Eufillin – pharmacological drug, belonging to the group of xanthines. All dosage forms contain the active ingredient - aminophylline, which is a combination of theophylline and ethylenediamine.

The medication has a dilating effect on the bronchi, relaxing them smooth muscle and eliminating spasms. In addition, it improves the functioning of epithelial cilia respiratory tract, improves contractions of the diaphragmatic, intercostal and other respiratory muscles.

Eufillin stimulates the vasomotor and respiratory centers and improves/activates blood circulation. Additionally, the drug reduces tone blood vessels(mainly brain vessels, skin and kidneys).

Eufillin photo of tablets and ampoules (injections)

It has a peripheral venodilating effect, reduces pulmonary vascular resistance, and reduces pressure in the “lesser” circulation. Increases renal blood flow and has a moderate diuretic effect.

Eufillin has a tocolytic effect, which increases the acidity of gastric juice. In high concentrations it has an enileptogenic effect.

The active substance of aminophylline is theophylline. It is well and quickly absorbed from gastrointestinal tract and has high bioavailability. Penetrates through the placental barrier into breast milk. Metabolized in the liver and excreted through the kidneys.

Indications for use of Eufillin

• chronic obstructive bronchitis;
• bronchial asthma (prevention of bronchospasm, drug of choice for exercise-induced asthma, additional remedy for other forms of asthma);
• emphysema;
• paroxysmal night apnea (Pickwick syndrome);
• chronic pulmonary heart disease.

Eufillin injections are prescribed intravenously for acute attacks bronchial asthma and strokes.

Eufillin tablets are a means of systemic use for the treatment of obstructive respiratory diseases.

Instructions for use of Eufillin, dosage

Eufillin injections

Intravenous injection of Eufillin - administered in a slow stream over 4-6 minutes at a dose of 0.12 - 0.24 g (5-10 ml of a 2.4% solution, which is pre-diluted in 10-20 ml of isotonic sodium chloride solution).

The drug is administered intravenously under control of heart rate, respiration and blood pressure.

The injection of Eufillin gives a pronounced antispasmodic effect in case of hepatic colic, enhances the secretion of the pancreas, therefore, when various diseases digestive organs, accompanied by exocrine pancreatic insufficiency, as well as if the latter arose as a result of chronic pancreatitis, intravenous injections of 10 ml of a 2.4% solution are prescribed.

Intramuscular injection - 2-3 ml of 12% aminophylline solution or 1-1.5 ml of 24% aminophylline solution are administered. It is recommended to inject into the upper sector of the gluteal muscle at a dose of 100–500 mg per day.

If the patient has status asthmaticus, he is prescribed an infusion of the drug in the amount of 720 or 750 mg.

The duration of therapy with the injection form of the drug cannot be more than 14 days.

Eufillin tablets

Take the medication orally - in tablets, 0.1–0.2 g 2–3 times a day after meals.

Adults and adolescents weighing more than 50 kg, depending on the clinical situation, are prescribed 150-300 mg (1-2 tablets) 3 times a day, in severe cases 300 mg (2 tablets) 4 times a day with an interval of 6 hours. The average daily dose is 600-1200 mg or 4-8 tablets in 3-4 doses.

If it is necessary to alleviate the condition of chronic obstructive pulmonary disease in an acute state, it is recommended to start with a dose of the drug of 5-6 mg/kg. Eufillin must be taken carefully, constantly monitoring its amount in the blood.

The maximum daily dose in adults is 10-13 mg/kg (0.4-0.5 ml/kg), in children aged 6-17 years - 13 mg/kg body weight (0.5 ml/kg), from 3 years to 6 years – 20-22 mg/kg (0.8-0.9 ml/kg).

The amount of Eufillin prescribed to a child is determined by the doctor, taking into account the weight and age of the child, as well as the severity of the disease.

Features of application

Prescribing Eufillin to patients with chronic heart and liver failure, pneumonia or viral infection, as well as elderly patients, requires caution and a reduction in drug doses.

During treatment with Eufillin, you should refrain from drinking alcohol.

It should be noted that the drug "Eufillin" can increase the level of uric acid in urine. When using this medication, extreme caution must be exercised when taking it at the same time. large quantity products and drinks containing caffeine.

During the period of therapy with Eufillin, it is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions due to possible side effects.

Side effects and contraindications Eufillin

Dyspeptic disorders (digestive disorders), with intravenous administration dizziness, hypotension (low blood pressure), headache, migraines, palpitations, convulsions, when used rectally, irritation of the rectal mucosa.

Overdose

In reviews of Eufillin, it is noted that in case of an overdose of the drug, generalized convulsions, photophobia, sleep disorders, ventricular arrhythmias, tachycardia, facial hyperemia, tachypnea, nausea, vomiting, diarrhea, anorexia. If these symptoms develop, it is necessary to discontinue the drug and actively stimulate its elimination from the body.

Contraindications:

• heart rhythm disturbance;
• myocardial infarction;
• extrasystole;
• heart failure;
• paroxysmal tachycardia;
• coronary insufficiency.

Intravenous administration to children under 14 years of age is contraindicated.

During pregnancy and lactation, the use of the drug is possible only for health reasons. The use of aminophylline during pregnancy may result in potentially dangerous concentrations of theophylline and caffeine in the blood plasma of the newborn. Newborns whose mothers received aminophylline during pregnancy (especially in the third trimester) require medical supervision to monitor possible symptoms theophylline intoxication.

Analogues of Eufillin, list

Analogs of Eufillin include drugs (list):

1. Aminophylline-Eskom;
2. Theotard;
3. Diprophylline;
4. Omnitus;
5. Berodual;
6. Tavipek;
7. Pertussin;
8. Ventolin;
9. Seretide;
10. Spiriva;
11. Fenoterol.

It is important to understand that the given instructions for use of Eufillin, price and reviews do not apply to analogues of the drug and cannot be used as a guide for use, replacement or other actions. All therapeutic actions must be carried out by a specialist; when replacing Eufillin with an analogue, it may be necessary to adjust the dosage or the entire course of treatment.

INSTRUCTIONS for medical use of the drug

Registration number:

Tradename:

Eufillin

International nonproprietary name:

Aminophylline

Chemical name:

3,7-dihydro-1,3-dimethyl-III-purine-2,6-dione and 1,2 ethylenediamine

Dosage form:

pills

Composition per tablet:

Active substance:
Aminophylline (aminophylline) - 150 mg

Excipients:
Calcium stearate - 2 mg
Potato starch - 48 mg

Description:

Round, flat-cylindrical tablets, white or white with a yellowish tint, with a bevel.

Pharmacotherapeutic group:

Bronchodilator.

ATX code

Pharmacological properties

Pharmacodynamics
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 “lesser” 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
After oral administration, it is quickly and completely absorbed, bioavailability is 90-100%. Food reduces the rate of absorption without affecting its magnitude (large volumes of liquid and proteins speed up the process). The higher the dose taken, the lower the absorption rate. The time to reach maximum concentration is 1-2 hours. 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. The connection with plasma proteins in adults is 60%, in patients with liver cirrhosis - 36%. Penetrates into breast milk (10% of the dose taken), through the placental barrier (concentration in fetal blood serum is slightly higher than in maternal serum). Aminophylline exhibits bronchodilating properties in 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 content of the drug in the blood of 5-10 mcg/ml. Metabolized at physiological pH values ​​with the release of free theophylline, which is further metabolized in the liver with the participation of several isoenzymes of cytochrome P 450. As a result, 1, 3-dimethyluric acid (45-55%) is formed, which has pharmacological activity, but is inferior to theophylline in 1 -5 times. Caffeine is an active metabolite and is formed in small quantities. In children over 3 years of age and in adults (unlike younger children), the phenomenon of caffeine accumulation is absent. Half-life in children over 6 months. - 3.7 hours; in adults - 8.7 hours; for “smokers” (20-40 cigarettes per day) - 4-5 hours (after quitting smoking, pharmacokinetics normalize after 3-4 months); in adults with chronic obstructive pulmonary disease, pulmonary heart disease and pulmonary heart failure - over 24 hours. Excreted by the kidneys.

Indications for use:

Broncho-obstructive syndrome of any origin: bronchial asthma (the drug of choice in patients with exercise-induced asthma and as an additional remedy for other forms), chronic obstructive pulmonary disease, pulmonary emphysema, chronic obstructive bronchitis, pulmonary hypertension, cor pulmonale, sleep apnea.

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, hemorrhage into the retina of the eye, childhood(up to 3 years).

Carefully

Severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread vascular atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased convulsive readiness, hepatic and/or renal failure, peptic ulcer of the stomach and duodenum (history), bleeding from the gastrointestinal tract in a recent history, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, hyperplasia prostate gland, pregnancy, lactation period, elderly age, childhood.
Prescribed simultaneously with anticoagulants.

Directions for use and dosage:

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.

Side effect

From the outside nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor.

From the outside of cardio-vascular system: palpitations, tachycardia (including in the fetus when taken by a pregnant woman in the third trimester), arrhythmias, cardialgia, decreased blood pressure, increased frequency of angina attacks.

From the outside digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation peptic ulcer, diarrhea, with long-term use - loss of appetite.

Allergic reactions: skin rash, itching, fever.

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

Overdose

Symptoms: loss of 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 activated carbon, laxative drugs, 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 - for 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 glucocorticosteroids, mineralocorticosteroids (hypernatremia), agents for 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 antibiotics of the macrolide group, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon-alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and with influenza vaccination, the intensity of action is aminofil Lina 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

Be careful when consuming large quantities of caffeine-containing foods or drinks during the treatment period; you must refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Release form:

Tablets 150 mg.
10 tablets in a blister pack made of polyvinyl chloride film and aluminum foil or polyethylene-coated paper.
30 tablets in an orange glass jar of the BTS type.
30 tablets per BP type polymer jar.
Each jar or 1, 2, 3 blisters with instructions for use is placed in a cardboard pack.

Storage conditions:

In a dry place, protected from light, at a temperature not exceeding 20 ° C.
Keep out of the reach of children.

Best before date:

5 years.
Do not use after the expiration date.

Conditions for dispensing from pharmacies:

On prescription.

Company manufacturer:

JSC "Biosintez", Russia, Penza.

The instructions for use classify the drug Eufillin as a bronchodilator with antispasmodic and vasodilating properties. Tablets 150 mg, injections in ampoules for injection in solution intravenously and intramuscularly are prescribed to stimulate the vasomotor and respiratory centers, to improve blood circulation. Reviews from patients and recommendations from doctors report that this medicine helps in the treatment of status asthmaticus and bronchial obstruction.

Release form and composition

Pharmacies receive:

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

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

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

What does Eufillin help with (tablets and injections)?

Indications for use of the medicine in tablets:

• chronic obstructive bronchitis (COB);
• bronchial asthma (BA);
• chronic “pulmonary heart”;
• Pickwick's syndrome (paroxysmal sleep apnea);
• emphysema.

Eufillin is the drug of choice for exercise-induced asthma; for other forms of the disease it is used in combination with other drugs.

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

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

Instructions for use

Eufillin tablets

Taken orally, adults should be prescribed 150 mg per dose 1-3 times a day after meals. Children 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 Eufillin for adults orally: single - 0.5 g, daily - 1.5 g.

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

Injection

Individual treatment regimen, which depends on the indications, age, and clinical situation. The solution is administered intravenously, intramuscularly, or through a dropper.

pharmachologic effect

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

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

This helps reduce the flow of calcium ions into the cells, which are responsible for muscle contraction, and relax the bronchial muscles. The medicine also reduces the tone of blood vessels, mainly those located in the skin, kidneys and brain. This helps to relax the venous walls in the pulmonary circulation, reducing the pressure in it.

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

Contraindications

The use of Eufillin according to the instructions is contraindicated:

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

Side effects

Negative effects of using Eufillin tablets:

• hematuria, albuminuria;
• sleep disturbances, anxiety, dizziness, convulsions, tremor;
• hypoglycemia (rare);
• irregular heart rhythm, palpitations.

Against the background of injection therapy, the following are possible:

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

Side effects are dose-dependent, that is, to relieve them, it is often enough to reduce the dose of the drug.

Local reactions to the injection of the solution manifest themselves in the form of skin hyperemia, pain and the formation of a seal at the injection site.

Children, pregnancy and breastfeeding

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

special instructions

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

Drug interactions

The instructions indicate increased side effects of glucocorticoids, mineralocorticoids and adrenergic stimulants when taken simultaneously with this medicine. Also, the drug is not used simultaneously with other xanthine derivatives.

Analogues of the drug Eufillin

Analogues are determined by structure:

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

Analogs have a similar effect:

1. Theotard.
2. Neo-Theophedrine.
3. Teobiolong.
4. Diprophylline.
5. Theobromine.
6. Neoteopek A.
7. Theophylline.
8. Teofedrine-N.

Vacation conditions and price

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

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

Post Views: 485

A drug Eufillin- a drug for systemic use for obstructive respiratory diseases, is a bronchodilator, antispasmodic, vasodilator. The mechanism of action of theophylline is primarily due to the blocking of adenosine receptors, inhibition of PDE, an increase in the content of intracellular cAMP, and a decrease in the intracellular concentration of calcium ions. Relaxes smooth muscles internal organs(bronchi, gastrointestinal tract, biliary tract, uterus), coronary, cerebral and pulmonary vessels, dilates coronary arteries, reduces peripheral vascular resistance. Increases the tone of the respiratory muscles (intercostal muscles and diaphragm), reduces pulmonary vascular resistance and improves blood oxygenation, activates the respiratory center medulla oblongata, increases its sensitivity to carbon dioxide, improves alveolar ventilation, which leads to a decrease in the severity and frequency of apnea episodes. Theophylline eliminates vasospasm, increases collateral blood flow and oxygen saturation, reduces perifocal and general cerebral edema, reduces cerebrospinal fluid and, accordingly, intracranial pressure. Improves the rheological properties of blood, reduces thrombus formation, inhibits platelet aggregation (inhibiting platelet activation factor and prostaglandin F2alpha), increases the endurance of red blood cells to deformation, and normalizes microcirculation. Exhibits an antiallergic effect, suppressing mast cell degranulation and reducing the level of allergy mediators (serotonin, histamine, leukotrienes). Increases renal blood flow, has a diuretic effect due to a decrease in tubular reabsorption, increases the excretion of water, chlorine ions, and sodium.
Therapeutic effects develop 5-15 minutes after injection.

Pharmacokinetics

.
The binding of theophylline to plasma proteins is: in healthy adults - about 60%, in patients with liver cirrhosis - 35%. Penetrates through histohematic barriers, distributed into tissues. About 90% of theophylline is metabolized in the liver with the participation of several isoenzymes of cytochrome P 450 to inactive metabolites - 1,3-dimethyluric acid, 1-methyluric acid and 3-methylxanthine. Excreted mainly by the kidneys in the form of metabolites, up to 13% of the drug is excreted unchanged in adults, and up to 50% of the drug in children. Partially passes into breast milk. The half-life of theophylline depends on age and the presence of concomitant diseases and is: in adult patients with bronchial asthma - 6-12 hours, in smokers - 4-5 hours, in elderly patients, with heart failure, impaired liver function, pulmonary edema , chronic obstructive pulmonary diseases - more than 24 hours.
Therapeutic concentrations of theophylline in the blood are: to achieve a bronchodilator effect - 10-20 mcg / ml, for a stimulating effect on the respiratory center - 5-10 mcg / ml. Toxic concentrations are above 20 µg/ml.

Indications for use

Eufillin intended for relief of broncho-obstructive syndrome in bronchial asthma, bronchitis, emphysema, disorders of the respiratory center (night paroxysmal apnea), “pulmonary heart”.

Mode of application

A drug Eufillin administered intravenously. The dose is selected individually, taking into account the possibility of different withdrawal rates.
If the patient is using oral theophylline preparations, the dose of parenteral theophylline should be reduced.
When administering the drug, the patient is in a lying position; The doctor monitors blood pressure, heart rate, respiratory rate and the general condition of the patient.
The solution should be prepared immediately before use - for jet administration, a single dose of the drug should be diluted in 10-20 ml of 0.9% sodium chloride solution; for intravenous drip administration, a single dose of the drug should be pre-diluted in 100-150 ml of 0.9% sodium chloride solution.
Administer intravenously as a stream slowly (over at least 5 minutes), intravenously as a drip at a rate of 30-50 drops per minute.
When administering the drug, calculate the dose as theophylline in milligrams, taking into account that 1 ml of the drug contains 20 mg of theophylline.
For adults, administer intravenously in a stream at a daily dose of 10 mg/kg body weight (an average of 600-800 mg theophylline), distributed over 3 injections. For cachexia and in persons with initial low body weight, reduce the daily dose to 400-500 mg, while during the first administration no more than 200-250 mg should be administered.
If increased heart rate, dizziness, or nausea occur, the rate of administration should be reduced or switched to drip administration of the drug.
Children over 14 years of age: intravenous drip at a dose of 2-3 mg/kg body weight.
Maximum daily doses that can be used without monitoring the concentration of theophylline in blood plasma: children 3-9 years old - 24 mg/kg body weight, 9-12 years old - 20 mg/kg body weight, 12-16 years old - 18 mg/kg body weight body, patients over 16 years of age - 13 mg/kg body weight (or 900 mg).
Higher doses for adults. Intravenously: single - 250 mg, daily - 500 mg.
Higher doses for children. Intravenously: single dose - 3 mg/kg body weight.
The duration of treatment depends on the severity of the disease, sensitivity to the drug and ranges from several days to two weeks (but not more than 14 days).
Do not use in patients with severe renal and/or hepatic impairment (see “Contraindications”).
Procedure for working with the ampoule.
1. Separate one ampoule from the block and shake it, holding it by the neck.
2. Squeeze the ampoule with your hand (there should be no leakage of the drug), roll it up with rotational movements and separate the head.
3. Immediately connect the syringe to the ampoule through the hole.
4. Turn the ampoule over and slowly draw its contents into the syringe.
5. Place the needle on the syringe.
The drug should not be used for administration to children under 3 years of age. For children over 3 years of age, the use of the drug is possible for health reasons, but not longer than 14 days.

Side effects

From the outside immune system: skin rash, skin itching, angioedema, shock, anaphylactic shock, bronchospasm.
From the skin and subcutaneous tissue skin hyperemia, exfoliative dermatitis.
Neurological disorders: epileptiform seizures, confusion/loss of consciousness, agitation, anxiety, sleep disturbances, insomnia, dizziness, headache, irritability, tremors, convulsions, hallucinations.
Cardiac disorders: increased heart rate, cardialgia, arrhythmias, tachycardia, extrasystole, decreased blood pressure, heart failure, increased frequency of angina attacks, collapse (with rapid administration).
Gastrointestinal disorders: nausea, vomiting, diarrhea, heartburn, exacerbation of peptic ulcer, stimulation of gastric juice secretion, stomach pain, loss of appetite, gastroesophageal reflux, intestinal atony.
From the urinary system: increased diuresis, difficulty urinating.
Metabolic disorders: metabolic acidosis, hypokalemia, hypercalcemia, hyperuricemia, hyperglycemia, acid-base imbalance in the blood, rhabdomyolysis.
General disorders: feeling of heat, low-grade fever, excessive sweating, weakness, shortness of breath.
Local reactions: reactions at the injection site (induration, hyperemia, pain).

Contraindications

Contraindications to the use of the drug Eufillin are: hypersensitivity to the components of the drug, as well as to other xanthine derivatives (caffeine, pentoxifylline, theobromine), acute heart failure, angina pectoris, acute myocardial infarction, paroxysmal tachycardia, extrasystole, severe arterial hyper- and hypotension, widespread vascular atherosclerosis, pulmonary edema , hemorrhagic stroke, retinal hemorrhage, history of bleeding, gastric ulcer and duodenum(in the acute stage), gastroesophageal reflux, epilepsy, increased convulsive hyperactivity, uncontrolled hypothyroidism, hyperthyroidism, thyrotoxicosis, impaired liver and / or kidney function, porphyria, sepsis.

Pregnancy

Use of the drug Eufillin Contraindicated during pregnancy. Theophylline passes into breast milk, so breastfeeding should be stopped during treatment.

Interaction with other drugs

Ephedrine, beta-agonists, caffeine and furosemide enhance the effect Eufillina.
Increases the likelihood of developing side effects of GCS, mineralocorticoids (hypernatremia), drugs for general anesthesia (increases the risk of ventricular arrhythmias, seizures).
In combination with phenobarbital, phenytoin, rifampicin, isoniazid, carbamazepine or sulfinpyrazone, a decrease in the effectiveness of aminophylline is observed, which may require an increase in the dose of the drug.
Aminoglutethimide and moracizine, as inducers of microsomal oxidation, increase the clearance of aminophylline, which may require an increase in its dose.
Clearance decreases when prescribed in combination with macrolide antibiotics, lincomycin, allopurinol, cimetidine, isoprenaline, beta-blockers, which may require a dose reduction.
Antidiarrheal drugs, intestinal sorbents weaken, and oral estrogen-containing contraceptives, H2 histamine blockers, slow calcium channel blockers, mexiletine - enhance the effect (they bind to the cytochrome 450 enzymatic system and change the metabolism of aminophylline).
When used in combination with enoxacin and other fluoroquinolones, small doses of ethanol, disulfiram, recombinant interferon alpha, methotrexate, propafenone, thiabendazole, ticlopidine, verapamil, and with influenza vaccination, the intensity of action of aminophylline may increase, which may require a reduction in its dose.
When using levofloxacin and theophylline simultaneously, it is necessary to monitor the level of theophylline in the blood and adjust the dose accordingly.

Overdose

At plasma theophylline concentrations above 20 mg/kg, facial skin flushing, insomnia, motor agitation, anxiety, photophobia, anorexia, diarrhea, nausea, vomiting, epigastric pain, gastrointestinal bleeding, tachypnea, tachycardia, angina, ventricular arrhythmias, tremor, generalized convulsions, hyperventilation, arterial hypotension. In severe poisoning, epileptoid seizures may develop (especially in children, without the occurrence of any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, skeletal muscle necrosis, confusion, impaired renal function with myoglobinuria.

Severe complications and signs of intoxication resulting from chronic overdose are more common in elderly patients (over 60 years of age) with plasma theophylline concentrations exceeding 30 mg/kg. When the concentration of the drug in the blood plasma is above 40 mg/kg, coma may develop.
Treatment: depends on the severity of symptoms and includes drug withdrawal, hemodynamic correction, stimulation of theophylline excretion from the body (forced diuresis, hemosorption, plasma sorption, hemodialysis, peritoneal dialysis), prescription of symptomatic drugs, oxygen therapy, artificial ventilation. To relieve seizures, use diazepam. The use of barbiturates is inappropriate.
For effectiveness and safety, the serum concentration of the drug should be maintained within 10-15 mg/kg; if it is not possible to determine the concentration of theophylline in the blood, its daily dose should not exceed 10 mg/kg.

Storage conditions

Keep out of the reach of children. Store in original packaging at a temperature not exceeding 25 ° C.

Release form

Eufillin - solution for injection.
Packaging: 5 ml in ampoules No. 10, No. 50, No. 100 and 10 ml in ampoules No. 10.

Compound

1 ml of the drug Euphyllin - 20 mg of theophylline.
Excipients: sodium acetate trihydrate, sodium hydroxide, water for injection.

Additionally

Before administration, the solution Eufillin must be warmed to body temperature.
The ability to influence the reaction rate when driving vehicles or other mechanisms
During treatment, it is not recommended to engage in activities that require increased attention, rapid mental and motor reactions (driving vehicles).
The drug suppresses therapeutic effects lithium carbonate and beta blockers. The administration of beta-blockers interferes with the bronchodilating effects of aminophylline and can cause bronchospasm.
Eufillin potentiates the effect of diuretics by increasing glomerular filtration and reducing tubular reabsorption.
With caution, aminophylline is prescribed simultaneously with anticoagulants, other theophylline or purine derivatives. It is not recommended to use aminophylline with drugs that excite the central nervous system (increases neurotoxicity). When used with non-selective inhibitors recapture monoamines may inhibit psychomotor reactions.
At serious illnesses cardiovascular system, liver, viral infection, with prolonged hyperthermia, prostate hypertrophy, severe hypoxia, diabetes mellitus, glaucoma, elderly people (over 60 years old), the dose of the drug should be reduced and used with caution.
For patients who smoke, it is recommended to increase the dose due to the accelerated elimination of the drug from the body.
Fever, regardless of its cause, can reduce the rate at which theophylline is eliminated.
The effects of the drug can be significantly enhanced by simultaneous consumption of foods high in caffeine or theobromine (coffee, tea, chocolate).

Main settings

Name:	EUPHYLLINE
ATX code:	R03DA05 -

Active substance

Aminophylline

Dosage form

solution for infusion

Manufacturer

Dalkhimfarm, Russia

Compound

1 ml of solution for intramuscular administration contains:
active ingredient: aminophylline 24 mg.

pharmachologic effect

Pharmaceutical group: bronchodilator.
Pharmaceutical action: Bronchodilator, methylxanthine derivative; inhibits PDE, 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.
Relaxes the bronchial muscles, stimulates the respiratory center and improves alveolar ventilation, which ultimately leads to a reduction in the severity and frequency of apnea episodes.
It has a stimulating effect on the activity of the heart, increases strength and heart rate, 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 lowers pressure in the pulmonary circulation. Increases renal blood flow and has a moderate diuretic effect. Expands extrahepatic bile ducts.
Stabilizes mast cell membranes, inhibits the release of mediators of allergic reactions.
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 epileptogenic effect.
Pharmacokinetics: After oral administration, it is quickly and completely absorbed, however, the bioavailability and kinetics of absorption depend on the dosage form of the drug. Bioavailability for rapid release tablets and liquids dosage forms- 90-100%. When using prolonged dosage forms, absorption parameters and bioavailability may vary. Food reduces the rate of absorption without affecting its magnitude (large volumes of liquid and proteins speed up the process). The higher the dose taken, the lower the absorption rate. TCmax with intravenous administration of 0.3 g - 15 min, Cmax value - 7 μg/ml. TCmax for conventional dosage forms - 1-2 hours, for extended-release forms - 4-7 hours, for enteric-coated tablets - 5 hours. The volume of distribution is in the range of 0.3-0.7 l/kg (30-70% of the “ideal” weight body), on average 0.45 l/kg. Communication with plasma proteins in adults - 60%, in newborns - 36%, in patients with liver cirrhosis - 36%. Penetrates into breast milk (10% of the dose taken), through the placental barrier (the concentration in the fetal blood serum is slightly higher than in the maternal serum).
Aminophylline exhibits bronchodilating properties in 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 content of the drug in the blood - 5-10 mcg/ml.
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 newborns and children under 6 months, in whom, due to the extremely long half-life of caffeine, its significant accumulation occurs in the body (up to 30% of that for aminophylline).
In children over 3 years of age and in adults, the phenomenon of caffeine accumulation is absent.
T1/2 in newborns and children under 6 months - more than 24 hours; in children over 6 months - 3.7 hours; in adults - 8.7 hours; for “smokers” (20-40 cigarettes per day) - 4-5 hours (after quitting smoking, pharmacokinetics normalize after 3-4 months); in adults with COPD, pulmonary heart disease 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.

Indications

• Broncho-obstructive syndrome (mainly to relieve attacks) with:
  • Bronchial asthma.
  • Bronchitis.
  • Pulmonary emphysema.
  • Cardiac asthma.
• Hypertension in the pulmonary circulation.
• Relief of cerebral vascular crises of atherosclerotic origin.
• Included combination therapy for ischemic strokes and chronic failure cerebral circulation to reduce intracranial pressure and cerebral edema.

Contraindications

Hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine), epilepsy, peptic ulcer of the stomach and duodenum (in the acute stage - for oral forms, especially non-extended-release tablets), gastritis with high acidity, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, retinal hemorrhage, children's age (up to 3 years, for prolonged oral forms - up to 12 years).
Carefully. Severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread vascular atherosclerosis, HOCM, frequent ventricular extrasystole, increased convulsive readiness, liver and/or renal failure, peptic ulcer of the stomach and duodenum (history), bleeding from the gastrointestinal tract in recent history, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy. pregnancy, lactation, old age, childhood (especially for oral forms).

Side effects

From the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor.
From the cardiovascular system: palpitations, tachycardia (including in the fetus when taken by a pregnant woman in the third trimester), arrhythmias, decreased blood pressure, cardialgia, increased frequency of angina attacks.
From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with long-term use - loss of appetite.
Allergic reactions: skin rash, skin itching, fever.
Other: chest pain, tachypnea, flushing, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.
Side effects decrease with decreasing dosage of the drug.
Local reactions: compaction, hyperemia, pain at the injection site.
At rectal administration- proctitis, irritation of the rectal mucosa.

Interaction

When used simultaneously with sympathomimetics, a mutual enhancement of action occurs; with beta-blockers and lithium preparations - the effect is mutually reduced. The intensity of action of aminophylline may decrease (due to an increase in its clearance) when used simultaneously with phenobarbital, rifampicin, isoniazid, carbamazepine, sulfinpyrazone, phenytoin, as well as in smokers.

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

Xanthine derivatives can potentiate hypokalemia caused by the action of β2-adrenergic receptor stimulants, corticosteroids and diuretics.

Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline.
Pharmaceutically incompatible with acid solutions.

How to take, course of administration and dosage

Eufillin is prescribed intramuscularly, 1 ml (240 mg) of solution deep into the upper quadrant of the gluteal muscle.

Eufillin is administered parenterally up to 3 times a day, for no more than 14 days. The concentration of aminophylline in blood serum should not exceed 20 mcg/ml.

• Higher doses of aminophylline for intramuscular administration
  • For adults: single dose - 0.5 g, daily - 1.5 g.
  • For children: single dose - 7 mg/kg, daily dose - 15 mg/kg.

Correction of the dosage regimen may be required for heart failure, liver dysfunction, and chronic alcoholism.

In elderly patients, a dose reduction may be required (single dose - 0.3 g).

from 1 year to 9 years - 22 mg/kg;
from 9 to 12 years - 20 mg/kg;
from 12 to 16 years - 18 mg/kg;
over 16 years old - 13 mg/kg.
Children are prescribed intramuscularly at a dose of 15 mg/kg/day. IV at the age of up to 3 months - 30-60 mg/day, 4-12 months - 60-90 mg/day, 2-3 years - 90-120 mg, 4-7 years - 120-240 mg, 8- 18 years - 250-500 mg/day. The duration of parenteral administration is no more than 14 days.
For neonatal apnea, the initial dose (a condition characterized by periods of absence of breathing for 15 seconds and accompanied by cyanosis and bradycardia) is 5 mg/kg (by nasogastric tube), maintenance dose is 2 mg/kg in 2 divided doses. The duration of treatment is several weeks, in rare cases - months.
Can be administered rectally in the form of microenemas. Dose for adults - 0.24-0.48 g in 20-25 ml of warm water; for children - less, according to age.
Higher doses for adults orally, intramuscularly and rectally - single 0.5 g, daily 1.5 g; IV - single dose 0.25 g, daily 0.5 g.
Higher doses for children orally, intramuscularly and rectally - single 7 mg/kg, daily 15 mg/kg; IV - single dose 3 mg/kg.

Overdose

Symptoms: loss of appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, flushing of the facial skin, 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, administration of activated charcoal, laxatives, intestinal lavage with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasma sorption, hemodialysis (low efficiency, peritoneal dialysis is ineffective), symptomatic therapy (including metoclopramide and ondansetron - when vomiting). If convulsions occur, maintain airway patency and administer oxygen therapy. To stop 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 (iv).