What helps "Pentoxifylline". Instructions for the use of injections and tablets. Pentoxifylline is the best drug for blood circulation

Instructions for use

Attention! The information is provided for informational purposes only. This manual should not be used as a guide to self-medication. The need for appointment, methods and doses of the drug are determined solely by the attending physician.

general characteristics

international and chemical names: pentoxifylline; 3,7-dimethyl-1-(5-oxohexyl)-3,7-dihydro-1H-perine-2,6-dione);

basic physical and chemical properties: transparent colorless or slightly yellowish liquid;

compound: 1 ml contains pentoxifylline 0.02 g;

Excipients: sodium chloride, water for injection.

Release form. Injection.

Pharmacotherapeutic group

Drugs affecting the cardiovascular system. Peripheral vasodilators (Peripheral vasodilators- drugs that dilate small arteries and veins, acting directly on the smooth muscles of the vessels). ATS code CO4A D03.

Pharmacological properties

Pharmacodynamics. A tool that improves microcirculation (microcirculation- blood supply to tissues, the movement of blood in the smallest vessels), angioprotector. The mechanism of action is due to the inhibition of phosphodiesterase and the accumulation of cyclic adenosine-monophosphoric acid with a decrease in the concentration of intracellular calcium in vascular smooth muscles and in blood cells. brakes aggregation (Aggregation(attachment) - the process of combining elements into one system) platelets and erythrocytes (red blood cells- red blood cells containing hemoglobin. They carry oxygen from the lungs to the tissues and carbon dioxide from the tissues to the respiratory organs. Produced in red bone marrow. 1 mm3 of a healthy person's blood contains 4.5-5.0 million erythrocytes), increases their elasticity, reduces the level of fibrinogen in plasma (Plasma- the liquid part of the blood, which contains formed elements (erythrocytes, leukocytes, platelets). Various diseases (rheumatism, diabetes mellitus, etc.) are diagnosed by changes in the composition of blood plasma. Medicines are prepared from blood plasma and enhances fibrinolysis, reducing blood viscosity and improving its rheological properties. It has a weak myotropic vasodilating effect, somewhat reduces the total peripheral vascular resistance and has a moderate positive inotropic (Inotropic- changes the force of heart contraction) action. Slightly expands coronary (Coronary- the surrounding organ in the form of a crown (crown), related to the coronary arteries of the heart, for example, coronary circulation) vessels. Helps to improve the supply of oxygen to tissues, to the greatest extent - in the limbs and in central nervous system (central nervous system- the main part of the nervous system, represented by the spinal cord and brain. Functionally, the peripheral and central nervous systems represent a single whole. The most complex and specialized part of the central nervous system is the cerebral hemispheres). At occlusion (Occlusion- the act of closing or the state of closing. Occlusive dressing - closing dressing) of affected peripheral arteries (intermittent claudication) leads to lengthening of walking distances, elimination of night cramps of the calf muscles and pain at rest.

Pharmacokinetics. Quickly and completely absorbed. By binding to the membranes of erythrocytes, it undergoes biotransformation (Biotransformation- a set of chemical transformations of a medicinal or xenogeneic substance in the body) first in erythrocytes, then in the liver with the formation of two main metabolites: 1-5-hydroxyhexyl-3,7-dimethylxanthine and 1-3-carboxypropyl-3,7-dimethylxanthine. It is excreted mainly by the kidneys, a small part (4%) - through the intestines, can be excreted through breast milk.

Indications for use

Cerebrovascular pathology, in particular atherosclerosis (Atherosclerosis- a systemic disease characterized by damage to the arteries with the formation of lipid (mainly cholesterol) deposits in the inner lining of the vessels, which leads to a narrowing of the lumen of the vessel up to complete blockage) cerebral vessels, conditions after the transferred myocardial infarction (myocardial infarction- ischemic necrosis of the myocardium, due to a sharp decrease in the blood supply to one of its segments. The basis of MI is an acutely developed thrombus, the formation of which is associated with the rupture of an atherosclerotic plaque); diabetic nephroangiopathy and other diabetic angiopathy (Angiopathy- any pathology of the blood or lymphatic vessels), peripheral circulatory disorders ( Raynaud's disease (Raynaud's disease- a disease of the cardiovascular system, in which there are paroxysmal disorders of the arterial blood supply to the hands and (or) feet, arising under the influence of cold or excitement due to trophic disorders), endar-teriitis, etc.); vascular pathology of the eye (acute and chronic (Chronic- a long, ongoing, protracted process, occurring either constantly or with periodic improvements in condition) insufficient blood supply to the retina and choroid). Functional hearing disorders of vascular origin.

Dosage and administration

Intraarterially, intravenously, intramuscularly. In acute disorders of the brain (ischemic stroke) and peripheral circulation, 0.1 g of the drug is administered intravenously in 250-500 ml of 0.9% sodium chloride solution or 5% solution glucose (Glucose- grape sugar, a carbohydrate from the group of monosaccharides. One of the key metabolic products that provides energy to living cells)(duration of administration 90-180 minutes); intra-arterially - first at a dose of 0.1 g in 20-50 ml of 0.9% sodium chloride solution, then - 0.2-0.3 g in 30-50 ml of the solvent. The rate of administration is 0.1 g (5 ml of a 2% solution of Pentoxifylline) for 10 minutes. The daily dose for intravenous administration can subsequently be increased by 50–100 mg until a maximum daily dose of 300 mg is reached. In severe cases, the introduction of 400 mg / day in 2 divided doses is acceptable.
Intramuscularly deep - 100-200 mg 2-3 times a day. Parallel to parenteral (parenteral- dosage forms administered bypassing the gastrointestinal tract, by applying to the skin and mucous membranes of the body; by injection into the vascular bed (artery, vein), under the skin or muscle; by inhalation, inhalation (see Enteral)) application can be used orally, in a daily dose of 800-1200 mg in 2-3 doses. In severe disorders of local circulation in adults and children over 12 years of age (weighing more than 50 kg), the drug is prescribed 0.6 g 2 times a day.

Side effect

Headache, dizziness, nervousness, drowsiness or insomnia. Tachycardia (Tachycardia- an increase in heart rate to 100 or more beats per minute. Occurs with physical and nervous stress, diseases of the cardiovascular and nervous systems, diseases of the endocrine glands, etc.), attacks angina pectoris (angina pectoris- a syndrome caused by myocardial ischemia and characterized by the episodic appearance of a feeling of discomfort or pressure in the precordial region, which in typical cases occur during exercise and disappear after its cessation or administration of nitroglycerin under the tongue (angina pectoris)), arrhythmia (Arrhythmia- violation of the normal rhythm of the heart. Arrhythmia manifests itself in an increase (tachycardia) or slowdown (bradycardia) of heart contractions, in the appearance of premature or additional contractions (extrasystole), in heart attacks (paroxysmal tachycardia), in the complete irregularity of the intervals between individual heart contractions (atrial fibrillation)), hypotension. Nausea, vomiting, gastralgia, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis, increased concentration of hepatic enzymes (Enzymes- specific proteins that can significantly accelerate chemical reactions occurring in the body, without being part of the final reaction products, i.e. are biological catalysts. Each type of enzyme catalyzes the transformation of certain substances (substrates), sometimes only a single substance in a single direction. Therefore, numerous biochemical reactions in cells are carried out by a huge number of different enzymes. Enzyme preparations are widely used in medicine) in the blood, changes in body weight, edema (Edema- swelling of tissues as a result of a pathological increase in the volume of interstitial fluid), dyspeptic phenomena. Leukopenia (Leukopenia- the content of leukocytes in peripheral blood is less than 4000 per 1 μl, due to the impact on the body of various damaging factors), pancytopenia (Pancytopenia- a pronounced decrease in the number of red blood cells, all types of white blood cells and platelets in the circulating blood), thrombocytopenia, hypofibrinogenemia, bleeding. Hyperemia (Hyperemia- plethora caused by increased blood flow to any organ or tissue area (arterial, active hyperemia) or its difficult outflow (venous, passive, congestive hyperemia). Accompanies any inflammation. Artificial hyperemia is caused for therapeutic purposes (compresses, heating pads, banks)) skin, rarely - rash, itching (Itching- a modified feeling of pain due to irritation of the nerve endings of pain receptors), hives (Hives- a disease characterized by the formation of limited or widespread itchy blisters on the skin and mucous membranes).
With intravenous and intra-arterial administration - a decrease in blood pressure.

Contraindications

Hypersensitivity (Hypersensitivity- increased patient response to the usual dose of the drug) to methylxanthine derivatives, acute infarction myocardium (Myocardium- the muscular tissue of the heart, which makes up the bulk of its mass. Rhythmic coordinated contractions of the myocardium of the ventricles and atria are carried out by the conduction system of the heart), heavy bleeding, pronounced atherosclerosis of the coronary and cerebral vessels (intra-aortic administration is contraindicated), hemorrhagic stroke (Stroke- acute violation of cerebral circulation (hemorrhage, etc.) with hypertension, atherosclerosis, etc. Manifested by headache, vomiting, impaired consciousness, paralysis, etc.), retinal hemorrhages, pregnancy, breastfeeding, children under 12 years of age.

Overdose

Symptoms: decrease in blood pressure, hyperemia of the skin, hypotension, drowsiness, agitation (Agitation- nervous anxiety associated with confusion, manifested in people under unexpected, unpleasant or dangerous circumstances, during natural disasters), convulsions, impaired consciousness, signs of gastrointestinal bleeding (vomiting the color of "coffee grounds"), fever.

Treatment: general resuscitation measures to restore cardiovascular activity (including normalization of blood pressure) and respiratory function; the use of diazepam in convulsive syndrome. specific antidote (Antidotes- drugs used to treat poisoning in order to neutralize the poison and eliminate the pathological disorders caused by it) no.

Application features

When using Pentoxifylline, the patient should be in a horizontal position. Treatment should be carried out under the control of blood pressure. With arterial hypotension, the dose is increased gradually. Patients with severe atherosclerosis should not be administered intra-arterially.
In heart failure, the administration of cardiac glycosides (Glycosides- organic substances, the molecules of which consist of a carbohydrate and a non-carbohydrate component (aglycone). Widely distributed in plants, where they can be a form of transport and storage of various substances).
Before the introduction of Pentoxifylline, it is necessary to achieve compensation of blood circulation.
In diabetic patients taking hypoglycemic agents, the appointment of large doses of Pentoxifylline can cause hypoglycemia (dose adjustment is required).
When assigned with anticoagulants (Anticoagulants- drugs that reduce blood clotting) it is necessary to monitor the indicators of the blood coagulation system.
Patients who have undergone recent surgery should systematically monitor the level hemoglobin (Hemoglobin- red respiratory pigment of blood. It consists of a protein (globin) and an iron-containing compound (heme). Carries oxygen from the respiratory organs to the tissues and carbon dioxide from the tissues to the respiratory organs) and hematocrit.
Use the drug with caution in patients with peptic ulcers of the stomach and duodenum (Duodenum- the initial section of the small intestine (from the outlet of the stomach to the jejunum). The length of the human duodenum is equal to the diameters of 12 fingers (hence the name))(risk of bleeding).
In elderly patients and patients with liver and kidney diseases, the dose of Pentoxifylline is reduced. At creatinine clearance (Creatinine clearance- an indicator characterizing the glomerular filtration rate. The level of creatinine in the blood is used to assess the efficiency of the kidneys. Creatinine clearance is the volume of blood plasma that is cleared of creatinine in 1 minute when passing through the kidneys) less than 10 ml / min appoint 50-70% of the dose.

Interaction with other drugs

Enhances the effect of antihypertensive and antidiabetic drugs (the dose of the drug should be reduced). When used together with sympatholytics (sympatholytics- medicinal substances that prevent the transfer of excitation from sympathetic nerves to effectors (for example, to the muscles of the vascular wall, which causes vasodilation)), ganglioblock-torami, vasodilators (Vasodilators- 1) vasomotor nerve fibers that expand the lumen of blood vessels. 2) Drugs that cause dilation of blood vessels) possible lowering of blood pressure; with ketolorac, meloxicam - an increase in prothrombin time with a risk of bleeding; with heparin, fibrinolytic drugs and indirect anticoagulants - increased anticoagulant action. Cimetidine significantly increases the concentration of Pentoxifylline in the blood with an increased likelihood of side effects.

Product General Information

Best before date. 2 years.

Storage conditions. Keep out of the reach of children, protected from light, at a temperature not exceeding 25 ° C.

Holiday conditions. On prescription.

Package. Solution for injections (Injection- injection, subcutaneous, intramuscular, intravenous, etc. introduction into the tissues (vessels) of the body of small amounts of solutions (mainly drugs)) 2%, 5 ml in ampoules No. 5.

Manufacturer.LLC "Pharmaceutical company "Health".

Location. 61013, Ukraine, Kharkov, st. Shevchenko, 22.

Website. www.zt.com.ua

Preparations with the same active ingredient

  • Pentoxifylline dragee - "Darnitsa"
  • Pentoxifylline tablets - "Darnitsa"
  • Pentoxifylline tablets - "Health"

This material is presented in free form on the basis of the official instructions for the medical use of the drug.

In diseases caused by disorders of the circulatory system, a course of Pentoxifylline is prescribed. According to the instructions for use of the drug, intravenous and intra-arterial administration of an angioprotector is indicated in the acute and severe phase of various pathologies. The drug from the line of antispasmodics enhances blood microcirculation due to vasodilation, its saturation with oxygen.

The main characteristics of the drug

The official name of the drugPentoxifylline. Synthetic active substance is a derivative of dimethylxanthine
Pharmacotherapeutic groupBelongs to the line of peripheral vasodilators - drugs that have an expanding effect on the area of ​​vascular smooth muscle
In what form is Pentoxifylline produced?Tablets with a dosage of 100, as well as 400 mg
Tablets with a dosage of 400, as well as 600 mg, with prolonged action
Ampoules with a dosage of 5 ml with a solution for injection
Purpose of PentoxifyllineThe action of the drug is based on the inhibition (slowdown) of phosphodiesterase during the accumulation of cyclic AMP (a group of enzymes) in the cell mass of the smooth muscles of the vessels penetrating the tissues of human organs

An important result of the use of Pentoxifylline, as an angioprotector, is the inhibition of platelet aggregation, which contributes to blood thinning and improvement of its rheological properties.

Due to a weak myotropic effect and a slight expansion of the coronary vessels, Pentoxifylline enriches the tissues of organs with oxygen. In severe form of the disease, as well as the acute phase of the disease, the use of the drug in ampoules is recommended.

Instructions: features of the action of a vasodilator

Pharmacology: how the drug acts on the body

  • Pentoxifylline is part of the hemorheological group of drugs that restore the plasticity of erythrocytes, which improves the saturation of blood vessels with them. The result is the restoration of blood circulation in tissue structures, which is necessary for symptoms of hypoxia.
  • The instruction informs that during treatment with Pentoxifylline, the threat of aggregation (gluing) of erythrocytes is reduced, which increases the blood supply to organs due to the free penetration of cells into the space of the extravascular bed. Intravenous administration increases blood volume without changing heart rate.
  • Due to the antianginal effect of the drug, there is an increase in the lumen of the coronary arteries, which enhances the saturation of the myocardium with oxygen. The influx of oxygen into the blood (oxygenation) is realized by expanding the pulmonary vessels, increasing the tone of the respiratory muscles, the diaphragm.
  • Pentoxifylline, administered intravenously, affects the function of collateral circulation, increasing the throughput of the bypass branches of blood vessels (collaterals). According to the instructions, the appointment of the drug helps to increase the bioenergetic activity of the nervous system and brain performance by reducing blood viscosity.
  • The introduction of Pentoxifylline intravenously with lesions of the arteries of the extremities contributes to the restoration of peripheral circulation. The result is relief from pain and cramps in the area of ​​the calf muscles, an increase in the distance traveled when walking in patients suffering from intermittent claudication.

Important! The instruction warns against the inadmissibility of self-medication with Pentoxifylline tablets. The introduction of the solution intravenously or intra-arterially is associated with certain features. Therefore, the procedure should be performed by a health worker according to the scheme prescribed by the doctor.

Pharmacokinetics: what happens to the drug in the body

  • Suction. Due to its good penetrating ability, the active substance is completely absorbed. The instruction reports that the Pentoxifylline solution for injection, when administered intravenously, begins to act faster.
  • Distribution. After taking the tablets, the transformation of dimethylxanthine occurs in the liver with the formation of the main metabolites. Four hours later, Pentoxifylline, administered intravenously, reaches its maximum concentration in blood plasma, maintaining therapeutic activity during the day.
  • Excretion of dimethylxanthine is carried out by the kidneys, a small part of the drug is evacuated by the intestines. Intravenous administration of the drug reduces the half-life of the substance to 30 minutes. With the appointment of Pentoxifylline during the lactation period, its traces are found in breast milk.

What diseases are angioprotector prescribed for?

The use of Pentoxifylline is relevant in the treatment of diseases associated with impaired peripheral circulation. The instruction recommends including the drug in the treatment regimen for the following pathologies:

  • obliterating endarteritis;
  • symptoms of progression of coronary heart disease;
  • signs of cerebrovascular accident (acute as well as chronic);
  • problems with hearing and vision due to vascular pathologies;
  • in case of atherosclerotic, dyscirculatory encephalopathies;
  • with the development of ischemic (cerebral) stroke;
  • after trophic disorders of the tissue cover against the background of microcirculation problems (the consequences of thrombophlebitis, trophic ulcers, gangrene, frostbite);
  • development of diabetic angiopathy, angioneuropathy (symptoms of Raynaud's disease).

From the instructions it is known that after intravenous administration of a solution of Pentoxifylline, the saturation of organs with blood improves due to its dilution. The drug has a fairly wide range of applications, due to the ability of dimethylxanthine to dilate blood vessels, the drug helps to increase ventilation of the lungs. Therefore, it is included in the treatment regimen for bronchial asthma, as well as obstructive bronchitis.

The effect on peripheral vascular tone explains the connection of Pentoxifylline to the treatment of vascular impotence, algomenorrhea, the threat of miscarriage, and muscular dystrophy.

When is angioprotective therapy contraindicated?

As for any medication, the instructions for Pentoxifylline stipulate a number of situations when the use of the drug is contraindicated:

  • in the presence of hypersensitivity to xanthine derivatives;
  • during the acute stage of myocardial infarction or hemorrhagic stroke;
  • with obvious symptoms of atherosclerosis of a cerebral or coronary nature;
  • in case of extensive bleeding, porphyria;
  • with serious violations of the heart rhythm, uncontrolled hypertension.

The instruction warns that any form of release of the drug is not prescribed to children under the age of 18, as well as to women during pregnancy and lactation. However, with a lack of blood supply to the placenta, treatment with Pentoxifylline in special cases is provided under the supervision of a physician. Preference is given to the use of a dropper, as the most gentle form of intravenous drug administration.

Methods of using the drug

oral intake

Guided by the information given in the instructions, the medicine in tablets is taken orally after meals for 1-3 months. Treatment begins with a daily dose of 600 mg, dividing it into three doses, two tablets at a time, the daily dose limit is no more than 1200 mg. After achieving positive results of treatment, the dosage is gradually reduced, taking one tablet three times a day. Oral therapy is designed for a month.

Parenteral application

Intended for injection Pentoxifylline is packaged in ampoules containing 5 ml of treatment solution. The powder of the active substance is dissolved in water with the addition of sodium chloride. According to the instructions, the introduction of an antispasmodic to a patient in the supine position can be performed by several methods with the complex development of cerebrovascular or angiopathic pathologies.

  • Intravenously, the drug is administered by drip, dissolving one ampoule of Pentoxifylline in a 250 ml container with a sodium chloride solution, which can be replaced with a glucose solution if necessary. Drip administration of the drug solution should take place slowly - one and a half to two hours. If the procedure is well tolerated, the volume of the daily dose is increased to 300 mg.
  • Parenterally, you can enter the drug directly into the artery, starting with a dose of 100 mg of the substance in a solution of sodium chloride (50 ml). In accordance with the indications, the dose of the following injections is increased to 200-300 mg (10-15 ml), the volume of the solvent is up to 50 ml. For 10 minutes, 5 ml of a solution of Pentoxifylline 2% concentration (100 mg) is injected.

Important! The instruction recommends monitoring the rate of receipt of the vasodilator so that it does not exceed 100 mg of the solution received by the patient within an hour. In other words, in 60 minutes, one ampoule should be introduced into the patient's body.

When choosing an intramuscular method of drug delivery, injections are given three times a day. For one injection, 100-200 mg of the active substance is required, it should be injected deep into the muscle tissue. Parenteral use of Pentoxifylline can be supplemented by taking tablets, but without exceeding the daily dose. The duration of the therapeutic course and the volume of the daily dosage are set by the doctor, focusing on the individual characteristics of the patient's health, taking into account the severity of the clinical symptoms of the diagnosed pathology.

Side effects of Pentoxifylline injections

  • The nervous system can signal a headache with dizziness, the development of convulsive and anxiety syndromes.
  • The skin of the face is able to respond with hyperemia, flushing, the development of swelling of the whole body, as well as brittle nails.
  • The problems of the digestive system are indicated by symptoms of exacerbation of gastric diseases, problems with the intestines, weight loss.
  • Failures in the work of the cardiovascular system are manifested by heart rhythm disturbances, a decrease in blood pressure, and the progress of angina pectoris.
  • Allergy manifestations, visual defects, changes in laboratory blood tests (liver tests, etc.) are not excluded.

The use of Pentoxifylline for the treatment of operated patients, as well as patients with erosive pathologies of the gastrointestinal tract, should be continuously monitored to eliminate the risk of internal bleeding. A feature of intravenous therapy in the elderly is the use of small doses after checking the compatibility of the drug with other drugs.

Additional information from the instructions

Special instructions for useCaution requires the appointment of injections with low blood pressure
During the use of Pentoxifylline, it is necessary to control blood pressure
With the introduction of dimethylxanthine in conjunction with taking anticoagulants, it is important to monitor the parameters of blood clotting
Actions in case of overdoseImmediately rinse the digestive tract, take enterosorbents. Further treatment is aimed at relieving symptoms, bleeding requires a prompt response.
Terms of interaction between drugsPentoxifylline (intravenously) enhances the effect of anticoagulants, thrombolytics, antibiotics
Accelerates the action of drugs to reduce pressure, antidiabetic drugs
Interaction with Cimetidine leads to an increase in the stable concentration of Pentoxifylline in the blood.

The drug is available without a prescription, but the use of the drug should be agreed with the doctor. In the absence of Pentoxifylline, in the pharmacy network, you can pick up an analogue of the drug. Suitable for injection drugs Trental and Agapurin, produced in 5 ml ampoules and dragee form. The drug Vasonite is produced only in tablets containing 600 mg of the active substance.

Being engaged in bodybuilding, athletes use Pentoxifylline to enhance the blood supply to tissue structures. Half an hour after taking the medicine, it is possible to achieve a powerful pumping that lasts more than one hour. However, one should not forget about medical supervision due to the threat of side effects.

What can replace the drug "Pentoxifylline"? An analogue of this drug will be presented in the materials of the article. From it you will learn about what the said medication is intended for, in what forms it goes on sale, how it should be used, and so on.

Composition, form, packaging

In what form is the drug "Pentoxifylline" sold? Instructions for use (analogs of this drug can be found in any pharmacy) indicates that this medication is available in different forms, namely:

  • In tablets (400 and 100 mg), which are covered with a pink shell. One carton may contain 60 or 20 pieces.
  • In dragee (400 and 100 mg). One pack of cardboard can contain 60 or 20 pieces.
  • In tablets of prolonged action (600 and 400 mg), which are enteric-coated and have a division line. A carton box usually contains 50 pieces.
  • In ampoules with solution for injection. The composition of this drug includes pentoxifylline, as well as sodium chloride and water.

Pharmacological features

What properties does the drug "Pentoxifylline" have? An analogue of this remedy has the same features as the mentioned medication itself. It belongs to a new pharmacological group of hemorheological agents. It is able to restore the plasticity of erythrocytes and reduce their deformation. This increases the permeability of vessels that have a narrow lumen.

Such properties of the drug lead to an improvement in microcirculation, positively affecting tissues during hypoxia.

How does Pentoxifylline work? Analogues imported and Russian have the same therapeutic effect as the remedy itself. After using the drug, it reduces the aggregation of red blood cells, which subsequently easily increase the blood supply to the organs and penetrate into the extravascular bed.

It is impossible not to say that the medication in question reduces blood viscosity, thereby contributing to the disaggregation of platelets. As a result of such exposure to the drug, minute and stroke volumes of blood increase, but heart rate indicators do not change.

Thus, pulmonary vasodilatation improves blood O2 filling, and coronary artery dilatation increases O2 delivery to the myocardium.

The drug in question is able to increase the tone of the diaphragm and respiratory muscles. Under its influence, the volume of blood that flows through the collaterals increases, and blood circulation in them also increases.

What other features does the drug "Pentoxifylline" have? The analogue of this drug and the drug itself increase the concentration of ATP in the brain, and also improve blood circulation in disturbed areas (for example, with ischemic stroke).

It should also be noted that the mentioned medication has a positive effect on the central nervous system and its work. With damage to the peripheral arteries, the use of this remedy leads to an increase in walking distances, including in such a disease as obliterating endarteritis.

Pharmacokinetic indicators

How long is the drug "Pentoxifylline" absorbed? Instructions for use (analogs of this medication are listed below) informs us that this medication has excellent penetrating ability, including through the blood-brain barrier.

The half-life of the drug when administered intravenously is 30 minutes. When taking the drug inside, it is completely adsorbed from the gastrointestinal tract.

The drug is transformed in the liver, where it forms dimethylxanthine metabolites. In the blood, the maximum concentration of the drug is reached within 4 hours after application. At the same time, it remains at a therapeutic level for about a day.

The drug is excreted mainly by the kidneys (about 95%). Through the intestines, the drug comes out slightly.

In women who are breastfeeding, the drug may be excreted along with milk. It should also be noted that the excretion of this drug is slow in patients with severe kidney, liver and elderly patients.

Indications for use

For what purposes can a patient be prescribed a medication "Pentoxifylline"? Analogues and substitutes for the drug have the same indications for use.

Currently, such an effective drug is used to treat many diseases. Let's list them right now:


Contraindications for use

For what diseases is it forbidden to use the drug "Pentoxifylline"? An analogue of this medication and the drug itself should not be taken by people with intolerance to the main components, as well as other representatives of the xanthine group.

In addition, the drug in question is contraindicated in patients who have recently suffered or acute myocardial infarction, as well as those suffering from severe atherosclerosis of the heart and arteries of the brain, porphyria.

It is prohibited to use the medication intravenously for arrhythmias, bleeding, low blood pressure, retinal hemorrhages. Also, the medicine is contraindicated in lactation and gestation, children under 18 years of age.

With extreme caution, this remedy is prescribed to operated people (in order to prevent bleeding of the mucous membranes and internal organs), as well as to patients with severe kidney and liver diseases, with peptic ulcer of the gastrointestinal tract, gastritis and heart failure.

Application methods

How is Pentoxifylline used? Instructions for use, reviews (analogues of this remedy may have other dosages) of experienced doctors indicate that this medication is taken orally and parenterally (depending on the severity of the disease).

Oral administration of the drug begins with a dose of 200 mg (that is, 2 tablets three times a day, after meals). After achieving a therapeutic effect, the indicated amount is halved. The course of treatment with tablets should last no more than a month.

In severe and acute diseases of the internal organs, the medication is prescribed in ampoules. There are 2 ways of administering the drug: intravenous and intra-arterial. The first procedure is carried out by means of a dropper. To do this, use 1 ampoule per 250 ml or sodium chloride. The indicated dosage is administered within 2 hours.

As for the intra-arterial administration of the drug, it is prescribed at a dose of 0.1 g per 50 ml of sodium chloride solution.

Side effects

Among the most common side effects are the following:

  • dizziness, anxiety, sleep disturbances, convulsions, mood changes, headache;
  • exacerbation of cholecystitis, increased activity of liver transaminases, development of cholestatic hepatitis;
  • vomiting, feeling of fullness in the stomach, nausea, diarrhea, loss of appetite;
  • urticaria, anaphylactic shock, itching, redness of the skin of the face;
  • the occurrence of arrhythmias, pain in the heart, lowering blood pressure, angina pectoris;
  • thrombocytopenia, leukopenia;
  • accommodation, visual impairment;
  • exacerbation of bronchial asthma, bronchospasm, respiratory failure;
  • bleeding of various etiologies.

The drug "Pentoxifylline": analogues, price

Analogues of the drug in question are the following drugs:

  • dragee "Agapurin" (100 mg), as well as a solution for injection in ampoules (100 mg);
  • coated tablets "Vazonite" (600 mg);
  • dragee, tablets and solution for injection "Trental".

It should be especially noted that "Trental" is an original drug. It is prescribed to patients with encephalopathies of various origins.

As for the price, it is different for all the listed drugs. An analogue of "Trental" "Pentoxifylline" can be purchased for 120 rubles, the original drug - for 520 rubles, "Agapurin" - for 300 rubles, and "Vazonit" - for 400 rubles.

Navigation

In the middle of the last century, antispasmodics were mainly used to treat conditions against the background of lesions of the central and peripheral vessels. They brought relief by eliminating the spasm of the walls of the blood channels, but did not give a stable therapeutic effect. In the 70s, scientists created the drug "Pentoxifylline". This is a synthetic derivative of purine that can change the physical parameters of the blood, thereby improving microcirculation. Subject to the provisions of the instructions for the use of the drug and the precise implementation of the doctor's prescriptions, one can count on a stable positive trend in therapy carried out during tissue hypoxia.

Compound

Pentoxifylline is the active ingredient that gave the drug its name. A more common patented trade name for the drug is Trental.

The tablet form of the drug additionally contains lactose, potato starch, talc and other components that give the elements the necessary physical properties. Solutions of the drug, in addition to pentoxifylline, contain water and sodium chloride.

Release form

The product is presented as a solution produced in glass ampoules and tablets. The liquid form of the drug is intended for intravenous jet or drip administration and intramuscular injections. "Pentoxifylline" solution contains 2 or 20 mg of the active substance per 1 ml of the composition, depending on its purpose.

The composition of the tablets of the drug contains 100, 400 or 600 mg of the main component. "Pentoxifylline" 100 and 400 is represented by pink elements, standard in terms of the triggering mechanism, packaged in 20 or 60 pieces. "Pentoxifylline" 400 may take the form of a prolonged-release drug. In this case, the dragees are covered with a membrane that is absorbed in the intestine. Pentoxifylline 600 has the same features.

pharmachologic effect

The main result of taking the remedy is the improvement of blood microcirculation in problem areas. It provides a complex mechanism of action of the drug, which has a number of chemical and biological properties.

The effect of the drug on the body:

  • restoration of the structure of red blood cells, increasing their plasticity, reducing the risk of deformation. Erythrocytes get the opportunity to penetrate even into narrowed channels, which prevents the development of hypoxia in tissues or eliminates its consequences;
  • decrease in blood viscosity due to the breakdown of groups of glued platelets. The volume of circulating biomass in the vessels increases, while the heart rate does not change;
  • elimination of spasm of the walls of the blood channels, leading to an increase in their lumen. The heart, brain, lungs and other internal organs begin to receive oxygen and nutrients in a larger volume;
  • an increase in the concentration of ATP in the brain. A substance that has a great influence on the course of metabolic processes and the formation of energy, allows you to restore the work of ischemic areas. This is of therapeutic benefit during the rehabilitation period after a brain accident.

The drug increases the functionality of peripheral vessels. In particular, its reception improves the quality of gait and increase the distance traveled in case of obliterating arteritis.

Pharmacodynamics and pharmacokinetics

The drug has a high penetrating ability, regardless of the method of application. Ingestion leads to its complete absorption by the mucous membrane of the digestive tract. The half-life of the drug when administered intravenously is on average 30 minutes. The transformation of the product and its decomposition into metabolites mainly occurs in the liver. The maximum concentration of the active substance in the blood plasma occurs after four hours and remains at the therapeutic level during the day.

About 95% of the decay products are excreted in the urine, a small amount is excreted in the feces. In old age, with reduced functionality of the liver or kidneys, drug processing is slowed down. In lactating women, a high concentration of the composition is observed in breast milk.

Indications for the use of "Pentoxifylline"

Experts position "Pentoxifylline" as a product of increased efficiency, useful in the treatment of many pathologies. The decision on the relevance of the use of the drug should be made by the doctor based on the results of the diagnosis.

Indications for the use of the drug:

  • encephalopathy provoked by vascular atherosclerosis;
  • persistent increase in blood pressure due to narrowing of the lumen of the blood channels;
  • functional insufficiency of brain tissue against the background of its organic lesions;
  • cerebral catastrophe of ischemic type;
  • bronchial asthma or a predisposition to the condition;
  • stones and sand in the kidneys;
  • encephalopathy;

You will learn more about dyscirculatory encephalopathy from

  • Raynaud's disease;
  • obstructive bronchitis;
  • various disorders of blood supply to tissues, including gangrene, frostbite, ulcers;
  • impotence due to a decrease in the functionality of the blood channels;
  • muscular dystrophy, spasm of smooth muscles.

This is not a complete list of indications for drug-based therapy. It is often introduced into complex approaches to combat pathologies caused by muscle spasms, ischemia, and problems with tissue nutrition.

Contraindications

The use of the drug is accompanied by a number of features. In some cases, it will have to be completely abandoned, in others, treatment should be accompanied by increased caution and medical monitoring of the dynamics. Sometimes prohibitions or warnings apply only to a certain dosage form of the product.

Contraindications to the use of the drug are the following conditions:

  • intolerance to a particular product or derivatives of the xanthine group;
  • acute period after myocardial infarction or cerebral hemorrhage;
  • porphyria;
  • advanced stages of atherosclerosis of the vessels of the brain and heart;
  • arrhythmia, bleeding, hypotension, retinal hemorrhage prohibit intravenous administration of the drug;
  • pregnancy (there are exceptions) and breastfeeding;
  • age under 18;
  • recent surgery - the use of the drug creates a risk of internal bleeding;
  • severe pathologies of the kidneys and / or liver.

Increased caution in therapy should be shown to persons with erosive gastritis, heart failure, ulcerative lesions of the mucosa of the digestive tract. The tool is not forbidden to be combined with herbal or vitamin-based supplements.

Side effects

Subject to the rules of therapy, the drug is well tolerated in most cases. Sometimes it can provoke negative reactions from the body, the type and severity of which depend on the individual characteristics of the patient.

Possible side effects from taking the drug:

  • neurological - sleep problems, unreasonable fears or anxiety, headaches, dizziness, mood swings, convulsive muscle twitches;
  • skin and its derivatives - swelling and redness of the face, a feeling of a rush of heat to certain parts of the body or its large areas. Fragility of nails and hair;
  • hematopoiesis - a reduced content of platelets and / or leukocytes in a blood cell;
  • digestive organs - a feeling of fullness in the stomach, nausea or vomiting, loss of appetite, loose stools. Patients with chronic cholecystitis may develop an exacerbation. Intestinal atony is rarely noted, cholestatic hepatitis develops;
  • heart and blood vessels - discomfort in the chest or pain in the heart area, changes in heart rate, lowering blood pressure, increased heart rate. In people with angina, an exacerbation of the clinical picture is possible;
  • immune response - manifests itself in the form of an allergic reaction. Most often it is urticaria, itching and swelling of the skin of the face. When using large doses of the drug, there is a risk of anaphylactic shock, angioedema;
  • respiratory system - bronchospasm, an attack of bronchial asthma, respiratory failure;
  • other systems and organs - external and internal bleeding, visual impairment.

To prevent the listed side effects, the medication should be taken strictly under the supervision of a doctor. Long-term treatment with medication is necessarily accompanied by monitoring the dynamics, regular assessment of blood composition. The appearance of a negative response does not always become an indication for the withdrawal of the product, the final decision is made by the specialist.

Instructions for use "Pentoxifylline": method and dosage

Tablets are taken orally, intramuscular, intraarterial and intravenous injections are performed using a solution. It is possible to set up a dropper. The schedule of therapy, the dosage of the drug, the duration of its use are selected taking into account the patient's condition, diagnosis, and the desired result. There are universal treatment regimens, but in most cases an individual approach is preferred.

Solution "Pentoxifylline" - instructions for use

The drug in ampoules is used for serious diseases of the internal organs, when the action medication should be prompt and maximally pronounced. There are several options for therapy, the appropriate one is selected by the doctor, based on the characteristics of the situation. In all cases, for the procedure, the patient must take a supine position.

Rules for the introduction of an injection solution for various manipulations:

  • intravenously - bolus injection of 100 mg of the drug for 5-10 minutes up to 2 times a day, after diluting the composition in saline or 5% glucose at the rate of 50 mg of the active substance per 10 ml of liquid. Or, first, 50 mg of the drug is administered to the patient in this way, and then infusion therapy is started. For her, 100 mg of "Pentoxifylline" is diluted in 250-500 ml of glucose or 0.9% sodium chloride and instilled in 90-180 minutes. In severe cases, the dosage is increased daily by 50 mg, reaching a maximum of 300 mg;
  • intramuscularly - the composition is injected deep into the muscle at 100-200 mg up to 3 times a day;
  • intra-arterial - jet version of the introduction is similar to the intravenous approach. Drip composition give 100-300 mg, diluted in 20-100 ml of saline for 10-30 minutes no more than 1 time per day.

The standard course is 10 injections, but this figure can be adjusted in both directions. Injections and a dropper can be supplemented with oral administration of the drug. In this case, the dosage of the solution is usually not changed, adjusting the volume of the active substance entering the body by selecting the appropriate tablets. With reduced functionality of the kidneys and / or liver, the standard volumes of the drug should be reduced by 30-50%.

Tablets "Pentoxifylline" - instructions for use

Depending on the type and severity of the disease, patients are prescribed 300-1600 mg of the active substance per day. day. When combined with oral therapy with parenteral daily dose is 800-1200 mg of the main component. The daily volume is divided into 2-3 doses. Tablets are recommended to be taken whole, without chewing, but with plenty of water.

As a standard, a preparation with a volume of 100 mg of the active substance is used for administration. Prolonged forms are used in special cases and are taken no more than 2 times a day. The average course of therapy is 3-4 weeks. Before its completion, after obtaining the desired therapeutic result, the dosage gradually begins to be reduced, reaching up to 300 mg.

Overdose

Exceeding the therapeutic doses of the drug threatens the development of an overdose. The risks are especially high when the drug is administered intravenously or intra-arterially in a jet. Regardless of the severity of the symptoms of an emergency, you should consult a doctor for specialized medical care.

The clinical picture of drug overdose may be characterized by the following symptoms:

  • headache and dizziness;
  • nausea, vomiting like "coffee grounds";
  • general weakness;
  • drop in blood pressure;
  • tremor of the limbs, convulsions;
  • fainting;
  • respiratory depression;
  • anaphylactic shock.

First aid for this condition includes gastric lavage, taking enterosorbents, for example, activated charcoal, at the rate of 1 tablet per 10 kg of body weight. If necessary, drugs are used to restore the normal level of blood pressure, eliminate signs of respiratory dysfunction. Serious complications, accompanied by impaired consciousness, require the introduction of adrenaline. Vomiting "coffee grounds" indicates the development of gastric bleeding, to stop which a whole range of measures is carried out.

Interaction

The increased pharmacological activity of the drug requires careful consideration of complex therapy based on it. The drug enhances the effect of drugs with antihypertensive properties. It also increases the effectiveness of insulin in the treatment of diabetes, especially when the hormone is used in large volumes. Incorrect calculation of the dosage threatens in this case with hypoglycemic coma.

Combining the drug with Ketorolac or Meloxicam creates a risk of bleeding. In combination with vasodilators or ganglion blockers, the drug causes a drop in blood pressure. Simultaneous administration of the drug with heparin and other fibrinolytics enhances the blood-thinning properties of the latter. The use of other xanthines during therapy is fraught with an increase in nervous excitation.

The use of Pentoxifylline in combination with Cimetidine is not recommended. This combination increases the level of active pharmacological compounds in the blood, increasing the likelihood of side effects and their severity. You should refrain from taking the product during antibacterial treatment, otherwise the consequences may be unexpected.

Terms of sale

Pentoxifylline is a prescription drug that can only be purchased with a doctor's prescription.

Storage conditions and shelf life

Ampoules and tablets should be stored in a dark place, out of the reach of children, at a temperature not exceeding 30°C. The shelf life of both dosage forms is 3 years.

Analogues of "Pentoxifylline"

Pharmacies offer many drugs based on pentoxifylline, similar in their properties and characteristics. The synonyms of the base agent include tablets "Pentoxifylline" SZ or "Pentoxifylline" SR Zentiva. The most affordable and effective analogues are considered "Trental", "Agapurin", "Vazonite".

Features of analogues of the drug:

  • "Trental" is an original product in the form of a dragee. It is often prescribed for encephalopathies, vascular disorders, after an ischemic stroke. The effectiveness of taking the drug in the treatment of hearing problems against the background of a decrease in the functionality of the blood channels has been proven;
  • "Agapurin" - also available in the form of a solution (20 mg of the active substance per 1 ml) and tablets (100 and 400 mg of the base component);
  • "Vazonit" - prolonged-release tablets containing 600 mg of pentoxifylline. The analogue has a long shelf life - 5 years.

It is forbidden to independently replace the medicine prescribed by the doctor with synonyms or analogues. Some drugs in this group contain additional substances that can cause a negative response of the body. There is also a high probability of making a mistake in recalculating the therapeutic dose.

"Pentoxifylline" during pregnancy

The drug is officially forbidden to use at any time of bearing a child. This contraindication is not based on the negative effect of the drug, but on the lack of reliable information about the results of such treatment. Despite the provisions of the instructions for use, the medication is sometimes used during pregnancy.

The main indication for course therapy is fetoplacental insufficiency against the background of impaired blood supply to the placenta. Ignoring the condition threatens the development of fetal hypoxia, its death, and termination of pregnancy. The form of the product and its dosage are selected individually. The use of the drug is carried out under constant monitoring of the vital signs of the fetus. Women's feedback and statistics on this approach are mostly positive.


Pentoxifylline is a drug of the angioprotective group, the action of which is based on the restoration of blood microcirculation in the capillaries. The composition of the drug contains the substance of the same name pentoxifylline. There are two forms of release for this medicine:

  • Tablets of 100 mg of active ingredient each;
  • Solution for injection 2%, 5 ml - 1 ml contains 20 mg of the active substance.

Indications for the use of Pentoxifylline

Pentoxifylline is indicated for diseases of various organs and systems of human organs, among them diseases of the spinal column. These are such as:

  • Severe bruises of the spine and its structures;
  • Spinal (spinal) stroke;
  • Atherosclerosis of the vessels of the spine;
  • Fracture of the spine and its consequences;

Contraindications to the use of Pentoxifylline

Pentoxifylline is contraindicated for prescription and use in the following conditions and diseases of the patient:

  • Children under 18;
  • recent surgery (less than a week ago);
  • lactation period;
  • Heart rhythm disturbances (arrhythmia);
  • Pregnancy at any time;
  • kidney failure;
  • Allergy to the drug and its components;
  • Tendency to external and internal bleeding;
  • Ulcer of the stomach and duodenum;
  • Myocardial infarction, acute period;
  • Liver failure;
  • Heart failure;
  • Low blood pressure (arterial hypotension).

The principle of action of Pentoxifylline

Once in the patient's blood, Pentoxifylline enters the affected capillaries. There, the active substance of this drug helps to restore the elasticity of the walls of erythrocytes, reduces the increased clotting of platelets, improves the rheology (fluidity) of the blood by reducing its viscosity. Also, the walls of blood vessels expand somewhat due to a decrease in spasm in them.

Pentoxifylline normalizes and restores metabolism in tissues, stabilizes gas exchange. The blood flow through the vessels of the spinal cord after a stroke quickly normalizes, and nerve conduction is restored (this is possible due to proper nutrition and blood supply to the nerve endings in the affected area).

Instructions for use Pentoxifylline

Pentoxifylline tablets

Pentoxifylline tablets are recommended to be taken orally, without chewing, after meals, with a sufficient amount of liquid, 100-400 mg 2-3 times a day. The maximum allowable daily dosage is 1200 mg of the drug (12 tablets). The course of treatment is selected individually and can vary from 2 weeks to several months.

Pentoxifylline in the form of a solution for injection

The solution for injection is intended exclusively for intravenous administration (drip or jet). To prepare a dropper with the drug, physiological saline (0.9% sodium chloride) or 5% glucose is mixed with 1-6 ampoules of Pentoxifylline and this mixture is administered within one hour. Multiplicity of reception - 1-2 times a day. The maximum daily dosage is 12 ampoules (1200 mg).

For jet administration, 1 ampoule (5 ml) is administered for 5 minutes 1-2 times a day, without diluting.

Side effects of Pentoxifylline

In extremely rare cases, Pentoxifylline can cause side effects. The main ones include the following:

  • Stomach ache;
  • visual impairment;
  • Vomiting accompanied by nausea;
  • convulsions;
  • Diarrhea, constipation or their alternation;
  • Increased nervousness;
  • An attack of angina pectoris (squeezing short-term pain behind the sternum);
  • Insomnia at night and drowsiness during the day;
  • Increased heart rate;
  • Dizziness;
  • Decreased blood pressure;
  • Anaphylactic shock;
  • itchy skin;
  • Headache;
  • Quincke's edema.

If one or more side effects occur, you should stop taking Pentoxifylline, contact your doctor, gastric lavage and, if necessary, take symptomatic medicines.

If the prescribed dosage of the drug is not observed, the following symptoms may develop:

  • Increased heart rate;
  • Nausea;
  • Increase in body temperature;
  • Vomiting "coffee grounds" (a sign of stomach bleeding);
  • convulsions;
  • Decreased blood pressure numbers;
  • fainting;
  • Dizziness.

If there are signs of an overdose of Pentoxifylline, it is necessary to wash the stomach, take symptomatic agents and enterosorbents.

special instructions

Pentoxifylline is contraindicated during pregnancy and lactation. This is due to the lack of data on the effect of the drug on the fetus and child development.

For children under 18 years of age, the use of the drug is contraindicated, because there is no reliable data on its effect on the development of the child.

The intake of alcoholic beverages does not affect the properties of Pentoxifylline.

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