Pentoxifylline solution for injection 20 mg/ml 5 ml ampoule 10 pcs. in Moscow
The dose and method of administration are determined by the severity of circulatory disorders, as well as on the basis of individual tolerability of the drug. The dosage is set by the doctor in accordance with the individual characteristics of the patient. The usual dose is from 100 mg to 600 mg of the drug, diluted in 250 ml or 500 ml of 0.9% sodium chloride solution or Ringer's solution, 1 or 2 times a day
Compatibility with other infusion solutions must be tested separately; Only clear solutions can be used.
100 mg of the drug should be administered over at least 60 minutes. In addition to infusion therapy, pentoxifylline can be prescribed for oral administration. In this case, the total daily dose of pentoxifylline (intravenous infusion + oral administration) should not exceed 1200 mg. Depending on concomitant diseases (for example, chronic heart failure), it may be necessary to reduce the injected volumes. In such cases, it is recommended to use a special infuser for controlled infusion.
In more severe cases, especially in patients with severe pain at rest, with gangrene or trophic ulcers (stages III-IV according to the Fontaine classification), a long-term intravenous infusion of the drug at a dose of 1200 mg over 24 hours is indicated. This dose can be divided into two 600 mg infusions, each administered over at least 6 hours. In this case, the individual dose can be calculated using the formula: 0.6 mg of pentoxifylline per kg of body weight per hour. The daily dose calculated in this way would be 1000 mg of pentoxifylline for a patient weighing 70 kg and ll50 mg of pentoxifylline for a patient weighing 80 kg. During maintenance therapy, switch to oral pentoxifylline.
In patients with renal failure (creatinine clearance less than 30 ml/min), it is necessary to reduce the dosage by 30-50%, which depends on the patient’s individual tolerability of the drug.
A dose reduction, taking into account individual tolerance, is necessary in patients with severe liver dysfunction.
In elderly patients, dose reduction may be required (increased bioavailability and decreased elimination rate). Treatment can be started in low doses in patients with low blood pressure, as well as in patients at risk due to a possible decrease in blood pressure (patients with severe coronary heart disease or with hemodynamically significant cerebral vascular stenoses). In these cases, the dose can only be increased gradually
Pentoxifylline concentrate for the preparation of solution for infusion 20 mg/ml in 5 ml ampoules No. 10
Name
Pentoxifylline.
Release form
Solution for infusion.
Dosage
20 mg / 1 ml 5 ml Pack quantity: 10 pcs.
Manufacturer
Borisovsky ZMP.
INN
Pentoxifylline.
FTG
Vasodilating agent.
Compound
One ampoule (5 ml) of solution contains: active ingredient: pentoxifylline – 100 mg; excipients: sodium chloride, water for injection.
Description
Transparent colorless or slightly yellowish liquid.
Pharmacotherapeutic group
Peripheral vasodilators. Purine derivatives. ATX code – C04AD03.
Pharmacological properties
Pharmacodynamics
The drug is a methylxanthine derivative, an angioprotector, improves microcirculation. The mechanism of action of pentoxifylline is associated with inhibition of phosphodiesterase and accumulation of cyclic AMP in vascular smooth muscle cells, blood cells, and other tissues and organs. Blocks adenosine receptors. Inhibits platelet aggregation, increases the elasticity of erythrocytes, reduces the increased concentration of fibrinogen in plasma and enhances fibrinolysis, which reduces blood viscosity and improves its rheological properties. In addition, it has a weak myotropic vasodilator effect, somewhat reduces total peripheral vascular resistance and has a positive inotropic effect, improves oxygen supply to tissues (to the greatest extent in the limbs and central nervous system, to a moderate extent in the kidneys). The drug slightly dilates the coronary vessels.
Pharmacokinetics
Metabolism Metabolism mainly occurs in the liver, where a number of pharmacologically active metabolites are formed, the main of which are 1-(5-hydroxyhexyl)-3,7-dimethylxanthine (metabolite I) and 1-(3-carboxypropyl)-3,7-dimethylxanthine (metabolite V). Cmax of pentoxifylline and the main products of its biodegradation is achieved within 1 hour, and the concentrations of metabolites in the blood plasma are 5–8 times higher than the concentration of the parent substance. Excretion T1/2 of pentoxifylline is 1.6 hours. It is excreted mainly by the kidneys in the form of metabolites (more than 90%), less than 4% of the administered dose is excreted in feces, and can be excreted by lactating mammary glands. Pharmacokinetics in special clinical situations In patients with severely impaired renal function, the excretion of metabolites is slowed down. In patients with impaired liver function, an increase in T1/2 of pentoxifylline was observed.
Indications for use
Stage IIb peripheral circulatory disorders according to the Fontaine classification (“intermittent” claudication): as initial or maintenance treatment when prescribing oral pentoxifylline, in combination with surgical treatment or in the preoperative period, or if surgical treatment is not possible; diabetic angiopathy. Trophic disorders (for example, leg ulcers or gangrene). Cerebrovascular diseases of atherosclerotic origin. Degenerative changes against the background of pathology of the vessels of the inner ear and hearing loss (deafness, hearing loss, etc.), circulatory disorders in the retina and choroid.
Contraindications
– acute myocardial infarction; – massive bleeding; – cerebral hemorrhage; – extensive hemorrhage in the retina of the eye; – hemorrhagic diathesis; – stomach and intestinal ulcers; – pregnancy; - lactation; – children and adolescents up to 18 years of age; – hypersensitivity to pentoxifylline, other methylxanthine derivatives or components of the drug.
Precautionary measures
Caution should be exercised when prescribing the drug to patients with: arterial hypotension (risk of low blood pressure), impaired renal function (creatinine clearance (CC) below 30 ml/min) (risk of accumulation and increased risk of side effects), severe liver dysfunction ( risk of accumulation and increased risk of side effects), increased tendency to bleeding, including as a result of the use of anticoagulants or disorders of the blood coagulation system (risk of developing more severe bleeding). Treatment should be carried out under blood pressure control. In patients with diabetes mellitus taking hypoglycemic agents, the administration of large doses can cause severe hypoglycemia (dose adjustment is required). When used simultaneously with anticoagulants, it is necessary to carefully monitor the indicators of the blood coagulation system. In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit levels is necessary. In older adults, a dose reduction (reduced elimination rate) may be necessary. The safety and effectiveness of pentoxifylline in children has not been sufficiently studied. Smoking may reduce the therapeutic effectiveness of the drug. The compatibility of the pentoxifylline solution with the infusion solution should be checked on a case-by-case basis. When performing intravenous infusions, the patient should be in a supine position. Each ampoule contains less than 1 mmol of sodium. But when introducing the contents of 2 or more ampoules, the total amount of sodium will be more than 1 mmol per dose, which must be taken into account in patients on a low sodium diet. In patients with systemic lupus erythematosus and other systemic connective tissue diseases, pentoxifylline is prescribed only after a careful benefit-risk assessment.
Use during pregnancy and lactation
The safety of using pentoxifylline during pregnancy has not been established, and therefore prescribing the drug is not recommended. Pentoxifylline is excreted in breast milk, so breastfeeding should be discontinued during treatment.
Impact on the ability to drive vehicles and other mechanisms
There is no data on the effect on the ability to drive vehicles and other machinery. However, the possibility of developing side effects (dizziness, etc.) should be taken into account and caution should be exercised when driving vehicles and engaging in potentially hazardous activities.
Directions for use and doses
The dose and method of administration are determined by the doctor depending on the severity of circulatory disorders and individual tolerance to the drug. The usual dose is 1-2 continuous infusions per day (morning and afternoon), each containing from 100 mg of pentoxifylline (1 ampoule of 5 ml) to 300 mg of pentoxifylline (3 ampoules of 5 ml). The contents of the ampoules are diluted in 250–500 ml of solvent (0.9% sodium chloride solution, Ringer's solution, 5% glucose solution). The recommended rate of administration is 100 mg of pentoxifylline (1 ampoule/hour). In addition to infusion therapy, pentoxifylline can be prescribed orally, but the daily dose of pentoxifylline should not exceed 1200 mg. Depending on concomitant diseases (heart failure), it may be necessary to reduce the injected volumes. In such cases, it is recommended to use a special infuser for controlled infusion. In patients with renal failure (creatinine clearance below 30 ml/min), it is necessary to reduce the dosage by 50–70%, which depends on the individual tolerability of the drug to the patients. A dose reduction, taking into account individual tolerance, is necessary for patients with severe liver dysfunction. Treatment can be started in small doses in patients with low blood pressure, as well as in those at risk due to a possible decrease in pressure (patients with severe coronary heart disease or with hemodynamically significant stenoses of cerebral vessels). In these cases, the dose can only be increased gradually. In old age, it is recommended to reduce the dosage and control blood pressure, especially when used in conjunction with antihypertensive and vasodilating agents. There is no experience with the use of pentoxifylline in children and adolescents.
Side effect
Criteria for the frequency of side effects: very often (≥1/10); often (≥1/100 to
Overdose
Symptoms: nausea, dizziness, tachycardia, decreased blood pressure, arrhythmia, skin hyperemia, chills, loss of consciousness, areflexia, tonic-clonic convulsions. Treatment: carry out symptomatic therapy. The patient should be placed in a horizontal position with legs elevated. A specific antidote is unknown. Carry out monitoring of the vital functions of the body and general measures aimed at maintaining them, monitor the patency of the respiratory tract; for convulsions - diazepam.
Interaction with other drugs
Pentoxifylline can enhance the effect of drugs that lower blood pressure (ACE inhibitors, nitrates, etc.). Parenteral use of pentoxifylline in high doses may enhance the hypoglycemic effect of insulin and oral hypoglycemic agents in patients with diabetes mellitus. Pentoxifylline can enhance the effect of drugs that affect the blood coagulation system (direct and indirect anticoagulants, thrombolytics) and antibiotics (for example, cephalosporins). When co-administered with ciprofloxacin, an increase in the concentration of pentoxifylline in the blood serum was observed, which may lead to an increase in the frequency and/or severity of side effects. Cimetidine significantly increases the concentration of pentoxifylline in the blood plasma (risk of side effects). Co-administration with other xanthines may lead to excessive nervous stimulation. In some patients, concomitant use of pentoxifylline and theophylline may result in increased theophylline levels. This may result in more or worse theophylline-related side effects.
Package
5 ml in glass ampoules. 10 ampoules along with the package insert are placed in a cardboard box. 5 ampoules are placed in a polyvinyl chloride film insert. 2 inserts with ampoules, together with an insert leaflet, are placed in a cardboard pack. 10 ampoules, together with a leaflet, are placed in a cardboard pack with one or two cardboard inserts for fixing the ampoules.
Release from pharmacies
On prescription.
Storage
In a place protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Best before date
3 years. Do not use after expiration date.
Buy Pentoxifylline concentrate for the preparation of solution for infusion 20 mg/ml in 5 ml ampoules No. 10 in the pharmacy
Price for Pentoxifylline concentrate for the preparation of solution for infusion 20 mg/ml in 5 ml ampoules No. 10
Instructions for use for Pentoxifylline concentrate for the preparation of solution for infusion 20 mg/ml in 5 ml ampoules No. 10
Pentoxifylline, 60 pcs., 100 mg, enteric-coated tablets
Trental®
Trental® 400
Tablets 100, 400 mg
The dosage is set by the doctor in accordance with the individual characteristics of the patient.
Inside,
swallow whole, during or immediately after a meal, with plenty of water.
The usual dose is 1 tablet. Trentala® 100 mg 3 times a day, followed by a slow increase in dose to 200 mg 2-3 times a day. The maximum single dose is 400 mg.
The usual dose is 1 tablet. Trental® 400 mg 2-3 times a day.
The maximum daily dose is 1200 mg. In patients with impaired renal function (Cl creatinine <30 ml/min), the dosage can be reduced to 1-2 tablets. per day.
Trental®
Solution for infusion
The dosage is set by the doctor in accordance with the individual characteristics of the patient.
IV
, drip, dose and method of administration are determined by the severity of circulatory disorders, as well as on the basis of individual tolerability of the drug.
The usual dose is two intravenous infusions per day (morning and afternoon), each containing 200 mg of pentoxifylline (2 amps of 5 ml) or 300 mg of pentoxifylline (3 amps of 5 ml) in 250 ml or 500 ml 0 .9% sodium chloride solution or Ringer's solution. Compatibility with other infusion solutions must be tested separately; Only clear solutions can be used.
Pentoxifylline (100 mg) should be administered over at least 60 minutes.
Depending on concomitant diseases (heart failure), it may be necessary to reduce the injected volumes. In such cases, it is recommended to use a special infuser for controlled infusion.
After the daily infusion, an additional 2 tablets may be prescribed. Trentala® 400 mg. If 2 infusions are separated by a longer interval, then 1 table. Trental 400 mg of the two additionally prescribed, can be taken earlier (at approximately noon).
If, due to clinical conditions, intravenous infusion is possible only once a day, an additional 3 tablets may be prescribed after it. Trentala® 400 mg (at noon - 2 tablets and in the evening - 1 tablet). Long-term intravenous infusion of Trental - over 24 hours is indicated in more severe cases, especially in patients with severe pain at rest, with gangrene or trophic ulcers (stages III-IV according to Fontaine).
The dose of Trental® administered parenterally over 24 hours, as a rule, should not exceed 1200 mg of pentoxifylline, while the individual dose can be calculated using the formula: 0.6 mg of pentoxifylline per kg of body weight per hour. The daily dose calculated in this way will be 1000 mg of pentoxifylline for a patient weighing 70 kg and 1150 mg of pentoxifylline for a patient weighing 80 kg. In patients with renal failure (Cl creatinine <30 ml/min), it is necessary to reduce the dosage by 30–50%, which depends on the individual tolerability of the drug to the patient.
For all dosage forms, the dosage is set by the doctor in accordance with the individual characteristics of the patient. A dose reduction, taking into account individual tolerance, is necessary in patients with severe liver dysfunction. Treatment can be started in small doses in patients with low blood pressure, as well as in those at risk due to a possible decrease in blood pressure (patients with severe coronary artery disease or with hemodynamically significant stenoses of cerebral vessels). In these cases, the dose can only be increased gradually.
Pentoxifylline, solution for infusion 2 mg/ml
Pharmacodynamics. Pentoxifylline is the main representative of the pharmacological group of drugs - hemorheological drugs. It increases the plasticity (deformability) of red blood cells, which allows them to penetrate into vessels with a changed lumen (diameter) and improve blood supply to tissues, especially against the background of hypoxia. It reduces their ability to aggregate, facilitates penetration into the extravascular bed, which also promotes tissue oxygenation. Pentoxifylline inhibits fibrinogen biosynthesis and reduces blood viscosity. Under the influence of the drug, the formation of pseudopodia in platelets is reduced. It is characteristic that with such a multifaceted intervention of pentoxifylline in the processes ensuring hemostasis, the risk of bleeding does not increase. During inflammation, pentoxifylline has the ability to reduce the adhesion and aggregation of polymorphonuclear leukocytes, inhibit the “metabolic explosion” and prevent their damaging effect on endothelial cells. It inhibits the activity of phosphodiesterase, inhibits the destruction of cAMP, reduces the concentration of intracellular calcium and enhances the effects of adenosine. 06/02/2014 Pentoxifylline has a weak vasodilator effect and prevents vascular contraction under the influence of vasoconstrictor stimuli. In recent years, it has been established that pentoxifylline has the ability to inhibit the production of proinflammatory cytokines (primarily tumor necrosis factor and interleukins-1,-2,-6). Pharmacokinetics. When administered intravenously, pentoxifylline enters the tissue and penetrates well through the blood-brain barrier. The half-life of pentoxifylline varies between 0.4 - 0.8 hours. It undergoes biotransformation in the liver with the formation of two main metabolites: 1-(5-hydroxyhexyl)-3,7-dimethylxanthine (metabolite-1) and 1-(3-carboxypropyl )-3,7-dimethylxanthine (metabolite-5), which have similar activity and have a half-life of 1 to 1.6 hours. 1.5 - 2 hours after infusion, the concentration of metabolites exceeds the content of the original compound by 5-8 times. By the 8th hour, the concentration of pentoxifylline and its metabolites in the blood decreases significantly (up to 10% of the initial value). Excreted mainly by the kidneys (up to 95%), mainly in the form of metabolite-5. Less than 4% of the drug is excreted in feces. In breastfeeding women it is secreted by the lactating glands. Due to the large volume of distribution and strong binding to erythrocytes, the pharmacokinetics of pentoxifylline during hemodialysis practically does not change.
