Instructions for Trental
Composition Trental:
Active ingredient: pentoxifylline - 400.0 mg. Excipients: povidone - 10.0 mg, hyetellose - 140.0 mg, talc - 12.5 mg, magnesium stearate - 2.5 mg.
Shell composition Trental:
hypromellose - 10.902 mg, titanium dioxide (E 171) - 2.680 mg, talc - 0.820 mg, macrogol-8000 - 0.550 mg.
Trental
Pharmacodynamics Trental:
Trental® 400 reduces blood viscosity and improves blood rheological properties (fluidity) due to:
- improving impaired deformability of red blood cells;
- reduce platelet aggregation and red blood cells;
- decrease in fibrinogen concentration;
- reducing the activity of leukocytes and reducing the adhesion of leukocytes to the vascular endothelium.
As an active ingredient, the Trental® 400 preparation contains a xanthine derivative - pentoxifylline. The mechanism of its action is associated with the inhibition of phosphodiesterase and the accumulation of cyclic adenosine monophosphate (cAMP) in the smooth muscle cells of blood vessels and blood cells.
Having a weak myotropic vasodilator effect, pentoxifylline somewhat reduces the total peripheral vascular resistance and slightly dilates the coronary vessels.
Pentoxifylline has a weak positive inotropic effect on the heart. Improves microcirculation in areas of impaired circulation. Treatment with Trental® 400 leads to an improvement in the symptoms of cerebrovascular accidents.
In case of occlusive diseases of the peripheral arteries, the use of the Trental® 400 preparation leads to an increase in the walking distance, elimination of night cramps in the calf muscles and the disappearance of pain at rest. Trental
Pharmacokinetics Trental:
After oral administration, pentoxifylline is almost completely absorbed. Pentoxifylline undergoes a “primary passage” effect through the liver. The absolute bioavailability of the starting substance is 19 ± 13%. The concentration of the main active metabolite of 1- (5-hydroxyhexyl) -3,7-dimethylxanthine (metabolite I) in blood plasma is twice the concentration of the initial pentoxifylline. Trental
Metabolite I is with pentoxifylline in reversible biochemical redox equilibrium. Therefore, pentoxifylline and metabolite I are considered together as an active unit. As a result, the availability of the active substance is much greater.
The prolonged release of pentoxifylline allows you to maintain a constant (peakless) concentration in the blood, which ensures better tolerability of the drug in this dosage form. The half-life of pentoxifylline after oral administration is 1.6 hours. Pentoxifylline is completely metabolized and more than 90% is excreted through the kidneys in the form of unconjugated water-soluble metabolites.
Patients with impaired renal function In patients with impaired renal function, the excretion of metabolites is slowed down. Patients with impaired liver function In patients with impaired liver function, the half-life of pentoxifylline is lengthened and absolute bioavailability increases. Trental
Side effects Trental:
The following are the adverse reactions that have been reported in clinical trials and in post-marketing use of the drug (frequency unknown). Disorders from the nervous system: headache, dizziness, aseptic meningitis, cramps.
Mental disorders: agitation, sleep disturbances, anxiety. Disturbances from the heart: tachycardia, arrhythmia, decreased blood pressure, angina pectoris. Violations of the vessels: “flushing” of blood to the skin, bleeding (including bleeding from blood vessels of the skin, mucous membranes, stomach, intestines).
Digestive disorders: xerostomia (dry mouth), anorexia, intestinal atony, a feeling of pressure and overflow in the stomach, nausea, vomiting, diarrhea. Disorders from the liver and biliary tract: intrahepatic cholestasis, increased activity of “liver” transaminases, increased activity of alkaline phosphatase. Disorders from the blood and lymphatic system: leukopenia, thrombocytopenia, pancytopenia, hypofibrinogenemia. Violations of the organ of vision: visual impairment, scotoma.
Disturbances from the skin and subcutaneous tissues: skin itching, erythema (redness of the skin), urticaria, increased fragility of nails, edema. Immune system disorders: anaphylactic / anaphylactoid reactions, angioedema, anaphylactic shock, bronchospasm. Trental
Special conditions Trental:
Treatment should be carried out under the control of blood pressure. In patients with diabetes taking hypoglycemic agents, the administration of large doses can cause severe hypoglycemia (dose adjustment of hypoglycemic agents and glycemic control may be necessary).
When prescribing the drug Trental® 400 simultaneously with anticoagulants, it is necessary to monitor the indicators of the blood coagulation system. In patients who have recently undergone surgery, regular monitoring of hemoglobin and hematocrit is necessary.
Patients with low and unstable blood pressure need to reduce the dose of pentoxifylline. In elderly patients, a reduction in the dose of pentoxifylline may be required (increased bioavailability and decreased excretion rate). The safety and efficacy of pentoxifylline in children has not been sufficiently studied.
Smoking can reduce the therapeutic effectiveness of the drug Trental. Impact on the ability to drive vehicles and engage in potentially hazardous activities Considering possible side effects (such as dizziness), care must be taken when driving and engaging in potentially hazardous activities.
Indications Trental:
• Occlusive peripheral arterial disease of atherosclerotic or diabetic origin (for example, “intermittent” lameness, diabetic angiopathy).
• Trophic disorders (for example, trophic ulcers of the legs, gangrene).
• Cerebrovascular accidents (consequences of cerebral atherosclerosis, such as decreased attention span, dizziness, memory impairment), ischemic and post-stroke conditions.
• Circulatory disorders in the retina and choroid of the eye.
• Otosclerosis, degenerative changes against the background of vascular pathology of the inner ear and hearing loss.
Contraindications Trental:
• Hypersensitivity to pentoxifylline, other methylxanthines or to any excipient of the drug.
• Massive bleeding (risk of increased bleeding).
• Extensive retinal hemorrhage (risk of increased bleeding).
• Hemorrhages in the brain.
• Acute myocardial infarction.
• Age to 18 years.
• Pregnancy (insufficient data).
• The period of breastfeeding (insufficient data). Carefully
• Severe cardiac arrhythmias (risk of worsening arrhythmias).
• Arterial hypotension (the risk of a further decrease in blood pressure, see the section "Dosage and administration").
• Chronic heart failure.
• Peptic ulcer of the stomach and duodenum.
• Impaired renal function (creatinine clearance below 30 ml / min) (risk of cumulation and increased risk of side effects, see section “Dosage and administration”).
• Severe impairment of liver function (risk of cumulation and increased risk of side effects, see section “Dosage and administration”).
• Recent surgery.
• Increased tendency to bleeding, for example, as a result of the use of anticoagulants (including indirect anticoagulants [vitamin K antagonists] or in case of disorders in the blood coagulation system (risk of more severe bleeding), see the section “Interaction with other drugs”.
• Concomitant use with hypoglycemic agents (insulin and hypoglycemic agents for oral administration), see the section “Interaction with other medicines”.
• Concomitant use with ciprofloxacin (see section “Interaction with other drugs”). Trental
Use during pregnancy and during breastfeeding Pregnancy The drug Trental® 400 is not recommended for use during pregnancy (as there is insufficient data).
The period of breastfeeding Pentoxifylline passes into breast milk in small quantities.
If it is necessary to use the drug, breast-feeding should be stopped (given the lack of experience with use).
Drug Interactions Trental:
With antihypertensive drugs, Pentoxifylline increases the risk of developing arterial hypotension while it is used with antihypertensive drugs (e.g., angiotensin converting enzyme inhibitors (ACEs)) or other drugs that have a potential antihypertensive effect (e.g. nitrates).
With drugs that affect the blood coagulation system, Pentoxifylline can 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) in post-marketing studies, there have been cases of increased anticoagulant action (risk of bleeding).
Therefore, at the beginning of taking pentoxifylline or changing its dose, it is recommended to control the severity of anticoagulant action in patients taking this combination of drugs, for example, to conduct regular monitoring of INR (international normalized ratio).
With cimetidine, cimetidine increases the concentration of pentoxifylline and the active metabolite I in the blood plasma (risk of adverse reactions). With other xanthines Co-administration with other xanthines can lead to excessive nervous excitement. With hypoglycemic agents (insulin and hypoglycemic agents for oral administration)
The hypoglycemic effect of insulin or hypoglycemic agents for oral administration may be enhanced with the simultaneous use of pentoxifylline (an increased risk of hypoglycemia). Strict monitoring of the condition of such patients is required, including regular glycemic control. With theophylline In some patients with the simultaneous use of pentoxifylline and theophylline, an increase in theophylline concentration is noted. In the future, this can lead to an increase or intensification of side effects associated with theophylline. Trental
With ciprofloxacin In some patients with the simultaneous use of pentoxifylline and ciprofloxacin, an increase in the concentration of pentoxifylline in the blood plasma is noted. In the future, this can lead to an increase or intensification of side effects associated with the use of this combination.
With platelet aggregation inhibitors. With the simultaneous use of pentoxifylline with platelet aggregation inhibitors (clopidogrel, eptifibatid, tirofiban, epoprostenol, iloprost, abciximab, anagrelide, NSAIDs [except for selective inhibitors of cyclooxygenase-2-dipyloidide amide, acetylide increasing the risk of bleeding.
Therefore, due to the risk of bleeding, pentoxifylline should be used with caution at the same time as the above platelet aggregation inhibitors (see section "With caution").
Dosage Trental:
The dosage is set by the doctor in accordance with the individual characteristics of the patient. The usual dose is: one Trental® 400 tablet two or three times a day. The maximum daily dose is 1200 mg. Trental
The drug Trental should be swallowed whole during or immediately after a meal, drinking plenty of water. In patients with impaired renal function (creatinine clearance below 30 ml / min), the dosage can be reduced to 1-2 tablets per day. Dose reduction, taking into account individual tolerance, is necessary in patients with severe hepatic impairment.
Treatment can be started in small doses in patients with low blood pressure, as well as in people at risk due to a possible decrease in blood pressure (patients with severe coronary artery disease or with hemodynamically significant stenosis of the cerebral vessels). In these cases, the dose can only be increased gradually. Trental
Overdose Trental:
Symptoms of overdose: dizziness, nausea, vomiting such as "coffee grounds", a drop in blood pressure, tachycardia, arrhythmia, redness of the skin, loss of consciousness, chills, areflexia, tonic-clonic convulsions. In the event of the above violations, you must immediately consult a doctor. The treatment is symptomatic.
When the first signs of an overdose appear (sweating, nausea, cyanosis), the drug is immediately stopped. If the drug has been taken recently, measures should be taken to prevent further absorption of the drug by eliminating it (gastric lavage) or slowing down absorption (for example, taking activated charcoal).
Particular attention should be directed to maintaining blood pressure and respiratory function. With convulsive seizures, diazepam is administered. The specific antidote is unknown. Trental
