AGAPURIN tablets 600mg
Instructions for use Agapurin Wed 600 (Agapurin Sr 400)
Trade name: Wed Agapurin 600
Active substance: Pentoxifylline
English title: Agapurin SR 600
Ukrainian title: Wed Agapurin 600
ATC classification: C04AD03
Active substance: pentoxifylline;
1 tablet contains 400 mg or 600 mg of pentoxifylline;
Other ingredients: hypromellose, povidone 40, talc, magnesium stearate, coloring white Sepifilm 752, dimethicone emulsion SE 2, macrogol 6000.
Chronic peripheral arterial circulatory disorders and arteriovenous by atherosclerosis, diabetes (diabetic angiopathy), degenerative disorders (post-thrombotic syndrome, trophic ulcers, gangrene, frostbite) taangioneyropatii (paresthesias, acrocyanosis, Raynaud's disease);
Cerebrovascular disease (a condition sprichineniyaterosklerozom, for example, reduced ability to concentrate, dizziness, memory loss, and the condition after stroke with persistuyuchimisimptomamy cerebrovascular ischemia);
Acute and chronic retinal and horioidalnasudinna failure;
Circulatory disorders of the inner ear.
Increased sensitivity to pentoxifylline, and other methylxanthine derivatives or to any of the ingredients of the drug.
Acute myocardial infarction.
Bleeding in the brain or other clinically significant bleeding.
Ulcers of the stomach and / or intestines.
If during treatment with pentoxifylline is bleeding in the retina of the eye, the use of the drug should be immediately discontinued.
Dosage and administration.
If you do not appoint another dose, then take 1 tablet depot Agapurin Wed 400 mg three times daily or 600 mg Agapurin Wed 2 times a day (equivalent to 1200 mg of pentoxifylline in the day).
For patients with low or unstable blood pressure levels should be adjusted dose.
The dose for patients with renal insufficiency (creatinine clearance less than 30 ml / min) should be selected, taking into account individual tolerance.
For patients with severe hepatic dysfunction should be reduced dose at the physician, in each case must take into account the severity of disease and tolerability.
Dysfunction of the inner ear caused by circulatory disorders (including hearing loss and sudden hearing loss.
If not set a different dosage, then take 1 tablet depot Agapurina two or three times a day (the equivalent of 800-1200 mg pentoxifylline per day).
For patients with low or unstable blood pressure levels should be adjusted dose.
In patients with renal insufficiency (creatinine clearance less than 30 ml / min), the dose should be titrated up to 50-70% of the standard dose, taking into account the individual tolerance, for example, the use of pentoxifylline 400 mg twice a day instead of 400 mg three times a day.
In patients with severe liver dysfunction decision to lower the dose the doctor has to take, given the severity of the disease and tolerability of the drug in the patient.
Method and duration of administration.
Agapurin dose determined by a doctor taking into account individual patient characteristics. Usually drug Agapurin appoint 400-600 mg 2-3 times a day. The maximum daily dose should not exceed 1.2 g pentoxifylline.
The tablets should be taken after meals, not chewing, drinking plenty of fluids (about 100 ml).
For patients with a significant decrease in renal function (creatinine clearance less than 30 ml / min), the dose can be reduced to 1-2 tablets per day. For patients with severe hepatic impairment, of the groups at risk with respect to the effects of blood pressure (eg, severe coronary vessels, significant stenosis of major vessels of the brain) should begin treatment with a low dose, individually select doses and increase them gradually with the portability treatment.
In the case of accelerated passage through the gastrointestinal tract (the use of laxatives, diarrhea, surgical shortening of the intestine), in some cases, it may be the excretion remains tablet. If premature elimination occurs only from time to time, do not give this much attention.
Symptoms. Dizziness, nausea, low blood pressure, tachycardia, flushing, fainting, fever, agitation, areflexia, tonic-clonic seizures, arrhythmia, vomiting as "coffee grounds."
Therapeutic measures. If overdose has occurred recently, you can spend a gastric lavage or use activated charcoal to prevent further absorption.
Treatment should be symptomatic, as the specific antidote is unknown. To prevent complications, it may be necessary observation in intensive care.
Emergency measures in case of severe hypersensitivity reactions (shock). At the first sign (for example, skin reactions (urticaria, flushing, restlessness, headache, sudden sweating, nausea) should establish venous catheter. Along with the usual emergency measures, such as placing the patient in the supine position with elevated legs, Airway Management and the introduction of oxygen, as shown emergency medical treatment, including intravenous replacement of fluids, epinephrine (adrenaline) intravenous glucocorticoids (eg, 250 -1000 mg intravenous methylprednisolone) and receptor antagonists.
Depending on the severity of clinical symptoms may need artificial respiration, and in the case of cardiac arrest - the restoration of vital functions in accordance with the usual recommendations.
Application Agapurin during pregnancy or breast-feeding. Since there is enough experience with pentoxifylline pregnant women, it should not be used during pregnancy.
During lactation Pentoxifylline passes into breast milk. Due to lack of sufficient clinical experience with the drug during lactation is possible if, in the opinion of the doctor, the expected positive effect for the mother outweighs the potential risk to the child.
Children. Due to the lack of sufficient clinical experience AgapurinSR 400 mg should not be given to children.
Special security measures.
The drug should be used under regular medical supervision.
Features of the application.
Especially careful medical supervision is necessary for patients with cardiac arrhythmias, hypotension, coronary sclerosis and those who have had a heart attack or surgery.
Patients with systemic lupus erythematosus or mixed connective tissue disease pentoxifylline can be assigned only after a detailed analysis of the possible risks and benefits.
Of the risk for hemorrhage, while the use of pentoxifylline and oral anticoagulants should conduct close monitoring and frequent testing of blood coagulation parameters.
Since at the time of treatment with pentoxifylline of the risk of aplastic anemia, need regular blood monitoring of the picture.
In patients with renal insufficiency (creatinine clearance less than 30 mL / min) or severe liver dysfunction excretion of pentoxifylline may be delayed. Need proper monitoring.
Patients with renal insufficiency. In patients with renal insufficiency (creatinine clearance less than 30 ml / min) dose titration should be carried out to 50 - 70% of the standard dose, taking into account individual tolerance, for example, should take pentoxifylline 400 mg twice a day instead of 400 mg three times a day.
Patients with severe liver dysfunction. In patients with severe liver dysfunction decision to lower the dose the doctor has to take, given the severity of the disease and tolerability in each individual patient.
Influence on ability to drive a car or other mechanisms. Not known.
In cases where during treatment dizziness and other side effects, you should refrain from driving and using machinery.
Interaction with other medicinal products and other forms of interaction. Pentoxifylline potentiates the effect of anticoagulants, fibrinolytic agents, increases the effects of antihypertensive (eg enzyme inhibitors angiotenzinkonvertuyuchogo) drugs, nitrates, and hypoglycemic agents (such as insulin and oral antidiabetic drugs. Need for close supervision of patients who are taking other medications along with pentoxifylline.
In some patients, concomitant use of pentoxifylline and theophylline may lead to increased levels of theophylline, which may increase or enhance the side effects associated with theophylline.
Pentoxifylline improves blood rheology (flow), reducing high blood viscosity. Its pharmacological properties due to the fact that it:
impairments improves the ability of erythrocytes by inhibiting phosphodiesterase with a further increase intracellular concentrations of cAMP and ATP, as well as inhibiting the aggregation of red blood cells;
inhibits platelet aggregation;
lowers abnormally high levels of plasma fibrinogen;
inhibits the activation of leukocytes and adhesion of leukocytes to the endothelium of blood vessels.
Effect of pentoxifylline on the incidence of cardiac or cerebrovascular disease and / or the mortality has not been studied.
Sustained release of the drug pentoxifylline to occur within 10-12 hours, during which time the blood supported by its constant level. The released pentoxifylline rapidly and almost completely absorbed. After that there is a pronounced first-pass metabolism of substances, so its systemic availability is only 20-30%.
Pentoxifylline is almost completely metabolized in the liver. The main active metabolite 1 - (5-hydroxyhexyl) -3,7-theobromine (a metabolite I) is in the plasma concentration of two times the concentration of the starting material, with which it is in the back of the biochemical balance. Therefore, pentoxifylline and metabolite I considered active unit. Pentoxifylline-phase output, the initial half-life of the original substance is 0.4-0.8 hours, and for the metabolites - 1.0-1.6 hours. Terminal half-life of pentoxifylline from plasma is approximately 1.6 hours.
Output is primarily through the kidneys in the form of water-soluble non-conjugated polar metabolites, only 4% of those treated with the feces. In the original state pentoxifylline appears in trace amounts.
In patients with severe renal or hepatic dysfunction, the half-life is longer, and the absolute bioavailability increases.