Instructions Pentotren solution for infusions 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; magnesium chloride, hexahydrate; sodium lactate solution; water for injections.
Dosage form
Solution for infusion.
Main physicochemical properties: clear colorless or slightly yellowish liquid.
Pharmacotherapeutic group
Peripheral vasodilators. Purine derivatives. ATC 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 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, CNS, 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 hepatic impairment, an increase in the half-life of pentoxifylline has been 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 microcirculation disorders (postthrombophlebitic syndrome, trophic ulcers, gangrene, frostbite); obliterating endarteritis; angioneuropathy (Raynaud's disease); eye circulatory disorders (acute, subacute, chronic circulatory insufficiency in the retina and choroid of the eye); inner ear dysfunction of vascular genesis, accompanied by hearing loss.
Contraindication
Hypersensitivity to pentoxifylline, other methylxanthines or to any of the excipients of the drug; massive bleeding (risk of increased bleeding); extensive retinal hemorrhage, cerebral hemorrhage (risk of increased bleeding); if retinal hemorrhage occurs during treatment with pentoxifylline, the drug should be discontinued immediately; acute myocardial infarction and severe cardiac arrhythmia; gastric ulcer and/or intestinal ulcers; hemorrhagic diathesis; pregnancy or breastfeeding.
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.
There are reports of increased anticoagulant activity 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.
Pentoxifylline 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.
In some patients, concomitant use of the drug with ciprofloxacin may lead to an increase in the concentration of pentoxifylline in the blood serum. As a result, the frequency and severity of adverse reactions associated with the simultaneous use of drugs may increase.
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, drug therapy should be discontinued immediately.
When using pentoxifylline in patients with chronic heart failure, the phase of circulatory compensation should first be achieved.
In patients with diabetes mellitus treated with insulin or oral antidiabetic agents, the effect of these drugs on blood sugar levels may be increased when using high doses of the drug. In these cases, the dose of insulin or oral antidiabetic agents should be reduced and the patient should be especially carefully monitored.
Patients with systemic lupus erythematosus 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 monitoring of complete blood counts is required.
In patients with renal insufficiency (creatinine clearance below 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 cardiac arrhythmia; with myocardial infarction; with arterial hypotension; with severe atherosclerosis of the cerebral and coronary vessels, especially with concomitant arterial hypertension and heart rhythm disturbances (in these patients, angina attacks, arrhythmias and arterial hypertension are possible when taking the drug); with renal failure (creatinine clearance below 30 ml/min); with severe hepatic failure; with a high tendency to bleeding, due, for example, to treatment with anticoagulants or blood clotting disorders; with a history of gastric and duodenal ulcers, patients who have recently undergone surgical treatment (increased risk of bleeding, in connection with which systematic monitoring of hemoglobin and hematocrit levels is required); for whom a decrease in blood pressure is a high risk (for example, in patients with severe ischemic heart disease or stenosis of the vessels supplying blood to the brain); who are simultaneously treated with pentoxifylline and vitamin K antagonists; who are simultaneously treated with pentoxifylline and antidiabetic agents;
who are simultaneously receiving treatment with pentoxifylline and ciprofloxacin (see section "Interaction with other medicinal products and other types of interactions");
who are simultaneously receiving treatment with pentoxifylline and theophylline (see section "Interaction with other medicinal products and other types of interactions").
Important information about excipients.
This medicinal product contains 6.2 mg/ml sodium, which should be taken into consideration by patients on a controlled sodium diet.
Ability to influence reaction speed when driving vehicles or other mechanisms
Does not affect.
Use during pregnancy or breastfeeding
Pregnancy
There is insufficient experience with the use of the drug in pregnant women. Therefore, the drug should not be prescribed during pregnancy.
Breastfeeding period
Pentoxifylline passes into breast milk in small amounts. If treatment with pentoxifylline is prescribed, breastfeeding should be discontinued.
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 regimen is recommended for adults:
Intravenous infusion of 100–600 mg of pentoxifylline 1–2 times daily. The administration of 100 mg of pentoxifylline should last at least 60 minutes.
The infusion can be supplemented with oral pentoxifylline, with the maximum daily dose (infusion and oral) being 1200 mg.
In severe cases of the patient (especially with persistent pain, gangrene or trophic ulcers), it is possible to carry out an infusion of pentoxifylline for 24 hours. With this administration scheme, the dose is 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 - 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 the parenteral course of treatment is determined by the treating physician.
After the patient's condition improves, it is recommended to continue treatment using the tablet form of the drug.
Children
There is no experience with the use of the drug in children.
Overdose
Symptoms: weakness, dizziness, decreased blood pressure, fainting, arrhythmia, tachycardia, drowsiness or agitation, loss of consciousness, hyperthermia, areflexia, tonic-clonic seizures, coffee-ground vomit as a sign of gastrointestinal bleeding, nausea, hot flashes.
Treatment is symptomatic. 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.
From the organs of vision: visual impairment, lacrimation, conjunctivitis, retinal hemorrhages, retinal detachment, scotoma.
Gastrointestinal: hypersalivation, gastrointestinal disorders, feeling of pressure in the stomach, nausea, vomiting, anorexia, flatulence, diarrhea, constipation, intestinal atony.
From the liver and biliary tract: exacerbation of cholecystitis, cholestatic hepatitis, intrahepatic cholestasis.
Nervous system: dizziness, headache, aseptic meningitis, tremor, paresthesia, convulsions.
Psychiatric: agitation and sleep disturbances, anxiety, hallucinations.
Cardiovascular system: arrhythmia, tachycardia, angina pectoris, cardialgia, blood pressure fluctuations, feeling of tightness behind the sternum, feeling of heat (hot flashes), bleeding, 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.
Immune system disorders: anaphylactic reactions, anaphylactoid reactions, angioedema, bronchospasm and anaphylactic shock.
Skin and subcutaneous tissue disorders: itching, rash, redness of the skin, urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome, increased nail fragility.
General disorders and administration site conditions: cases of hypoglycemia, increased sweating, fever, chills have been reported.
Laboratory indicators: increased transaminase levels, increased alkaline phosphatase levels.
Reporting of suspected adverse reactions.
Reporting suspected adverse reactions after the marketing authorisation of a medicinal product is an important procedure. It allows for continued monitoring of the benefit-risk balance of the medicinal product in question. Healthcare professionals should report any suspected adverse reactions via the national reporting system.
Expiration date
3 years.
The expiration date determines the use of the medicine until the last day of the month.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ° C. Do not freeze.
Keep out of reach of children.
Packaging
200 ml in a bottle.
Vacation category
According to the recipe.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Location of the manufacturer and its business address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
