Agapurin Retard

Agapurin RETARD is known in international pharmacology under the name Pentoxifylline. According to the ATC code, the drug belongs to a group of drugs that affect the cardiovascular system, in particular, it is a vasodilator. As for the pharmacological group, Agapurin is an adenosinergic drug that has angioprotective properties and is able to correct microcirculatory processes.

Agapurin is distinguished by its ability to protect the vascular wall, prevent the aggregation of blood elements and, due to the relaxation of the muscles of the vascular wall, increase their lumen and ensure the activation of microcirculation.

The drug is manufactured in the Czech Republic. The class of diseases for which Agapurin is used includes such pathological processes as vascular occlusion, ENT diseases, subarachnoid hemorrhage, atherosclerotic lesions of the inner wall of a blood vessel, peripheral vascular diseases, impaired sensitivity of the skin, including frostbite. In addition, it is necessary to add gangrene and ulcerative lesions with impaired blood circulation in a certain area of the body.

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Indications Agapurina Retarda

Due to the fact that Agapurin has an effect on blood vessels, thereby controlling the volume of blood that flows to an organ or tissue, the indications for the use of Agapurin RETARD are based on this main ability.

The drug is widely used for circulatory disorders of varying degrees in the peripheral areas. Among such pathological conditions, it is worth highlighting atherosclerotic lesions, vascular damage with the development of intermittent claudication, in pathology of the endocrine system, in particular, in diabetes mellitus, as well as in obliterating endarteritis.

Disruption of local blood supply with progression of trophic changes contributes to the development of varicose ulcerative defects, gangrene and post-stroke syndrome.

Indications for the use of Agapurin RETARD also include angioneuropathy, which is manifested by changes in sensitivity, pallor of the skin of the fingers, tips of the ears, nose, called acrocyanosis, and spasm of the distal extremities with the development of Raynaud's disease.

Agapurin has proven itself well in atherosclerotic lesions of the brain vessels with impaired cerebral circulation. Due to its ability to activate microcirculation, the drug is widely used in acute and chronic stages of insufficient blood supply to the retina and choroid, as well as in functional disorders of the structures of the inner ear.

Release form

Depending on the severity of the pathological condition, it is necessary to select a drug such that its release form ensures maximum efficiency due to its rate of absorption and onset of action.

Thus, if Agapurin needs to be taken in a short course during the acute stage of the disease to ensure a constant concentration of the active substance in the bloodstream, then it is recommended to use the tablet preparation. Each tablet has a round-convex shape, and the active substance itself is protected by a white outer shell.

The tablet contains 400 mg or 600 mg of pentoxifylline, the active ingredient, as well as auxiliary components such as povidone, eudragit, talc, macrogol and magnesium stearate. Agapurin RETARD has a dosage of 600 mg of pentoxifylline. Each blister contains 10 tablets, and one package contains 2 blisters.

The release form in the form of dragees suggests use for the prevention of vascular pathology or as maintenance therapy after the end of the acute period. Each dragee contains 100 mg of pentoxifylline, which in turn is significantly less than in tablets, therefore, using dragees, it is difficult to overdose on the drug. One bottle contains 60 dragees.

As for the injection administration of the drug, it is used for quick access of Agapurin to the vascular bed with immediate onset of action. In addition, this form of release is used for some diseases of the gastrointestinal tract to avoid its additional load with drugs. Each 1 ml of solution contains 20 mg of the active substance. Since each ampoule has 5 ml of the drug, it contains 100 mg of pentoxifylline, as in one dragee. The box contains 5 ampoules.

Pharmacodynamics

Pharmacodynamics of Agapurin RETARD is determined by the main properties of the active substance. Thus, there is a blockade of adenosine receptors, inhibition of phosphodiesterase activity and accumulation of cAMP in platelets, as a result of which they are less prone to aggregation.

In addition, pentoxifylline helps restore the ability of erythrocytes to change their shape and reduces their aggregation. In parallel, a decrease in the level of fibrinogen and a decrease in the adhesion of leukocytes to the endothelium are noted, which is ensured by a decrease in their activity with further traumatization of the endothelium. All these processes improve the rheological properties of blood by reducing viscosity.

Ultimately, the pharmacodynamics of Agapurin RETARD ensures activation of microcirculation, improving blood "fluidity" and reducing the risk of thrombosis. Pentoxifylline does not have a strong positive inotropic effect on the heart muscle. This means that Agapurin RETARD is not able to increase the force of heart contraction.

Pharmacokinetics

When using Agapurin intravenously, its concentration in the bloodstream depends on the rate of administration and dilution of the drug. As a result of proper selection, it is possible to maintain a constant concentration over a long period of time.

As for oral administration of the drug, the pharmacokinetics of Agapurin RETARD is based on its ability to be absorbed almost completely (more than 95%) as it passes through the gastrointestinal tract. After taking one tablet of the drug, pentoxifylline slowly begins to be released over 10-12 hours, due to which a constant concentration of the active substance can be maintained for up to 12 hours.

After complete absorption, pentoxifylline undergoes primary transformation, which ultimately provides an excess of 1-(5-hydroxyhexyl)-3,7-dimethylxanthine twice as compared to pentoxifylline. When taken orally, the half-life of the drug reaches 16 hours.

Pharmacokinetics Agapurin RETARD provides complete metabolism of pentoxifylline and its excretion (about 90%) by the kidneys in the form of bound, water-soluble polar metabolites. In this regard, it is necessary to take the drug with caution in people with serious disorders of the excretory system. In addition, the decay, half-life and absolute bioavailability increase in people with liver dysfunction.

Dosing and administration

The drug is taken orally. Since one tablet of Agapurin RETARD contains 600 mg of the active substance, it is necessary to take 2 tablets per day with an interval of approximately 12 hours between doses. The total volume of pentoxifylline per day should not exceed 1200 mg when taken orally to avoid the development of side effects.

The tablet must be taken whole, washed down with a sufficient amount of water. Basically, no more than 100 ml is required. In relation to food intake, Agapurin can be taken both during and after meals.

The method of administration and dosage should be reviewed and especially carefully monitored in people with insufficient urinary system function, in particular, kidneys. The adequacy of their work is assessed by determining creatinine clearance, which in such cases falls below 30 ml/min. With such indicators, the maximum daily dosage of pentoxifylline is 600 mg.

One tablet per day is allowed for people with severe liver failure. The method of administration and dosage should also be adjusted in case of low blood pressure and unstable hemodynamics in case of coronary artery disease or stenosis of cerebral vessels. In such cases, it is necessary to start with minimal doses, then gradually increase them.

Use Agapurina Retarda during pregnancy

Self-administration of this drug is strictly prohibited during pregnancy or lactation. However, under the supervision of specialists, it is still possible to use Agapurin RETARD during pregnancy. Everything depends on the woman's health.

If the doctor decides to prescribe, then it is necessary to take into account the pregnancy period in advance, since it is not advisable to take any medication before 12 weeks. This is due to the rapid formation of all fetal organs, the process of which may be disrupted.

The use of Agapurin RETARD during pregnancy is permitted in acute conditions of the pregnant woman, when there is a threat to the fetus or the expectant mother. The drug is used to improve microcirculatory processes in order to provide a sufficient volume of oxygen and nutrients to the fetus.

Particular attention is required by the pathological condition called fetoplacental insufficiency. In addition, the chronic stage of this process also negatively affects the nutrition of the fetus. The drug can be taken orally or by injection. The dosage and method of administration of the drug is decided exclusively by the doctor.

Contraindications

Contraindications for the use of Agapurin RETARD include acute and longer-term conditions, including acute disruption of the blood supply to the heart muscle, as a result of which a certain area of the muscle does not receive the necessary volume of blood and a heart attack develops.

In addition, retinal hemorrhages and acute cerebral hemorrhages are also contraindications to the use of Agapurin. Acute conditions in which massive bleeding with loss of a large volume of circulating blood is observed prevent the prescription of this drug. Do not forget about the individual characteristics of each person and intolerance to both pentoxifylline itself and auxiliary substances.

There is no experience with the use of the drug in children under 18 years of age, therefore, in order to avoid the development of severe side effects, its use is not recommended.

Contraindications to the use of Agapurin RETARD, as already mentioned, include the period of pregnancy and breastfeeding.

Side effects Agapurina Retarda

The drug in most cases does not cause adverse effects, but side effects of Agapurin RETARD are still possible if some recommendations are not followed. Among them, it is necessary to highlight strict adherence to the dosage and frequency of administration, as well as refusal to use it if there are contraindications.

In some cases, there may be a disruption in the digestion process with the appearance of nausea, vomiting, upset stomach and a feeling of fullness in the stomach.

Side effects of Agapurin RETARD on the nervous system are characterized by some changes in the psycho-emotional state with the appearance of headaches, increased excitability, sleep disturbances and increased sweating.

Skin reactions may manifest as a decrease in the sensitivity threshold with rashes and itching, which usually decreases as the dosage is reduced and Agapurin is completely discontinued.

From the endocrine system and metabolism in general, a decrease in blood glucose levels can be noted. As for the cardiovascular system, there is increased heart rate, conduction and rhythm disturbances in the heart, attacks of chest pain and bleeding, especially in people with an increased tendency to this.

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Overdose

An overdose is possible in cases where the drug was taken in unreasonably increased doses or in the absence of therapy correction in case of kidney or liver pathology. To avoid this condition, regular medical monitoring of the condition of a person taking pentoxifylline is necessary.

However, if a large dose of the drug was taken, the overdose may initially manifest itself as nausea, dizziness, disturbances in the conduction and rhythm of the heart, increased heart rate and decreased systemic arterial pressure.

In addition, symptoms of urticaria, disturbances of the psycho-emotional state with increased excitability, irritability, a feeling of “hot flashes”, up to the development of tonic-clonic seizures and a complete lack of motor activity and reflexes are possible.

If the vomit resembles "coffee beans", then one should suspect bleeding from the upper digestive system, for example, from the stomach.

For therapeutic purposes, it is advisable to activate the excretion and stop further absorption of pentoxifylline into the bloodstream. To do this, perform gastric lavage and use activated carbon or another sorbent. In case of bleeding, it is necessary to use hemostatic agents up to surgical methods of stopping bleeding.

Interactions with other drugs

The interaction of Agapurin RETARD with other drugs is based on the potentiating effect of both pentoxifylline itself and other drugs. For example, when using Agapurin together with antihypertensive and other vasoconstrictors, the effect of the latter is enhanced, which can lead to an excessive decrease in blood pressure.

The same is observed when pentoxifylline is combined with adrenergic agents and ganglionic blockers. Parallel administration with xanthines ensures activation of the nervous system.

Interactions of Agapurin RETARD with other drugs, such as insulin and other oral hypoglycemic agents, provide the influence of the latter with a greater effect, which leads to an excessive decrease in blood glucose. As a result, it is recommended to measure blood sugar levels more often, and then, based on the data obtained, subject to continued therapy with Agapurin, adjust its dosage.

Increased risk of bleeding in people taking pentoxifylline and anticoagulants, antiplatelet agents or thrombolytic agents together. In this case, prothrombin time should be monitored and checked regularly.

As for pentoxifylline, its effect can be potentiated by cimetidine with the development of unwanted side effects.

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Storage conditions

The storage conditions of Agapurin RETARD ensure its longer shelf life and provision of the necessary therapeutic effects. If the storage rules of the drug are not followed, it may lose its therapeutic properties before the specified period of the last use of pentoxifylline. Ultimately, one can expect not only effects that do not correspond to the drug, but also the appearance of various side effects.

Thus, the storage conditions of Agapurin RETARD suggest its location in a place without exposure to direct sunlight and moisture. The temperature regime must also be observed, so the temperature corresponds to a mark no higher than 25 degrees.

In addition, it is important to remember that storage requires that children have no access to the drug. They may take a large dose of the drug, after which side effects and symptoms of overdose or poisoning may occur. Moreover, it is important to remember that studies on the use of pentoxifylline in childhood have not been conducted, so it is not fully known what kind of reactions can be expected from the administration of the drug.

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Shelf life

The expiration date is no less important than the storage conditions. They provide the known therapeutic effects of Agapurin for a certain period of time. The expiration date shows the duration of the period during which the drug has the necessary therapeutic property, it is necessary in each individual case.

Thus, Agapurin has a shelf life of 4 years. For 4 years, the manufacturer guarantees the presence of proven medicinal effects of pentoxifylline without the development of side effects, provided that the rules for its use are followed.

The shelf life of the drug also depends on its storage conditions, since if this requirement is not taken into account, pentoxifylline not only loses its beneficial properties, but can also provoke the development of undesirable side effects of varying severity.

After the specified date of the last dose of the drug, it is strictly forbidden to use Agapurin RETARD, as its effects are unpredictable.