood plasma.
Application features
At the first signs of an anaphylactic/anaphylactoid reaction, treatment with Pentoxifylline should be discontinued immediately and medical attention should be sought.
When using Pentoxifylline in patients with chronic heart failure, the phase of circulatory compensation should first be achieved.
In patients with diabetes mellitus and receiving treatment with insulin or oral antidiabetic agents, the use of high doses of Pentoxifylline may increase the effect of these drugs on blood sugar levels (see section "Interaction with other medicinal products and other types of interactions").
In these cases, the dose of insulin or oral antidiabetic agents should be reduced and the patient should be monitored closely.
Patients with systemic lupus erythematosus (SLE) or other connective tissue diseases
Pentoxifylline should only be prescribed after a thorough analysis of the possible risks and benefits.
Since there is a risk of developing aplastic anemia during treatment with pentoxifylline, regular monitoring of complete blood counts is required.
In patients with renal insufficiency (creatinine clearance less than 30 ml/min) or severe liver dysfunction, the elimination of pentoxifylline may be delayed. Appropriate monitoring is required.
Particularly careful supervision is necessary for:
patients with severe cardiac arrhythmias; patients with arterial hypotension; patients with severe atherosclerosis of cerebral and coronary vessels, especially with concomitant arterial hypertension and heart rhythm disturbances. These patients may experience attacks of angina pectoris, arrhythmia and arterial hypertension when taking the drug; patients with renal failure (creatinine clearance below 30 ml/min); patients with severe hepatic failure;
patients with a high tendency to bleed, for example due to anticoagulant treatment or blood clotting disorders. For bleeding, see section "Contraindications";
patients who have recently undergone surgical treatment (increased risk
bleeding, which requires systematic monitoring of hemoglobin and hematocrit levels); patients for whom a decrease in blood pressure is a high risk (for example, patients with severe ischemic heart disease or stenosis of the vessels supplying
blood to the brain);
patients receiving concomitant treatment with pentoxifylline and antagonists
vitamin K or platelet aggregation inhibitors (see section "Interaction with other medicinal products and other types of interactions");
patients receiving concomitant treatment with pentoxifylline and antidiabetic agents (see section "Interaction with other medicinal products and other types of interactions");
patients receiving simultaneous treatment with pentoxifylline and ciprofloxacin (see section "Interaction with other medicinal products and other types of interactions");
patients receiving concomitant treatment with pentoxifylline and theophylline (see section "Interaction with other medicinal products and other types of interactions").
The drug contains lactose, therefore patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use the drug.
Ability to influence reaction speed when driving vehicles or other mechanisms
There is no data, but the possibility of adverse reactions from the nervous system and visual organs should be taken into account.
Use during pregnancy or breastfeeding
Pregnancy.
There is insufficient experience with the use of the drug in pregnant women, therefore, prescribing Pentoxifylline during pregnancy is not recommended.
Breast-feeding.
Pentoxifylline passes into breast milk in small amounts, so breastfeeding should be discontinued during treatment with Pentoxifylline.
Method of administration and doses
Pentoxifylline is prescribed in the amount of 2-4 tablets 2-3 times a day. The tablets should be taken after meals, without chewing, with sufficient liquid. The maximum daily dose should not exceed 1.2 g.
For patients with labile or low blood pressure or with significantly reduced renal function (creatinine clearance less than 30 ml/min); for patients at particular risk of the consequences of lowering blood pressure (for example, with severe coronary artery disease, severe stenosis of the main cerebral vessels), treatment should be started with low doses, selected individually and increased gradually, taking into account the tolerability of treatment.
Children
There is no experience with the use of the drug in children.
Overdose
Initial symptoms of acute overdose with pentoxifylline are nausea, dizziness or decreased blood pressure. In addition, symptoms such as fever, agitation, hot flashes, tachycardia, loss of consciousness, areflexia, arrhythmia, tonic-clonic seizures and vomiting of "coffee grounds" as a sign of gastrointestinal bleeding may develop.
Overdose treatment
In order to treat acute overdose and prevent complications, general and specific intensive medical supervision and therapeutic measures are necessary.
Adverse reactions
Some patients may experience side effects of the drug, namely:
Cardiovascular system: arrhythmia, tachycardia, angina pectoris, hypotension/hypertension, hot flashes, peripheral edema;
from the blood system and blood-forming organs: thrombocytopenia with thrombocytopenic purpura, aplastic anemia (partial or complete cessation of the formation of all blood cells, pancytopenia), which can be fatal, bleeding, leukopenia/neutropenia;
from the nervous system: dizziness, headache, aseptic meningitis, tremor, paresthesia, convulsions, agitation and sleep disturbances, hallucinations;
Gastrointestinal: gastrointestinal disorders, feeling of pressure in the stomach, flatulence, nausea, vomiting or diarrhea, constipation, hypersalivation;
Skin and subcutaneous tissue disorders: itching, redness of the skin and urticaria, toxic epidermal necrolysis and Stevens-Johnson syndrome, rash;
from the immune system: anaphylactic reactions, anaphylactoid reactions, angioedema, bronchospasm and anaphylactic shock;
Liver and biliary tract: intrahepatic cholestasis;
on the part of the organs of vision: visual impairment, conjunctivitis, retinal hemorrhages, retinal detachment;
laboratory indicators: increased transaminase levels;
Other: cases of hypoglycemia, increased sweating, and increased body temperature have been reported.
Expiration date
3 years.
Storage conditions
Store in original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Packaging
10 tablets in a blister, 5 blisters in a cardboard pack.
Vacation category
According to the recipe.
Producer
Technolog PJSC.
Location of the manufacturer and its business address
Ukraine, 20300, Cherkasy region, Uman city, Stara Prorizna Street, building 8.
