The drug Trental, which improves blood circulation, is produced in the form of tablets and a concentrated solution for infusion. The cost of the medicine depends on the form of the medicine and packaging. You can buy Trental at a price of 100-300 rubles per package.
The active substance in pentoxifylline is a xanatine derivative. The component is contained in the following quantities:
- 100 mg, 400 mg in soluble film-coated tablets.
- 20 mg in one ml solution for infusion.
In order to exclude possible allergic reactions when taking the product, it is necessary to pay attention to the auxiliary components that were used to create the drug. Trental instructions also contain all recommendations for use and focus on contraindications.
Composition and release form
Trental® Enteric film-coated tablets - 1 tablet. pentoxifylline - 100 mg excipients: lactose; starch; talc; colloidal silicon dioxide; magnesium stearate shell: methacrylic acid copolymer; sodium hydroxide; macrogol (polyethylene glycol) 8000, talc; titanium dioxide (E171) in a blister 10 pcs; There are 6 blisters in a cardboard pack. Concentrate for the preparation of solution for infusion - 1 ml pentoxifylline - 20 mg excipients: sodium chloride; water for injection in ampoules of 5 ml; There are 5 ampoules in a cardboard pack. Trental® 400 Extended-release film-coated tablets - 1 tablet. pentoxifylline - 400 mg excipients: povidone (PVP); hyaetellose (hydroxyethylcellulose); talc; magnesium stearate shell composition: hypromellose (hydroxypropyl methylcellulose); benzyl alcohol; titanium dioxide; talc; macrogol (polyethylene glycol) 6000; 10 pcs in blister; There are 2 blisters in a cardboard pack.
Dosage
The dose and method of administration are determined by the doctor after examining the patient. In this case, the severity of the circulatory disorder against the background of a specific disease and the person’s condition must be taken into account. Treatment must be carried out under strict control of blood pressure.
According to the instructions attached to the drug, oral administration is permitted in accordance with the following recommendations:
- Treatment intake: 3 tablets (100 mg) three times a day.
- Possible increase in dosage to 6 (100 mg) tablets three times a day.
- The maximum single dose is no more than 2 (100 mg) tablets.
Tablets are usually indicated for maintenance therapy. They are taken after meals. They must be swallowed with plenty of clean water. If there are pathologies of the kidneys and liver, then the dosage is reduced by 2 times. There are also other recommendations in the instructions that need to be studied.
The infusion solution is prepared from 100 - 600 mg of medication. It is diluted in 0.9% sodium chloride solution (250 - 500 ml). Droppers are placed 1-2 times a day. It is imperative to test for compatibility when using other infusion solutions.
pharmachologic effect
Trental is a drug with a blood-thinning effect, which is used to improve blood circulation in atherosclerosis and diabetes mellitus
Pharmacokinetics
Tablets 100, 400 mg After oral administration, pentoxifylline is quickly and almost completely absorbed. After almost complete absorption, pentoxifylline is metabolized. The absolute bioavailability of the original substance is (19±13)%. The main active metabolite 1-(5-hydroxyhexyl)-3,7-dimethylxanthine (metabolite-1) has a plasma concentration that is 2 times higher than the initial concentration of pentoxifylline. T1/2 of pentoxifylline after oral administration is 1.6 hours. Pentoxifylline is completely metabolized, more than 90% is excreted through the kidneys in the form of unconjugated water-soluble metabolites. The elimination of metabolites is delayed in patients with impaired renal function. In patients with impaired liver function, T1/2 of pentoxifylline is prolonged and absolute bioavailability increases.
Solution for infusion Pentoxifylline is extensively metabolized in red blood cells and the liver. Among the most well-known metabolites, metabolite-1 (M-1; hydroxypentoxifylline) is formed due to cleavage, and metabolite-4 (M-IV) and metabolite-5 (MV; carboxypentoxifylline) are formed due to oxidation of the main substance. M-l has the same pharmacological activity as pentoxifylline. More than 90% of the taken dose of pentoxifylline is excreted through the kidneys and 3-4% in the feces. T1/2 of pentoxifylline after intravenous administration of 100 mg was approximately 1.1 hours. In patients with severe liver dysfunction, T1/2 of pentoxifylline increases. Pentoxifylline has a large volume of distribution (168 L after 30 minutes of infusion of 200 mg) and a high clearance of approximately 4500-5100 ml/min. Pentoxifylline and its metabolites do not bind to plasma proteins. In severe renal impairment, the elimination of metabolites is slowed down.
Pharmacodynamics
Trental® improves the rheological properties of blood (fluidity) by affecting the pathologically altered deformability of red blood cells, inhibiting platelet aggregation and reducing high blood viscosity. Trental® improves microcirculation in areas of poor circulation. As an active ingredient, Trental® contains a xanthine derivative - pentoxifylline. The mechanism of its action is associated with the inhibition of phosphodiesterase and the accumulation of cAMP in the cells of vascular smooth muscles and blood cells. Providing a weak myotropic vasodilator effect, pentoxifylline slightly reduces peripheral vascular resistance and slightly dilates the coronary vessels. Treatment with Trental® leads to improvement of symptoms in cases of cerebrovascular accident. The success of treatment for occlusive lesions of the peripheral arteries (for example, intermittent claudication) is manifested in lengthening the walking distance, eliminating night cramps in the calf muscles and the disappearance of pain at rest.
Effects of the drug and indications
The drug trental, the instructions for use indicate, reduces blood viscosity and improves its fluidity. The active substance has a slight myotropic vasodilator effect. Such combinations of properties help, after taking the drug, to improve microcirculation in areas where circulatory disorders are observed. The active substance in the medicine is quickly absorbed into the gastrointestinal tract, which guarantees a quick effect. When smoking, the therapeutic effect of the drug is significantly reduced.
Trental tablets are indicated for use in cases of impaired peripheral circulation due to the development of atherosclerosis. Its effectiveness has been proven in a pathology known as “intermittent” claudication. This insidious pathology can immobilize a person at any time. Its main symptom is acute pain in the legs, caused by deterioration of blood circulation in the arteries and their narrowing.
Trental 100 is also prescribed, the instructions confirm this, for trophic disorders. The medicine alleviates the condition of patients with trophic ulcers, which often occur against the background of varicose veins and thrombophlebitis. The drug is indicated in the complex treatment of gangrene and frostbite.
It is recommended to use trental for cerebrovascular accidents. This pathology can be provoked by cerebral atherosclerosis. Symptoms of the disease are the following:
- Inability to concentrate.
- The occurrence of periodic dizziness.
- Problems remembering simple information.
Ischemic and post-stroke conditions are also indications for the drug. When using the drug, it is possible to improve the condition of patients against the background of rapid restoration of blood flow. Indications are degenerative changes in pathologies of the vessels of the inner ear, which lead to hearing loss.
Drug interactions
For all dosage forms, Pentoxifylline can enhance the effect of drugs that lower blood pressure (ACE inhibitors, nitrates). Pentoxifylline may enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins). Cimetidine increases the plasma concentration of pentoxifylline (risk of side effects). Co-administration with other xanthines may lead to excessive nervous stimulation. The hypoglycemic effect of insulin or oral antidiabetic agents may be enhanced when taking pentoxifylline (increased risk of hypoglycemia). Strict monitoring of such patients is necessary. 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.
Trental concentrate for the preparation of solution for infusion 20 mg/ml in 5 ml ampoules No. 5
Name
Trental conc. d/prig.r-ra d/inf. 20 mg/ml in amp. 5 ml in pack No. 5
Description
Almost transparent colorless solution.
Main active ingredient
Pentoxifylline
Release form
Concentrate
Dosage
20mg/ml
Pharmacodynamics
Trental® improves the rheological properties of blood (fluidity) by affecting the pathologically altered deformability of red blood cells, inhibiting platelet aggregation and reducing high blood viscosity. Trental® improves microcirculation in areas of poor circulation. As an active ingredient, Trental® contains a xanthine derivative - pentoxifylline. The mechanism of its action is associated with the inhibition of phosphodiesterase and the accumulation of cAMP in the cells of vascular smooth muscles and blood cells. Providing a weak myotropic vasodilating effect, pentoxifylline slightly reduces total peripheral vascular resistance and slightly dilates the coronary vessels. Treatment with Trental® leads to an improvement in the symptoms of cerebrovascular accidents. The success of treatment for occlusive lesions of the peripheral arteries (for example, intermittent claudication) is manifested in lengthening the walking distance, eliminating night cramps in the calf muscles and the disappearance of pain at rest.
Pharmacokinetics
Pentoxifylline does not bind to plasma proteins. Pentoxifylline is extensively metabolized in red blood cells and the liver. Among the most well-known metabolites, metabolite-1 (M-I; hydroxypentoxifylline) is formed due to cleavage, and metabolite-4 (M-IV) and metabolite-5 (M-V; carboxypentoxifylline) are formed due to oxidation of the main substance. M-I has the same pharmacological activity as pentoxifylline. Excreted primarily through the kidneys (95% after 24 hours) and 3-4% with feces and in the form of metabolites. The half-life is approximately one hour. Pentoxifylline has a large volume of distribution (168 L after a 30-minute infusion of 200 mg) and a high clearance of approximately 4500-5100 ml/min. Possible accumulation of metabolites in patients with severe renal failure. In older people, elimination occurs more slowly than in young people. In patients with severely impaired liver function, the half-life of pentoxifylline and bioavailability are increased.
Indications for use
Occlusive disease of peripheral arteries of atherosclerotic or diabetic origin (for example, with “intermittent claudication” or rest pain). Trophic disorders (for example, leg ulcers or gangrene). Cerebrovascular disease of atherosclerotic origin. Circulatory disorders in the retina and choroid of the eye and ears with degenerative vascular changes, decreased vision and hearing.
Directions for use and doses
Dose 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. When using a parenteral form of release, the infusion time should be at least 60 minutes per 100 mg of pentoxifylline. Peripheral circulatory disorders of atherosclerotic origin stage II (“intermittent” claudication) and circulatory disorders in the structures of the eye; Initial therapy or maintenance therapy for oral administration of the drug An infusion of 100 to 600 mg of pentoxifylline once or twice daily is recommended. An infusion of pentoxifylline in a suitable infusion solution is recommended. 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. When low-dose infusion is combined with oral administration of the drug, the recommended daily dose is 1200 mg of pentoxifylline (intravenously and orally). For further treatment, therapy can be carried out only by taking pentoxifylline orally. Peripheral circulatory disorders of atherosclerotic origin stages III and IV The recommended daily dose is 1200 mg of pentoxifylline as a continuous infusion in a suitable infusion solution over 24 hours or as an infusion of 600 mg twice a day for a period of at least 6 hours. An infusion of pentoxifylline in a suitable infusion solution is recommended. 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. For further treatment, therapy can be carried out only by taking pentoxifylline orally. Special cases In patients with renal failure (creatinine clearance below 30 ml/min), the dose should be adjusted to 50-70% of the standard dose, depending on the patient’s individual tolerability of the drug. A dose reduction based on 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 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. In old age, it is recommended to reduce the dosage and control blood pressure, especially when used in conjunction with antihypertensive and vasodilating agents. Children There is no data on the use of the drug in children. Pregnancy There is not enough experience regarding the use of the drug during pregnancy. Therefore, it is recommended not to use Trental® during pregnancy. Lactation Pentoxifylline passes into breast milk in small quantities. Since there is insufficient experience with the use of Trental® in breastfeeding women, the physician should carefully weigh the possible risks and benefits before prescribing the drug.
Use during pregnancy and lactation
Insufficient experience has been gained regarding the use of the drug during pregnancy. Therefore, it is recommended not to use Trental® during pregnancy. Lactation Pentoxifylline passes into breast milk in small quantities. Since there is insufficient experience with the use of Trental® in breastfeeding women, the physician should carefully weigh the possible risks and benefits before prescribing the drug.
Precautionary measures
Use Pentoxifylline with caution in the following situations: Diabetes: Due to the increased risk of bleeding, ophthalmic monitoring is necessary. Severe coronary or cerebral artery disease: due to an increased risk of low blood pressure. In patients with systemic lupus erythematosus (SLE) and mixed connective tissue diseases: Pentoxifylline should be used only after a careful benefit-risk assessment. Due to the risk of aplastic anemia during therapy with pentoxifylline, regular monitoring of blood counts should be performed. When the first signs of an anaphylactic/anaphylactoid reaction appear, the drug infusion should be stopped. Patients should be warned about this. Particularly careful monitoring is necessary: in patients with severe arrhythmias; in patients with acute myocardial infarction; in patients with hypotension; in patients with impaired renal function (creatinine clearance below 30 ml/min); in patients with severe liver dysfunction; in patients with an increased tendency to bleed, including as a result of the use of anticoagulants or with disorders in the blood coagulation system (risk of developing more severe bleeding); in patients with an increased risk of low blood pressure (patients with severe coronary heart disease and significant stenosis of blood vessels); in patients simultaneously receiving pentoxifylline and anti-vitamin K; in patients simultaneously receiving pentoxifylline and antidiabetic agents; in patients simultaneously receiving pentoxifylline and ciprofloxacin. 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 prescribed simultaneously with anticoagulants, it is necessary to carefully monitor the blood coagulation system. In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit levels is necessary. The administered dose should be reduced in patients with low and unstable blood pressure. In older adults, dose reduction may be necessary (increased bioavailability and decreased rate of elimination). The safety and effectiveness of pentoxifylline in children have 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. The drug contains sodium in the amount of 12.4 mg - 15.1 mg (0.54 - 0.66 mmol) per ampoule. This must be taken into account in patients on a sodium-controlled diet.
Interaction with other drugs
Pentoxifylline can enhance the effect of drugs that lower blood pressure (ACE inhibitors, nitrates). Pentoxifylline may enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins). Cimetidine increases the plasma concentration of pentoxifylline (risk of side effects). Co-administration with other xanthines may lead to excessive nervous stimulation. The hypoglycemic effect of insulin or oral antidiabetic agents may be enhanced when taking pentoxifylline (increased risk of hypoglycemia). Strict monitoring of such patients is necessary. 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. Coadministration with ciprofloxacin may increase serum concentrations of pentoxifylline in some patients. Thus, adverse reactions associated with co-administration of the drug may increase and intensify.
Contraindications
hypersensitivity to pentoxifylline, other methylxanthines or to any of the components of the drug; acute myocardial infarction; massive bleeding; extensive hemorrhages in the retina; ulcers in the stomach and/or intestines, hemorrhagic diathesis.
Compound
1 ml contains: active ingredient: pentoxifylline – 20 mg; excipients: sodium chloride – 7 mg, water for injection – up to 1 ml.
Overdose
Symptoms of overdose: weakness, sweating, nausea, cyanosis, dizziness, decreased blood pressure, tachycardia, fainting, drowsiness or agitation, arrhythmia, hyperthermia, areflexia, loss of consciousness, tonic-clonic convulsions, signs of gastrointestinal bleeding (vomiting like coffee grounds ). Treatment is symptomatic: special attention should be paid to maintaining blood pressure and respiratory function. Convulsive seizures are treated with diazepam. When the first signs of overdose appear, immediately stop administering the drug. Provides a lower position for the head and upper body.
Side effect
In cases where Trental® is used in large doses or at a high rate of infusion, the following side effects may sometimes occur: from the nervous system: headache, dizziness, anxiety, sleep disturbances, convulsions, aseptic meningitis, tremor, paresthesia, intracranial hemorrhage; on the part of the skin and subcutaneous fat: hyperemia of the facial skin, itching, erythema (redness of the skin), “flushes” of blood to the skin of the face and upper chest, edema, increased brittleness of nails, epidermal necrolysis, Stevens-Johnson syndrome, sweating ; from the digestive system: gastrointestinal disorders, epigastric discomfort, bloating, nausea, vomiting, diarrhea, xerostomia, anorexia, intestinal atony; from the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina pectoris, decreased blood pressure; from the blood and lymphatic system: thrombocytopenia, bleeding from blood vessels of the skin, mucous membranes, stomach, intestines, aplastic anemia (pancytopenia); from the organ of vision: visual impairment, conjunctivitis, retinal hemorrhage, retinal detachment; allergic reactions: anaphylactic or anaphylactoid reactions, such as bronchospasm, itching, skin flushing, urticaria, angioedema, anaphylactic shock; from the kidneys and urinary tract: bleeding from the genitourinary system; from the liver and biliary tract: intrahepatic cholestasis and increased activity of “liver” transaminases; mental disorders: agitation, sleep disorders; laboratory and instrumental studies: increased concentration of alkaline phosphatase, increased blood pressure; general disorders: fever, peripheral edema. If side effects occur, you must stop taking the drug. If the listed adverse reactions occur, as well as reactions not listed in the instructions for use, you should consult a doctor.
Storage conditions
Store in a place protected from light at temperatures from 8°C to 25°C. Keep out of the reach of children!
Overdose
Tablets 100, 400 mg Symptoms: dizziness, retching, drop in blood pressure, tachycardia, arrhythmia, redness of the skin, loss of consciousness, chills, areflexia, tonic-clonic convulsions. Solution for infusion Symptoms: weakness, sweating, nausea, cyanosis, dizziness, decreased blood pressure, tachycardia, fainting, drowsiness or agitation, arrhythmia, hyperthermia, areflexia, loss of consciousness, tonic-clonic convulsions, signs of gastrointestinal bleeding (caffeine-type vomiting grounds). Treatment: symptomatic, special attention should be paid to maintaining blood pressure and respiratory function. Convulsive seizures are relieved by the administration of diazepam. When the first signs of overdose appear (excessive sweating, nausea, cyanosis), immediately stop taking the drug. Provides a lower position for the head and upper body. Monitor the free patency of the airways.
Contraindications
An absolute contraindication is intolerance to the active substance and other components in the medication. The drug is not prescribed for people under the age of 18, as well as during pregnancy and lactation. Other contraindications for Trental 100, the instructions for use focus on:
- Severe bleeding of any etiology.
- Hemorrhages in the brain and retina.
- Myocardial infarction.
With extreme caution and only after assessing the patient’s condition, the drug is prescribed for the following pathologies:
- Cardiac arrhythmia.
- Low blood pressure.
- Chronic heart failure.
- Stomach and duodenal ulcers.
- Kidney failure.
- Liver pathologies.
Do not use the medicine after surgery, or if you are prone to bleeding.
