Eufillin, instructions for use in ampoules (intravenously) of which is present in each package, belongs to the category of bronchodilators. The use of the solution is carried out parenterally (drip, jet, intramuscular). Eufillin (shots) is prescribed for adults, tablets are more suitable for children.

Eufillin is a solution for intravenous administration, which is a colorless transparent liquid poured into glass ampoules. The active ingredient is aminophylline, its concentration does not exceed 24 mg / ml. Distilled water acts as an additive. Ampoules are packaged in cardboard boxes (5 pcs each). Produced in the Russian Federation, the Republic of Belarus and Ukraine.

pharmachologic effect

Eufillin (intravenously and for intramuscular administration) has a diuretic, antispasmodic, tocolytic and bronchodilatory effect on the body. The solution for injection helps with pathologies accompanied by obstruction (obstruction) of the respiratory tract. Eufillin intramuscular can be considered a medicine for systemic use.

The principle of action of Eufillin in ampoules is based on the ability of the drug to block the adenosine (purine) receptors of bronchial cells and accelerate the accumulation of cyclic adenosine monophosphate in them. With regular use, there is a decrease in the rate of entry of calcium ions through the channels of cell membranes and a decrease in muscle contractile activity.

Therapeutic effect of Eufillin:

• improvement of alveolar ventilation;
• stimulation of breathing;
• increased sensitivity of the respiratory center;
• improving the activity of the respiratory and intercostal muscles;
• increase in mucociliary coefficient;
• stimulation of diaphragm contractions;
• bronchial relaxation.

The drug can be used for sleep apnea: the drug normalizes breathing, provides an influx of oxygen and reduces the concentration of carbon dioxide. The drug is able to stimulate the activity of the heart muscle, normalizing the frequency of its contractions. Accelerates blood microcirculation, reduces the tension of the walls of blood vessels.

Diuretic properties are manifested in the form of an increase in the volume of blood flow in the kidneys. Eufillin in ampoules expands the bile ducts, improves the rheological properties of blood and minimizes the risk of blood clots. The tocolytic effect is manifested in the form of a decrease in contractility and excitability of the myometrium. When using Eufillin in high doses, an epileptogenic effect is observed.

When it enters the systemic circulation, the active ingredient is 60% bound to plasma proteins. Metabolism is carried out by the liver. The half-life is 3-6 hours. Excreted by the kidneys or intestines (partially).

Indications and contraindications for use

In the instructions present in each box of Euphyllin, possible contraindications and indications for use are prescribed. The drug is prescribed for the following pathologies:

• left ventricular failure (bronchospasm, Cheyne-Stokes breathing);
• prolonged migraines;
• hypertension of the pulmonary circle;
• cerebrovascular insufficiency of the brain;
• broncho-obstructive syndrome with emphysema, cardiac asthma or bronchitis.

The main contraindications are:

• severe liver and kidney disease;
• sepsis;
• porphyria;
• hyperthyroidism;
• thyrotoxicosis;
• hypothyroidism of uncontrolled type;
• gastroesophageal reflux;
• increased threshold of convulsive readiness;
• epileptic seizures;
• ulcerative lesions of the stomach and duodenum (in the acute stage);
• hemorrhages in the retina;
• bleeding (gastric, intestinal in anamnesis);
• hemorrhagic stroke;
• vascular atherosclerosis;
• pulmonary edema;
• severe arterial hypertension;
• paroxysmal hypotension;
• tachycardia;
• extrasystole;
• angina;
• myocardial infarction;
• acute heart failure;
• individual intolerance to the active ingredient or additional substances.

The high risk of side effects makes it impossible to use Eufillin in children under the age of 14 years. Lactation and pregnancy are considered relative contraindications. Children under 3 years of age do not inject the solution into a vein. Droppers with Euphyllin for osteochondrosis dilate blood vessels, helping to stop a pain attack. Regardless of the form of release, the drug can be taken with bronchial asthma.

Eufillin during pregnancy

Eufillin is prescribed for women in a position for health reasons in the absence of a threat to the life of the mother and child. According to reviews, a pregnant woman's heart rate increases, dizziness and weakness appear.

Children in the womb, to whom Eufillin was prescribed in the last trimester, should be under medical supervision for the first 28-30 days after birth. In gynecology, the drug is used for edema, placental insufficiency and gestosis as part of complex therapy. There is no clear treatment regimen, the attending physician selects the dosage individually.

Eufillin: instructions for use in ampoules

Many are interested in the question of whether it is possible to drink the drug in ampoules. Experts do not recommend taking the solution inside. Eufillin can be administered intramuscularly and intravenously. The drug may be present in the composition of microclysters and inhalation solution.

Intramuscular administration

Intramuscularly, the patient is administered no more than 1 ml of the drug once. At the ampoule, the tip is carefully broken off, the solution is drawn into a sterile syringe and excess air is released. For injections, thick and long needles are considered the most suitable: it is problematic to remove thin ones from the muscle, they constantly slide off the holder. The drug is injected into the upper corner of the buttock. Eufillin injection is painful, discomfort can persist for several hours. A hematoma often forms at the injection site. The drug is not administered subcutaneously.

Intravenous administration

Intravenous administration provides faster absorption of the active ingredient. Patients in serious condition are given a single loading dose of the drug: up to 5.5 mg / kg. To prepare a dropper, up to 20 ml of Eufillin is injected into a solution of sodium chloride (0.9%, 15-20 ml). The resulting mixture is poured into the remaining saline solution (up to 500 ml), drip administration is carried out for 30-40 minutes.

Asthmatic status requires intravenous administration of up to 720 mg of aminophylline. The daily norm is not more than 0.5 ml / kg. For an adult patient, a single patient dose (provided that the solution is injected into a vein) is 6-7 mg / kg. The drug must be diluted with sodium chloride. The duration of the jet injection is 2-4 minutes.

Adolescents are prescribed medication at a dose of 16 mg / kg per day. It is expedient to divide the therapeutic norm into several introductions. If necessary, it can be increased with the permission of a specialist. The course of treatment is 10-14 days.

Insertion with a probe

Newborns who are in serious condition, the drug is administered through a nasogastric tube. A narrow bore catheter is passed through the nasal cavity into the stomach. For the introduction of the drug most often use the Levin catheter. The probe is installed by a medical professional with the appropriate qualifications. The dosage regimen is selected by the pediatrician.

Microclysters

Microclyster with Eufillin can be prepared independently, at home. To do this, take 0.5 mg of the drug and dissolve it in 20 ml of boiled water at room temperature. The finished solution is collected in a rubber bulb (the tip is disinfected in advance) and administered rectally. The procedure is repeated every 3-4 hours. Enemas are contraindicated in children under 16 years of age.

Electrophoresis with the use of the drug is prescribed for adults suffering from osteochondrosis and arthritis. For children, the procedure is prescribed for dysplasia or to relieve intracranial pressure. Electrophoresis allows you to achieve the desired concentration of the main component in the affected tissues.

The drug acts pointwise, so systemic side effects are rare. Electrophoresis is prescribed for newborns older than 30 days. A napkin soaked in the solution is applied to the sore spot and the electrodes are fixed. The duration of the procedure does not exceed 15 minutes, during which time the medicine penetrates into the affected areas. The course of treatment is 8-10 sessions.

To restore the functional activity of the internal organs after birth injuries, newborns undergo electrophoresis according to Ratner. The child is given 2 napkins soaked in various drugs: 1 - a solution of aminophylline (on the cervical vertebrae), 2 - a solution of papaverine (on the ribs). Current strength - no more than 2 mA. Duration - 15 minutes. The procedure has practically no contraindications, apart from skin diseases, arterial hypertension, arrhythmia and heart failure.

Inhalations

Inhalations with Eufillin are prescribed for adults and children with bronchial obstruction and dry cough. The active ingredient quickly penetrates the systemic circulation and reaches the affected organ. The procedure is carried out using a special device - a nebulizer. Eufillin diluted in warm water is poured into a special compartment. The released vapors must be inhaled for 10 minutes. The procedure is repeated 2 times a day.

Side effects and overdose

Side effects occur with an incorrectly selected dosing regimen. These include:

• tachypnea;
• pain in the chest;
• flushed face;
• increased sweating;
• hematuria;
• frequent urge to urinate;
• albuminuria;
• hypoglycemia;
• fever
• rashes on the skin;
• loss of appetite;
• change in taste preferences;
• exacerbation of an ulcer;
• uncontrolled vomiting;
• heartburn;
• pain in the epigastric region;
• diarrhea
• bouts of nausea;
• angina pectoris of uncontrolled type;
• lowering blood pressure;
• cardialgia;
• cardiopalmus;
• arrhythmia;
• sleep disorders (drowsiness/insomnia);
• tremor;
• psychoemotional overexcitation (anxiety, aggression, irritability);
• dizziness;
• headache.

Ailments are often dose-dependent, so experts recommend adjusting the dosing regimen in the direction of decreasing it if side effects appear.

Overdose symptoms develop with a multiple increase in the daily allowance. The characteristic features are:

• convulsions, light or sound phobia;
• tremor;
• arrhythmia;
• overexcitation;
• hyperemia of the skin;
• uncontrolled vomiting;
• prolonged diarrhea.

Eufillin does not have a specific antidote. A patient who has symptoms of an overdose must be taken to the nearest medical facility: gastric lavage and taking enterosorbents will not help in this case. Removal of toxins is carried out by enhancing the processes of natural detoxification (formed diuresis).

If the dose introduced into the body exceeds 0.5 mg / ml, then the patient is provided with respiratory support (artificial ventilation of the lungs), hemodialysis, hemosorption and plasmapheresis are performed. The doctor should monitor the hemodynamic parameters. If the patient has convulsions, Diazepam is administered intramuscularly. Barbiturates are strictly prohibited.

special instructions

A toxic effect develops if the concentration of the main component in the blood reaches 0.03 mg / ml. Eufillin has a stimulating effect on the respiratory organs only if the content of the substance in the blood does not exceed 0.01 mg / ml. Children under 3 years of age and elderly patients require careful use, the medication for this category of patients is prescribed as a last resort.

The drug can be used in geriatrics: it is prescribed in minimal doses. During the treatment period, experts recommend completely abandoning drinks containing caffeine and taurine. Chocolate and strong black hare are to be excluded from the diet. Before injection, the syringe with the solution should be held in your hands for a while so that it warms up.

Alcohol compatibility

The drug has a negative compatibility with alcohol. Before starting treatment, the patient is instructed to completely abandon the use of drinks that contain ethanol.

Interaction with other drugs

Beta-blockers, caffeine, ephedrine and Furosemide can enhance the effect of Eufillin, so these components are rarely combined. The therapeutic activity of the drug is reduced by Carbamazepine, Sulfinpyrazone, Rifampicin, Isoniazid, Phenobarbital and Phenytoin, so the dose of the bronchodilator is increased. In patients who smoke more than 15-20 cigarettes per day, there is an accelerated metabolism of Eufillin.

With the simultaneous use of antiviral drugs, beta-blockers, Disulfiram, Fluvoxamine, Viloxazine, Lincomycin, Cimetidine, Isoprenaline, Allopurine, macrolide antibiotics with Eufillin, the therapeutic dose of the latter should be increased. If the patient was prescribed a bronchodilator in combination with fluoroquinolone antibiotics, the dose of Eufillin is reduced by 25%.

Hypoglycemia develops with the combined use of diuretics, glucocorticosteroids and a drug with a bronchodilatory effect. Eufillin enhances the therapeutic effect of anticoagulants. Solutions of levulose, glucose and fructose are incompatible with the drug. The drug can be diluted only with sodium chloride.

Terms of dispensing from pharmacies

The drug, regardless of the form of release, requires a prescription from pharmacies. Before buying, the patient must present to the pharmacist a form with the seal of the attending physician. The drug is included in list B. The approximate cost is from 15 rubles.

Storage conditions and shelf life

Opened packages are strictly forbidden to be kept in the public domain. They are stored in a safe place for pets and children. For these purposes, cabinet shelves are used (preferably the top ones). Storage temperature - no more than 18 ° C. Shelf life - 24 months.

Analogues (briefly)

The drug has several generics with a similar therapeutic effect. These include:

1. Theotard. Produced in the form of capsules. It contains theophylline, a derivative of xanthine. It has a bronchodilating effect, quickly eliminating the obstruction of the bronchial canals. The cost is 180-195 rubles.
2. Teopak. Release form - tablets. The main component is a phosphodiesterase inhibitor, a purine derivative. Due to the ability of the drug to have a vasodilatory effect, the blood flow in the kidneys increases, the smooth muscles of the bronchi relax. Price - from 200 rubles.
3. Aerofillin. The active substance is doxophylline. The drug is sold in the form of tablets. The antispasmodic is able to have a bronchodilatory effect. The contractile function of the smooth muscle tissue of the bronchi decreases with systematic use. The cost is 122 rubles.
4. Neophyllin. Long-acting tablets contain theophylline. Bronchodilator is able to improve the functional activity of the respiratory and intercostal muscles. Price - 55 rubles.

The drugs are in different price categories. Each of them has a number of contraindications, so medications are prescribed by a doctor after a detailed examination. Self-selection of medication is strictly prohibited.

Produced in the form of a solution, "Eufillin" is an effective bronchodilator. The tool is quite cheap, it helps well with various diseases, but it can cause side effects, so it must be used carefully. The drug inhibits the activity of purine receptors, reduces the ability of smooth muscle fibers to contract. "Eufillin" is used in accordance with the program developed by the doctor and only as directed by a specialist. Consider the main features of this medication and the rules for its use.

Technical information

The solution of "Euphyllin" is made transparent. The liquid is colorless or may have a very slight coloration. No solid elements are allowed, there should be no sediment or flakes. The manufacturer indicates in the accompanying documentation the need to sell "Euphyllin" only if the patient has an official prescription issued by a doctor, confirmed by seals. "Eufillin" is presented for sale in cardboard boxes, which contain a dozen 10 ml ampoules. And in each such ampoule, in addition to auxiliary ingredients, there are 25 mg of the active substance.

According to the instructions accompanying the ampoule, "Eufillin" is produced using aminophylline. It is this compound that is the main substance that guarantees a bronchodilator effect. As an auxiliary compound, specially prepared and purified water is included. The level of its processing is deep enough to be able to inject this liquid into the body without fear. "Eufillin" belongs to the category of drugs that inhibit phosphodiesterase. This is a bronchodilator.

Pharmacology

The accompanying instruction packed in ampoules "Eufillin" allows us to talk about the belonging of the drug to the PDE category. The main active agent is theophyllionic ethylenediamine salt. Such a chemical molecule dissolves quickly and is effectively absorbed when it penetrates into organic tissues. The active compound contributes to the expansion of the bronchial lumen. It is assumed that this effect is due to the fact that the active substance relaxes the smooth muscle fibers of the respiratory system, thereby correcting the activity of the blood vessels of the pulmonary system and the muscles of the respiratory system. The scientists who conducted the study of aminophylline believe that this effect is associated with selective inhibition of the activity of a number of PDEs. As a result, the intracellular concentration of cyclic AMP increases.

Intended for intravenous infusion, "Eufillin", as stated in the accompanying official documentation from the manufacturer, contains an ingredient that can affect the body due to the third and fourth types of isoenzymes, which become less active. Potential side effects provoked by the drug are associated with the same processes and features. For example, it is noted that theophylline can cause a decrease in pressure, the appearance of a gag reflex. The active ingredient of the drug inhibits purine receptors. Scientists believe that this fact is one of the aspects of the complex effect on the bronchial system.

The nuances of efficiency

Intended for intravenous administration, "Eufillin" allows you to stabilize the activity of the respiratory system, thereby leveling the excessive reactivity, if any, associated with the inhalation of allergens. The effect of the drug is observed at a late stage of the body's response to the penetration of the stimulus. At the moment, it is not possible to specify in detail which mechanism ensures the effectiveness of the drug. Scientists have found that it is associated with the inhibition of PDE, not due to inhibition of the activity of adenosine. Some tests and studies have shown that under the influence of aminophylline, the content of T-suppressors in the peripheral circulatory system increases. At the same time, such cellular structures become more active.

In the accompanying instructions intended for injections "Eufillin", the manufacturer indicates the fact of an increase under the influence of the active component of mucociliary clearance. At the same time, the drug causes diaphragmatic contractions and stabilizes the functionality of the muscular system of the respiratory system, ribs. The substance activates the respiratory center and makes it more receptive to carbon dioxide. It has been established that the drug is able to improve the quality of ventilation at the level of the alveoli. As a result, the severity of each new episode of apnea decreases, and the frequency of such events decreases. Under the influence of the drug, the respiratory function stabilizes, the blood is more efficiently filled with oxygen molecules, the concentration of carbon dioxide will fall. "Eufillin" helps to activate pulmonary ventilation with a lack of potassium in the body.

Multifaceted effect

The instructions for use accompanying Eufillin for injections specify the presence of a stimulating effect on cardiac function from the drug. The strength of contractions of the organ increases, the heart rate increases, the coronary blood flow stabilizes. Under the influence of the drug, the myocardium consumes oxygen molecules more actively. At the same time, the tone of the vascular walls decreases, and the effect is mainly observed in the kidneys, skin, and brain. A venodilating peripheral effect was noted. "Eufillin" helps to reduce pulmonary vascular resistance, activates the renal blood flow. The main ingredient has a moderate diuretic effect. The flow of bile outside the liver under the influence of theophylline becomes somewhat wider.

The drug is able to stabilize the membrane cellular structures of mast elements - the manufacturer indicates this in the instructions for the use of intramuscular "Euphyllin". In ampoules, a drug is produced for injective administration in order to slow down the release of allergy mediators. Inhibits platelet aggregation, platelet activating factor. The resistance of erythrocytes to deformations increases, the rheological features of the blood become better. "Eufillin" helps to reduce the ability of blood to form blood clots, stabilizes the flow of fluid at the level of the smallest vessels. The tocolytic effect was revealed. "Eufillin" leads to an increase in the level of acidity of juices secreted in the stomach. If you use the drug in too high a dose, an epileptogenic effect is possible.

Kinetics

The manufacturer describes the reactions occurring in the body after using the drug intramuscularly in the instructions for use of "Euphyllin". Ampoules must be completed with such a document. It clarifies the fact that aminophylline, entering the human body, soon enters into transformation processes if the acidity level is average, inherent in the human body. During the interaction, theophylline is released. Bronchodilating qualities can be observed when the concentration of this compound in the circulatory system reaches 10-20 μg / ml. If the content exceeds 20 units, the drug affects in a toxic way, can be regarded as a toxin. The center responsible for breathing is excited when the content of the active ingredient in the circulatory system is 5-10 units.

In the accompanying ampoule "Euphyllin" instructions for use specifies the ability of theophylline to enter into strong bonds with whey proteins. On average, about 40% of the received dose enters into such reactions. In the presence of any pathologies, as well as in infancy, the indicator of binding is observed lower. In adults, protein binding can reach 60%, while in infants - no more than 36%. If hepatic cirrhosis is detected, on average approximately 36% of theophylline is bound to plasma proteins. The active compound is able to penetrate the placental barrier. The plasma concentration inherent in the fetus is somewhat higher than that observed in the mother's body. Theophylline is found in the milk secreted by the female mammary glands.

Pharmacokinetics: continuing consideration

The manufacturer in the instructions for use issued to the ampoules of "Euphyllin" specifies: theophylline is processed by liver cells. The process proceeds with the involvement of cytochrome isoenzymes. The most significant is CYP1A2. The transformation is accompanied by the generation of trimethylxanthine and a number of acids. All reaction products are eliminated by urine. In the original form, no more than one tenth of the dose taken is excreted from the body of an adult patient. In infants, an impressive percentage is eliminated as caffeine, since the internal systems responsible for its processing have not yet been formed. In its original form, about half of the dose used is eliminated from the body.

The half-life in asthmatics who are not addicted to smoking is estimated at 6-12 hours, if there are no pronounced pathological processes in other organs. In smokers, the period is reduced to 4-5 hours, in children the parameter is estimated in the range from one to five hours, and in infants and premature births it varies between 10-45 hours. The half-life becomes longer in the elderly, as well as in patients suffering from insufficiency of the heart. The duration may increase against the background of hepatic diseases. Clearance becomes less with liver failure and pulmonary edema, COPD. Its decrease can be provoked by chronic dependence on alcohol and insufficiency of the heart. Ethylenediamine does not correct the kinetic parameters of theophylline.

Indications for the use of "Euphyllin" are status asthmaticus and apnea, including in infants. You can use the remedy if there are problems with blood flow in the brain, characterized by an ischemic type of flow. The drug is used as an element of complex treatment. It may be given to persons with left ventricular insufficiency accompanied by bronchial spasm and respiratory disturbances as described by Cheyne-Stokes. It is recommended to administer the drug intravenously against the background of edematous syndrome caused by improper functioning of the kidneys, combining with other drugs. In case of insufficiency of the heart, you can use "Eufillin" both in the acute type and in the case of the chronic - but strictly in combination with other drugs.

The optimal format of application, frequency of use and single, daily doses are chosen by the attending physician. Not only the indications for use play a role, but also the age of the patient, the variant of administration. The treatment program depends on whether the patient smokes, as well as the clinical condition of the patient as a whole.

In the accompanying ampoule "Euphyllin" instructions for use indicate the need to administer the drug into muscle tissue. The drug should be injected as deeply as possible. The recommended area is the gluteal muscle, upper right square. For one injection, no more than a milliliter of solution should be administered. Injectable use up to three times a day is allowed. The duration of the course cannot exceed two weeks. In plasma, theophylline concentration should be less than 20 μg / ml.

With intramuscular injection, a single maximum dose for an adult is 0.5 g. More than one and a half grams should not be received per day. For a minor, up to 7 mg/kg can be administered at a time. For a day, the maximum volume is 15 mg / kg.

The instructions for use offered for the ampoules of "Euphyllin" indicate that in some cases an individual correction of the treatment program is necessary. In particular, this is possible with heart failure, liver disorders. As a rule, dosages are adjusted if the patient is chronically dependent on alcohol. In old age, reduced doses should be used, not more than 0.3 g per procedure. Dependent on nicotine products, the dosage is increased, since theophylline is more rapidly absorbed from the body. For one procedure, you can enter up to 0.7 g of the drug.

Unwanted Effects

The possibility of such is indicated by the instructions accompanying the tablets and ampoules of "Euphyllin". Injections of this drug are more likely to cause side effects if the medication is administered unnecessarily quickly. At the same time the heart hurts at some, pressure decreases. This is also possible in the fetus if the drug is used by a pregnant woman. Under the influence of the drug, the head may hurt and feel dizzy, some people have sleep disturbances, anxiety appears. May vomit and vomit, there is a risk of heartburn and ulcers, stool disorders. In some, the content of albumin, blood, increases in urine. There is a possibility of an allergy, manifested in the form of skin rashes, a feverish state.

Occasionally, the drug is accompanied by hypoglycemia. Describing the features of the introduction intramuscularly, intravenously, the instructions for the use of "Eufillin" warns of the possibility of a local reaction. In the area of ​​​​administration of the drug, reddening of the skin and an increase in its density, a feeling of pain are possible. Tachypnea is rarely noted. Some complained of hot flashes, soreness in the chest, increased diuresis, excessive activity of the sweat glands.

When the drug should not be taken

Eufillin injections are prohibited if a person has increased or decreased pressure in the arteries, the condition is assessed as serious. Do not use the remedy for tachyarrhythmia. Contraindications are peptic ulcers of the stomach, intestinal tract, which have become aggravated at the moment, as well as severe malfunctions in the liver and kidneys.

"Eufillin" can not be prescribed to epileptics and against the background of gastritis, in which an excess amount of acids is generated in the gastrointestinal tract. Hemorrhagic stroke and hemorrhage affecting the ophthalmic system, in particular the retina, are considered restrictions on the appointment. Children "Eufillin" should not be prescribed if there is a need to use ephedrine. It is not recommended to use the product under the age of three years in principle. Do not administer the drug if the patient's body is overly susceptible to theophylline, aminophylline.

Pregnancy and breastfeeding period

The documentation accompanying the Euphyllin ampoule clarifies the ability of the active ingredient to penetrate the placental barrier. The use of aminophylline by pregnant women is accompanied by the risk of increasing caffeine, theophylline in the child's blood serum. Such indicators can become dangerous for the health and life of the child. If a woman was forced to receive Eufillin injections during gestation, especially if this accompanied the third trimester of gestation, the baby should be examined immediately after birth. It is recommended to observe the child in order to establish theophylline poisoning in time.

If a woman feeds a child naturally, during this period she receives Eufillin injections, the likelihood of irritation of the baby increases. This is due to the fact that it was The ability of theophylline to penetrate into the substance secreted by the mammary glands was revealed.

In the instructions for use accompanying the Euphyllin solution, the manufacturer considers in detail the features of the use of the drug by pregnant and lactating women. The manufacturer advises to prescribe this remedy only when the obvious benefits of the therapeutic course significantly outweigh the possible dangers to the child. A woman should be aware of all the risks that accompany the treatment program.

Application features

As can be concluded from the instructions for the use of "Euphyllin", the dosage of the drug in some cases must be adjusted on an individual basis. This is required by advanced age and specific diseases, including those affecting cardiac activity. If the patient was prescribed aminophylline first in one form, then it was decided to change to another, doctors should check the blood serum to take into account the concentration of the active component. Detailed clinical observation is recommended.

It is forbidden to simultaneously prescribe the patient "Eufillin" and xanthine derivatives. If a course of the described drug is prescribed, products containing xanthine compounds - tea, high-strength coffee should be excluded from the diet. If you need to take blood-thinning drugs, you need to be especially careful. Caution requires a combination with purines, theophylline derivatives. You should not use "Eufillin" if the patient needs beta-blockers. It is not recommended to use aminophylline in combination with a glucose solution.

Aminophylline (aminophylline)

Composition and form of release of the drug

Solution for intravenous administration in the form of a colorless or slightly colored transparent liquid.

Excipients: water for injection - up to 1 ml.

5 ml - ampoules (5) - packs of cardboard.
5 ml - ampoules (10) - packs of cardboard.
10 ml - ampoules (5) - packs of cardboard.
10 ml - ampoules (10) - packs of cardboard.

pharmachologic effect

Bronchodilator, PDE inhibitor. It is an ethylenediamine salt (which facilitates solubility and increases absorption). It has a bronchodilatory effect, apparently due to a direct relaxing effect on the smooth muscles of the respiratory tract and blood vessels of the lungs. It is believed that this action is caused by selective suppression of the activity of specific PDEs, which leads to an increase in the intracellular concentration of cAMP. The results of experimental studies in vitro show that the main role, apparently, is played by type III and IV isoenzymes. Suppression of the activity of these isoenzymes can also cause some side effects of aminophylline (theophylline), incl. vomiting, arterial hypotension and tachycardia. Blocks adenosine (purine) receptors, which may be one of the factors affecting the bronchi.

Reduces airway hyperresponsiveness associated with the late phase of the inhalation response through an unknown mechanism that is not related to PDE inhibition or blockade of the action of adenosine. There are reports that aminophylline increases the number and activity of T-suppressors in the peripheral blood.

Increases mucociliary clearance, stimulates diaphragm contraction, improves the function of the respiratory and intercostal muscles, stimulates the respiratory center, increases its sensitivity to carbon dioxide and improves alveolar ventilation, which ultimately leads to a decrease in the severity and frequency of apnea episodes. By normalizing the respiratory function, it helps to saturate the blood with oxygen and reduce the concentration of carbon dioxide. Enhances lung ventilation in conditions of hypokalemia.

It has a stimulating effect on the activity of the heart, increases strength and heart rate, increases coronary blood flow and increases myocardial oxygen demand. Reduces the tone of blood vessels (mainly the vessels of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, lowers pressure in the pulmonary circulation. Increases renal blood flow, has a moderate diuretic effect. Expands the extrahepatic bile ducts. Stabilizes mast cell membranes, inhibits the release of mediators of allergic reactions. It inhibits platelet aggregation (suppresses the platelet activating factor and PgE 2α), increases the resistance of erythrocytes to deformation (improves the rheological properties of blood), reduces thrombosis and normalizes microcirculation. It has a tocolytic effect, increases the acidity of gastric juice. In high doses, it has an epileptogenic effect.

Pharmacokinetics

In the body, aminophylline is metabolized at physiological pH to release free theophylline. Bronchodilating properties are manifested at concentrations of theophylline in the blood of 10-20 μg / ml. Concentration over 20 mg/ml is toxic. The excitatory effect on the respiratory center is realized at a lower concentration - 5-10 µg/ml.

The binding of theophylline to plasma proteins is approximately 40%; in newborns, as well as in adults with diseases, the binding is reduced. Plasma protein binding in adults is about 60%, in newborns - 36%, in patients with liver cirrhosis - 36%. Penetrates through the placental barrier (the concentration in the serum of the fetus is slightly higher than in the mother's serum). It is allocated with breast milk.

Theophylline is metabolized in the liver by several cytochrome P450 isoenzymes, the most important of which is CYP1A2. In the process of metabolism, 1,3-dimethyluric acid, 1-methyluric acid and 3-methylxanthine are formed. These metabolites are excreted in the urine. In unchanged form, 10% is excreted in adults. In newborns, a significant part is excreted in the form of caffeine (due to the immaturity of the pathways for its further metabolism), unchanged - 50%.

Significant individual differences in the rate of hepatic metabolism of theophylline are the cause of pronounced variability in clearance values, plasma concentrations, and half-life. Hepatic metabolism is influenced by factors such as age, addiction to tobacco smoking, diet, diseases, and concomitant drug therapy.

T 1/2 of theophylline in non-smoking patients with bronchial asthma with virtually no pathological changes in other organs and systems is 6-12 hours, in smokers - 4-5 hours, in children - 1-5 hours, in newborns and premature babies - 10 -45 h.

T 1/2 of theophylline increases in the elderly and in patients with heart failure or liver disease.

Clearance decreases with heart failure, liver dysfunction, chronic alcoholism, pulmonary edema, COPD.

Ethylenediamine does not affect the pharmacokinetics of theophylline.

Indications

For parenteral use: status asthmaticus (adjunctive therapy), neonatal apnea, ischemic cerebrovascular accident (as part of combination therapy), left ventricular failure with bronchospasm and respiratory failure of the Cheyne-Stokes type, edematous syndrome of renal genesis (as part of complex therapy) ; acute and chronic insufficiency (as part of combination therapy).

For oral administration: broncho-obstructive syndrome of various origins (including bronchial asthma, COPD, including pulmonary emphysema, chronic obstructive bronchitis), hypertension in the pulmonary circulation, cor pulmonale, sleep apnea; acute and chronic heart failure (as part of combination therapy).

Contraindications

Severe arterial hyper- or hypotension, tachyarrhythmias, peptic ulcer of the stomach and duodenum in the acute phase, hyperacid gastritis, severe liver and / or kidney dysfunction, epilepsy, hemorrhagic stroke, retinal hemorrhage, simultaneous use with children, children's age ( up to 3 years, for prolonged oral forms - up to 12 years), hypersensitivity to aminophylline and theophylline.

Dosage

Individual, depending on the indications, age, clinical situation, route and scheme of administration, nicotine addiction.

Side effects

From the nervous system: dizziness, sleep disturbances, anxiety, tremor, convulsions.

From the side of the cardiovascular system: palpitations, heart rhythm disturbances; with rapid on / in the introduction - the appearance of pain in the heart, a decrease in blood pressure, tachycardia (including in the fetus when taken in the third trimester of pregnancy), arrhythmias, a decrease in blood pressure, cardialgia, an increase in the frequency of angina attacks.

From the digestive system: nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea; with prolonged ingestion - anorexia.

From the urinary system: albuminuria, hematuria.

Allergic reactions: skin rash, itching, fever.

From the side of metabolism: rarely - hypoglycemia.

Local reactions: compaction, hyperemia, soreness at the injection site; with rectal application, irritation of the mucous membrane of the rectum, proctitis.

Others: chest pain, tachypnea, flushing, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

drug interaction

With simultaneous use with sympathomimetics, there is a mutual enhancement of action; with and preparations of lithium - the effect is mutually reduced. The intensity of the action of aminophylline may decrease (due to an increase in its clearance) when used simultaneously with phenobarbital, rifampicin, carbamazepine, sulfinpyrazone, phenytoin, and also in smokers.

The intensity of the action of aminophylline may increase (due to a decrease in its clearance) when used simultaneously with macrolide antibiotics, lincomycin, quinolones, allopurinol, beta-blockers, cimetidine, disulfiram, fluvoxamine, hormonal contraceptives for oral administration, isoprenaline, viloxazine and vaccination against flu.

Xanthine derivatives can potentiate hypokalemia due to the action of β2-adrenergic stimulants, corticosteroids, and diuretics.

Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline.

Pharmaceutically incompatible with acid solutions.

special instructions

Use with caution in severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased convulsive readiness, with liver and / or kidney failure, peptic ulcer of the stomach and duodenum (in history), with recent bleeding from the gastrointestinal tract, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, with prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy, in elderly patients, in children (especially inside).

Correction of the dosage regimen of aminophylline may be required for heart failure, impaired liver function, chronic alcoholism, fever, acute respiratory infections.

In elderly patients, a dose reduction may be required.

When replacing the used dosage form of aminophylline with another, clinical observation and monitoring of theophylline concentration in blood plasma is necessary.

Aminophylline is not used simultaneously with other xanthine derivatives. During the period of treatment, the use of foods containing xanthine derivatives (strong coffee, tea) should be avoided.

Use with caution simultaneously with anticoagulants, with other derivatives of theophylline or purine.

Simultaneous use with beta-blockers should be avoided.

Aminophylline should not be used simultaneously with glucose solution.

Do not use rectally in children.

Pregnancy and lactation

Theophylline crosses the placental barrier. The use of aminophylline during pregnancy can lead to the creation of potentially dangerous concentrations of theophylline and caffeine in the blood plasma of the newborn. Newborns whose mothers received aminophylline during pregnancy (especially in the third trimester) require medical supervision to control possible symptoms of theophylline intoxication.

Theophylline is excreted in breast milk. When using aminophylline in a nursing mother during lactation, irritability may occur in a child.

Thus, the use of aminophylline during pregnancy and lactation (breastfeeding) is possible in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus or child.

Use in the elderly

With caution: elderly patients (dose reduction may be required).

The drug Eufillin instructions for use refers to bronchodilators with antispasmodic and vasodilating properties. Tablets 150 mg, injections in ampoules for injection in solution intravenously and intramuscularly are prescribed to excite the vasomotor and respiratory centers, to improve blood circulation. Patient reviews and doctors' recommendations report that this drug helps in the treatment of status asthmaticus and bronchial obstruction.

Release form and composition

Pharmacies receive:

1. Solution for intramuscular injection 240 mg / ml (injections in ampoules for injection).
2. Solution for intravenous administration 24 mg / ml (injections in ampoules, in droppers).
3. Tablets 150 mg.

One tablet contains 150 mg of the active substance - aminophylline, as well as calcium stearate and potato starch.

The composition of the injection solution contains aminophylline at a concentration of 24 mg/ml. Water d / i is used as an auxiliary component.

What helps Eufillin (tablets and injections)?

Indications for use of the drug in tablets:

• chronic obstructive bronchitis (COB);
• bronchial asthma (BA);
• chronic "cor pulmonale";
• Pickwick's syndrome (paroxysmal sleep apnea);
• emphysema.

Eufillin is the drug of choice for BA of physical exertion, in other forms of the disease it is used in combination with other drugs.

Injections in ampoules are prescribed in cases where the patient is diagnosed with:

• migraine;
• left ventricular failure, accompanied by periodic breathing of the Cheyne-Stokes type and bronchospasm (in combination with other drugs);
• broncho-obstructive syndrome with bronchitis, asthma, cardiac asthma (mainly for relief of attacks) or emphysema;
• hypertension in the pulmonary circulation;
• cerebrovascular insufficiency of the brain (the solution is used in combination with other drugs to reduce intracranial pressure).

Instructions for use

Eufillin tablets

Taken orally, adults should be prescribed 150 mg per dose 1-3 times a day after meals. Children inside should be prescribed at the rate of 7-10 mg / kg per day in 4 divided doses. The duration of the course of treatment is from several days to several months, depending on the course of the disease and the tolerability of the drug.

The highest doses of Eufillin for adults inside: single - 0.5 g, daily - 1.5 g.

Higher doses for children inside: single - 7 mg / kg, daily - 15 mg / kg.

Injection

An individual treatment regimen, which, depending on the indications, age, clinical situation. The solution is administered intravenously, intramuscularly, through a dropper drip.

pharmachologic effect

Eufillin relaxes the smooth muscles of the bronchi and eliminates spasms, thus exerting an expanding effect on them. In addition, it improves the functioning of the cilia of the epithelium of the respiratory tract, improves the contraction of many muscles, including intercostal and diaphragmatic.

The drug is able to stimulate the respiratory center located in the medulla oblongata and improve pulmonary ventilation, helping to saturate the blood with oxygen and reduce the amount of carbon dioxide in it. The mechanism of action of Eufillin on the human body is the inhibition of one of the enzymes - phosphodiesterase.

This helps to reduce the entry of calcium ions into the cells, which are responsible for muscle contraction, to relax the muscles of the bronchi. Also, the drug reduces the tone of blood vessels, mainly vessels located in the skin, kidneys and brain. This helps to relax the venous walls in the pulmonary circulation, reducing the pressure in it.

The use of Eufillin makes it possible to improve the blood supply to the kidneys, which leads to an increase in the amount of urine and the acceleration of its excretion. Also, the drug improves the rheological properties of blood, slowing down platelet aggregation, which makes red blood cells more resistant to damage. Taking the drug can lead to a tocolytic effect on the uterus, as well as increase the acidity of gastric juice.

Contraindications

The use of Eufillin according to the instructions is contraindicated:

• hyperthyroidism;
• with prostate adenoma;
• peptic ulcer;
• diarrhea
• in the acute period of myocardial infarction;
• paroxysmal tachycardia;
• with its intolerance;
• at collapse;
• epilepsy;
• disorders in the liver and kidneys;
• extrasystole.

Side effects

Negative effects of using Eufillin tablets:

• hematuria, albuminuria;
• sleep disturbances, anxiety, dizziness, convulsions, tremor;
• hypoglycemia (rare);
• cardiac arrhythmias, palpitations.

Against the background of injection therapy are possible:

• headache, anxiety, dizziness, agitation, irritability, tremor, insomnia;
• skin itching, skin rashes, fever;
• tachypnea, chest pain, hypoglycemia, albuminuria, increased diuresis, hematuria, increased sweating, feeling of heat in the face;
• arrhythmias, tachycardia (including in the fetus if the woman took the drug in the 3rd trimester of pregnancy), palpitations, cardialgia, lowering blood pressure, unstable angina;
• nausea, diarrhea, heartburn, gastralgia, vomiting, exacerbation of symptoms of peptic ulcer, GER, with prolonged use - loss of appetite.

Side effects are dose-dependent, that is, for their relief, it is often enough to reduce the dose of the drug.

Local reactions to the introduction of the solution are manifested in the form of skin hyperemia, soreness and the formation of a seal at the injection site.

Children, during pregnancy and lactation

Eufillin is able to cross the placenta and into breast milk, so its use during pregnancy and lactation is limited. In childhood The drug is contraindicated in children (up to 3 years, for prolonged oral forms - up to 12 years). Do not use rectally in children.

special instructions

Exercise caution when consuming large amounts of caffeinated foods or drinks during treatment.

drug interaction

The instruction reports an increase in the side effects of glucocorticoids, mineralocorticoids and adrenostimulants while taking this medication. Also, the drug is not used simultaneously with other xanthine derivatives.

Eufillin's analogs

According to the structure, analogues are determined:

1. Eufillin-Darnitsa.
2. Aminophylline.
3. Aminophylline-Eskom.

Analogues have a similar effect:

1. Theotard.
2. Neo-Theophedrin.
3. Theobiolong.
4. Diprofillin.
5. Theobromine.
6. Neoteopek A.
7. Theophylline.
8. Teofedrin-N.

Holiday conditions and price

The average price of Eufillin (tablets 150 mg No. 30) in Moscow is 12 - 17 rubles. Released by prescription.

Store in a dry, dark place at a temperature not exceeding 20 °C. Keep away from children. Shelf life - 5 years.

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In this article, you can read the instructions for using the drug Eufillin. Reviews of site visitors - consumers of this medicine, as well as opinions of doctors of specialists on the use of Eufillin in their practice are presented. We kindly ask you to actively add your reviews about the drug: the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not declared by the manufacturer in the annotation. Euphyllin analogues in the presence of existing structural analogues. Use for the treatment of status asthmaticus and bronchial obstruction in adults, children, as well as during pregnancy and lactation.

Eufillin- a bronchodilator, a xanthine derivative. Inhibits phosphodiesterase, increases the accumulation of cyclic adenosine monophosphate in tissues, blocks adenosine (purine) receptors; reduces the flow of calcium ions through the channels of cell membranes, reduces the contractile activity of smooth muscles.

It relaxes the muscles of the bronchi, increases mucociliary clearance, stimulates diaphragm contraction, improves the function of the respiratory and intercostal muscles, stimulates the respiratory center, increases its sensitivity to carbon dioxide and improves alveolar ventilation, which ultimately leads to a decrease in the severity and frequency of apnea episodes. By normalizing the respiratory function, it helps to saturate the blood with oxygen and reduce the concentration of carbon dioxide.

It has a stimulating effect on the activity of the heart, increases the strength and number of heart contractions, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly the vessels of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, reduces pressure in the "small" circle of blood circulation. Increases renal blood flow, has a moderate diuretic effect.

Expands the extrahepatic bile ducts.

It inhibits platelet aggregation (suppresses the platelet activating factor and PgE2 alpha), increases the resistance of erythrocytes to deformation (improves the rheological properties of blood), reduces thrombosis and normalizes microcirculation.

It has a tocolytic effect, increases the acidity of gastric juice.

When used in high doses, it has an enileptogenic effect.

Pharmacokinetics

In the body, aminophylline (the active substance of the drug Eufillin) is metabolized at physiological pH values ​​with the release of free theophylline. Bronchodilating properties are manifested at concentrations of theophylline in blood plasma of 10-20 μg / ml. Concentration over 20 mg/ml is toxic. The excitatory effect on the respiratory center is realized at a lower concentration - 5-10 µg/ml. Penetrates through the placental barrier (the concentration in the serum of the fetus is slightly higher than in the mother's serum). It is allocated with breast milk. In unchanged form, 10% is excreted in adults. In newborns, a significant part is excreted in the form of caffeine (due to the immaturity of the pathways for its further metabolism), unchanged - 50%.

Indications

• status asthmaticus (adjunctive therapy);
• apnea of ​​newborns;
• violation of cerebral circulation by ischemic type (as part of combination therapy);
• left ventricular failure with bronchospasm and respiratory failure of the Cheyne-Stokes type;
• edematous syndrome of renal genesis (as part of complex therapy);
• acute and chronic heart failure (as part of combination therapy);
• broncho-obstructive syndrome of various origins (including bronchial asthma, COPD, including pulmonary emphysema, chronic obstructive bronchitis);
• hypertension in the pulmonary circulation;
• "pulmonary" heart;
• sleep apnea.

Release form

Tablets 150 mg.

Solution for intravenous administration 24 mg / ml (injections in ampoules, in droppers).

Solution for intramuscular injection 240 mg / ml (injections in ampoules for injection).

Instructions for use and dosage

Pills

Inside, adults should be prescribed 150 mg per dose 1-3 times a day after meals. Children inside should be prescribed at the rate of 7-10 mg / kg per day in 4 divided doses. The duration of the course of treatment is from several days to several months, depending on the course of the disease and the tolerability of the drug.

The highest doses of aminophylline for adults inside: single - 0.5 g, daily - 1.5 g. Highest doses for children inside: single - 7 mg / kg, daily - 15 mg / kg.

Injection

Individual, depending on the indications, age, clinical situation, route and scheme of administration (intravenously, intramuscularly, through a drip), nicotine addiction.

Side effect

• dizziness;
• headache;
• insomnia;
• excitation;
• anxiety;
• irritability;
• tremor;
• heartbeat;
• tachycardia (including in the fetus when taken by a pregnant woman in the 3rd trimester);
• chest pain;
• lowering blood pressure;
• abdominal pain;
• nausea, vomiting;
• heartburn;
• exacerbation of peptic ulcer;
• diarrhea;
• loss of appetite;
• skin rash;
• fever;
• sensation of flushes to the face;
• hematuria;
• increased diuresis;
• increased sweating.

Contraindications

• hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine);
• epilepsy;
• peptic ulcer of the stomach and duodenum (in the acute stage);
• gastritis with high acidity;
• severe arterial hyper- or hypotension;
• tachyarrhythmias;
• hemorrhagic stroke;
• retinal hemorrhage;
• children's age (up to 3 years).

Use during pregnancy and lactation

With caution, pregnancy, lactation.

special instructions

Exercise caution when consuming large amounts of caffeinated foods or drinks during treatment.

Influence on the ability to drive vehicles and control mechanisms

It is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

drug interaction

Increases the likelihood of side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), general anesthesia (increases the risk of ventricular arrhythmias), xanthines and central nervous system stimulants (increases neurotoxicity), beta-agonists.

Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline.

Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracizin, being inducers of microsomal liver enzymes, increase the clearance of aminophylline, which may require an increase in its dose.

With simultaneous use with antibiotics of the macrolide group, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, small doses of ethanol (alcohol), disulfiram, fluoroquinolones, recombinant interferon-alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and when vaccinated against influenza the intensity of the action of Eufillin may increase, which may require a reduction in its dose.

Enhances the action of beta-adrenergic stimulants and diuretics (including by increasing glomerular filtration), reduces the effectiveness of lithium preparations and beta-blockers. Compatible with antispasmodics, do not use in conjunction with other xanthine derivatives.

Eufillin's analogues

Structural analogues for the active substance:

• Aminophylline;
• Aminophyllin-Eskom;
• Eufillin-Darnitsa;
• Eufillin injection 2.4%;
• Eufillina solution for injections 24%.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases that the corresponding drug helps with and see the available analogues for the therapeutic effect.