Pharmacological properties
Pentoxifylline (3,7-dimethyl-1-(5-oxohexyl)-3,7-dihydro-1n-purine-2,6-dione) is a methylxanthine derivative.
The mechanism of action of pentoxifylline is due to the inhibition of PDE and the accumulation of cAMP in vascular smooth muscle cells, blood cells, as well as in other tissues and organs. Pentoxifylline inhibits the aggregation of platelets and erythrocytes, increases their elasticity, reduces the increased concentration of fibrinogen in the blood plasma and enhances fibrinolysis, helping to reduce blood viscosity and improve its rheological properties. in addition, pentoxifylline has a weakly expressed myotropic vasodilator effect, slightly reduces blood pressure and has a positive inotropic effect. Due to the use of pentoxifylline, microcirculation and oxygen supply to tissues improves, to a greater extent in the limbs, central nervous system, and moderately in the kidneys. the drug slightly dilates the coronary vessels. After oral administration in a dose of 100 mg, pentoxifylline is almost completely absorbed in the digestive tract. The maximum concentration of pentoxifylline and its main metabolite is achieved 1 hour after administration. The drug has a first pass effect through the liver. The bioavailability of pentoxifylline averages 19% (6–32%). The main pharmacologically active metabolite 1-(5-hydroxyhexyl)-3,7-dimethylxanthine is determined in the blood plasma in a concentration that is 2 times higher than the concentration of the unchanged substance and is in a state of reverse biochemical equilibrium with it. In this regard, pentoxifylline and its metabolite should be considered as an active entity. The half-life of pentoxifylline is 1.6 hours. Pentoxifylline is completely metabolized, 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, the excretion of metabolites is slowed down. In patients with impaired liver function, an increase in the half-life of pentoxifylline and an increase in its bioavailability are noted.
Trental 400, 20 pcs., 400 mg, extended-release film-coated tablets
Antihypertensive drugs.
Pentoxifylline increases the risk of developing arterial hypotension when used simultaneously with antihypertensive drugs (for example, ACE inhibitors) or other drugs with a potential antihypertensive effect (for example, nitrates).
Drugs affecting the blood coagulation system.
Pentoxifylline may enhance the effect of drugs that affect the blood coagulation system (direct and indirect anticoagulants, thrombolytics, antibiotics such as cephalosporins).
With the combined use of pentoxifylline and indirect anticoagulants (vitamin K antagonists), post-marketing studies have reported cases of increased anticoagulant action (risk of bleeding). Therefore, when starting to take pentoxifylline or changing its dose, it is recommended to monitor the severity of the anticoagulant effect in patients taking this combination of drugs, for example, regularly monitor the INR.
Cimetidine.
Cimetidine increases the concentration of pentoxifylline and active metabolite I in the blood plasma (risk of adverse reactions).
Other xanthines.
Co-administration with other xanthines may lead to excessive nervous stimulation.
Hypoglycemic agents (insulins and hypoglycemic agents for oral administration).
The hypoglycemic effect of insulin or oral hypoglycemic agents may be enhanced by simultaneous use of pentoxifylline (increased risk of hypoglycemia). Strict monitoring of the condition of such patients is necessary, including regular glycemic control.
Theophylline.
In some patients, with simultaneous use of pentoxifylline and theophylline, an increase in theophylline concentration is observed. This may subsequently lead to an increase or worsening of theophylline-related side effects.
Ciprofloxacin.
In some patients, with simultaneous use of pentoxifylline and ciprofloxacin, an increase in the concentration of pentoxifylline in the blood plasma is observed. In the future, this may lead to an increase or intensification of side effects associated with the use of this combination.
Platelet aggregation inhibitors.
With simultaneous use of pentoxifylline with platelet aggregation inhibitors (clopidogrel, eptifibatide, tirofiban, epoprostenol, iloprost, abciximab, anagrelide, NSAIDs (except selective COX-2 inhibitors), acetylsalicylic acid, ticlopidine, dipyridamole), a potential additive effect may develop, increasing the risk of bleeding . Therefore, due to the risk of bleeding, pentoxifylline should be used with caution simultaneously with the above platelet aggregation inhibitors (see "With caution").
Indications
Atherosclerotic encephalopathy, ischemic stroke, dyscirculatory encephalopathy, peripheral circulatory disorders caused by atherosclerosis, diabetes mellitus, inflammation; trophic tissue disorders caused by damage to arteries or veins, microcirculation disorders (postthrombophlebitic syndrome, trophic ulcers, gangrene, frostbite); obliterating endarteritis; angioneuropathy (Raynaud's disease, paresthesia); circulatory disorders of the eye (acute, subacute and chronic circulatory failure in the retina and choroid); dysfunction of the inner ear of a vascular nature, accompanied by hearing loss.
Indications for use of the drug Trental
Atherosclerotic encephalopathy, ischemic stroke, dyscirculatory encephalopathy, peripheral circulatory disorders caused by atherosclerosis, diabetes mellitus, inflammation; trophic tissue disorders caused by damage to arteries or veins, microcirculation disorders (postthrombophlebitic syndrome, trophic ulcers, gangrene, frostbite); obliterating endarteritis; angioneuropathy (Raynaud's disease, paresthesia); circulatory disorders of the eye (acute, subacute and chronic circulatory failure in the retina and choroid); dysfunction of the inner ear of a vascular nature, accompanied by hearing loss.
Application
The dose of trental for intravenous infusion is 100–600 mg (in 250–500 ml of lactated ringer solution, infusion solution or 5% glucose solution) 1 or 2 times a day. the duration of the IV infusion is from 60 to 360 minutes, that is, the administration of 100 mg of pentoxifylline should last at least 60 minutes. the infusion can be supplemented with oral administration of trental.
If the patient's condition is severe (constant pain, gangrene, trophic ulcers), it is possible to administer an IV infusion of Trental for 24 hours. The dose is administered at the rate of 0.6 mg/kg/hour. The daily dose for a patient weighing 70 kg is 1000 mg, for a patient weighing 80 kg - 1150 mg. Regardless of body weight, the maximum daily dose is 1200 mg. The volume of the administered solution is calculated individually, taking into account concomitant diseases and the patient’s condition and averages 1.0–1.5 l/day.
The dose of Trental for intravenous injection is 100 mg. Administration is carried out slowly (over at least 5 minutes) 1–2 times a day. The patient must be in a lying position.
Orally, Trental is prescribed in a dose of 2–4 tablets 2–3 times a day after meals, without chewing, with a sufficient amount of liquid.
The maximum total daily dose for parenteral and oral administration is 1.2 g.
Instructions for use TRENTAL
The dose and route of administration depend on the type and severity of circulatory disorders and individual tolerance to the drug.
Inside
prescribed in doses of up to 800-1200 mg/day in 2-3 doses, after meals. Enteric-coated tablets are swallowed whole with a small amount of water. The daily dose is divided into 3 doses. The initial dose is 600 mg/day. As the condition improves, the dose can be reduced to 300 mg/day. Prolonged dosage forms are prescribed 2-3 times a day.
The drug can be administered orally simultaneously with parenteral administration. In addition to the infusion of Trental, delayed-release tablets may be added. If the clinical condition improves, treatment can be continued with extended-release tablets.
IV in the form of infusions
the drug is administered on average 200-300 mg (2-3 ampoules of 5 ml) per day (morning and afternoon). A concentrated solution of the drug in ampoules is diluted in 250-500 ml of infusion solution.
After the daily infusion, an additional 2 delayed-release tablets may be prescribed. If the two infusions are separated by a longer interval, then 1 extended-release tablet of the additional two prescribed may be taken earlier, around noon.
If, in accordance with the clinical situation, intravenous infusions are possible only once a day, then additionally after the infusion, 3 delayed-release tablets can be prescribed (2 delayed-release tablets at noon and 1 in the evening).
Long-term intravenous infusion of Trental for 24 hours is indicated in more severe cases, especially in patients with severe pain at rest, with gangrene or ulceration (Fontan stages III-IV).
When administered parenterally within 24 hours, the dose of Trental, as a rule, should not exceed 1.2 g, with an individual dose prescribed at the rate of 600 mcg/kg/h. 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 impaired renal function (creatinine clearance less than 30 ml/min)
A dose reduction of 30-50% may be required, depending on individual tolerability of the drug.
A dose reduction based on individual tolerance is necessary in patients with severe liver dysfunction
.
For patients with low blood pressure, as well as those at risk for arterial hypotension (with severe coronary artery disease or hemodynamically significant stenoses of the cerebral vessels), the drug is prescribed in small doses at the beginning of treatment, and a gradual dose increase is possible in the future.
Rules for the preparation and administration of infusion solution
The concentrated solution for preparing a solution for infusion must be diluted in appropriate solvents:
- saline or Ringer's solution. Testing for compatibility with other infusion solutions should be carried out separately. Only clear solutions can be used.
Trental 100 mg should be administered at least 60 minutes before.
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 pump to control the volume of infusions.
Side effects
Nausea, vomiting, heaviness in the epigastric region, diarrhea, headache, dizziness, aseptic meningitis (when taken in high doses), anxiety, sleep disturbances, facial flushing, flushing, tachycardia, angina pectoris, arterial hypotension, skin itching, rash, urticaria, angioedema, extremely rarely - anaphylactic shock. very rarely, mainly when used simultaneously with anticoagulants or antiplatelet agents, bleeding (capillary from the skin and mucous membranes, gastrointestinal). The cause-and-effect relationship of bleeding with taking trental has not been proven. in isolated cases thrombocytopenia was observed.
Use of the drug Trental
The dose of Trental for intravenous infusion is 100-600 mg (in 250-500 ml of Ringer's lactate solution, infusion solution or 5% glucose solution) 1 or 2 times a day. The duration of the IV infusion is from 60 to 360 minutes, that is, the administration of 100 mg of pentoxifylline should last at least 60 minutes. The infusion can be supplemented with oral administration of Trental. If the patient's condition is severe (constant pain, gangrene, trophic ulcers), it is possible to administer an IV infusion of Trental for 24 hours. The dose is administered at the rate of 0.6 mg/kg/hour. The daily dose for a patient weighing 70 kg is 1000 mg, for a patient weighing 80 kg - 1150 mg. Regardless of body weight, the maximum daily dose is 1200 mg. The volume of the administered solution is calculated individually, taking into account concomitant diseases and the patient’s condition and averages 1.0 - 1.5 l/day. The dose of Trental for intravenous injection is 100 mg. Administration is carried out slowly (over at least 5 minutes) 1–2 times a day. The patient must be in a lying position. Orally Trental is prescribed in the following dose: 2-4 tablets 2-3 times a day after meals, without chewing, with a sufficient amount of liquid. The maximum total daily dose for parenteral and oral administration is 1.2 g.
special instructions
The drug is prescribed with caution to patients with severe atherosclerosis of the cerebral and coronary vessels, especially with concomitant hypertension, heart rhythm disturbances, angina attacks, as well as patients with arterial hypotension or labile blood pressure. in these cases, the dose of the drug should be increased gradually, especially when administered parenterally. caution is also required when prescribing the drug to patients with a history of peptic ulcers of the stomach and duodenum; patients who have recently undergone surgery. in these cases, the risk of bleeding is increased, so systematic monitoring of hemoglobin and hematocrit levels is necessary.
Before prescribing Trental, patients with chronic heart failure should achieve circulatory compensation.
For patients with labile or low blood pressure, patients at risk (severe coronary artery disease or severe stenosis of the main vessels of the brain), treatment should begin with the drug in low doses, select doses individually and increase them gradually, taking into account the tolerability of treatment.
In patients with diabetes mellitus receiving insulin therapy or treatment with oral hypoglycemic agents, when using Trental in a high dose, the effect of these drugs on blood glucose levels may be enhanced. In these cases, the dose of insulin or oral hypoglycemic agents should be reduced and regular clinical monitoring should be carried out.
If renal function is impaired (creatinine clearance 30 ml/min), the dose of the drug is selected individually, reducing it by approximately 30–50%. In case of severe liver failure, the dose of Trental should also be reduced depending on individual tolerability of the drug.
Trental
Trental (INN - pentoxifylline) is an original drug from the group of vasodilators from the Indian division of the world famous pharmaceutical company. The first use of trental dates back to 1972, when it was used to treat intermittent claudication. In addition to the vasodilator, the drug has an antiplatelet (prevents platelets from adhering to each other) and angioprotective (protects blood vessels) effect. Due to its ability to improve blood fluidity, reduce platelet aggregation, stimulate capillary circulation and make red blood cells more elastic, trental has found wide use in various circulatory pathologies. The main “weapon” of trental, pentoxifylline, is very close in its chemical “pedigree” to theophylline and theobromine. All its pharmacological advantages are due to the exclusive possession of the secret inhibitory effect on type 4 phosphodiesterases, which entails an increase in the concentration of cAMP in platelets and ATP in erythrocytes against the background of a decrease in the content of calcium ions in cells. Numerous clinical studies conducted in accordance with all the rules of evidence-based medicine indicate the ability of trental to have a purely positive effect on microcirculation and blood circulation in general. And it cannot be otherwise: after all, this drug is capable of dilating blood vessels, simultaneously reducing their general and peripheral resistance, increasing stroke and minute blood volumes without a significant change in pulse rate.
The concentration of cAMP increases not only in platelets, but also in the smooth muscle cells of the vascular walls, which leads to their relaxation.
As already mentioned, Trental is a branded original drug. In the mid-2000s of the last century, a study of the rheological properties of trental in comparison with generic pentoxifylline preparations was carried out on the basis of Yaroslavl State University. At the same time, the original drug showed itself to be a more pronounced antiplatelet agent (46%) than generics (20-35%). Without exception, all drugs studied reduced the size and rate of formation of aggregates, but only trental showed a consistent and significant decrease in all aggregation characteristics.
Trental is available in three dosage forms: tablets, extended-release tablets and concentrate for the preparation of a solution for intravenous and intra-arterial administration. The frequency of administration and dosage regimen are established by the attending physician according to the individual characteristics of each individual patient. During the course of treatment using Trental, it is recommended to monitor blood pressure, and if the patient has recently undergone surgery, then systematic monitoring of hemoglobin levels and hematocrit is indicated. An important clarification: when administering trental intravenously, the patient must be in a supine position.
Actual information
Trental (pentoxifylline) is a methylxanthine derivative with powerful hemorheological properties (reduces blood viscosity). The drug belongs to drugs that affect the cardiovascular system and is included in the group of “peripheral vasodilators”.
Pentoxifylline is approved for the treatment of individuals with intermittent claudication due to peripheral arterial occlusive disease. The drug was first marketed in Europe in 1972 and in the United States in 1985. Animal and human studies have demonstrated hemorheological and immunomodulatory properties.
Pharmacological properties
Pharmacokinetics
The drug is easily absorbed from the gastrointestinal tract, but undergoes primary metabolism in the liver. Some of its metabolites are active. The apparent plasma half-life of pentoxifylline is reported to be 0.4–0.8 hours; for metabolites it ranges from 1.0–1.6 hours. Most of the drug dose is excreted in the urine, mainly in the form of metabolites, and less than 4% is excreted in the feces.
Adverse Side Effects
Drug Trental
may cause nausea, gastrointestinal disorders (nausea, vomiting, diarrhea), dizziness, headache, tremor.
These reactions are dose related and as the dose is reduced their severity decreases. Hot flashes, angina, palpitations, cardiac arrhythmias, and hypersensitivity reactions may also occur. Bleeding events have been reported rarely, usually due to risk factors for bleeding. Also, with an overdose of pentoxifylline, fever, weakness, flushing, arterial hypotension, drowsiness, agitation and convulsions are possible. Interactions
Trental
(pentoxifylline) may enhance the effect of antihypertensive drugs.
High parenteral doses of pentoxifylline may enhance the effect of insulin and hypoglycemic drugs in patients with diabetes mellitus. Pentoxifylline should not be administered with ketorolac as there is an increased risk of bleeding and/or prolongation of prothrombin time. There may also be an increased risk of bleeding when using meloxicam. Pentoxifylline may increase serum theophylline levels. Application
Pentoxifylline is prescribed for the treatment of peripheral vascular diseases. Although the drug is often classified as a vasodilator, its main action appears to be to reduce blood viscosity, probably through effects on red blood cells, platelet adhesion and aggregation. It has been reported to increase blood flow to ischemic tissues and improve tissue oxygenation in patients with peripheral vascular disease and to increase oxygen content and has been used for cerebrovascular disorders. Trental
also inhibits the production of the cytokine tumor necrosis factor alpha (TNF α), and this property is being studied in a number of diseases.
Pentoxifylline is administered parenterally at the beginning of therapy (iv infusion, which lasts 60–360 minutes; if the patient’s condition is assessed as severe, then the infusion can be carried out over 24 hours. In some cases, the drug can be administered as an intravenous injection. Dose The drug is calculated individually and depends on many factors. After improvement of the patient's condition, it is recommended to carry out therapy using a tablet dosage form. For the treatment of peripheral vascular diseases, the usual oral dose is 400 mg 3 times / day in a modified release form. The dose can be reduced to 400 mg 2 r / day (as maintenance therapy). The drug should be taken with food to reduce the risk of gastrointestinal disorders. In severe forms of liver or kidney failure, a dose reduction may also be necessary. Beneficial effects may not be obvious until 2–8 week therapy.
Kidney, liver failure
UK manufacturers state that a dose reduction of pentoxifylline may be required in patients with severe liver impairment, while accumulation may occur in patients with severe renal impairment (creatinine clearance (CR) less than 30 ml/min) who receive more than 400 mg 1– 2 rubles/day.
Venous ulcers on the legs
A systematic review of pentoxifylline used in the treatment of venous leg ulcers found that it is an effective adjunct to compression bandaging and may even be effective on its own (Wylie D., 2007).
In the United States of America, this compound is prescribed for the treatment of intermittent claudication. Studies in humans and animals have shown that drug therapy leads to various physiological changes at the cellular level, which may be important in the treatment of various groups of human diseases. Immune modulation (the process of changing one or more parameters) includes increased leukocyte deformability and chemotaxis, decreased endothelial leukocyte adhesion, decreased neutrophil degranulation and superoxide release, decreased production of tumor necrosis factor from monocytes, decreased sensitivity of leukocytes to interleukin-1 and tumor necrosis factor, inhibition T and B lymphocytes and decreased activity of natural killer cells. Hypercoagulable states are improved by decreased platelet aggregation and adhesion, increased plasminogen activator, increased plasmin, antithrombin III, decreased fibrinogen, alpha-2-antiplasmin, alpha-1-antitrypsin, and decreased alpha-2-macroglobulin. Wound healing and connective tissue disruption are a response to increased fibroblast collagenases and decreased production of collagen, fibronectin, and glycosaminoglycans. (Samlaska CP, 1994).
Pentoxifylline is a methylxanthine derivative that is used for microcirculatory disorders as a vasoactive drug. Novel immunomodulatory properties of pentoxifylline have been reported, including downregulation of the synthesis of tumor necrosis factor-α and other inflammatory cytokines. Research has shown that pentoxifylline may be effective for a wide range of skin conditions (Maakmak SK, 2012).
Refractory or recurrent leg ulcers usually indicate the presence of impaired venous or arterial microcirculation (or both). According to the current hypothesis, local oxygen and nutrient deficiency occurs because the capillary lumens narrow and become permeable to fibrinogen and proteins due to activated leukocytes and inadequate fibrinolysis. The result is the deposition of a relatively impermeable perivascular fibrin sheath that prevents adequate delivery of oxygen and nutrients. Therefore, therapy should be aimed at eliminating these deficiencies and improving wound healing. Pentoxifylline ( Trental
), used in combination with local wound treatment and appropriate antibacterial therapy, has significantly improved the healing of refractory leg ulcers. Pentoxifylline can change the abnormal function of white blood cells, red blood cells, platelets, and also reduce blood viscosity and vascular permeability. The mechanisms of action of pentoxifylline are described in the light of current hypotheses regarding the development of leg ulcers. Nine cases are also discussed in which pentoxifylline, when added to previously unsuccessful local wound care, improved or cured refractory ulcers (Brenman SA, 1991).
Venous leg ulcers are a common, recurrent and disabling condition. The mainstay of treatment is the use of firm compression bandages or stockings to support the veins in the leg. Some leg ulcers take many months or years to heal, and treatment is aimed at preventing infection and promoting healing. Trental
in tablet form is prescribed to improve blood circulation.
A review of studies shows that pentoxifylline, 400 mg tablet taken three times a day, increases the likelihood of recovery. Trental
is an effective adjunct to compression bandages for the treatment of venous ulcers. In the absence of compression, pentoxifylline also appears effective for the treatment of venous ulcers. The main side effects were gastrointestinal disorders (nausea, indigestion and diarrhea).
Leg ulcers are sores on the lower limb that have not healed within four to six weeks. The condition is thought to affect about 1% of the population at some point in life and occurs more often in women than men. About 50–70% of leg ulcers are of venous origin.
The association between calf muscle deficiency and ulceration has long been known. Two hypotheses have been put forward to explain the microcirculatory changes observed in venous ulceration. A 1982 review suggested that venous hypertension increases capillary permeability, resulting in the formation of an impermeable pericapillary fibrin cuff causing local tissue ischemia. However, Coleridge Smith, 1988, argued that the fibrin cuff is secondary to capillary occlusion by white cell plugs, which creates distal ischemia. Trapped white cells release agents that damage the endothelium, increasing capillary permeability and allowing the formation of a fibrin cuff. More recently, Coleridge Smith suggested that it is the infiltration of the skin with protein products alone that promotes tissue destruction.
Another Cochrane review found that compression therapy increased the proportion of healed venous ulcers (O'Meara, 2012). However, despite the use of compression, a proportion of venous ulcers remain non-healing, and therapy adjunctive to compression may be beneficial. Trental
as an adjunct to compression therapy for venous ulcers has been the subject of research with conflicting results (Colgan, 1990; Dale, 1999).
As standard therapy, Trental
was also compared with placebo without compression (Weitgasser, 1983; Jull A.V. et al., 2012).
Conclusion
Pentoxifylline was first registered (in Germany) about 50 years ago. Then its main effect was to dilate blood vessels. Later, no hemorheological effect, in particular on the deformability of erythrocytes, was detected. Regardless of its pharmacological effects, clinical effectiveness in peripheral and cerebral artery diseases is well established. After some period, I became interested in the effect of the drug Trental
on leukocytes.
Both rheological and biochemical changes have been reported. The properties of this drug are being studied, and its therapeutic potential is also being studied, so there is a possibility that in the near future the use of Trental
will expand and go beyond angiology.
Product description certified by the manufacturer Sanofi
.
Verified by
Likar Turumkulova Irina
Pharmacological properties of the drug Trental
Pentoxifylline (3,7-dimethyl-1-(5-oxohexyl)-3,7-dihydro-1H-purine-2,6-dione) is a methylxanthine derivative. The mechanism of action of pentoxifylline is due to the inhibition of phosphodiesterase and the accumulation of cAMP in vascular smooth muscle cells, blood cells, as well as in other tissues and organs. Pentoxifylline inhibits the aggregation of platelets and erythrocytes, increases their elasticity, reduces the increased concentration of fibrinogen in the blood plasma and enhances fibrinolysis, helping to reduce blood viscosity and improve its rheological properties. In addition, pentoxifylline has a weak myotropic vasodilator effect, slightly reduces the peripheral vascular resistance and has a positive inotropic effect. Due to the use of pentoxifylline, microcirculation and oxygen supply to tissues improves, to a greater extent in the extremities, the central nervous system, and moderately in the kidneys. The drug slightly dilates the coronary vessels. After oral administration in a dose of 100 mg, pentoxifylline is almost completely absorbed in the digestive tract. The maximum concentration of pentoxifylline and its main metabolite is achieved 1 hour after administration. The drug has a first pass effect through the liver. The bioavailability of pentoxifylline averages 19% (6–32%). The main pharmacologically active metabolite 1-(5-hydroxyhexyl)-3,7-dimethylxanthine is determined in the blood plasma in a concentration that is 2 times higher than the concentration of the unchanged substance and is in a state of reverse biochemical equilibrium with it. In this regard, pentoxifylline and its metabolite should be considered as an active entity. 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, the excretion of metabolites is slowed down. In patients with impaired liver function, an increase in the half-life of pentoxifylline and an increase in its bioavailability are noted.
Note!
Description of the drug Trental table. p/o 100 mg No. 60 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
Side effects of the drug Trental
Nausea, vomiting, heaviness in the epigastric region, diarrhea, headache, dizziness, aseptic meningitis (when taken in high doses), anxiety, sleep disturbances, facial flushing, flushing, tachycardia, angina pectoris, arterial hypotension, skin itching, rash, urticaria, angioedema, extremely rarely - anaphylactic shock. Very rarely, mainly when used simultaneously with anticoagulants or antiplatelet agents, bleeding (capillary from the skin and mucous membranes, gastrointestinal). The cause-and-effect relationship of bleeding with taking Trental has not been proven. In isolated cases, thrombocytopenia was observed.
Trental 400
Trental 400 (pentoxifylline) is a vasodilator. Increases the ability of red blood cells to change their shape under the influence of external forces, prevents blood platelets and red blood cells from sticking together, reduces the level of factor I of the blood coagulation system, suppresses the activity of white blood cells and prevents their adhesion to the inner wall of blood vessels. The above effects of the drug provide an improvement in the rheological characteristics of the blood and a decrease in its viscosity. The active component of the drug, pentoxifylline, inhibits the activity of the phosphodiesterase enzyme and causes the accumulation of cAMP in smooth muscles. By acting on the smooth muscle framework of blood vessels, it has a mild vasodilator effect, to a certain extent reduces the overall resistance of the entire vascular system to the blood flow ejected by the heart, slightly increases the lumen of the heart vessels, and improves blood circulation in areas with impaired blood circulation. Helps improve cerebral blood circulation. If there are obstacles to normal blood circulation in the arteries of the lower extremities, the use of the drug helps to make walking easier and increase the daily distance walked, reduce the number of episodes of night cramps in the lower leg muscles, and relieve pain at rest. After oral administration, the active substance is almost completely absorbed in the gastrointestinal tract. The dosage form of Trental 400 provides a prolonged release of the active component without sharp peaks and valleys, as a result of which patients better tolerate drug therapy. The half-life of the drug is 1.6 hours. Elimination of the drug from the body is carried out along with urine. In persons with renal failure, the elimination time of Trental 400 is slowed down. The drug is prescribed for generalized damage to large and small blood vessels in diabetes mellitus, transient pain in the legs that occurs while walking, long-term non-healing ulcers of the legs resulting from impaired blood supply, circulatory disorders in the vessels of the brain, in the retina and choroid of the eye, otospongiosis, for ischemia, for recovery after strokes.
The drug is not used for individual intolerance to pentoxifylline, other methylxanthines, auxiliary components, heavy bleeding, extensive hemorrhages in the retina, brain, during pregnancy and lactation due to insufficient research of the drug in this category of patients. Trental 400 is not used in pediatric practice. The dose is selected in accordance with the clinical situation and the severity of the therapeutic response to treatment. A single dose is usually 1 tablet. Frequency of administration – 2-3 times a day. Chewing the tablet is not allowed. The optimal time to take it is with food or immediately after it. In persons with arterial hypotension, severe coronary heart disease, and hemodynamically significant narrowing of cerebral vessels, treatment begins with low doses with the possibility of gradually increasing it. Pharmacotherapy is carried out under regular monitoring of blood pressure. In diabetics taking hypoglycemic drugs, submaximal and maximum doses of Trental 400 can provoke severe hypoglycemic syndrome. When using Trental 400 together with drugs that inhibit the activity of the blood coagulation system and prevent the formation of blood clots, it is necessary to monitor coagulation parameters. In persons who have recently undergone surgery, regular monitoring of hemoglobin and hematocrit is necessary. Elderly patients have higher bioavailability and a reduced rate of elimination of the drug from the body, which may require dose adjustment. Tobacco smoking may reduce the effectiveness of treatment. One of the side effects of the drug is dizziness, which requires special care when driving a car and working with potentially dangerous mechanisms.
Special instructions for the use of the drug Trental
The drug is prescribed with caution to patients with severe atherosclerosis of the cerebral and coronary vessels, especially with concomitant hypertension (arterial hypertension), heart rhythm disturbances, angina attacks, as well as patients with arterial hypotension or labile blood pressure. In these cases, the dose of the drug should be increased gradually, especially when administered parenterally. Caution is also required when prescribing the drug to patients with a history of peptic ulcers of the stomach and duodenum; patients who have recently undergone surgery. In these cases, the risk of bleeding is increased, so systematic monitoring of hemoglobin and hematocrit levels is necessary. Before prescribing Trental, patients with chronic heart failure should achieve circulatory compensation. For patients with labile or low blood pressure, patients at risk (severe coronary artery disease or severe stenosis of the main vessels of the brain), treatment should begin with the drug in low doses, select doses individually and increase them gradually, taking into account the tolerability of treatment. In patients with diabetes mellitus receiving insulin therapy or treatment with oral hypoglycemic agents, when using Trental in a high dose, the effect of these drugs on blood glucose levels may be enhanced. In these cases, the dose of insulin or oral hypoglycemic agents should be reduced and regular clinical monitoring should be carried out. If renal function is impaired (creatinine clearance 30 ml/min), the dose of the drug is selected individually, reducing it by approximately 30–50%. In case of severe liver failure, the dose of Trental should also be reduced depending on individual tolerability of the drug.
