Agapurin 600 Retard

Agapurin 600 Retard belongs to the group of cardiovascular drugs, has pronounced angioprotective properties. Manufactured by JSC "Slovakopharma" (Slovak Republic).

Indications Agapurina 600 Retarda

This medicine is used for pathologies associated with disorders of microcirculatory functions, in particular:

• - in cases of circulatory disorders of the distal vascular sections caused by diabetes mellitus, atherosclerosis, inflammation of various origins;
• in the treatment of patients with intermittent claudication syndrome;
• in case of cerebral circulation disorder due to ischemia;
• diseases of the brain caused by atherosclerosis or trophic disorders;
• paresthesia, Raynaud's disease;
• soft tissue pathologies, which include the development of trophic ulcers, gangrenous lesions, the consequences of thrombophlebitis, and impaired tissue nutrition due to prolonged exposure to cold;
• obliterating endarteritis;
• disorders of the blood circulation of the fundus;
• hearing loss and other otopathologies caused by microcirculatory disorders.

Release form

The drug Agapurin 600 Retard is available in film-coated tablet form. Each tablet contains 600 mg of the 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 considered to be the activation of microcirculation. In addition, this drug is able to expand and strengthen blood vessels. This effect is due to the ability to weaken the activity of phosphodiesterase enzymes, increase the total amount of adenosine monophosphoric acid and reduce the number of calcium ions in the blood and vessel walls. The effective substance of the drug affects the aggregation properties of erythrocytes and platelets, reduces the amount of fibrinogen, activates the process of fibrinolysis. Along with these changes, blood rheology and the quality of erythrocytes are significantly improved, the energy potential of cellular structures is enhanced.

The use of the drug is accompanied by a decrease in the general indicators of distal pressure, dilation of the heart vessels, which serves as an excellent prevention of tissue hypoxia. The blood is actively saturated with oxygen: this occurs due to the dilation of the pulmonary vessels and increased diaphragmatic tone. With an unchanged pulse rate, the stroke and minute volume of blood increases.

Agapurin 600 Retard prevents tissue oxygen deficiency, this is especially noticeable in improving the blood supply to the upper and lower extremities, as well as the brain. The bioelectric activity of the central nervous system is enhanced by increasing the amount of ATP in the brain tissue.

The use of the medicinal drug in patients with impaired distal vascular patency improves blood flow and reduces the frequency of convulsive nocturnal contractions of the leg muscles.

Pharmacokinetics

The internal method of taking the drug allows the active substance to be absorbed in the digestive system without forming a bond with plasma proteins. Metabolism is observed mainly in the liver, where pharmacological metabolites are formed. Biological transformation also occurs at the erythrocyte level.

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

The active substance may be found in breast milk.

The half-life can range from 20 to 90 minutes. The drug is excreted mostly in urine, partly in feces. It does not accumulate in the body.

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

Dosing and administration

The exact dosage, as well as the duration of the therapeutic course of the drug Agapurin 600 Retard, is determined only by a medical specialist on an individual basis, taking into account the clinical signs of pathology, the patient's condition, the presence of contraindications and the dynamics of the drug's effect.

The standard regimen for taking the drug is to take it orally immediately after eating. The tablet should not be chewed, it should be swallowed whole with a glass of clean water or juice. The drug is taken once at first, and if necessary - twice a day at 600 mg (for example, in the morning after breakfast and in the evening after dinner), preferably at about the same time every day.

It is not recommended to take more than two tablets per day.

For patients with renal dysfunction, the dosage of the drug is reduced by 50%, at the discretion of the attending physician.

Use Agapurina 600 Retarda during pregnancy

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

Contraindications

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

Other possible contraindications include:

• porphyria disease (pigment metabolism disorder);
• increased bleeding, predisposition to hemorrhages, blood clotting disorders;
• cardiac arrhythmia;
• acute form of myocardial infarction, stroke;
• sclerotic changes in the coronary and/or cerebral vessels;
• pregnancy, breastfeeding, childhood and adolescence.

Among the relative contraindications are the following:

• low blood pressure;
• atherosclerosis;
• cardiac conduction disorders;
• impaired functions of the liver and urinary system;
• gastric ulcer and duodenal ulcer;
• postoperative condition of the patient.

Side effects Agapurina 600 Retarda

The use of the drug may result in the occurrence of some side effects:

• weight loss, dyspepsia, dry mouth, digestive disorders, cholecystitis, gastrointestinal hemorrhages;
• headaches, unmotivated fatigue, anxiety, insomnia at night and drowsiness during the day, hand tremors, convulsions, decreased visual function;
• increased heart rate, irregular heartbeat, heart pain, decreased blood pressure, subcutaneous hemorrhages, decreased fibrinogen and platelet levels in blood tests;
• in patients with heart failure, an increase in angina symptoms may be observed;
• dermatitis, anaphylaxis, allergic edema;
• rush of blood to the face, swelling, changes in the nail plates and hair, hyperthermia;
• the activity of liver enzymes increases.

Overdose

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

• increased heart rate;
• disorder of coordination functions;
• feeling of weakness and fatigue;
• dizziness;
• decrease in blood pressure;
• increase in temperature indicators;
• pronounced redness of the facial area;
• dyspeptic disorders.

If excessive use of the drug continues, areflexia, seizures, and bloody vomiting may occur.

If a single, excessively large dose of tablets is taken, a disturbance of consciousness and depression of respiratory functions may occur.

There is no specific antidote for taking a large amount of the drug. Use a suspension of sorbent preparations, gastric lavage, symptomatic treatment. Vomiting can only be induced immediately after accidentally taking a large dose of the drug. If time has passed after taking an excessive dose and convulsions appear, vomiting can be dangerous.

If an overdose is suspected, stop taking the drug immediately and consult a doctor. If the patient's general condition is unsatisfactory, provide him with maximum rest, access to fresh air, put him in a lying position and wait for the ambulance to arrive. Emergency care may include intravenous administration of epiphedrine (adrenaline).

The patient's condition must be monitored until complete regeneration of respiratory functions and cardiac activity.

Interactions with other drugs

Simultaneous use of the drug with antibiotics, thrombolytics, anticoagulants enhances each other's medicinal effect. During such combined use, blood clotting parameters should be monitored throughout the entire therapeutic course.

The combined use of Agapurin 600 Retard enhances the effect of insulin preparations, tablet antidiabetic forms and blood pressure lowering agents. Such combined use of drugs should be carried out with mandatory dosage adjustment.

Histamine H²-receptor blockers (cimetidine) may increase the content of the active substance Agapurin in the blood serum.

The combined use of Agapurin with other methylxanthine derivatives (theophylline, aminophylline, euphylline, theobromine) can provoke overexcitation 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 preparation Agapurin 600 Retard should be stored in a dark, dry place. The optimal temperature at which the preparation is stored may fluctuate within the range of 14-24°C. It is necessary to protect the storage areas of medicines from children.

The shelf life of the tablet medication is up to 4 years. After 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 drug have been violated, or damaged packaging is found.

The drug Agapurin 600 Retard is available in pharmacies with a prescription from a medical specialist.

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