Types of aminophylline. Eufillin effect on the body. Medical instructions for use

INN: Aminophylline

Manufacturer: Borisov Medical Preparations Plant OJSC

Anatomical-therapeutic-chemical classification: Aminophylline

Registration number in the Republic of Kazakhstan: No. RK-LS-5 No. 018340

Registration period: 13.10.2016 - 13.10.2021

Instructions

Tradename

Eufillin

International nonproprietary name

Aminophylline

Dosage form

Solution for intravenous administration 24 mg/ml

Compound

One ampoule (5 ml) contains:

active substance- aminophylline (aminophylline) 120 mg (in terms of anhydrous substance),

excipient - water for injections.

Description

Transparent colorless or slightly yellowish liquid

Farmacotherapy group

Drugs for the treatment of obstructive airway diseases.

Other drugs for the treatment of obstructive airway diseases for systemic use. Xanthines. Aminophylline.

ATX code R 03DA 05

Pharmacological properties

Pharmacokinetics

After intravenous administration, 60% is in a state associated with blood proteins (with cirrhosis of the liver, the proportion of the protein-bound fraction decreases to 35%, and in newborns this figure is 36%). Penetrates well through histohematic barriers and is evenly distributed in the blood, extracellular fluid and muscle tissue. Does not accumulate in adipose tissue. Penetrates through the placental barrier and into mother's milk. The volume of distribution is 0.3-0.7 l/kg (average 0.45 l/kg).

The bronchodilator effect is manifested when its concentration in the blood plasma is maintained at a level of 10-20 mcg/ml. Concentrations of aminophylline in plasma above 20 mcg/ml are toxic.

Subject to intensive metabolism in the liver (about 90%), under under the influence of methylases and cytochrome P450, it is partially converted into caffeine. In children up to 3 years caffeine concentration can reach 30% of aminophylline concentrations. In adults and children over 3 years of age, the phenomenon of caffeine accumulation is not observed.

Excreted by the kidneys, 10% in adults and about 50% in children - in unchanged. Half-life of aminophylline (T1/2) in for newborns and children under 6 months is >24 hours; in children over 6 months - 3.7 hours; in adults who do not suffer from bronchopulmonary pathology - 8.7 hours. In persons who smoke 20-40 cigarettes per day, T1/2 shortens to 4-5 hours. In persons with obstructive pulmonary diseases, heart failure and cor pulmonale, the half-life period is extended to 24 hours.

Pharmacodynamics

It has bronchodilating, vasodilating, antispasmodic, tocolytic and diuretic effects.

The mechanism of action is associated with a blocking effect on A Type 2 purine receptors of smooth muscle cells. Eufillin causes relaxation of the smooth muscles of the bronchi, coronary, cerebral and pulmonary vessels, the muscles of the gastrointestinal tract and biliary tract. Eufillin reduces the hyperreactivity of the respiratory tract in response to the entry of allergens into them.

Eufillin increases the contractility of skeletal muscles (including respiratory muscles - the diaphragm, intercostal muscles) and slows down the development of their fatigue. It has a stimulating effect on the heart muscle, increasing the force of its contraction (positive inotropic effect). The dilation of the vessels of the renal glomeruli is accompanied by an increase in blood filtration in the kidneys and a short-term increase in diuresis. Stimulates the respiratory center of the medulla oblongata, improves alveolar ventilation and causes reducing the frequency and severity of episodes of sleep apnea. Eufillin suppresses the rhythmic contractions of the pregnant uterus, increases the secretion of hydrochloric acid in the stomach, slightly reduces the ability of platelets to adhesion and aggregation.

Indications for use

As part of complex therapy

Broncho-obstructive syndrome in bronchial asthma, bronchitis, emphysema, cardiac asthma (mainly to relieve attacks)

Ischemic cerebrovascular accident (as part of combination therapy)

Hypertension in the pulmonary circulation

Left ventricular failure with bronchospasm and respiratory failure of the Cheyne-Stokes type (as part of combination therapy)

    status asthmaticus (additional therapy)

Directions for use and doses

For adults: administer intravenously slowly (over 4-6 minutes) 5-10 ml of a 24 mg/ml solution (0.12-0.24 g), which is pre-diluted in 10-20 ml of isotonic sodium chloride solution. If palpitations, dizziness, or nausea occur, the rate of administration is slowed down or switched to drip administration, for which 10-20 ml of a 24 mg/ml solution (0.24-0.48 g) is diluted in 100-150 ml of isotonic sodium chloride solution; administered at a rate of 30-50 drops per minute. Eufillin is administered parenterally up to 3 times a day, for no more than 14 days. Higher doses of aminophylline for adults: single - 0.25 g, daily - 0.5 g. In emergency conditions, adults are administered intravenously at a dose of 6 mg/kg, diluted in 10-20 ml of 0.9% N aCI solution, injected slowly into for at least 5 minutes. For status asthmaticus, intravenous drip administration is indicated - 720-750 mg. The drug is not recommended for children under 14 years of age due to side effects.

Higher doses for children intravenously: single - 3 mg/kg, daily - 0.25-0.5 g.

Side effects

    dizziness, headache, anxiety, sleep disturbances, tremors, convulsions, flushing, increased sweating

    chest pain, palpitations (tachypnea), irregular heart rhythm, with rapid intravenous administration - an attack of angina, a sharp decrease in blood pressure

    anorexia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea

    albuminuria, hematuria, increased diuresis

    allergic skin reactions (urticaria, exfoliative dermatitis), fever

    hypoglycemia (in some cases)

    phlebitis at the injection site.

Side effects decrease with decreasing dosage of the drug.

Contraindications

    hypersensitivity to aminophylline and other methylxanthines

    acute phase of myocardial infarction, severe coronary insufficiency

    hypertrophic obstructive cardiomyopathy

    severe arterial hypotension and hypertension

    paroxysmal tachycardia, extrasystole

    hemorrhagic stroke

    retinal hemorrhage

    severe liver and/or kidney dysfunction

    epilepsy

    thyrotoxicosis, pulmonary edema

    children up to 14 years old

Drug interactions

Ephedrine, β-adrenergic stimulants, caffeine and furosemide enhance the effect of the drug.

In combination with phenobarbital, phenytoin, rifampicin, isoniazid, carbamazepine and sulfinpyrazone, acceleration of aminophylline metabolism is observed, which is accompanied by a decrease in its effect and may require an increase in the doses of the drug used.

In people who smoke (20-40 cigarettes per day), an acceleration of aminophylline metabolism is also observed.

When prescribed in combination with macrolide antibiotics, lincomycin, allopurinol, cimetidine, isoprenaline, combined oral contraceptives, disulfiram, fluvoxamine, viloxazine, influenza vaccines and β - adrenergic blockers slow down the elimination of the drug, which is accompanied by an increase in its plasma concentration and may require a dose reduction.

If aminophylline is used together with fluoroquinolones, the dose aminophylline is reduced to 1/4 of the usually recommended dose.

When xanthines are administered together with benzylpenicillin, its chemical inactivation occurs.

Eufillin weakens the therapeutic effects of lithium salts, pyridoxine and β-blockers. In turn, the prescription of β-blockers weakens the bronchodilator effect of aminophylline. When taking aminophylline together with β-adrenergic agonists, glucocorticosteroids and diuretics, the risk of developing hypoglycemia increases.

Eufillin increases the likelihood of developing undesirable effects of mineralocorticosteroids (hypernatremia), fluorinated derivatives of anesthetics (ventricular arrhythmias), and drugs that excite the central nervous system (neurotoxicity).

Co-administration of xanthines with cardiac glycosides is dangerous development of intoxication by the latter.

Compatible with antispasmodics, do not use in combination with other xanthine derivatives. When used simultaneously with small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon alpha, methotrexate, mexiletine, propafenone, tibeabendazole, ticlopidine, verapamil and with influenza vaccination, the intensity of action of aminophylline may increase, which may require a reduction in its dose.

Pharmaceutically incompatible with acid solutions, glucose, fructose and levulose solutions. When preparing for infusion, the pH of the solutions used should be taken into account.

special instructions

Use in geriatrics

The use of aminophylline in persons over 55 years of age should be carried out with lower doses of the drug.

The drug is prescribed with caution, under constant medical supervision, to patients who have:

Severe dysfunction of the liver and kidneys (hepatic and/or

renal failure)

History of gastric and duodenal ulcers

History of bleeding from the gastrointestinal tract

Severe coronary insufficiency

Common vascular atherosclerosis

Frequent ventricular extrasystole

Increased seizure readiness

Uncontrolled hypothyroidism (possible accumulation) or

thyrotoxicosis

Sepsis, prolonged hyperthermia

Gastroesophageal reflux

Prostate hypertrophy.

Eufillin is not used simultaneously with other xanthine derivatives.

During the treatment period, you should avoid consuming foods and drinks containing xanthine derivatives (strong tea, coffee, chocolate, cocoa, mate).

Pregnancy and lactation

The use of aminophylline during pregnancy can lead to the creation of potentially dangerous concentrations of theophylline and caffeine in the body of the newborn and fetus. Newborns whose mothers received aminophylline during pregnancy (especially in the third trimester) require medical supervision to monitor possible symptoms of methylxanthine intoxication. Prescribing the drug during pregnancy and lactation requires an assessment of the potential risk to the child and is carried out only for extreme health conditions. Breastfeeding should be discontinued while taking the drug.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Considering the side effects of the drug, you should refrain fromot driving and activitiespotentially hazardous activities that require increasedconcentration and speed of psychomotor reactions

Overdose

Symptoms : occur at drug concentrations in plasma more than 20 mcg/ml. Characterized by prolonged vomiting, diarrhea, hyperemia face, arrhythmia, agitation, photophobia, tremors and convulsions, hyperventilation, sharp decrease in blood pressure. At a level of blood levels above 40 mcg/ml coma develops.

Treatment: assistance measures include drug withdrawal, forced diuresis using loop diuretics: furosemide, trosemide, at a level of more than 50 mcg/ml - hemosorption is indicated, plasmapheresis. Hemodialysis or peritoneal dialysis are ineffective. For convulsive syndrome - intramuscular administration of diazepam (barbiturates are contraindicated!). To relieve arrhythmias, intravenous lidocaine or verapamil is used. For vomiting, intravenous metoclopramide or ondansetron is used. The use of etaprazine or other antipsychotics as antiemetics is contraindicated! As a specific antidote for aminophylline intoxication, intravenous jet administration of riboxin (inositol) in an isotonic sodium chloride solution is used (glucose or dextrose solutions should not be used for dilution).

Release form and packaging

5 ml of the drug is placed in glass ampoules. 10 ampoules, together with a knife or scarifier for opening the ampoules, are placed in a cardboard box with a corrugated liner made of corrugated paper. The box is covered with a label-banderole made of offset paper or paper for multicolor printing, or printing paper. The boxes, together with instructions for medical use in the state and Russian languages, are packed in group packaging.

The number of instructions for medical use in the state and Russian languages ​​must correspond to the number of packages.

Instructions for use:

Eufillin is a bronchodilator.

Pharmacological properties

Euphyllin belongs to the group of xanthines. It contains the main active ingredient - theophylline. The drug has a dilating effect on the bronchi, relaxing their smooth muscles and eliminating spasms. In addition, it improves the functioning of the cilia of the respiratory tract epithelium, improves the contractions of the diaphragmatic, intercostal and other respiratory muscles. Eufillin stimulates the respiratory center in the medulla oblongata, improves pulmonary ventilation, oxygen saturation of the blood and reduces the carbon dioxide content in it, that is, normalizes respiratory function.

The mechanism of action of Eufillin is the inhibition of the phosphodiesterase enzyme, due to which cAMP accumulates in the tissues, the flow of calcium ions into the cells, which are responsible for muscle contraction, is reduced, and this relaxes the bronchial muscles.

According to the instructions, aminophylline stimulates cardiac activity, increasing the frequency and force of myocardial contraction. It can reduce the tone of blood vessels, mainly the skin, kidneys and brain. By having a relaxing effect on the venous walls in the pulmonary circulation, the drug reduces pressure in it.

The use of Eufillin improves blood supply to the kidneys, thereby increasing the formation and excretion of urine.

The drug slows down platelet aggregation and makes red blood cells more resistant to damage, that is, it improves the rheological properties of blood.

Eufillin is known to have a tocolytic effect on the uterus; it also increases the acidity of gastric juice.

The product is well absorbed from the digestive tract, its bioavailability reaches 100%. When taken simultaneously with food, absorption slows down somewhat. It passes into breast milk and through the placenta. Euphyllin metabolism occurs in the liver, and it is excreted from the body in the urine.

Release form

Eufillin according to the instructions is produced in tablets of 150 mg, in ampoules in the form of 2.4% and 24% solution.

Indications

The drug is used to relieve attacks of bronchial asthma, heart failure, angina pectoris, pulmonary edema and other conditions associated with congestion. According to reviews, Eufillin effectively reduces blood pressure during hypertensive crises. It is used in the complex treatment of stroke and other ischemic conditions of the brain, and in the treatment of neonatal apnea.

Contraindications

The use of Eufillin is contraindicated in cases of intolerance, during the acute period of myocardial infarction, collapse, paroxysmal tachycardia, extrasystole, epilepsy, hyperthyroidism, peptic ulcer, disorders of the liver and kidneys, prostate adenoma, diarrhea. The use of the drug in tablets is not recommended for children under 6 years of age.

Instructions for use of Eufillin

In the form of a solution, the drug is administered intravenously and intramuscularly; parenteral use is justified in the treatment of emergency conditions. In this case, the dosage is calculated individually, depending on the severity of the condition and the patient’s weight.

For adults in emergency situations, the dose of Eufillin according to the instructions is selected at the rate of 6 mg/kg, it is diluted in 20 ml of physiological sodium chloride solution, and administered intravenously slowly over at least 5 minutes.

Asthmatic status requires infusion administration of the drug in the amount of 720 - 750 mg. Parenteral administration of Eufillin is not recommended for longer than 14 days.

To alleviate the condition of chronic obstructive pulmonary diseases in the acute phase, start with a dose of 5–6 mg/kg of the drug. If necessary, it should be increased very carefully, under control of its content in the blood.

Eufillin tablets are taken 0.15 g 1 to 3 times a day, after meals. The course of treatment can last from several days to several months.

For apnea of ​​newborns, when breathing stops last for 15 seconds with a simultaneous decrease in heartbeat, the initial dose of this drug for newborns is 5 mg/kg/day in 2 divided doses. The drug is administered through a nasogastric tube. When the condition stabilizes, switch to a maintenance dose of 2 mg/kg/day in 2 divided doses. The duration of use can range from several weeks to several months.

Depending on the severity of the condition and indications for Eufillin in children, the daily dose varies from 6 to 15 mg/kg.

For elderly patients, caution should be exercised when treating with the drug. According to reviews, Eufillin enhances the side effects of glucocorticoids, mineralocorticoids and adrenergic stimulants. Do not use this product simultaneously with other xanthine derivatives.

Side effects of Eufillin

According to reviews, Eufillin can cause such undesirable effects as insomnia, dizziness, agitation, headaches, tremors, increased heart rate, arrhythmias, heart pain, decreased blood pressure, abdominal pain, nausea, heartburn, vomiting, diarrhea, allergic reactions, increased sweating, decreased blood glucose, changes in urine tests.

Euphyllin (lat. euphyllinum) is a bronchodilator, a phosphodiesterase inhibitor.

Synonyms and analogues of aminophylline

Aminophylline has only one synonym – aminophylline, which contains the same active substance. In addition, there are analogs that contain another active substance, but have a similar spectrum of action:

  • diprophylline;
  • neo-theofebrine;
  • neotheopec;
  • theobiolong;
  • theobromine;
  • Teopek;
  • theophedrine;
  • theotard.

pharmachologic effect

The effect of aminophylline is primarily due to the content of theophylline in it. Ethylenediamine enhances antispasmodic (relieving spasms) activity and promotes the dissolution of the drug. The mechanism of action of aminophylline is basically similar to the mechanism of action of theophylline. Important features of aminophylline are its solubility in water and the possibility of its parenteral (intravenous or intramuscular) administration. Like theophylline, aminophylline relaxes the muscles of the bronchi, reduces the resistance of blood vessels, dilates the coronary (heart) vessels, lowers pressure in the pulmonary artery system, increases renal blood flow, and has a diuretic (diuretic) effect associated primarily with a decrease in tubular reabsorption (reabsorption of water in the renal tubules ), causes an increase in urinary excretion of water and electrolytes, especially sodium and chlorine ions. The drug strongly inhibits platelet aggregation (sticking together).

Indications for use

Eufillin is used for bronchial asthma and bronchospasms of various origins (to relieve attacks), hypertension in the pulmonary circulation, for cardiac asthma (especially accompanied by bronchospasm and Cheyne-Stokes breathing), to improve renal blood flow, to relieve cerebral vascular crises of atherosclerotic origin and improve cerebral blood circulation, reducing intracranial pressure and cerebral edema during ischemic strokes, and chronic cerebral circulatory failure.

Contraindications

  • hypersensitivity to aminophylline and other methylxanthine derivatives;
  • myocardial infarction in the acute phase;
  • tachyarrhythmia;
  • hypertrophic obstructive cardiomyopathy;
  • peptic ulcer of the stomach and duodenum in the acute phase;
  • severe impairment of liver and/or kidney function;
  • hyperthyroidism;
  • epilepsy;
  • taking ephedrine (in children);
  • children under 6 years of age.

Instructions for use of Eufillin

In the form of a solution, the drug is administered intravenously and intramuscularly; parenteral use is justified in the treatment of emergency conditions. In this case, the dosage is calculated individually, depending on the severity of the condition and the patient’s weight.

For adults in emergency situations, the dose of Eufillin according to the instructions is selected at the rate of 6 mg/kg, it is diluted in 20 ml of physiological sodium chloride solution, and administered intravenously slowly over at least 5 minutes.

Asthmatic status requires infusion administration of the drug in the amount of 720 - 750 mg. Parenteral administration of Eufillin is not recommended for longer than 14 days.

To alleviate the condition of chronic obstructive pulmonary diseases in the acute phase, start with a dose of 5–6 mg/kg of the drug. If necessary, it should be increased very carefully, under control of its content in the blood.

Eufillin tablets are taken 0.15 g 1 to 3 times a day, after meals. The course of treatment can last from several days to several months.

For apnea of ​​newborns, when breathing stops last for 15 seconds with a simultaneous decrease in heartbeat, the initial dose of this drug for newborns is 5 mg/kg/day in 2 divided doses. The drug is administered through a nasogastric tube. When the condition stabilizes, switch to a maintenance dose of 2 mg/kg/day in 2 divided doses. The duration of use can range from several weeks to several months.

Depending on the severity of the condition and indications for Eufillin in children, the daily dose varies from 6 to 15 mg/kg.

For elderly patients, caution should be exercised when treating with the drug. According to reviews, Eufillin enhances the side effects of glucocorticoids, mineralocorticoids and adrenergic stimulants. Do not use this product simultaneously with other xanthine derivatives.

Side effects

When taking aminophylline, side effects from various organs and systems are possible:

From the side of the central nervous system: dizziness, anxiety, sleep disturbances, convulsions, tremor;

From the cardiovascular system: palpitations, decreased blood pressure, arrhythmias, cardialgia, tachycardia (in the third trimester of pregnancy - in the fetus as well), the occurrence of pain in the heart (with rapid intravenous administration), increased frequency of angina attacks;

From the digestive system: nausea, vomiting, heartburn, gastroesophageal reflux, diarrhea, exacerbation of peptic ulcer, anorexia (with prolonged use);

From the urinary system: hematuria, albuminuria;

Allergic reactions: fever, skin rash, itching;

From the side of metabolism: hypoglycemia (rare);

Local reactions: soreness, thickening, hyperemia (at the injection site), proctitis, irritation of the rectal mucosa (when taken orally);

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

Overdose

Symptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, facial skin flushing, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremor, convulsions. In severe poisoning, epileptoid seizures may develop (especially in children without any warning signs), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, skeletal muscle necrosis, confusion, renal failure with myoglobinuria.

Treatment: drug withdrawal, gastric lavage, use of activated charcoal, laxatives, intestinal lavage with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasma sorption, hemodialysis (effectiveness is not high, peritoneal dialysis is not effective), symptomatic therapy (including metoclopramide and ondansetron - when vomiting). If convulsions occur, maintain airway patency and administer oxygen therapy. To relieve a seizure, intravenous diazepam 0.1-0.3 mg/kg (but not more than 10 mg). For severe nausea and vomiting, use metoclopramide or ondansetron (intravenously).

Interaction with other drugs

Increases the likelihood of developing side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), general anesthesia (increases the risk of ventricular arrhythmias), xanthines and drugs that excite the central nervous system (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 moracizine, being inducers of microsomal liver enzymes, increase the clearance of aminophylline, which may require an increase in its dose. With the simultaneous use of macrolides with antibiotics, lincomicin, allopurinol, tsimetidine, isoprenaline, ennoxacin, small doses of ethanol, disulfate, fluoroquinolones, recombinant interferon alpha, methotrexate, mexyletin, thiabendazole, thyclopidine, verapamyl flu vaccination intensity of aminophylline may increase, which may require a reduction in its dose. Enhances the effect 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 combination with other xanthine derivatives.

special instructions

Dosage adjustment is required for fever, chronic alcoholism, acute respiratory infections, liver dysfunction and heart failure. For elderly patients, the dose is usually reduced.

In case of replacing one dosage form with another, clinical observation is required to monitor the concentration of theophylline in the blood plasma. Euphyllyl cannot be used simultaneously with other xanthine derivatives. During treatment, it is necessary to exclude from the diet foods containing xanthine derivatives (tea, strong coffee). With caution - simultaneously with anticoagulants and other theophylline or purine derivatives. You should avoid taking the drug simultaneously with beta-blockers; it should not be used simultaneously with glucose solution.

Pregnancy and lactation

Be careful during pregnancy and lactation.

Use in childhood

Contraindicated: children (under 3 years).

For impaired renal function

Be careful with renal failure.

For liver dysfunction

Be careful with liver failure.

Use in old age

Be careful with old age

Vacation conditions

On prescription.

Storage conditions of the drug

In a dry place, protected from light. Keep out of the reach of children.

Shelf life of the drug

2 years. Do not use after expiration date. Do not use after the expiration date stated on the package.

In this article you can read the instructions for use of the drug Eufillin. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Eufillin in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Eufillin 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- bronchodilator, 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.

Relaxes the bronchial muscles, increases mucociliary clearance, stimulates contraction of the diaphragm, 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 respiratory function, it helps 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 those of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, and reduces pressure in the pulmonary circulation. Increases renal blood flow and has a moderate diuretic effect.

Expands extrahepatic bile ducts.

Inhibits platelet aggregation (suppresses platelet activating factor and PgE2 alpha), increases the resistance of red blood cells to deformation (improves the rheological properties of blood), reduces thrombus formation and normalizes microcirculation.

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

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

Pharmacokinetics

In the body, aminophylline (the active substance of the drug Euphyllin) is metabolized at physiological pH values ​​with the release of free theophylline. Bronchodilating properties appear at plasma theophylline concentrations of 10-20 mcg/ml. Concentrations above 20 mg/ml are toxic. The stimulating effect on the respiratory center is realized at a lower concentration - 5-10 mcg/ml. Penetrates the placental barrier (the concentration in the fetal blood serum is slightly higher than in the maternal serum). Excreted in breast milk. 10% is excreted unchanged in adults. In newborns, a significant portion is excreted in the form of caffeine (due to the immaturity of the pathways for its further metabolism), unchanged - 50%.

Indications

  • status asthmaticus (additional therapy);
  • apnea of ​​newborns;
  • ischemic cerebrovascular accident (as part of combination therapy);
  • left ventricular failure with bronchospasm and Cheyne-Stokes type breathing disorder;
  • edematous syndrome of renal origin (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;
  • night apnea.

Release forms

Tablets 150 mg.

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

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

Instructions for use and dosage

Pills

Orally, adults should be prescribed 150 mg per dose 1-3 times a day after meals. Children should be prescribed orally 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 tolerability of the drug.

Higher doses of aminophylline for adults orally: single - 0.5 g, daily - 1.5 g. Higher doses for children orally: 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;
  • decreased blood pressure;
  • abdominal pain;
  • nausea, vomiting;
  • heartburn;
  • exacerbation of peptic ulcer;
  • diarrhea;
  • decreased appetite;
  • skin rash;
  • fever;
  • feeling of flushing in 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 breastfeeding

Be careful during pregnancy and lactation.

special instructions

Use caution when consuming large amounts of caffeine-containing foods or drinks during treatment.

Impact on the ability to drive vehicles and operate machinery

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

Drug interactions

Increases the likelihood of developing side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), general anesthesia (increases the risk of ventricular arrhythmias), xanthines and drugs that excite the central nervous system (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 moracizine, being inducers of microsomal liver enzymes, increase the clearance of aminophylline, which may require an increase in its dose.

When used simultaneously with macrolide antibiotics, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, small doses of ethanol (alcohol), disulfiram, fluoroquinolones, recombinant interferon-alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and during influenza vaccination the intensity of action of Eufillin may increase, which may require a reduction in its dose.

Enhances the effect 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 combination with other xanthine derivatives.

Analogues of the drug Eufillin

Structural analogues of the active substance:

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

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

The instructions for using Eufillin in ampoules explain what kind of drug it is and when it is prescribed. The drug solution is used for intravenous and intramuscular drips, and inhalations are carried out with it. The Latin name of the drug is euphyllini, and you can buy it in pharmacies with a doctor's prescription.

A 2.4% solution of "Eufillin" is produced in ampoules of 5 and 10 ml; 1 ml contains 24 mg of aminophylline and water for injection. Methods by which the medicine should be administered:

  • intravenous jet;
  • intramuscular;
  • drip.

A glass ampoule sealed at the top contains a clear liquid. A high-quality solution is colorless, without foreign impurities and sediment. The drug is produced by Moskhimfarmpreparaty named after N.A. Semashko, as well as JSC Darnitsa, Kyiv.

The price of the product depends on the dosage and number of packed ampoules, ranging from 15 to 26 UAH.

Analogues of "Eufillin":

  • "Aerophylline";
  • "Neophylline";
  • "Puroxan";
  • "Teopek";
  • "Theotard";
  • "Teophidrine."

The instructions state that these drugs have a bronchodilator effect and their use gives the same therapeutic effect as the use of Eufillin.

Before using substitutes, you should consult your doctor. He will prescribe another drug if there are contraindications to this.

Pharmacological ability

The action of "Eufillin" is aimed at reducing the tone of smooth muscles. Under the influence of the drug, muscle spasms are reduced. This property of the medicine is used by official medicine to treat congestive conditions; the injection improves vascular circulation and helps cleanse the bronchi. Eufillin injections have the following therapeutic effects:

  • relieve spasm in the bronchi;
  • activate the respiratory center;
  • increase myocardial heart rate;
  • improve coronary circulation;
  • reduce vascular tone;
  • prevent the development of allergies.

The range of pathologies for which the Eufillin solution is used is quite wide, but the main indication for the use of the drug is the relief of bronchospasm.

When to use

"Eufillin" is injected intramuscularly or intravenously to eliminate a critical condition, regardless of the factors that caused it. Tablets should be taken for a chronic form of the disease with periodic exacerbations. The doctor determines the course of taking the medicine, as well as the method of its use.

Eufillin in ampoules helps with the following pathologies:

  • bronchial asthma;
  • lingering cough;
  • obstructive bronchitis;
  • pulmonary emphysema;
  • sleep apnea of ​​newborns;
  • heart asthma;
  • stagnation of the pulmonary circulation.

For the treatment of apnea, newborns are administered a solution of “Eufillin” using a probe (dosage 0.5 g per 1 kg of baby’s weight). Adult patients are prescribed the drug parenterally; it should be injected in case of respiratory dysfunction of the Cheyne-Stokes type (shallow and rapid breathing) in combination with other medications.

Methods of application

The intravenous stream should be administered slowly, monitor the patient’s condition, and talk to him during the procedure. It is important to prepare the injection solution correctly. To do this, 5 ml of the drug is diluted in 15 ml of sodium chloride, the mixture is heated to 35-37 degrees, and then the injection is performed. So the product does not cause irritation and is well tolerated by patients.

It is better if the drug enters the body by drip. The preparation technology is the same, but 20 ml of 2.4 percent aminophylline is diluted with 150 ml of saline solution.

The technique of administering the medicine requires such a speed that its effect lasts for a day (the dispenser on the dropper is set at 35-45 drops per minute).

An intramuscular injection is made into the upper outer square of the buttock. To do this, take a long needle and make sure that its cross-section is wider than for intravenous injection. This will allow the medicine to enter the muscle layer and spread throughout the body through the bloodstream. This way, the effect of the drug will occur earlier than if “Eufillin” accumulates in the fat layer (when pricked with a small needle).

Use during pregnancy

The guidelines for the use of Eufillin limit the use of the medicine during pregnancy. Drooping through the placenta, the drug has a negative effect on the fetus. It does not cause developmental pathologies, but after birth the baby develops arrhythmia, intoxication, and vomiting.

The medication does not lead to irreversible changes in the fetus, so it can be prescribed with caution to pregnant women if there are indications (edema, placental insufficiency).

But during treatment, a woman must strictly adhere to the recommended dosage. You cannot self-prescribe a drug to relieve symptoms. Gynecologists, when prescribing Eufillin, take into account the benefits of use and the potential harm of the drug.

Use by pediatricians

Eufillin is often used to treat respiratory tract pathologies in adults. But there are such critical conditions in babies when injections of the drug are administered at 3 months of age. For older children, IV and IM injections are given to relieve acute symptoms caused by bronchospasm. After administration of the medicine, the child is under medical supervision, since the drug has a pronounced effect on the function of the cardiovascular system.

Inhalations with aminophylline

This drug does not have any effect when used as an inhalation solution.

It is known that the medicine has a therapeutic effect only when it enters the bloodstream.

Accumulating on the mucous membrane of the nasopharynx and throat, the product cannot enter the blood, and the expectorant effect is achieved due to the effect of water evaporation on the respiratory tract.

The antispasmodic effect of "Eufillin" is observed only with intravenous or intravenous administration, and inhalations with it are ineffective.

Cough treatment

Cough syndrome, in which the discharge of sputum is difficult, worsens the condition of patients, causes pain in the lungs, is accompanied by whistling and wheezing, and impaired respiratory function. To dilate the bronchi and facilitate sputum production, patients are injected with Eufillin. After stopping the attack, patients are transferred to tablets (adults, 1 tablet, and children, 1/4 three times a day), gradually reducing the number of doses to 1 time at night. It is useful to inhale with mineral water. This promotes rapid secretion.

Electrophoresis with "Eufillin"

There are many pathological conditions caused by muscle hypertonicity. To relieve spasms and improve blood circulation, electrophoresis with Eufillin is used. This procedure is carried out in a hospital, where the patient is under the supervision of a doctor. Adults are prescribed for the following pathologies:

  • osteochondrosis;
  • joint diseases;
  • decreased cerebral circulation;
  • damage to the facial nerve;
  • chronic bronchitis.

"Eufillin" for electrophoresis is prescribed by pediatricians for the following disorders in infants:

  • increased intracranial pressure;
  • the “fontanel” does not overgrow for a long time;
  • muscle hypertonicity;
  • cerebrovascular accident.

The drug, administered through a weak electric current, is well tolerated by patients and does not cause adverse reactions, since the substance accumulates in the affected area, bypassing the gastrointestinal tract and kidneys.

"Eufillin" for cellulite

To keep the skin smooth and silky, many girls use Eufillin for massage or wrap.

It improves blood circulation, relieves swelling, warms and tightens the skin by removing excess fluid. But before use, you should read the instructions, since the medicine has many contraindications.

When not to use

The drug has a negative effect on the gastrointestinal tract, so Eufillin is contraindicated for people with peptic ulcers, hyperacid gastritis or liver dysfunction. In addition, it should not be prescribed to patients in the following situations:

  • allergy to components;
  • hyper- or hypotension;
  • cerebral hemorrhage;
  • epileptic seizures;
  • arrhythmia;
  • tachycardia;
  • multifocal atherosclerosis;
  • myocardial infarction.

Also contraindications for use are pathologies of the thyroid gland, pregnancy and lactation. Eufillin is prescribed with caution to elderly people.

Adverse reactions and overdose

Almost any drug can cause unwanted manifestations in the body. "Eufillin" is no exception.

There are quite a few possible side effects when using this medicine. Here is an approximate list of the main negative reactions:

  • Quincke's edema;
  • skin rashes;
  • fainting;
  • insomnia;
  • irritation;
  • arrhythmia;
  • dyspeptic disorders.

If the amount of accumulated medication in the body exceeds 20 mg/kg of weight, the patient develops symptoms of a drug overdose:

  • hyperemia of the skin;
  • convulsions;
  • excitation;
  • heart rhythm disturbance;
  • hypotension;
  • kidney dysfunction;
  • confusion.

Such disorders are often noted in elderly patients.

Accumulation of the drug in doses up to 40 mg/kg causes coma.

Interaction with other drugs

"Eufillin" for injections cannot be diluted with solutions containing acid.

Also, it should not be taken with glucocorticoids (Prednisolone, Dexamethasone), since the risk of unwanted effects increases. Adsorbents reduce the effectiveness of Eufillin, so you should drink it an hour after or an hour before taking sorbents.

The healing properties of the drug are enhanced by the use of macrolides or alcohol. Then the dose of the drug is reduced.

The drug increases the effect of diuretics and beta-agonists.

Shelf life and storage conditions

The product is valid for two years from the date of production. It must be stored in its original packaging at an air temperature no higher than 25*C.

Make sure that the drug is kept out of the reach of children and should not be exposed to direct sunlight. The medicine is dispensed in the prescription department of the pharmacy.