Instructions for use "Eufillin" in ampoules. The price of the drug in the pharmacy chain. Release form Eufillin

Many of us have experienced diseases when breathing was difficult, shortness of breath tormented, it was impossible to cough. Often, the doctor prescribed a remedy such as Eufillin, which brought instant relief. Asthmatics know about this drug firsthand: it is their constant companion, a savior during asthmatic attacks. Possessing powerful vasodilating and bronchodilatory effects, the drug quickly relieves unpleasant symptoms caused by bronchial obstruction, bronchospasm. It is most effective to use Eufillin intravenously.

pharmachologic effect

Eufillin is a bronchodilator, antispasmodic, vasodilator and bronchodilator. The active substance of the drug aminophylline has a relaxing effect. Expanding the bronchi, it helps to reduce the tone of their muscles and eliminate spasms. The drug has a beneficial effect on respiratory function, saturating the blood with oxygen and reducing the content of carbon dioxide in it. At the same time, the drug relieves pressure on the blood vessels, improving the functioning of the cardiovascular system, in particular, the functioning of the myocardium.

Eufillin stimulates the renal blood supply, due to which the formation and outflow of urine from the body increases, that is, it has a slight diuretic effect.

Providing a tocolytic effect, the drug increases the acidity of gastric juice. By slowing down platelet aggregation, the drug has a beneficial effect on red blood cells, making them more immune to damage, as well as thinning the blood.

The drug, getting into the digestive tract, quickly spreads through the bloodstream throughout the body. The onset of the effect slows down with the simultaneous use of food with Eufillin. Easily crosses the placenta and is excreted in breast milk.

The drug is processed in the liver and leaves the body with urine.

Forms of release and composition

The drug is produced in tablet form with a dosage of 150 mg.

The most common solution for injection, produced in ampoules. The content of the active substance in the solution can be 2.4 mg / ml or 240 mg / ml. The first option is used for intravenous administration, the second - for intramuscular injection. In a cardboard box there are 5 or 10 ampoules of 5 or 10 ml.

Eufillin, injections, contains:

  • aminophylline, active substance - 24 or 240 mg;
  • water for injection - 1 ml.

Indications for use

The medicine is prescribed in case of:

  • bronchial asthma;
  • asthmatic bronchitis;
  • chronic obstructive pulmonary disease;
  • emphysema;
  • the presence of a "pulmonary" heart;
  • Pickwick's syndrome (apnea);
  • increased intracranial pressure.

Parenteral solution for internal administration is used:

  • for the relief of asthmatic attacks;
  • with acute cerebrovascular accident (stroke) and cerebral edema;
  • in the presence of left ventricular failure with bronchospasm of the Cheyne-Stokes type;
  • in cases of apnea in newborns;
  • if there is acute or chronic heart failure;
  • to relieve intracranial pressure, as well as pressure in the pulmonary vessels;
  • with edema caused by kidney pathologies;
  • with neuralgia.

Contraindications

The drug, like any other drug of synthetic origin, has a number of contraindications. Eufillin is not used for:

  • some heart diseases (myocardial infarction) and cardiac arrhythmias (arrhythmias, extrasystole, tachycardia);
  • coronary insufficiency;
  • epileptic disease;
  • gastric and duodenal ulcer in the acute phase;
  • exacerbation of gastritis;
  • severe pathologies of the liver and kidneys;
  • the presence of hemorrhage in the retina;
  • allergies to aminophylline.

For the treatment of neuralgia and osteochondrosis, a dropper of Eufillin with Dexamethasone is used.

Carefully treat children under 14 years of age, pregnant and lactating women, the elderly, patients with vascular atherosclerosis and prostatic hyperplasia with the drug.

Eufillin, instructions for use in ampoules

The drug is prescribed by a doctor for each patient individually. This takes into account the diagnosis, the age of the patient and his weight.

If necessary, to stop bronchospasm, intravenous administration of the drug in large quantities is indicated. The medicine is administered through a dropper, the solution for which contains:

  • 10-20 ml of Eufillin;
  • 10-20 ml of 9% sodium chloride solution;
  • 0.5 l of saline.

The drug is administered within 30 minutes. For 1 kg of the patient's weight, 5-6 mg of the drug is needed. With the introduction of a dropper, it is necessary to control the patient's blood pressure and heart rate.

In order to relieve an attack of bronchial asthma, it is necessary to inject 750 ml of medication with a dropper.

For intravenous administration, Eufillin is mixed with a solution of sodium chloride. Intravenous injection is done slowly, for 6 minutes. With simultaneous treatment with Eufillin and Theophylline, the dosage of the first is halved.

An injection of Eufillin intramuscularly is quite painful. For injections, only thick needles are used. Dosage: single dose - 7 mg / kg, daily - 13 mg / kg. The drug is used more than three times a day. The duration of treatment is 14 days.

The drug is also used for inhalation, which is carried out with bronchospasm and asthmatic attacks in children. To prepare the solution you need:

  • ampoule of Eufillin 2.4%;
  • three ampoules of Dimedrol;
  • 150 ml of saline.

The dosage of the solution is prescribed by a pediatrician, depending on the diagnosis and body weight of the child. A nebulizer is used as an inhaler.

Side effects

The drug can cause numerous side effects. They appear:

  • headaches and dizziness;
  • agitated state, insomnia, anxiety, tremor, flushing, fever;
  • a sharp decrease in blood pressure, heart rhythm failures (tachycardia, arrhythmia, palpitations), exacerbation of angina pectoris;
  • nausea, vomiting, heartburn, exacerbations of gastritis and ulcers, diarrhea and loss of appetite;
  • allergic manifestations (itching, rash and other skin rashes, swelling, etc.), increased sweating;
  • increased shallow breathing and chest pain;
  • drop in blood sugar below normal;
  • an increase in the daily volume of urine, the presence of blood in the urine, the excretion of protein in the urine;
  • convulsions;
  • hardening and soreness at the injection site.

If side effects occur, stop treatment and consult your doctor.

Overdose

An overdose of Eufillin may manifest itself:

  • intestinal or stomach bleeding;
  • anxiety and sleep disorders;
  • nausea and vomiting with blood;
  • tachycardia;
  • lowering blood pressure;
  • puffiness of the face;
  • ventricular arrhythmia;
  • photophobia;
  • convulsions.

In case of drug poisoning, a person may fall into a coma.

In case of drug overdose, an ambulance should be called immediately.

Eufillin during pregnancy

Often, pregnant women have edema, which, sometimes, cannot be eliminated by the usual methods, that is, the use of diuretic drugs. In this case, Eufillin is prescribed, which, by expanding the blood vessels, stimulates the kidneys, helping them to remove excess fluid from the body.

They take the drug during pregnancy with extreme caution and only under the supervision of the attending physician, since, in the first two trimesters, the internal organs of the unborn baby are formed, and the medicine has the ability to penetrate the placental barrier. The remedy is used only when absolutely necessary. Start using it with small doses, gradually increasing the amount. Drug therapy is prescribed for short courses, no more than a few days. In rare cases, the reception is increased to 1 month.

Alcohol compatibility

Most medicines are incompatible with the use of alcohol. Eufillin also belongs to such drugs. Aminophylline is able to enhance the effect of many chemicals, in particular, alcohol. With the simultaneous use of the drug with alcohol can cause:

  • a sharp drop in blood pressure, up to collapse;
  • symptoms of suffocation;
  • violation of cardiac rhythms (arrhythmia, tachycardia, palpitations);
  • relaxation of the muscles of the lungs, which may impair respiratory function;
  • hemorrhage in the brain, if the vessels are weakened.

Rarely, the simultaneous use of alcohol and Eufillin can be fatal.

Interaction with other drugs

The drug is incompatible with medicines containing any acids. Joint use with certain types of antibiotics can enhance the effect of Eufillin, therefore, the dosage of the latter will need to be reduced. If you take the drug with Dexamethasone or Prednisolone, side effects may increase.

Drugs such as Carbamazepine, Difenin, Sulfinpyrazone, Phenytoin, Phenobarbital, etc., reduce the effect of aminophylline, therefore, its dosage is increased while being taken with these drugs.

The simultaneous use of Eufillin with diuretics and beta-adrenergic stimulants enhances the effect of the latter. The tool reduces the effectiveness of beta-blockers and lithium preparations.

Features of the use of Euphyllin

Intravenous administration of the drug is carried out, observing certain conditions:

  • before use, the medicine must be heated to the temperature of the human body;
  • start the introduction with a minimum dosage, gradually increasing it;
  • the drug is not diluted with glucose solution;
  • when administered, strict control of the patient's blood pressure and pulse is necessary. When they change, it is necessary to reduce the rate of administration;
  • with the introduction of large doses, control the content of Eufillin in the blood. If necessary, the dosage of the drug is reduced.

During drug therapy, one should refrain from carrying out work that requires maximum concentration of attention, as well as from driving vehicles.

The price of the drug in the pharmacy chain


The price may vary, depending on the pharmacy chain and its location.

Euphyllin's analogs

Analogues of the drug, having an identical effect:

  • Aminophylline;
  • Prednisolone;
  • Tizol;
  • Berodual and others.

Reviews

Patients speak of Eufillin as an effective and proven remedy that really works. Many, especially those who have lung problems, have medicine in their first aid kit. It also perfectly relieves swelling during pregnancy. Reviews speak for themselves:

Anna, 28 years old.

“During pregnancy, my legs swelled a lot. Popular diuretics did not bring the desired effect. At the next appointment, the attending physician was simply horrified, looking at my limbs, and prescribed injections of Eufillin. After several injections, the swelling went away, and my legs became the same. Just remember that the dosage of the medicine is prescribed by the doctor. It is necessary to be treated with the drug under his strict supervision.

Irina, 40 years old.

“I recently had bronchitis, after which problems with the lungs began. From time to time, she began to choke on simple bends. At the next such attack, the sister called an ambulance. The doctor injected Eufillin intravenously. Unpleasant symptoms immediately disappeared, and breathing returned to normal. Now I keep pills in my first-aid kit, which I immediately drink when an attack approaches. This remedy has become my lifeline.”

The drug Eufillin is an excellent tool that saves people's lives in unforeseen situations associated with suffocation of an asthmatic or cardiac nature. People suffering from breathing problems should always carry this medicine with them to avoid disastrous consequences.

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Instructions for the medical use of the medicinal product

Eufillin

Tradename

Eufillin

International non-proprietary name

Aminophylline

Dosage form

Solution for intravenous administration 24 mg/ml, 10 ml

Compound

1 ml of solution contains

active substance - aminophylline 24.0 mg

excipient- water for injections

Description

Clear colorless or slightly colored liquid

Pharmacotherapeutic group

Drugs for the treatment of obstructive respiratory diseases. Other drugs for the treatment of obstructive airways disease for systemic use.

xanthines

Aminophylline

ATX code R03DA05

Pharmacological properties

Pharmacokinetics

Bioavailability-90-100%. The time to reach the maximum concentration in blood plasma when administered intravenously is 0.3 g-15 minutes, the maximum concentration in blood plasma is 7 μg / ml. The volume of distribution is in the range of 0.3-0.7 l / kg (30-70% of the “ideal” body weight), with an average of 0.45 l / kg. Communication with plasma proteins in adults - 60%, in newborns - 36%, in patients with cirrhosis of the liver - 36%. Penetrates into breast milk (10% of the accepted dose), through the placental barrier (the concentration in the blood serum of the fetus is slightly higher than in the mother's serum).

Aminophylline exhibits bronchodilating properties at concentrations of 10-20 μg / ml. Concentrations above 20 mg/ml are toxic. The excitatory effect on the respiratory center is realized at a lower content of the drug in the blood - 5-10 μg / ml. It is metabolized at physiological pH values ​​with the release of free theophylline, which is further metabolized in the liver with the participation of several cytochrome P450 isoenzymes. As a result, 1,3-dimethyluric acid (45-55%) is formed, which has pharmacological activity, but is 1-5 times inferior to theophylline. Caffeine is an active metabolite and is formed in small quantities, with the exception of premature infants and children under 6 months of age, in which, due to the extremely long half-life of caffeine, its significant accumulation in the body occurs (up to 30% of that for aminophylline).

In children older than 3 years and in adults, the phenomenon of caffeine accumulation is absent. Half-life in newborns and children up to 6 months. - more than 24 hours; in children older than 6 months - 3.7 hours; in adults, 8.7 hours; in "smokers" (20-40 cigarettes per day) - 4-5 hours (after quitting smoking, normalization of pharmacokinetics after 3-4 months); in adults with chronic obstructive pulmonary disease, cor pulmonale and pulmonary heart failure - over 24 hours. Excreted by the kidneys. In newborns, about 50% of theophylline is excreted unchanged in the urine versus 10% in adults, which is associated with insufficient activity of liver enzymes.

Pharmacodynamics

Bronchodilator, purine derivative; inhibits phosphodiesterase, increases the accumulation of cAMP in tissues, blocks adenosine (purine) receptors; reduces the flow of Ca2 + 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.

Enhances lung ventilation in conditions of hypokalemia.

It has a stimulating effect on the activity of the heart, increases the strength and frequency 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, lowers pressure in the "small" circle of blood 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 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 epileptogenic effect.

Indications for use

    status asthmaticus (adjunctive therapy)

    cerebrovascular accident 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)

Dosage and administration

Adults:

Intravenously injected slowly (within 4-6 minutes) 5-10 ml of 24 mg/ml solution (0.12-0.24 g), which is pre-diluted in 10-20 ml of isotonic sodium chloride solution. When palpitations, dizziness, nausea appear, 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, no more than 14 days.

The highest doses of aminophylline for adults: single - 0.25 g, daily - 0.5 g.

For emergencies adults are injected intravenously at a dose of 6 mg / kg, diluted in 10-20 ml of 0.9% NaCl solution, injected slowly over at least 5 minutes.

With asthmatic status, intravenous drip is indicated - 720-750 mg.

Children:

The drug is contraindicated in children under 14 years of age due to side effects.

Higher doses for children from 14 to 18 years of age in / in - single 3 microns / kg, daily - 0.25 to 0.5 g.

Side effects

- dizziness, headache, insomnia, agitation, anxiety, irritability, tremor, fever, facial flushing

Palpitations, tachycardia, arrhythmia, decrease in blood pressure, up to collapse (with rapid intravenous administration), cardialgia, increased frequency of angina attacks

- gastralgia, diarrhea , nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, loss of appetite (with prolonged use)

- skin rash, itching, increased sweating

Compaction, hyperemia, soreness (at the injection site)

- chest pain, tachypnea

hypoglycemia

Increased diuresis, albuminuria, hematuria

The frequency of occurrence of side effects decreases with a decrease in the dose of the drug.

Contraindications

Children's age up to 14 years

Hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine)

Epilepsy

Severe arterial hyper- or hypotension

Severe tachyarrhythmias

Hemorrhagic stroke

Retinal hemorrhage

Carefully: pregnancy, age over 55 years and uncontrolled hypothyroidism (possibility of cumulation), sepsis, prolonged hyperthermia, gastroesophageal reflux, peptic ulcer of the stomach and duodenum (history), prostate adenoma.

Drug Interactions

Ephedrine, beta-agonists, caffeine and furosemide enhance the effect of the drug. In combination with phenobarbital, difenin, rifampicin, isoniazid, carbamazepine or sulfinpyrazone, a decrease in the effectiveness of aminophylline is observed, which may require an increase in the doses of the drug used. The clearance of the drug is reduced when administered in combination with macrolide antibiotics, lincomycin, allopurinol, cimetidine, isoprenaline, beta-blockers, which may require a dose reduction. Oral estrogen-containing contraceptives, antidiarrheal drugs, intestinal sorbents weaken, and H2-histamine blockers, slow calcium channel blockers, mexiletin enhance the effect (they bind to the cytochrome P450 enzymatic system and slow down the metabolism of aminophylline). In the case of use in combination with enoxacin and other fluoroquinolines, the dose of aminophylline is reduced. The drug inhibits the therapeutic effects of lithium carbonate and beta-blockers. Appointment of beta-blockers - interferes with the bronchodilating effect of eufillin and can cause bronchospasm. Eufillin potentiates the action of diuretics by increasing glomerular filtration and reducing tubular reabsorption. With caution, aminophylline is prescribed simultaneously with anticoagulants, with other derivatives of theophylline or purine. It is not recommended to use aminophylline with agents that excite the central nervous system (increases neurotoxicity). The drug should not be used with dextrose solutions; it is not compatible with glucose, fructose and levulose solutions. The pH of the solutions to be mixed should be taken into account: pharmaceutically incompatible with acid solutions.

Increases the likelihood of side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), general anesthesia (increases the risk of ventricular arrhythmias).

With simultaneous use with enoxacin, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon alfa, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil, and with influenza vaccination, the intensity of the action of aminophylline may increase, which may require a reduction in its dose.

special instructions

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

With severe violations of the liver and kidneys (liver and / or kidney failure)

Peptic ulcer of the stomach and duodenum (in history), with bleeding from the gastrointestinal tract in a recent history

In severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris)

With widespread atherosclerosis of the vessels

With hypertrophic obstructive cardiomyopathy

With frequent ventricular extrasystoles

With increased convulsive readiness

With uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis

With prolonged hyperthermia

With gastroesophageal reflux

With prostatic hypertrophy.

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 fetus and newborn. Newborns whose mothers received aminophylline during pregnancy (especially the third trimester) need medical supervision to control possible symptoms of methylxanthines intoxication. Prescribing the drug during pregnancy requires a careful assessment of the benefits for the treatment of the mother and the potential risk to the fetus, is made only for extreme health reasons.

Breastfeeding while taking the drug should be discontinued.

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

Given the possibility of developing side effects of the drug, during the period of treatment, one should refrain from driving vehicles and engaging in potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms: anorexia, diarrhea, nausea, vomiting, pain in the epigastric region, gastrointestinal bleeding, tachycardia, ventricular arrhythmia, tremor, generalized convulsions, hyperventilation, a sharp decrease in blood pressure.

Treatment: withdrawal of the drug, stimulation of its excretion from the body (forced diuresis, hemosorption, plasma sorption, hemodialysis, peritoneal dialysis) and the appointment of symptomatic agents. Diazepam (by injection) is used to stop seizures. Barbiturates should not be used. With severe intoxication (eufillin content more than 50 g / l), hemodialysis is recommended.

Producer: LLC "Pharmaceutical company" Zdorovye "Ukraine

ATC code: R03D A05

Farm group:

Release form: Liquid dosage forms. Injection.



General characteristics. Compound:

International and chemical names: aminophylline (aminophylline), 3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione-1,2-ethanediamine;main physical and chemical properties: clear colorless or slightly colored liquid;composition: 1 ml of solution contains theophylline 0.0192 g, ethylenediamine 0.0048 g;Excipients: water for injections.


Pharmacological properties:

Pharmacodynamics. Eufillin relaxes the muscles of the bronchi, dilates the coronary vessels, dilates the vessels of the pulmonary circulation, reduces the resistance of blood vessels, lowers pressure in the pulmonary artery system, increases renal blood flow, has a diuretic effect due to a decrease in tubular reabsorption, increases the excretion of water, chloride ions, sodium, etc. ., inhibits platelet aggregation. Eufillin has a positive inotropic effect against the background of a relative one, increases the electrical instability of the myocardium. The cardiostimulating effect of Eufillin is due to the inhibition of phosphodiesterase activity and the accumulation of cAMP in the myocardium, which leads to increased glycogenolysis and stimulates metabolism. At the same time, Eufillin increases myocardial oxygen demand. In addition, it blocks adenosine receptors, inhibits the effects of prostaglandins on smooth muscles, and reduces the release of histamine and leukotrienes from mast cells. Intravenous administration of Eufillin relieves angiospasm, increases collateral circulation and oxygen saturation, reduces perifocal and general edema of the brain tissue, lowers cerebrospinal fluid and, accordingly, intracranial pressure.
It activates the respiratory center of the medulla oblongata, increases its sensitivity to carbon dioxide and improves alveolar ventilation, which ultimately leads to a decrease in the severity and frequency of apnea episodes.

Pharmacokinetics. In the blood, up to 60% binds to plasma proteins (in healthy adults), in newborns - 36%, and in patients with cirrhosis of the liver - about 35%. The volume of distribution is in the range of 0.3 - 0.7 l/kg. In the liver, with the participation of cytochrome P 450, it is partially converted into caffeine. The half-life of aminophylline depends on age, as well as on the presence of concomitant diseases and is in newborns and children up to 6 months - more than 24 hours; in children older than 6 months - 3.7 hours; in adults not suffering from asthma - 8.7 hours; in adults with obstructive pulmonary disease, cor pulmonale and heart failure - more than 24 hours.
It is excreted by the kidneys, incl. 10% in adults and 50% in children, unchanged.
The bronchodilating effect of eufillin is manifested when its concentration in the blood is 10-20 μg / ml. Concentration over 20 mcg/ml is toxic. The excitatory effect on the respiratory center is realized at a concentration of eufillin in the blood of 5-10 μg / ml.

Indications for use:

Euphyllin is used for bronchial asthma and bronchospasm of various genesis (for relief of 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 circulation, reduction of intracranial pressure and in ischemic strokes, in chronic cerebrovascular insufficiency.


Important! Get to know the treatment

Dosage and administration:

Eufillin is prescribed intravenously for acute attacks of bronchial asthma and strokes.
Intravenously, aminofillin is injected in a stream slowly over 4-6 minutes at a dose of 0.12 - 0.24 g (5-10 ml of a 2.4% solution, which is previously diluted in 10-20 ml of isotonic sodium chloride solution). With the appearance of palpitations, dizziness, nausea, the introduction is slowed down or switched to a drip injection of the drug. To do this, 10-20 ml of a 2.4% solution of aminophylline (0.24-0.48 g) is diluted in 100-150 ml of isotonic sodium chloride solution and administered at a rate of 30-50 drops per minute. Children are administered intravenously in a single dose of 2-3 mg / kg (preferably by drip). Due to the occurrence of side effects, eufillin is not recommended for children under 14 years of age by this route.
For rectal administration in microclysters, 10-20 ml of a 2.4% solution is diluted in 20-25 ml of warm water.
The drug is injected into a vein under the control of blood pressure, heart rate, respiratory rate and general well-being.
The highest doses of aminophylline for adults in a vein: single - 0.25 g, daily - 0.5 g. In extremely severe cases, especially in intensive care, doses can be increased.
Higher doses for children intramuscularly and rectally - 7 mg / kg, daily - 15 mg / kg; intravenous single dose of 3 mg/kg.
Due to the fact that Eufillin has a stimulating effect, it should not be used immediately before bedtime. When prescribing the drug at night, it is advisable to combine Eufillin with sleeping pills.

Application Features:

During pregnancy and lactation, the use of the drug is possible only for health reasons.
Due to the insufficient activity of the biotransformation enzyme systems of the liver (and the possibility of cumulation) in newborns and people over 55 years old, aminophylline is prescribed with caution.
Intravenous administration to children under 14 years of age is contraindicated.

Side effects:

With a rapid introduction into a vein - palpitations, sometimes accompanied by rhythm disturbance, a sharp decrease in blood pressure. With rectal administration, irritation of the rectal mucosa is possible. With increased sensitivity to ethylenediamine, exfoliative, fever are possible.

Interaction with other drugs:

Pharmaceutically incompatible with acid solutions. Do not use with glucose solution, substances containing xanthine derivatives, indirect anticoagulants, other theophylline or purine derivatives.
Ephedrine and products containing it increase the risk of side effects. Propranolol weakens the effect on heart rate and bronchial tone.
Compatible with antispasmodics.
Pharmaceutically incompatible with calcium chloride, alkaloid salts, dibazole. Inactivates sodium benzylpenicillin. Eufillin potentiates the action of diuretics by increasing glomerular filtration and reducing tubular reabsorption.

Information from the instructions for the use of "Euphyllin" in ampoules: indications, methods of application, side effects, contraindications, interaction with drugs.

"Eufillin" solution is used as a systemic bronchodilator, which is part of the xanthine group, for diseases accompanied by airway obstruction. The active substance is theophylline.

The drug is available in glass ampoules of 5 or 10 pieces per pack. They contain a solution of different concentrations. For intravenous administration, a composition with a 2.4% or 2% content of the active substance is intended. Ampoules with a 24% concentration are designed for intramuscular injection, so when using the medicine, you should carefully study the labeling. Let us consider in detail the instructions for using the Euphyllin solution in ampoules.

By inhibiting the activity of phosphodiesterase enzymes, the drug helps to increase the ATP derivative, cyclic adenosine monophosphate. By blocking purienergy receptors, the drug reduces the transport of calcium ions, effectively relieves smooth muscle spasm. As a result:

  • relaxation of the bronchi occurs;
  • increased ventilation of the alveolar space;
  • the work of the respiratory and intercostal muscles improves;
  • the resistance of the respiratory mucosa to external influences increases (mucociliary clearance);
  • the tension of the walls of blood vessels decreases, their lumen expands (also in the kidneys, brain and skin);
  • pressure in the pulmonary circulation decreases.

Activation of the respiratory center, a decrease in the resistance of blood vessels in the lungs leads to the entry of oxygen into the blood, a reduction in the depth and frequency of apnea attacks.

Also in the description it is indicated that "Eufillin" has the following effect:

  • increases blood flow through the vessels of the myocardium;
  • stimulates the work of the muscle, increasing the frequency and strength of contractions, increasing its need for O2;
  • expands the bile ducts;
  • activates the production of adrenaline by the adrenal glands;
  • when relaxing the blood vessels of the kidneys, it has a moderate diuretic effect.

The solution improves the properties of blood, inhibits thrombosis, enhances the resistance of red blood cells to destruction. The drug increases the concentration of gastric juice, has a relaxing effect on the muscles of the walls of the uterus (tocolytic effect). In high doses, it has an epileptogenic effect.

Pharmacokinetics

The drug has a high bioavailability, reaches the target in 100% (at least 90%). With the introduction of 300 mg into a vein, the maximum concentration is observed after 15 minutes. With optimal body weight, the interval in the distribution of the drug is 300 - 700 ml per kilogram of weight. With proteins, the connection can be traced depending on the age and pathologies of the liver:

  • in an adult is 60%;
  • in children in the first months after birth - 38%;
  • in people suffering from cirrhosis of the liver - 36%.

The penetration of "Euphyllin" into breast milk during lactation is 10%. During pregnancy, it is found that in the blood serum of the embryo, the accumulation of the drug is higher than that of the mother.

The drug affects the bronchi when detected in the blood from 10 to 20 μg per ml. Implementation of excitation to the respiratory center occurs at 5 - 10 μg per ml. Above 20 mg, toxic effects are observed.

The drug is metabolized in the liver, turning into dimethyl uric acid, and caffeine also belongs to the active metabolites. In adults, it is excreted in small amounts, in newborns and children under 6 months it is poorly excreted, accumulating in the body. After 3 years it is recycled without residue.

Excretion of the drug occurs through the kidneys. In infants, due to insufficiency of liver enzymes, half the dose is excreted unchanged.

When appointed

Eufillin solution is used:

  • with BOS (broncho-obstructive syndrome);
  • to stop attacks of bronchial and cardiac asthma;
  • to relieve intracranial hypertension in case of cerebral vascular dysfunction (cerebrovascular insufficiency);
  • with increased pressure in the pulmonary circulation;

The drug is prescribed in the complex treatment of left ventricular failure, accompanied by recurrent bronchospasm and Cheyne-Stokes syndrome.

Application

The dosage and method of administration of "Euphyllin" are prescribed individually in each case. The age, weight and disease of the patient are taken into account.

Intravenously

An infusion (infusion) of a large volume of the drug is used when it is urgent to stop an attack of bronchospasm:

  1. For a dropper, 10 - 20 ml of medication and the same amount of 9% sodium chloride solution are needed, the composition is diluted with 0.5 l (0.25) of saline. The dose is 5.6 mg per kilogram of the patient's weight. "Eufillin" is administered for 30 minutes.
  2. During an asthma attack, an intravenous infusion is performed, up to 750 mg of the drug is dripped.
  3. For intravenous injection, "Eufillin" is also diluted in a solution of sodium chloride. The composition is administered slowly over 6 minutes to avoid negative effects on the body.
  4. If the patient takes Teofilin, the dose is halved.

The daily volume of "Euphyllin" in ampoules, according to the instructions for use, in grams is calculated per kilogram of weight:

When the condition is removed, the patient is transferred to maintenance therapy. In this case, oral administration is more often prescribed, intramuscular injections are used when there are difficulties with taking pills, for example, stomach problems.

Intramuscular injections

The patient should know that Eufillin injections are painful and the residual pain syndrome worries for several more hours. For injections, thick needles are taken, if pricked with thin analogues, the point may remain in the tissues of the buttocks due to muscle spasm. The volume per day is 0.5 - 1 micron, it is distributed 3 times.

For inhalation

"Eufillin" is used as an inhalation for bronchial obstruction and during asthma attacks in children because of the ability to relieve spasm and dilate the bronchi. As a result, sputum separation is faster.

For the procedure, a nebulizer is used, the medicine enters the bronchi in the form of an aerosol. A solution for inhalation is prepared from an ampoule of "Euphyllin" and 3 ampoules of "Dimedrol", add 150 ml of distilled water or saline. The amount of medicine and how many procedures are required are determined only by the pediatrician, depending on the severity of the disease.

Steam inhalation is pointless to use, since only water vapor enters the bronchi.

For electrophoresis

For electrophoresis, "Eufillin" is used in the treatment of osteochondrosis and in destructive lesions of the joints for adult patients. For children, it is prescribed to reduce cranial pressure, relieve muscle tone of the limbs and with dysplasia.

The drug is injected through the action of current pulses through the skin in the form of oppositely charged ions. Irritatingly affecting the receptors of the skin and tissues, the current:

  • increases their activity;
  • stimulates blood circulation;
  • increases sensitivity to drugs;
  • accelerates the exchange processes.

The general effect of electrophoresis with "Eufillin" is to relieve pain, eliminate inflammation, dissolve seals, improve traffic due to vasodilation. Lingering in the layers of the skin and subcutaneous fat, the drug continues to have a therapeutic effect for more than a day.

The procedure is carried out using electrodes and pads made of several layers of gauze soaked in medicine. For adults, a 2% solution concentration is used. Duration 15 minutes, 10 sessions are performed for treatment.

This method of drug administration makes it possible to achieve the desired concentration directly in the damaged area. With a point effect, the composition does not cause systemic reactions, so the procedure is prescribed even for infants from the age of one month.

In newborns after birth injuries with cerebral palsy, hypertonicity of the muscles of the limbs, cerebrovascular accidents, the procedure is carried out according to Ratner. The method consists in the fact that 2 medications are used:

  1. The first pad is impregnated with "Eufillin" at a concentration of 0.5%, applied in the neck area.
  2. For the other, "Papaverine" 1% is used, it is pricked on the ribs of the chest on the right.

Usually, both adults and young patients tolerate electrophoresis, provided there are no contraindications.

It is not allowed to perform electrophoresis for all types of dermatoses, tachycardia, arterial hypertension

How does it interact

"Eufillin" does not interact with all drugs:

  1. Do not combine the drug with acid solutions.
  2. When used in parallel with Sulfinpyrazone, Phenytoin, Rifampicin, Phenobarbital, Isoniazid, Carbamazepine, contraceptives, metabolism is accelerated, which requires an increase in dosage.
  3. Mutual decrease in efficiency occurs during administration with adrenoblockers.
  4. Simultaneous use with macrolides and fluoroquinols, the influenza vaccine enhances the effect of the drug, which leads to a dose reduction.
  5. "Eufillin" enhances the effect of anticoagulants
  6. During the use of anesthetics, glucocorticosteroids, adrenomimetics, the risk of adverse reactions increases

For the entire period of treatment, it is forbidden to use substances containing xanthines, you can not drink tea and coffee.

Side effect

In some cases, side effects occur during the use of the drug:

  1. The central nervous system reacts with anxiety, irritability, sleep disturbance, dizziness, tremor, convulsive seizures.
  2. The digestive system. Manifested in the appearance of heartburn, vomiting, diarrhea, gastroesophageal reflux, exacerbation of peptic ulcer, gastralgia.
  3. Heart and blood vessels. In response to taking the medicine, there may be an increase in heart rate, arrhythmia, hypotension, pain in the heart occur with the rapid introduction of the solution into a vein. The urinary system responds in the appearance of protein and blood in the urine, increased urination.
  4. Allergy is manifested by itching, rash on the skin, fever.
  5. local reactions. At the injection site, seals, redness, swelling are formed, painful sensations are disturbing.

There may be a decrease in blood glucose levels, increased respiration (tachypnea), chest pain. Hot flushes to the face or increased sweating are noted. Unpleasant symptoms disappear when the drug is discontinued.


Contraindications

"Eufillin" has a wide range of contraindications, it is not prescribed for:

  • intolerance to the active substance;
  • pulmonary edema;
  • various manifestations of arrhythmia;
  • severe diseases of the kidneys and liver;
  • stages of myocardial infarction, stroke and heart failure;
  • retinal bleeding:
  • exacerbation of an ulcer;
  • the threat of bleeding;
  • diagnosis of epilepsy.

With caution, the drug is prescribed for septic processes, uncontrolled hypothyroidism due to the likelihood of cumulation of the drug. And also for the elderly, with prostate adenoma, widespread vascular atherosclerosis.

Children under 14 years of age are not recommended to use the Eufillin solution due to the high risk of adverse reactions. Up to 3 years, intravenous injections are rarely prescribed. Subsequently, the drug is used strictly according to indications.

Overdose

Signs of toxic effects appear when the plasma accumulation is 0.02 mg/ml. Typical symptoms:

  • puffiness of the face:
  • insomnia, agitation;
  • violation of acid-base balance;
  • tachypne;
  • loss of appetite;
  • prolonged vomiting, sometimes with blood;
  • intestinal and stomach bleeding;
  • tachycardia;
  • tremor, up to convulsions with severe poisoning, especially in children.

With continued use, a sick person may fall into a coma.

If negative signs appear, the administration of the drug is stopped. To remove "Euphyllin" from the blood, forced diuresis is used. When vomiting, Metoclopramide is prescribed, during convulsions, Diazepam is administered. The neutralizing agent for poisoning is "Riboxin", the solution is injected into a vein, oxygen inhalations are used. When the concentration in the body reaches 5 mg / ml, hemodialysis, plasmaphoresis or hemosorption are used.

Precautionary measures

The use of "Eufillin" for intravenous administration requires compliance with special conditions:

  1. Glucose solution is not used to dilute the solution due to the incompatibility of the means, therefore it is important to take into account the pH of the substance used.
  2. Intravenous administration begins with a minimum volume, then gradually increases.
  3. When the composition is administered, the patient's condition should be monitored, breathing, blood pressure and heart rate should be monitored. When the indicators change, the speed is reduced or the solution is injected drip.
  4. Before putting a dropper or injection, the medicine must be heated to the temperature of the human body.
  5. At high doses, blood levels of the drug are monitored. In patients with diseases of the heart, liver, with infectious processes, as well as in the elderly, the dosage of "Euphyllin" is reduced.

For the period of treatment, you should not drive a car or engage in activities that require concentrated attention.

KNF (drug is included in the Kazakhstan National Formulary of Medicines)

ED (Included in the List of drugs in the framework of the guaranteed volume of medical care, subject to purchase from a single distributor)

Manufacturer: Novosibkhimfarm OAO

Anatomical-therapeutic-chemical classification: Aminophylline

Registration number: No. RK-LS-5 No. 019836

Date of registration: 02.05.2013 - 02.05.2018

Limit price: 17.12 KZT

Instruction

  • Russian

Tradename

Eufillin

International non-proprietary name

Aminophylline

Dosage form

Solution for intravenous administration 24 mg/ml, 5 ml

Compound

1 ml of solution contains

active substance - aminophylline 24.0 mg

excipient- water for injections

Description

Clear colorless or slightly colored liquid

Pharmacotherapeutic group

Drugs for the treatment of obstructive respiratory diseases. Other drugs for the treatment of obstructive airways disease for systemic use.

xanthines

Aminophylline

Code ATXR03DA05

Pharmacological properties

Pharmacokinetics

Bioavailability-90-100%. The time to reach the maximum concentration in blood plasma when administered intravenously is 0.3 g-15 minutes, the maximum concentration in blood plasma is 7 μg / ml. The volume of distribution is in the range of 0.3-0.7 l / kg (30-70% of the “ideal” body weight), with an average of 0.45 l / kg. Communication with plasma proteins in adults - 60%, in newborns - 36%, in patients with cirrhosis of the liver - 36%. Penetrates into breast milk (10% of the accepted dose), through the placental barrier (the concentration in the blood serum of the fetus is slightly higher than in the mother's serum).

Aminophylline exhibits bronchodilating properties at concentrations of 10-20 μg / ml. Concentrations above 20 mg/ml are toxic. The excitatory effect on the respiratory center is realized at a lower content of the drug in the blood - 5-10 μg / ml. It is metabolized at physiological pH values ​​with the release of free theophylline, which is further metabolized in the liver with the participation of several cytochrome P450 isoenzymes. As a result, 1,3-dimethyluric acid (45-55%) is formed, which has pharmacological activity, but is 1-5 times inferior to theophylline. Caffeine is an active metabolite and is formed in small quantities, with the exception of premature infants and children under 6 months of age, in which, due to the extremely long half-life of caffeine, its significant accumulation in the body occurs (up to 30% of that for aminophylline).

In children older than 3 years and in adults, the phenomenon of caffeine accumulation is absent. Half-life in newborns and children up to 6 months. - more than 24 hours; in children older than 6 months - 3.7 hours; in adults, 8.7 hours; in "smokers" (20-40 cigarettes per day) - 4-5 hours (after quitting smoking, normalization of pharmacokinetics after 3-4 months); in adults with chronic obstructive pulmonary disease, cor pulmonale and pulmonary heart failure - over 24 hours. Excreted by the kidneys. In newborns, about 50% of theophylline is excreted unchanged in the urine versus 10% in adults, which is associated with insufficient activity of liver enzymes.

Pharmacodynamics

Bronchodilator, purine derivative; inhibits phosphodiesterase, increases the accumulation of cAMP in tissues, blocks adenosine (purine) receptors; reduces the flow of Ca2 + 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.

Enhances lung ventilation in conditions of hypokalemia.

It has a stimulating effect on the activity of the heart, increases the strength and frequency 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, lowers pressure in the "small" circle of blood 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 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 epileptogenic effect.

Indications for use

Asthmatic status (adjunctive therapy)

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

Dosage and administration

Adults:

Intravenously injected slowly (over 4-6 minutes) from 5-10 ml of a 24 mg/ml solution (0.12-0.24 g), which is previously diluted in 10-20 ml of isotonic sodium chloride solution. When palpitations, dizziness, nausea appear, 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, no more than 14 days.

The highest doses of aminophylline for adults: single - 0.25 g, daily - 0.5 g.

In emergencies, adults are administered intravenously at a dose of 6 mg / kg, diluted in 10-20 ml of 0.9% NaCl solution, injected slowly over at least 5 minutes.

With asthmatic status, intravenous drip is indicated - 720-750 mg.

Children:

The drug is contraindicated in children under 14 years of age due to side effects.

Higher doses for children from 14 to 18 years of age in / in - single 3 microns / kg, daily - 0.25 to 0.5 g.

Side effects

- dizziness, headache, insomnia, agitation, anxiety, irritability, tremor, fever, facial flushing

Palpitations, tachycardia, arrhythmias, decreased blood pressure,

up to collapse (with rapid intravenous administration), cardialgia, an increase in the frequency of angina attacks

- gastralgia, diarrhea , nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, loss of appetite (with prolonged use)

- skin rash, itching, increased sweating

Compaction, hyperemia, soreness (at the injection site)

- chest pain, tachypnea

hypoglycemia

Increased diuresis, albuminuria, hematuria

The frequency of occurrence of side effects decreases with a decrease in the dose of the drug.

Contraindications

Children's age up to 14 years

Hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine)

Epilepsy

Severe arterial hyper- or hypotension

Severe tachyarrhythmias

Hemorrhagic stroke

Retinal hemorrhage

Carefully:pregnancy, age older 55 years and uncontrolled hypothyroidism (possibility of cumulation), sepsis, prolonged hyperthermia, gastroesophageal reflux, peptic ulcer of the stomach and duodenum (history), prostate adenoma.

Drug Interactions

Ephedrine, beta-agonists, caffeine and furosemide enhance the effect of the drug. In combination with phenobarbital, difenin, rifampicin, isoniazid, carbamazepine or sulfinpyrazone, a decrease in the effectiveness of aminophylline is observed, which may require an increase in the doses of the drug used. The clearance of the drug is reduced when administered in combination with macrolide antibiotics, lincomycin, allopurinol, cimetidine, isoprenaline, beta-blockers, which may require a dose reduction. Oral estrogen-containing contraceptives, antidiarrheal drugs, intestinal sorbents weaken, and H2-histamine blockers, slow calcium channel blockers, mexiletin enhance the effect (they bind to the cytochrome P450 enzymatic system and slow down the metabolism of aminophylline). In the case of use in combination with enoxacin and other fluoroquinolines, the dose of aminophylline is reduced. The drug inhibits the therapeutic effects of lithium carbonate and beta-blockers. Appointment of beta-blockers - interferes with the bronchodilating effect of eufillin and can cause bronchospasm. Eufillin potentiates the action of diuretics by increasing glomerular filtration and reducing tubular reabsorption. With caution, aminophylline is prescribed simultaneously with anticoagulants, with other derivatives of theophylline or purine. It is not recommended to use aminophylline with agents that excite the central nervous system (increases neurotoxicity). The drug should not be used with dextrose solutions; it is not compatible with glucose, fructose and levulose solutions. The pH of the solutions to be mixed should be taken into account: pharmaceutically incompatible with acid solutions.

Increases the likelihood of side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), general anesthesia (increases the risk of ventricular arrhythmias).

With simultaneous use with enoxacin, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon alfa, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil, and with influenza vaccination, the intensity of the action of aminophylline may increase, which may require a reduction in its dose.

special instructions

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

With severe violations of the liver and kidneys (liver and / or kidney failure)

Peptic ulcer of the stomach and duodenum (in history), with bleeding from the gastrointestinal tract in a recent history

In severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris)

With widespread atherosclerosis of the vessels

With hypertrophic obstructive cardiomyopathy

With frequent ventricular extrasystoles

With increased convulsive readiness

With uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis

With prolonged hyperthermia

With gastroesophageal reflux

With prostatic hypertrophy.

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 fetus and newborn. Newborns whose mothers received aminophylline during pregnancy (especially the third trimester) need medical supervision to control possible symptoms of methylxanthines intoxication. Prescribing the drug during pregnancy requires a careful assessment of the benefits for the treatment of the mother and the potential risk to the fetus, is made only for extreme health reasons.

Breastfeeding while taking the drug should be discontinued.

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

Given the possibility of developing side effects of the drug, during the period of treatment, one should refrain from driving vehicles and engaging in potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Overdose:

Symptoms: anorexia, diarrhea, nausea, vomiting, pain in the epigastric region, gastrointestinal bleeding, tachycardia, ventricular arrhythmia, tremor, generalized convulsions, hyperventilation, a sharp decrease in blood pressure.

Treatment: withdrawal of the drug, stimulation of its excretion from the body (forced diuresis, hemosorption, plasma sorption, hemodialysis, peritoneal dialysis) and the appointment of symptomatic agents. Diazepam (by injection) is used to stop seizures. Barbiturates should not be used. With severe intoxication (eufillin content more than 50 g / l), hemodialysis is recommended.

Release form and packaging

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