Instructions Pentoxin solution for infusion 0.5 mg/ml bottle 200 ml
Composition
active ingredient: pentoxifylline;
1 ml of solution contains 0.5 mg of pentoxifylline;
Excipients: sodium chloride, potassium chloride, calcium chloride dihydrate, sodium lactate, water for injections.
Dosage form
Solution for infusion.
Main physicochemical properties: clear colorless or slightly yellowish liquid.
Pharmacotherapeutic group
Peripheral vasodilators. 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 cyclic adenosine monophosphate (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 has a weak myotropic vasodilator effect, slightly reduces total peripheral vascular resistance, and exhibits 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, and 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 down. In patients with impaired liver function, an increase in 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 damage to veins 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 function of the inner ear of vascular genesis, which are accompanied by hearing loss.
Contraindication
Pentoxin is contraindicated:
– patients with hypersensitivity to pentoxifylline, to other methylxanthines or to any of the excipients of the medicinal product;
– 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 and patients with severe cardiac arrhythmia;
– patients with gastric ulcer 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 who were simultaneously treated 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.
Pentoxin may enhance the hypotensive effect of antihypertensive agents and other drugs that can 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, non-steroidal anti-inflammatory drugs other than selective cyclooxygenase-2 inhibitors, acetylsalicylates [acetylsalicylic acid/lysine acetylsalicylate], ticlopidine, dipyridamole) with pentoxifylline should be carried out with caution.
Concomitant use with cimetidine may increase the concentration of pentoxifylline and metabolite I in blood plasma.
Pentoxifylline should not be used concomitantly with ketorolac due to an increased risk of bleeding and/or prolongation of prothrombin time.
Application features
At the first signs of an anaphylactic/anaphylactoid reaction, Pentoxin should be discontinued immediately and medical attention should be sought.
When using Pentoxin 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, when using high doses of Pentoxin, the effect of these drugs on blood sugar levels may be increased (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 especially carefully.
Patients with systemic lupus erythematosus (SLE) or other connective tissue diseases should be prescribed pentoxifylline only after a thorough analysis of the possible risks and benefits.
Since there is a risk of developing aplastic anemia during treatment with pentoxifylline, regular complete blood counts are 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 observation 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 angina attacks, arrhythmias and arterial hypertension when taking the drug);
– patients with renal insufficiency (creatinine clearance below 30 ml/min);
– patients with severe hepatic insufficiency;
– patients with a high tendency to bleed, due to, for example, treatment with anticoagulants or blood clotting disorders (for bleeding, see the section "Contraindications");
– patients who have recently undergone surgical treatment (increased risk of 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 vitamin K antagonists or platelet aggregation inhibitors (see section “Interaction with other medicinal products and other types of interactions”);
– patients receiving simultaneous 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 simultaneous treatment with pentoxifylline and theophylline (see section “Interaction with other medicinal products and other types of interactions”).
This medicinal product contains 3.0167 mg/ml sodium, which should be taken into consideration by patients on a controlled sodium diet.
Use during pregnancy or breastfeeding
Pregnancy. Experience with the use of the drug in pregnant women is insufficient. Therefore, the use of Pentoxin during pregnancy is not recommended.
Breastfeeding. Pentoxifylline passes into breast milk in small amounts. If Pentoxin is prescribed, breastfeeding should be discontinued.
Ability to influence reaction speed when driving vehicles or other mechanisms
Since the drug is used in a hospital setting, there is no data on such effects.
Method of administration and doses
Intravenous infusions are the most effective and well-tolerated forms of parenteral administration of the drug. The dosage regimen is determined by the doctor and depends on the severity of circulatory disorders, body weight and tolerability of the treatment. Infusion can be carried out only if the solution is clear.
The following treatment regimens are recommended for adults:
In severe cases of the patient's condition (especially in case of persistent pain, gangrene or trophic ulcers), Pentoxin may be infused over 24 hours. With this administration regimen, the dose should be determined at the rate of 0.6 mg/kg/hour. The daily dose calculated in this way for a patient weighing 70 kg is 1000 mg, for a patient weighing 80 kg is 1150 mg. Regardless of the patient's body weight, the maximum daily dose is 1200 mg.
The volume of infusion solution is calculated individually, taking into account concomitant diseases and the patient's condition, and is on average 1–1.5 liters per day.
The duration of parenteral treatment is determined by the treating physician. After the patient's condition improves, it is recommended to continue treatment using the oral form of pentoxifylline.
Children: There is no experience with the use of pentoxifylline in children.
Overdose
Initial symptoms of acute overdose of pentoxifylline are nausea, dizziness, increased or decreased blood pressure. In addition, symptoms such as fever, agitation, hot flashes, tachycardia, loss of consciousness, areflexia, arrhythmia, tonic-clonic seizures and vomit in the form of "coffee grounds" as a sign of gastrointestinal bleeding may develop.
Treatment of overdose should be symptomatic with special attention to cardiovascular support. Special emergency measures may be required to prevent bleeding.
Adverse reactions
The following are adverse reactions that have occurred during clinical trials and post-marketing experience. The frequency of occurrence is unknown.
Laboratory indicators: increased transaminase levels, increased alkaline phosphatase levels.
Gastrointestinal: gastrointestinal disorders, feeling of pressure in the stomach, flatulence, nausea, vomiting, diarrhea, constipation, hypersalivation, anorexia, intestinal atony.
Cardiovascular system: arrhythmia, tachycardia, angina pectoris, cardialgia, decreased blood pressure, increased blood pressure, feeling of tightness behind the sternum, feeling of heat (hot flashes), bleeding (e.g. from the skin, mucous membranes, gastrointestinal tract), peripheral edema.
Blood and lymphatic system disorders: thrombocytopenia with thrombocytopenic purpura and aplastic anemia (partial or complete cessation of the formation of all blood cells, pancytopenia), which can be fatal, leukopenia/neutropenia, hypofibrinogenemia.
Nervous system: dizziness, headache, aseptic meningitis, tremor, paresthesia, convulsions.
Skin and subcutaneous tissue disorders: rash, itching, redness of the skin, urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome.
Immune system disorders: anaphylactic reactions, anaphylactoid reactions, angioedema, anaphylactic shock.
From the liver and biliary tract: intrahepatic cholestasis, exacerbation of cholecystitis, cholestatic hepatitis.
Psychiatric: agitation and sleep disturbances, insomnia, hallucinations, anxiety.
From the organs of vision: visual impairment, lacrimation, conjunctivitis, retinal hemorrhages, retinal detachment, scotoma.
Respiratory, thoracic and mediastinal disorders: bronchospasm, shortness of breath.
General disorders and administration site conditions: hypoglycemia, increased sweating, fever, chills.
Reporting of suspected adverse reactions
Reporting adverse reactions after registration of a medicinal product is of great importance. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of a medicinal product to the State Expert Center of the Ministry of Health of Ukraine at the link: https://aisf.dec.gov.ua/.
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C, out of the reach of children. Do not freeze.
Incompatibility: The drug should not be mixed with other solutions in the same container.
Packaging
200 ml or 400 ml of solution in a bottle, 1 bottle in a pack.
Vacation category
According to the recipe.
Producer
Private Joint Stock Company "Infusion".
Location of the manufacturer and address of its place of business.
Ukraine, 23219, Vinnytsia region, Vinnytsia district, Vinnyts'ki Khutory village, Nemyrivske highway st., building 84A.
