Agapurin Retard

Agapurin RETARD in international pharmacology is known as Pentoxifylline. According to the ATS 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 agent that has angioprotective properties and is able to correct microcirculatory processes.

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

The drug is produced in the Czech Republic. The class of diseases for which Agapurin is applied includes such pathological processes as vascular occlusion, diseases of the ENT organs, subarachnoid hemorrhage, atherosclerotic lesion of the inner wall of the blood vessel, peripheral vascular disease, impaired sensitivity of the skin, including with frostbite. In addition, it is necessary to add gangrene and ulcerative lesions in case of circulatory disturbance of a certain part of the body. 

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Indications of the agapurina Retarda

Due to the fact that Agapurin affects the vessels, thereby controlling the volume of blood that enters the body or tissues, indications for the use of Agapurin Retard are based on its given basic ability.

The drug is widely used for circulatory disorders of various degrees in the peripheral departments. Among such pathological conditions it is necessary to distinguish atherosclerotic lesion, vascular damage with the development of intermittent claudication, in the pathology of the endocrine system, in particular, in diabetes mellitus, as well as with obliterating endarteritis.

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

Indications for use Agapurin RETARD also include angioneuropathies, which are manifested by a change in sensitivity, paleness of the skin of the fingers, tips of the ears, a nose called acrocyanosis, and spasm of the distal limbs with the development of Raynaud's disease.

Agapurin has well proven itself in the atherosclerotic lesions of cerebral vessels with cerebral circulation disorders. 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 of the eye, as well as in functional disorders of the structures of the inner part of the ear.

Release form

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

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

The tablet in its composition has 400 mg or 600 mg of pentoxifylline - an active ingredient, as well as auxiliary components such as povidone, eudragit, talc, macrogrol and magnesium stearate. Agapurin RETARD has a dosage of 600 mg of pentoxifylline. In each blister there are 10 tablets, and in one package - 2 blisters.

The release form in the form of a dragee assumes application for prophylaxis of a pathology of vessels or as maintenance therapy after the termination of the acute period. Each pellet has 100 mg of pentoxifylline, which in turn is significantly less than in tablets, therefore, using a pellet, it is difficult to overdose the drug. In one bottle there are 60 pills.

With regard to the injection management of the drug, it is used to quickly access Agapurin in the vascular bed with an immediate onset of action. In addition, this form of release is used in some diseases of the gastrointestinal tract in order to avoid its additional load of drugs. Each 1 ml of the solution contains 20 mg of the active ingredient. Since each ampoule has 5 ml of the drug, therefore, it contains 100 mg of pentoxifylline, as in one pellet. There are 5 ampoules in the box.

Pharmacodynamics

Pharmacodynamics Agapurin RETARD is due to the basic properties of the active substance. Thus, blockade of adenosine receptors, inhibition of phosphodiesterase activity and accumulation of cAMP in platelets are observed, as a result of which they are less slopes to aggregation.

In addition, pentoxifylline helps restore the ability of red blood cells to change their shape and reduces their aggregation. Parallel to this, there is a decrease in the level of fibrinogen and a decrease in the adhesion of leukocytes to the endothelium, 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 the viscosity.

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

Pharmacokinetics

With intravenous use of Agapurin, its concentration in the bloodstream depends on the rate of administration and dilution of the drug. As a result of correct selection it is possible to achieve maintenance of a constant concentration over a long period of time.

As for the 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 release during 10-12 hours, and therefore the constant concentration of the active substance can be maintained up to 12 hours.

After complete absorption, pentoxifylline undergoes a primary transformation, which ultimately ensures that 1- (5-hydroxyhexyl) -3,7-dimethylxanthine is exceeded twice as much as pentoxifylline. When taking the drug, the half-life reaches 16 hours.

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

Dosing and administration

The drug is taken orally. Since one tablet of Agapurin RETARD has 600 mg of active ingredient, therefore, 2 tablets should be taken per day with an interval between doses of approximately 12 hours. In a day, the total volume of pentoxifylline should not exceed 1200 mg when ingested to avoid the development of side effects.

The tablet should be consumed in a holistic form, with plenty of water. Basically, not more than 100 ml is required. In relation to food intake, Agapurin can be taken both during and after a meal.

The method of application and dose should be reviewed and especially carefully monitored by people who have insufficient function of the urinary system, in particular, the kidneys. Assessment of the adequacy of their work is done by determining the clearance of creatinine, which in such cases falls below 30 ml / min. At such rates, 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 dose should also be adjusted with reduced arterial pressure and the presence of unstable hemodynamics in coronary artery lesions or stenosis of cerebral vessels. In such cases, you should start with a minimum dose, then gradually increase them.

Use of the agapurina Retarda during pregnancy

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

If the doctor decided to appoint, then you must first take into account the length of pregnancy, because in a period of up to 12 weeks is not desirable to take any medication. This is due to the rapid laying of all organs of the fetus, the process of which can be disrupted.

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

Particular attention requires a pathological condition, called feto-placental insufficiency. In addition, the chronic stage of this process also adversely affects the nutrition of the fetus. The drug can be taken either orally, or in the form of injections. Dosage and the way of administration of the drug is decided solely by the doctor.

Contraindications

Contraindications to the use of Agapurin RETARD include acute and with a prolonged course of the condition, which includes an 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 develops a heart attack.

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

Experience in the use of the drug in children under 18 years is absent, therefore, to avoid the development of pronounced side effects, its use is not recommended.

Contraindications to the use of Agapurin Retard, as already mentioned, include the period of pregnancy and lactation.

Side effects of the agapurina Retarda

The drug in most cases does not cause adverse effects, but still possible side effects of Agapurin RETARD when some recommendations are not followed. Among them, it is necessary to emphasize the strict observance of dosage and the frequency of reception, as well as the refusal to use it in the presence of contraindications.

In some cases, there may be a violation of the process of digesting food with the appearance of nausea, vomiting, a disorder of the stool and a feeling of overflow of the stomach.

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

Skin reactions may be manifested by a decrease in the sensitivity threshold with rashes and itching, which usually decreases as the dosage is reduced and completely stops taking Agapurin.

From the endocrine system and metabolism in general, we can note a decrease in blood glucose. With regard to the cardiovascular system, there is a rapid heartbeat, conduction and rhythm disturbances in the heart, attacks of chest pain and the appearance of bleeding, especially in people with increased predisposition to it. 

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Overdose

Overdose is possible in cases when the drug was taken in unreasonably increased doses or in the absence of correction of therapy for kidney or liver pathology. To avoid this condition, regular monitoring of the doctor for the condition of a person who takes pentoxifylline is necessary.

However, if a large dose of the drug has been taken, then an overdose can be manifested at first by nausea, dizziness, a violation of the rhythm and performance of the heart, increased heart rate and a decrease in systemic blood pressure.

In addition, there may be symptoms of urticaria, a disturbance in the psycho-emotional state with increased excitability, irritation, a feeling of "hot tides", up to the development of tonic-clonic seizures and a complete lack of motor activity and reflexes.

If the vomit is reminiscent of "coffee beans", then it is necessary to suspect bleeding from the upper parts of the digestive system, for example, from the stomach.

With a therapeutic purpose, it is advisable to activate the excretion and stop further absorption of pentoxifylline into the bloodstream. To do this, you should perform gastric lavage and use activated charcoal or another sorbent. In case of bleeding, it is necessary to use blood-restoring means up to surgical methods of stopping bleeding.

Interactions with other drugs

Interactions Agapurin RETARD with other drugs is based on the potentiating effects of both pentoxifylline itself and other agents. For example, with the combined use of Agapurin and antihypertensive and other vasoconstrictors, there is an increase in the effect of the latter, which can lead to an excessive decrease in blood pressure.

The same is noted when pentoxifylline is combined with adrenergic agents and ganglion blockers. Parallel administration with xanthines provides activation of the nervous system.

Interactions Agapurin RETARD with other drugs, such as insulin and other oral hypoglycemic agents, provide the effect of the latter with great effect, which leads to an excessive decrease in glucose in the blood. Because of this, it is recommended to measure blood sugar more often, and further on the basis of the received data, under condition of continuing therapy with Agapurin, to correct its dosage.

An increased risk of bleeding in people who jointly take pentoxifylline and anticoagulants, antithrombocytic or thrombolytic agents. In this case, you should pay attention to prothrombin time and regularly monitor it.

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

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Storage conditions

The storage conditions of Agapurin RETARD cause its longer preservation and the provision of the necessary therapeutic effects. If the rules for storage of the drug are not observed, it may lose its therapeutic properties before the indicated time of the last use of pentoxifylline. In the end, we can expect not only the effects that do not correspond to the drug, but also the appearance of various side reactions.

Thus, the storage conditions of Agapurin RETARD assume its location in a place without direct sunlight and moisture. The temperature regime must also be respected, so the temperature corresponds to a mark not higher than 25 degrees.

 In addition, do not forget that storage provides for lack of access to the drug of children. They can take a large dose of the drug, after which there may be side effects and symptoms of an overdose or poisoning. It is all the more necessary to remember that studies on the use of pentoxifylline in childhood have not been carried out, therefore, it is not known exactly which reactions can be expected for the administration of the drug.

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Shelf life

The expiration date is not less important than the storage conditions. They provide known therapeutic effects of Agapurin for a certain period of time. The expiry date shows the length of the period during which the drug has the necessary therapeutic property, it is necessary in each individual case.

So, Agapurin has a shelf life of 4 years. For 4 years, the manufacturer guarantees the availability of proven medicinal effects of pentoxifylline without the development of adverse reactions, provided that the rules for its administration are met.

The term "viability" of the drug also depends on the conditions of its storage, since in the absence of taking into account this requirement, pentoxifylline not only loses its useful properties, but also can provoke the development of undesirable side effects of varying severity.

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