After oral administration of pentoxifylline is rapidly and almost completely absorbed.
After almost complete absorption of pentoxifylline is metabolized. The absolute bioavailability of pentoxifylline . The main active metabolite is proviron cycle has a concentration in the blood plasma, to twice the original concentration of pentoxifylline.
The half-life of pentoxifylline period after oral administration .
Pentoxifylline completely metabolized and more than 90% is excreted through kidneys in the form of water-soluble unconjugated metabolites. Excretion of metabolites is delayed in patients with impaired renal function.
In patients with impaired liver function the half-life of pentoxifylline is prolonged and absolute bioavailability increases.
Peripheral circulatory disorders of atherosclerotic (eg, intermittent claudication), diabetic angiopathy, trophic disorders (eg, leg sores, gangrene).
Violations of the cerebral circulation (the effects of cerebral arteriosclerosis, such as impaired concentration, dizziness, memory impairment ), ischemic and post stroke state.
circulatory disorders of the retina and choroid, otosclerosis, degenerative changes in the background pathology of vessels of the inner ear and hearing loss.
- with hypersensitivity to pentoxifylline, other methylxanthines or any of the excipients;
- with massive bleeding;
- with extensive hemorrhages in the retina of the eye;
- with bleeding in the brain;
- with acute myocardial infarction;
- under the age of 18 years;
- Pregnancy, lactation.
With caution the drug should be used in patients with:
- severe cardiac arrhythmias (fibrillation risk of deterioration);
- hypotension (risk of further reduction proviron cycle in blood pressure, see section “Dosage and Administration”.);
- chronic heart failure;
- gastric ulcer and duodenal ulcer;
- impaired renal function (creatinine clearance below 30 ml / min) (risk of accumulation and an increased risk of side effects, see section “Dosage and Administration”.);
- severe liver function impairment (risk of accumulation and an increased risk of side effects, see section “Dosage and Administration”.);
- after recently transferred surgical intervention;
- increased tendency to bleeding, for example, by the use of anticoagulants or blood coagulation system disorders (risk of heavier bleeding). Regarding bleeding cm. See section “Contraindications”.
Dosage and administration
Dosage is established as a doctor in accordance with the individual characteristics of the patient.
The usual dose is: One tablet of proviron cycle two or three times a day. The maximum daily dose – 1200 mg. The drug should be swallowed whole during or immediately after eating, drinking plenty of water.
In patients with renal impairment (creatinine clearance less than 30 mL / min), the dosage may be reduced to 1-2 tablets per day.
Reducing the dose, taking into account individual portability, it is necessary in patients with severe hepatic impairment.
Treatment can be initiated with low doses in patients with low blood pressure, as well as in patients who are at risk due to a possible reduction in blood pressure (patients with severe coronary artery disease or with hemodynamically significant stenoses of blood vessels brain). In these cases, the dose can be increased only gradually.
When Trental is used the following side effects may occur at high doses: the part of the nervous system : headache, dizziness, anxiety, sleep disorders, convulsions, from the skin and subcutaneous tissue : facial flushing, “tides” of blood to the skin of the face and upper chest, swelling, increased nail fragility, of the digestive system : dry mouth, anorexia, intestinal, feeling of pressure and fullness in the stomach, nausea, vomiting, diarrhea, with the cardiovascular system : tachycardia, arrhythmia, false angina, the progression of angina, lower blood pressure; from the hemostatic system and of hematopoiesis : leukopenia, thrombocytopenia, pancytopenia, bleeding from vessels in the skin, mucous membranes, stomach, intestines, gipofibrinogenemia; with the senses : visual disturbances, skatoma; allergic reaction :. itching, redness of the skin, urticaria, angioedema, anaphylactic shock cases of aseptic meningitis is very rare, intrahepatic cholestasis, and increased activity of “liver” transaminases, alkaline phosphatase.
The clinical picture:. Dizziness, retching, drop in blood pressure, tachycardia, arrhythmia, redness of the skin, loss of consciousness, vomiting, areflexia, tonic-clonic seizures
In the event of the above violations is an urgent need to consult a doctor.
Treatment is symptomatic: special attention should be directed to maintain blood pressure and respiratory function. Seizures relieve diazepam.
At the first signs of an overdose (excessive sweating, nausea, cyanosis), immediately stop taking the drug. Provides a lower position of the head and upper torso. Keep an eye on the free airway.
Interaction with other drugs
Pentoxifylline is able to enhance the effect of agents that reduce blood pressure .
Pentoxifylline may increase the effects of drugs that affect blood clotting (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins).
Cimetidine increases the concentration of pentoxifylline in plasma (the risk of side effects).
Co-administration with other xanthines can lead to excessive nervous excitement.
glucose-lowering effect of insulin or hypoglycemic drugs can be enhanced while taking pentoxifylline (increased risk of hypoglycaemia). There must be strict monitoring of these patients.
In some patients, concomitant use of pentoxifylline and theophylline may lead to increased levels of theophylline. This can lead to an increase or enhance the adverse effects associated with theophylline.
Treatment should be under the control of blood pressure. In patients with diabetes, taking hypoglycemic agents, the appointment of large doses can cause pronounced hypoglycemia (required dose adjustment).
When assigning simultaneously with anticoagulants should be carefully monitored for indicators of blood coagulation.
In patients who have recently had surgery, requires proviron cycle systematic monitoring of hemoglobin levels and hematocrit.
The dose should be reduced in patients with low and unstable blood pressure.
older people may require dose reduction (increased bioavailability and reduced clearance rate).
pentoxifylline safety and effectiveness in children have been insufficiently studied. Smoking may reduce the therapeutic efficacy of the drug.