Agapurin 600 Retard

Agapurin 600 Retard belongs to the group of cardiovascular drugs, has pronounced angioprotective properties. JSC "Slovakofarma" (the Republic of Slovakia) is produced.

Indications of the agapurina 600 Retard

This drug is used for pathologies that are associated with a disorder of microcirculatory functions, in particular:

• - with circulatory disorders of the distal vascular departments that have arisen due to diabetes mellitus, atherosclerosis, inflammations of various origin;
• when treating patients with the syndrome of intermittent claudication;
• in the disorder of cerebral circulation due to ischemia;
• cerebral diseases provoked by atherosclerosis or trophic disorders;
• phenomena of paresthesia, Raynaud's disease;
• pathology of soft tissues, among which include the development of trophic ulcers, gangrenous lesions, the effects of thrombophlebitis, impaired nutrition of tissues due to prolonged cold exposure;
• obliterating endarteritis;
• circulatory disorders of the fundus;
• deterioration of hearing and other otopathologies, provoked by microcirculatory disorder.

Release form

Medication Agapurin 600 Retard is available in tablet form, coated with a coating. Each tablet contains 600 mg of active substance (pentoxifylline, 3,7-dimethyl-1- (5-oxohexyl) -xanthine), as well as a number of auxiliary substances (copolymers, talc, magnesium stearate, polyvidone, etc.). 

Pharmacodynamics

Agapurin 600 Retard consists of a synthetic derivative of methylxanthine, the main property of which is the activation of microcirculation. In addition, this drug is able to expand and strengthen the vessels. This effect is due to the ability to weaken the activity of phosphodiesterase enzymes, to increase the total amount of adenosine monophosphoric acid and to reduce the number of calcium ions in the blood and vascular walls. The effective substance of the drug affects the aggregation properties of erythrocytes and platelets, reduces the amount of fibrinogen, activates the fibrinolysis process. Along with these changes, blood rheology and erythrocyte quality are significantly improved, and the energy potential of cellular structures is enhanced.

 The use of the drug is accompanied by a decrease in the overall indices of the distal pressure, expansion of the heart vessels, which serves as an excellent prophylaxis of tissue hypoxia. Blood is actively saturated with oxygen: this is due to dilatation of pulmonary vessels and strengthening of the diaphragmatic tone. With a constant pulse rate, the shock and minute amounts of blood are increased.

 Agapurin 600 Retard prevents tissue deficiency of oxygen, especially in improving blood supply to the upper and lower extremities, as well as the brain. The bioelectrical activity of the central nervous system increases due to the increase in the amount of ATP in the brain tissue.

 The use of medicinal medication in patients with violations of the patency of distal vessels favors blood flow and reduces the frequency of convulsive nocturnal musculature of the legs. 

Pharmacokinetics

The internal way of taking the drug allows to absorb the active substance in the digestive system, without forming a connection with plasma proteins. Metabolism is observed mainly in the liver, where pharmacological metabolites are formed. Biological transformation occurs on the erythrocyte level.

 The maximum content in the blood serum when using the tablet form of medication is observed after 60 minutes (if the tablets have a prolonged effect - after 120-240 minutes).

 The active substance can be found in breast milk.

 The half-life can be from 20 to 90 minutes. The drug is excreted in the urine, partly with feces. Has no properties to accumulate in the body.

 If the functionality of the urinary and liver systems is disrupted, as a consequence, the half-life of the drug decreases, and its bioavailability increases.

Dosing and administration

The precise dosage, as well as the duration of the therapeutic course, with the Agapurin 600 retard medication is determined only by the medical specialist individually, taking into account the clinical signs of the pathology, the patient's condition, the presence of contraindications and the dynamics of the drug's effect.

 The standard scheme of admission can be considered the use of the drug inside immediately after eating. The tablet can not be chewed, it should be swallowed whole, washed down with a glass of pure water or juice. The drug is taken first once, and if necessary - twice a day for 600 mg (for example, in the morning after breakfast and in the evening after dinner), preferably every day at about the same time.

 More than two tablets per day is not recommended.

 Patients with a disorder of renal function reduce the dosage of the drug to 50%, at the discretion of the treating doctor.

Use of the agapurina 600 Retard during pregnancy

The drug is contraindicated for use by pregnant women. If the doctor prescribes the drug during the period of breastfeeding, the child should be weaned for the duration of the entire course of treatment. 

Contraindications

The main and indisputable contraindication for the use of the drug is the patient's tendency to allergic reactions to the components of the drug.

 Among other possible contra-indications it is necessary to allocate:

• porphyrin disease (pigmentary disorder disorder);
• increased bleeding, predisposition to hemorrhages, violations of blood coagulation function;
• disturbances in the rhythm of cardiac activity;
• acute form of myocardial infarction, stroke;
• sclerotic changes in coronary and (or) cerebral vessels;
• pregnancy, breastfeeding, baby and adolescence.

 Among the relative contraindications are the following:

• decreased blood pressure;
• atherosclerosis;
• cardiac conduction abnormalities;
• impaired liver and urinary system;
• peptic ulcer of stomach and duodenum;
• patient's postoperative state.

Side effects of the agapurina 600 Retard

The use of the drug may lead to the appearance of some adverse reactions:

• weight loss, dyspepsia, dry mouth, digestive disorders, cholecystitis, gastrointestinal hemorrhage;
• pain in the head, unmotivated fatigue, anxiety, insomnia at night and drowsiness during the day, trembling in the hands, convulsive conditions, falling visual functions;
• heart palpitations, heart rhythm disturbances, heart pain, lowering blood pressure, the appearance of subcutaneous hemorrhages, in the analysis of blood - a decrease in the amount of fibrinogen and platelets;
• in patients with heart failure, there may be an increase in the symptoms of angina pectoris;
• dermatitis, anaphylaxis, allergic edema;
• a rush of blood to the face, swelling, changes in nail plates and hair, hyperthermia;
• the activity of liver enzymes increases.

Overdose

When using this drug in high dosages, the following symptoms may occur:

• cardiopalmus;
• disorganization of coordination functions;
• feeling of weakness and fatigue;
• dizziness;
• lowering blood pressure;
• increase in temperature indicators;
• pronounced redness of the facial area;
• dyspeptic disorders.

 If the excessive use of the drug continues, you can observe areflexia, the appearance of convulsive attacks, bloody vomiting.

 If a single, excessively large dose of tablets has been taken, there may be a disorder of consciousness, an inhibition of respiratory functions.

 There is no special antidote for consuming a large amount of the drug. Use the intake of a suspension of sorbent preparations, gastric lavage, symptomatic treatment. Vomiting can be caused only immediately after the accidental administration of a large dose of the drug. If after taking an overstated dose, time passes and convulsions appear, vomiting can be dangerous.

If you suspect an overdose, stop taking the drug immediately and contact the doctor. If the general condition of the patient is unsatisfactory, they are provided with maximum rest, access to fresh air, attach a reclining position and expect the arrival of an "ambulance". Emergency care may consist of intravenous injection of epiphedrine (adrenaline).

 Control over the patient's condition should be carried out before the complete regeneration of respiratory functions and cardiac activity. 

Interactions with other drugs

Simultaneous use of medications with antibiotic drugs, thrombolytic drugs, anticoagulants enhances the drug effect of each other. During such a combination, the blood coagulability should be monitored throughout the entire therapeutic course.

 Combined intake Agapurin 600 Retard enhances the action of insulin preparations, tableted antidiabetic forms and blood pressure lowering agents. Such joint use of medications should take place with mandatory dosage adjustment.

 Drugs-blockers of histamine H 2 -receptors (cimetidine) can increase the content of active substance Agapurin in the blood serum.

 Combined administration of Agapurin with other methylxanthine derivatives (theophylline, aminophylline, euphyllin, theobromine) can provoke an overexcitement of the nervous system.

 It is not recommended to smoke during the entire course of taking Agapurin: this reduces the effectiveness of the drug. 

Storage conditions

The tablet drug Agapurin 600 Retard should be stored in a dark, dry place. The optimum temperature at which the drug is stored can fluctuate within 14-24 ° C. It is necessary to protect the storage of medicinal products from access of children.

 Shelf life of the tablet medication is up to 4 years. At the end of this period, the use of the drug is prohibited, it must be disposed of. Also, the drug is not recommended for use if the storage conditions of the medicinal product have been violated, or a damaged package has been found.

 The drug Agapurin 600 Retard is released in the pharmacy network if you have a prescription from a medical specialist.

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