Composition
1 tablet contains:
Active ingredient:
pentoxifylline 400 mg
Pharmacological action
Pharmacodynamics
A drug that improves microcirculation, an angioprotector, a derivative of xanthine. Trental improves the rheological properties of blood (fluidity) by affecting the pathologically altered deformability of red blood cells, inhibiting platelet aggregation and reducing the increased blood viscosity. Improves microcirculation in areas of impaired blood circulation.
The mechanism of action of pentoxifylline is associated with inhibition of phosphodiesterase and accumulation of cAMP in vascular smooth muscle cells and blood cells.
Having a weak myotropic vasodilating effect, pentoxifylline slightly reduces OPSS and slightly dilates the coronary vessels.
Treatment with Trental leads to an improvement in the symptoms of cerebral circulatory disorders.
Treatment success in cases of occlusive peripheral artery disease (e. g. intermittent claudication) is shown by lengthening the walking distance, eliminating nocturnal cramps in the calf muscles, and eliminating pain at rest.
Pharmacokinetics
Suction
After oral use, pentoxifylline is almost completely absorbed from the gastrointestinal tract.
Bioavailability is on average 19%.
Metabolism
The main pharmacologically active metabolite of 1-(5-hydroxyhexyl) – 3,7-dimethylxanthine is determined in plasma at a concentration exceeding 2 times the concentration of the unchanged substance, and is in a state of reversible biochemical equilibrium with it. For this reason, pentoxifylline and its metabolite should be considered as an active whole, therefore, it can be considered that the bioavailability of the Active ingredient is significantly higher. Pentoxifylline is completely biotransformed in the body.
The elimination
of T1 / 2 pentoxifylline is 1.6 hours.
More than 90% is excreted by the kidneys as unconjugated water-soluble polar metabolites.
Pharmacokinetics in special clinical cases
In patients with severe renal impairment, the excretion of metabolites is slowed.
In patients with impaired liver function, an elongation of T1/2 of pentoxifylline and an increase in its bioavailability were noted.
Indications
- Violations of the peripheral circulation of atherosclerotic (for example intermittent claudication);
- diabetic angiopathy;
- trophic disorders (e. g. leg ulcers, gangrene);
- cerebrovascular disease (consequences of cerebral atherosclerosis, as, for example, impaired concentration, dizziness, memory loss);
- ischemic and post-stroke conditions
- of circulatory disorders in the retina and choroid;
- otosclerosis;
- degenerative changes in the background of the pathology of the vessels of the inner ear and hearing loss.
Contraindications
- Hypersensitivity to the components of the drug;
- massive bleeding;
- extensive retinal hemorrhages;
- brain hemorrhages;
- acute myocardial infarction;
- age up to 18 years;
- pregnancy and lactation (breastfeeding);
- hypersensitivity to other methylxanthines.
It should be used with caution in patients with: Â severe cardiac arrhythmias (risk of worsening arrhythmia), hypotension (risk of further lowering blood pressure), chronic heart failure, with gastric and duodenal ulcers, impaired renal function – creatinine clearance less than 30 ml/min (risk of accumulation and increased risk of side effects), with severe liver function disorders (risk of accumulation and increased risk of side effects), increased tendency to bleeding, including as a result of the use of anticoagulants or with disorders of the blood coagulation system (risk of more severe bleeding), after recent surgical procedures.
Side effects
When using Trental 400 in large doses, hot flashes (redness of the face or a feeling of heat), disorders of the digestive system, such as a feeling of pressure and overflow in the stomach, nausea, vomiting, diarrhea may occur; very rarely, cardiac arrhythmias (tachycardia).
From the central nervous system: possible-dizziness, headache, agitation, sleep disturbance; very rarely-cases of aseptic meningitis.
Allergic reactions: sometimes-pruritus, hyperemia of the skin, urticaria; rarely-severe anaphylactic / anaphylactoid reactions with the development of angioedema, bronchospasm and even shock.
From the digestive system: very rarely – increased activity of hepatic transaminases, intrahepatic cholestasis.
From the blood coagulation system: very rarely – thrombocytopenia; in patients with an increased tendency to bleeding – bleeding (for example, from the vessels of the skin, mucous membranes, stomach, intestines).
From the cardiovascular system: very rarely – angina attacks, tachycardia, hypotension.
Interaction
When used together, Trental potentiates the action of a number of antihypertensive and hypoglycemic agents (both insulin and oral hypoglycemic drugs).
Simultaneous use of pentoxifylline and theophylline can lead to an increase in theophylline levels in the blood and increase its side effects.
How to take, course of use and dosage
The average dose of the drug for oral use is 400 mg (1 tab. ) 2-3 times/day. The maximum daily dose is 1200 mg (3 tablets).
Tablets are taken whole, without chewing, during or immediately after a meal, with a sufficient amount of water.
In patients with severe renal impairment (creatinine clearance less than 30 ml / min)Â the dose can be reduced to 400-800 mg / day.
In patients with hepatic insufficiency, the dose of the drug is selected individually.
Overdose
Symptoms: dizziness, nausea, tachycardia, decreased blood pressure, chills, arrhythmia, areflexia, hyperemia of the skin, loss of consciousness, tonic-clonic convulsions.
Treatment: if necessary, conduct symptomatic therapy.
The patient should be given a horizontal position with raised legs.
The specific antidote is unknown.
Monitor vital functions of the body and general measures aimed at their maintenance, monitor the patency of the respiratory tract; in case of convulsions – diazepam.
Special instructions
Careful monitoring is necessary in patients with severe cardiac arrhythmias (risk of worsening arrhythmia), hypotension (risk of further lowering blood pressure), impaired renal function with creatinine clearance less than 30 ml/min (risk of accumulation and increased risk of side effects), severe liver function disorders (risk of accumulation and increased risk of side effects) and an increased tendency to bleeding, for example, when using anticoagulants or with disorders in the blood coagulation system (risk of more severe bleeding).
Caution should be exercised when prescribing Trental to patients with a history of gastric and duodenal ulcers; patients who have recently undergone surgery (the risk of bleeding is increased, and therefore systematic monitoring of hemoglobin and hematocrit levels is necessary).
In patients with hypotension and labile circulation, parenteral use of Trental is prescribed gradually, since it is possible to reduce blood pressure (up to collapse), and in some cases – angina attacks.
Patients with heart failure should receive appropriate treatment to compensate for blood flow. At the same time, the introduction of a large volume of liquids should be avoided.
In patients with impaired renal function, the dosage regimen should be selected individually.
Form of production
Delayed release, film-coated tablets.
Storage conditions
Store in a cool, dry place.
Active ingredient
Pentoxifylline
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Description
For adults as directed by your doctor
Indications
Consequences of stroke, Raynaud’s disease, Diabetic retinopathy, Frostbite, Cerebral circulation disorders, Trophic ulcers, Atherosclerosis, Vascular diseases of the eyes, Vascular lesions in diabetes mellitus
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