Eufillin is a 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 their smooth muscles and eliminating spasms. In addition, it improves the functioning of the cilia of the respiratory tract epithelium, improves the contractions of the diaphragmatic, intercostal and other respiratory muscles.
Eufillin stimulates the vasomotor and respiratory centers and improves/activates blood circulation. Additionally, the drug reduces the tone of blood vessels (mainly the vessels of the brain, skin and kidneys).
Euphyllin 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 the 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 of 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 the 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 reduced doses of the drug.
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 dangerous species 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, with rectal use, irritation of the rectal mucosa.
Overdose
Reviews of Eufillin note that in case of an overdose of the drug, generalized convulsions, photophobia, sleep disorders, ventricular arrhythmias, tachycardia, facial hyperemia, tachypnea, nausea, vomiting, diarrhea, and anorexia are observed. 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
Analogues of Eufillin include drugs (list):
- Aminophylline-Eskom;
- Theotard;
- Diprophylline;
- Omnitus;
- Berodual;
- Tavipek;
- Pertussin;
- Ventolin;
- Seretide;
- Spiriva;
- 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.
Pharmacodynamics
Euphylline is a complex of theophylline and ethylenediamine. Thanks to the presence of ethylenediamine, the solubility of the drug in water and the possibility of intravenous administration are achieved.
Theophylline is a bronchodilator from the methylxanthine group. The mechanism of action is primarily due to the blocking of adenosine receptors, inhibition of phosphodiesterase, an increase in the content of intracellular cAMP, a decrease in the intracellular concentration of calcium ions, as a result of which the smooth muscles of the bronchi, biliary tract, coronary, cerebral and pulmonary vessels relax, and peripheral vascular resistance decreases. By reducing vascular resistance in the pulmonary artery, it reduces pressure in the vessels of the pulmonary circulation and normalizes perfusion processes in the lungs. Improves contractility of the intercostal muscles and diaphragm, activates the respiratory center, improves alveolar ventilation and blood oxygen saturation, accelerates mucociliary transport. Prevents the release of inflammatory mediators, inhibits platelet aggregation. It increases renal blood flow and has a diuretic effect due to a decrease in tubular reabsorption of water and electrolytes. Increases the frequency and strength of heart contractions, increases coronary blood flow and myocardial oxygen demand.
Pharmacokinetics
Chemical binding to ethylenediamine does not affect the pharmacokinetics and bioavailability of theophylline. In adults, about 60% of theophylline is bound to plasma proteins. The volume of distribution of theophylline is about 0.5 l/kg. Theophylline is distributed in the blood, extracellular fluid and muscle tissue.
Penetrates through the placental barrier and into breast milk.
Metabolized in the liver with the participation of microsomal enzymes (CYP1A2 and to a lesser extent CYP2E1). The main metabolites are 1,3-dimethyluric acid and 3-methylxanthine. Excretion occurs through the kidneys. About 10% of the dose is excreted unchanged in the urine (in children - up to 50%). The metabolism of theophylline has significant interindividual variability, so serum concentrations and half-life may vary significantly. The average half-life is: in non-smoking adults – 7–9 hours; for smokers – 4–5 hours; for children over 6 months – 3–5 hours; in newborns – more than 24 hours.
The clearance of theophylline depends on age, body weight, diet, smoking habit, and concomitant use of other medicines. In patients with cardiac or respiratory failure, impaired liver function, or viral infection, the half-life is prolonged.
Indications for use
Broncho-obstructive syndrome in bronchial asthma and chronic obstructive pulmonary disease.
Contraindications
Hypersensitivity to ethylenediamine or allergy to theophyllines, caffeine and theobromine,
- simultaneous use with other xanthine-containing drugs. When therapeutic doses of aminophylline and/or theophylline are administered simultaneously, by more than one route of administration, or in more than one drug product, the risk of serious toxicity increases,
- children up to 6 months of age,
- acute porphyria,
- acute period of myocardial infarction,
- paroxysmal tachycardia.
Precautionary measures
To reduce the undesirable stimulating effects of aminophylline on the central nervous and cardiovascular systems, intravenous administration of the drug should be slow and the rate should not exceed 25 mg/min.
Eufillin has a narrow therapeutic index and serum concentrations should be monitored regularly, especially during initiation of therapy.
The drug should be administered with caution in patients over 55 years of age.
Elderly patients with cardiac or hepatic disease should be closely monitored for signs of theophylline toxicity.
Children are particularly susceptible to the effects of theophylline and caution is required when prescribing the drug to children.
There have been reports of seizures in children who were prescribed theophylline at plasma concentrations within the accepted therapeutic range. Alternative treatment should be considered in patients with a history of seizure activity, and if Eufillin, intravenous solution 24 mg/ml is used in such patients, they should be carefully monitored for possible signs of CNS hyperstimulation.
Due to the fact that the average half-life of theophylline is shorter in smokers than in non-smokers, the former group may require larger doses of aminophylline.
Caution should be exercised in patients who have received influenza immunization, those with influenza infection, or those with acute febrile illnesses.
Eufillin should be prescribed with caution to patients with heart failure, chronic obstructive pulmonary disease, renal or hepatic dysfunction and chronic alcoholism, since the clearance of aminophylline is reduced.
Serum potassium levels should be monitored during regular therapy. This is very important when combined therapy with beta-2 agonists, corticosteroids or diuretics, or in the presence of hypoxia.
The drug should be used with caution in patients with peptic ulcers, hyperthyroidism, glaucoma, diabetes mellitus, severe hypoxemia, hypertension and impaired cardiac function or circulation, as these conditions may be aggravated.
Methylxanthines may increase gastric acidity and appropriate precautions should be taken if used in patients with a history of peptic ulcers.
The drug Eufillin, solution for intravenous administration 24 mg/ml should not be prescribed simultaneously with other xanthine-containing drugs.
Theophylline should be used only after assessing the benefit/risk ratio in patients with unstable angina, hypertrophic obstructive cardiomyopathy, cardiac arrhythmias (tachycardia, extrasystole), hemorrhagic stroke, retinal hemorrhage.
Interaction with other drugs
The following drugs may decrease the clearance of aminophylline, resulting in theophylline concentration increases in plasma and creates the potential for increased toxicity:
- fluvoxamine (concomitant use of theophylline and fluvoxamine should generally be avoided. Where possible, patients should receive their theophylline dose (possibly reduced by half) and plasma theophylline levels should be closely monitored);
- cimetidine;
- macrolides (for example, erythromycin, clarithromycin);
- quinolones (for example, ciprofloxacin, norfloxacin);
- fluconazole;
- isoniazid;
- propranolol;
- allopurinol (for example, high doses 600 mg per day);
- oral contraceptives;
- mexiletine, propafenone;
- calcium channel blockers, diltiazem, verapamil;
- medicines based on St. John's wort;
- disulfiram;
- interferon alpha, influenza vaccines;
- methotrexate;
- zafirlukast;
- tacrine;
- thiabendazole;
- thyroid hormones.
The following medicines may reduce concentrationtheophylline in plasma:
- rifampicin;
- antiepileptics (for example, carbamazepine, phenytoin, primidone, phenobarbital);
- ritonavir;
- aminoglutethimide;
- sulfpyrazone.
Other interactions:
- xanthines (concomitant use of other xanthine derivatives, including theophylline and pentoxifylline, is contraindicated due to the risk of toxicity);
- lithium (aminophylline increases the excretion of lithium and may reduce its therapeutic effectiveness);
- benzodiazepines (theophylline can reduce the effect of benzodiazepines);
- quinolones (increased risk of seizures);
- general anesthetics (increased risk of seizures with ketamine, increased risk of arrhythmia with halothane);
- pancuronium (resistance to neuromuscular block with pancuronium has been reported in patients receiving aminophylline);
- sympathomimetics (aminophylline may exhibit synergistic toxicity with ephedrine and other sympathomimetics when used together and may lead to cardiac arrhythmia);
- β2-agonists (increased risk of cardiac arrhythmia (see also hypokalemia);
- β-blockers (antagonism with the bronchodilator effect of aminophylline);
- cardiac glycosides (the direct stimulating effect of aminophylline on the myocardium can increase the sensitivity and toxic potential of cardiac glycosides);
- adenosine (antagonism of the antiarrhythmic effect of adenosine with theophylline);
- leukotriene antagonists (in clinical studies, coadministration with theophylline resulted in a decrease in plasma levels of zafirlukast by approximately 30%, but did not affect plasma concentrations of theophylline. However, during post-marketing surveillance, there were rare cases of increased theophylline levels in patients using zafirlukast (see above));
- doxapram (increased stimulation of the central nervous system);
- hypokalemia (the hypokalemic effect of beta-2 agonists may be enhanced by concomitant treatment with aminophylline. There is an increased risk of hypokalemia when theophylline derivatives are prescribed together with corticosteroids and diuretics (see Precautions)).
Pregnancy and lactation
Studies of the effect on reproductive function in animals have not been conducted. It is not known whether theophylline can cause fetal harm when administered to pregnant women. Although safe use no potential risk to the fetus has been established regarding theophylline during pregnancy, and theophylline has been used during pregnancy without teratogenicity or other adverse effects on the fetus. Due to the risk of uncontrolled bronchial asthma, safety during pregnancy, when the administration of aminophylline is really necessary, is usually not questioned. The question of using aminophylline during pregnancy is decided by the doctor. Theophylline crosses the placenta.
Theophylline is distributed into breast milk and may occasionally cause irritation or other signs of toxicity in nursing infants and therefore should not be used by nursing mothers.
Impact on the ability to drive vehicles and operate machinery
The medicine may cause dizziness and other side effects. During the treatment period, you must refrain from driving vehicles and operating machinery.
Directions for use and dosage
The drug is intended for slow intravenous administration.
The solution should be administered very slowly over 4-6 minutes, 5-10 ml of the drug (0.12-0.24 g), which is pre-diluted with a small volume (5-10 ml) of 5% dextrose or 0.9% solution sodium chloride for injection.
Before administration, the solution must be warmed to body temperature. Eufillin is administered parenterally up to 3 times a day, for no more than 14 days. Higher doses of aminophylline for adults when administered intravenously: single - 0.25 g, daily - 0.5 g.
Maintenance therapy can be provided by administering large volumes of infusion solutions, the rate of administration is adjusted to ensure required amount drug every hour.
Typically, when administered by drip, 10-20 ml of the drug (0.24-0.48 g) is diluted in 100-150 ml of 0.9% sodium chloride solution and administered at a rate of 30-50 drops per minute.
Theophylline therapeutic plasma concentrations are considered to range from 5 to 20 mcg/mL, and levels above 20 mcg/mL are most likely associated with toxicity. There is also individual patient variation in the dosage required to achieve plasma theophylline concentrations within the desired therapeutic range.
During therapy, patients should be closely monitored for toxicity and, where possible, theophylline levels should also be monitored; doses should be based on ideal body weight; the drug is not recommended for children under 6 months of age due to significant fluctuations in the metabolism of theophylline in young children.
Patients not receiving drugs containing theophylline
A. A loading dose of aminophylline 6 mg/kg body weight can be administered intravenously slowly at a rate not exceeding 25 mg/min.
B. Depending on the patient's condition, the maintenance dose for the next 12 hours can be calculated as follows:
- children aged 6 months to 9 years: 1.2 mg/kg/hour (decrease to 1 mg/kg/hour after 12 hours);
- children aged 9 to 16 years and young adult smokers: 1 mg/kg/hour (reduction to 0.8 mg/kg/hour after 12 hours);
- healthy non-smoking adults: 0.7 mg/kg/hour (decrease to 0.5 mg/kg/hour after 12 hours);
- elderly patients and persons with cor pulmonale: 0.6 mg/kg/hour (decrease to 0.3 mg/kg/hour after 12 hours);
- patients with congestive heart failure or liver disease: 0.5 mg/kg/hour (reduction to 0.1-0.2 mg/kg/hour after 12 hours).
Patients already receiving theophylline
The loading dose can be calculated on the basis that every 0.5 mg/kg of theophylline administered as a loading dose would result in a 1 mcg/mL increase in serum theophylline concentration.
Ideally, administration should be delayed until serum theophylline is determined. If this is not possible and if the clinical situation requires that the drug be administered, then administer 3.1 mg/kg aminophylline (equivalent to 2.5 mg/kg theophylline anhydrous) on the basis that this may result in increased serum theophylline concentrations approximately 5 mcg/ml when administered as a loading dose.
In the future, the maintenance dose is recommended to be the same as described above.
Overdose
Eufillin has a narrow therapeutic index. Theophylline toxicity is most likely to occur at serum concentrations greater than 20 mcg/mL and becomes increasingly severe at higher serum concentrations.
Doses greater than 3 g may have serious effects in adults (40 mg/kg in a child). Lethal dose may be as little as 4.5 g in adults (60 mg/kg in children), but is usually higher.
When aminophylline is administered intravenously in large doses in patients with renal, liver failure or cardiovascular complications, or if the injection is given quickly, death is possible.
Symptoms: tachycardia, in the absence of hypoxia, fever, or during coadministration of sympathomimetic drugs, may be a sign of theophylline toxicity.
Gastrointestinal symptoms: anorexia, nausea, vomiting, diarrhea, vomiting blood.
Neurological symptoms: anxiety, insomnia, irritability, headache, agitation, hallucinations, extreme thirst, slight fever, dilated pupils and tinnitus. Seizures can occur even without previous symptoms of toxicity and often lead to death. In very severe cases, coma may develop.
Cardiovascular symptoms: palpitations, arrhythmias, arterial hypotension, supraventricular and ventricular arrhythmias.
Metabolic symptoms: Hypokalemia can develop quickly and can be severe. Hyperglycemia, albuminuria, hyperthermia, hypomagnesemia, hypophosphatemia, hypercalcemia, respiratory alkalosis, metabolic acidosis, and rhabdomyolysis may also develop.
Treatment: Treatment of overdose is supportive and symptomatic.
Serum theophylline and potassium levels should be checked. Repeated oral administration of activated charcoal promotes the removal of theophylline from the body, even after intravenous administration. Aggressive antiemetic therapy may be required to allow oral administration of activated charcoal.
Convulsions can be stopped by intravenous administration of diazepam 0.1-0.3 mg/kg to 10 mg/kg. Restoring fluid and electrolyte balance is essential. Hypokalemia should be corrected by intravenous infusion of potassium chloride. Sedation with diazepam may be required in agitated patients.
Propranolol can be administered intravenously to correct tachycardia, hypokalemia and hyperglycemia, provided that the patient does not suffer from asthma.
In general, theophylline is metabolized quickly and hemodialysis is not warranted. In patients with congestive heart failure or liver disease, hemodialysis may increase the clearance of theophylline by 2-fold.
Hemosorption should be considered if:
- intestinal obstruction prevents the administration of several doses of activated carbon;
- plasma concentrations of theophylline >80 mg/l (acute) or >60 mg/l (chronic). In the elderly, hemosorption should be considered at theophylline concentrations >40 mg/L. Clinical signs, rather than theophylline concentration, are the best leadership for treatment.
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The site provides background information for informational purposes only. Diagnosis and treatment of diseases must be carried out under the supervision of a specialist. All drugs have contraindications. Consultation with a specialist is required!
Eufillin is an antispasmodic drug that relaxes the smooth muscles of all internal organs, such as the uterus, bladder, bronchi, blood vessels, bile ducts, etc. Thanks to the relaxation of smooth muscles, Eufillin relieves spasms and excessive contractions of internal organs caused by any causative factor. Thus, Eufillin dilates blood vessels, relieves bronchospasm, reduces the contractile activity of the uterus, eliminating the threat of miscarriage or premature birth, etc.Release forms, names and composition of Eufillin
Currently, Eufillin is produced by various pharmaceutical factories in the countries of the former USSR, in most cases under the same name - "Eufillin". However, some pharmaceutical factories, having decided to register their own name, which would distinguish their product from many others, use various options names containing the word "Eufillin". Usually in such cases, some word or abbreviation is added to “Eufillin”, which is related to the name of the drug’s manufacturing plant, for example, Eufillin-Darnitsa, Eufillin-UBF and some others. However, all these drugs are actually the same thing, since they are produced using the same technology, developed back in the USSR. In the following text, under the name “Eufillin” we will mean all the described medications that differ from each other only by a few letters in the name.So, Eufillin is available in three dosage forms:
- Tablets for oral administration;
- Solution for intravenous administration;
- Solution for intramuscular administration.
All dosage forms of Euphyllin include the substance as an active substance aminophylline in the following different quantities:
- Tablets – 150 mg of aminophylline;
- Solution for intravenous administration – 24 mg of aminophylline per 1 ml (2.4%);
- Solution for intramuscular administration – 240 mg of aminophylline per 1 ml (24%).
Solutions for intramuscular and intravenous injections contain only purified water and a preservative as auxiliary components, which may be different for drugs produced by different pharmaceutical factories. Therefore, to obtain complete and accurate information about the auxiliary components of this particular injection solution, it is recommended that you carefully study the instructions included with the medicine. Euphyllin tablets contain calcium stearate and potato starch as excipients.
Tablets are available in packs of 10, 15, 20, 25, 30, 40, 50, 75, 80 and 100 pieces. A solution for intravenous administration of 2.4% is available in ampoules of 5 ml and 10 ml. A solution for intramuscular administration of 24% is available in 1 ml ampoules.
Eufillin - recipe
The prescription for Eufillin solution for intravenous injection is written as follows:
Rp: Sol. Euphyllini 2.4% – 10 ml
D.t.d. No. 10 inamp.
S. dilute 0.9% NaCl (saline) 10 ml, inject slowly intravenously 10 ml.
The prescription for Euphyllin solution for intramuscular injection is written in exactly the same way as for the solution for intravenous administration, but with the only difference - after the words “Sol. Euphyllini” the concentration of 24% is indicated. After the letter S, the doctor can indicate how the solution should be administered. However, often the doctor does not write in the prescription how to administer the solution, but explains the rules and methodology for performing injections to a person in words.
The prescription for Eufillin tablets is written as follows:
Rp: Tab. Euphyllini 150 mg
D.t.d. No. 10 intab.
S. Take 1 tablet 3 times a day.
In recipes, after the letters “Rp” the Latin name of the drug (in this case Euphyllini) and its dosage form (Sol. - solution or Tab. - tablets) are indicated. After the name, the concentration of the solution or the dosage of the tablets is written. On the next line after the letters "D.t.d." under the No. icon the number of ampoules or tablets that the pharmacist must dispense to the person presenting the prescription is indicated. Finally, on the last line of the prescription, after the letter “S,” the doctor writes how the drug should be used. This information is intended for the patient himself.
Therapeutic effect of the drug
Eufillin reduces the contractile activity of smooth muscles that are present in those internal organs, which need to perform spastic muscle contractions in order to move their contents, for example, bronchi, bile ducts, uterus, bladder, blood vessels, intestines, etc. All of the listed organs are involved in the movement of any content: air passes through the bronchi, blood flows through the vessels, etc. Accordingly, to perform their functions, these internal organs perform contractile movements provided by smooth muscles.If the smooth muscles are strained excessively, then instead of rhythmic contractions, a spasm develops, the lumen of the organ sharply narrows, and various substances either stop being transported altogether, or the speed of this process slows down significantly. After all, a small amount of blood flows through a narrow lumen in a blood vessel, and air also passes through sharply narrowed bronchi with great difficulty, etc. To restore the normal patency of the organ and ensure regular transportation of substances at the required speed and in the required quantity, it is necessary to eliminate the spasm of the smooth muscles, that is, to relax them. After the muscles relax, the lumen of the organ expands and all substances can pass through it unhindered. Eufillin causes just such relaxation of smooth muscles and, accordingly, relief of their spasm with restoration of patency.
Since smooth muscles are present in many internal organs, and Eufillin has a non-selective effect, when it is used, all smooth muscle structures relax and, accordingly, multiple effects occur on the part of various systems.
Thus, Eufillin has the following therapeutic effects on various organs and tissues:
- Relaxes the muscles of the bronchi, expands their lumen and, thereby, relieves bronchospasm;
- Stimulates the functioning of the respiratory center in the brain;
- Reduces the number and severity of apnea attacks;
- Increases the strength and frequency of heart contractions;
- Increases the intensity of cardiac blood flow and myocardial oxygen demand;
- Reduces the tone of blood vessels, relaxing them and lowering blood pressure;
- Improves peripheral microcirculation in tissues;
- Increases blood supply to the kidneys and, thereby, has a moderate diuretic effect;
- Expands the bile ducts, relieving spasm and pain;
- Prevents the development of allergic reactions;
- Reduces the adhesion of platelets to each other and the formation of blood clots;
- Increases the resistance of red blood cells to deformation;
- Has a tocolytic effect (relaxes the uterus and eliminates the threat of miscarriage or premature birth);
- Increases the acidity of gastric juice;
- In high dosages it can provoke attacks of epilepsy.
Eufillin - indications for use
Indications for the use of tablets and injection solutions are different and are reflected in the table.| Indications for the use of Eufillin solutions for intravenous and intramuscular injections | Indications for the use of Euphyllin tablets |
| Asthmatic status | Broncho-obstructive syndrome (bronchospasm) of any origin, for example, with asthma, pulmonary hypertension, sleep apnea, COPD, etc. |
| Apnea in newborns | |
| Ischemia-type cerebrovascular accident (as part of complex therapy) | |
| Left ventricular failure, combined with bronchospasm and Cheyne-Stokes respiration | |
| Renal edema (as part of complex therapy) |
That is, the tablets are recommended for use in the chronic course of the disease with periodically recurring episodes of bronchospasm. And intravenous or intramuscular injections are indicated only for acute, emergency, life-threatening conditions, regardless of the cause that provoked them.
Non-standard use of the drug (for what procedures is it used)
Eufillin is used in the treatment of various conditions and diseases in which it is necessary to improve blood microcirculation and reduce tension and tissue tone. In such situations, it is recommended to deliver Eufillin to the affected areas during electrophoresis, as this ensures penetration of the drug into the tissue.Electrophoresis with Eufillin is used in the following cases:
- Osteochondrosis;
- Arthrosis and arthritis of various joints;
- Chronical bronchitis;
- Cerebrovascular accident;
- Increased intracranial pressure;
- Hypertonicity or hypotonicity of muscles in children;
- Dysplasia of the femoral head in infants;
- Long-term non-closure of the fontanel in infants;
- Nerve lesions in adults (eg, facial nerve).
Instructions for use
Let's consider the various nuances of using Eufillin tablets and solutions separately to avoid confusion.Eufillin tablets - instructions for use
The tablets should be taken after meals, swallowed whole and washed down with a small amount of water (half a glass is enough). If necessary (for example, if you have difficulty swallowing), the tablet can be broken into halves or quarters and swallowed one after another. To treat bronchospasm, adults need to take Eufillin 150 mg (1 tablet) 2 to 3 times a day. For children, the dosage of tablets is calculated individually based on body weight, based on the ratio of 7 – 10 mg per 1 kg of weight. The amount of Eufillin calculated in this way is divided into 4 doses. For example, a child weighing 20 kg needs to take 10 * 20 = 200 mg of Euphyllin per day. This amount - 200 mg should be divided into 4 doses - 200/4 = 50 mg. Thus, a child weighing 20 kg should take 50 mg (1/3 tablet) of Euphyllin 4 times a day.
The maximum permissible single dose of Eufillin for adults is 500 mg (3.3 tablets), and the daily dose is 1500 mg (10 tablets). For children, the highest single dosage is 10 mg per 1 kg, and the daily dosage is 15 mg per 1 kg.
The duration of therapy with Eufillin is determined individual characteristics body and the rate of normalization of the condition. So, for some people, to relieve bronchospasm, it is enough to take Eufillin for several days, while others will have to take the drug for 2 to 5 months in a row. The duration of treatment is determined by the attending physician, who knows the person’s medical history, is aware of his reactions to drugs, the individual rate of normalization of the condition and the decrease in bronchial smooth muscle tone.
If a person takes Eufillin on his own, then it is necessary to stop therapy no earlier than 4 to 5 days after complete relaxation of the bronchi has occurred, which is manifested in ease of breathing.
In addition to the indicated regimen for using Eufillin tablets, which implies independent treatment, which initially consisted of taking the drug orally, there is also the option of maintenance therapy. This maintenance therapy consists of a course of use of Eufillin tablets after relief of an acute condition using intravenous injections of a solution of the same drug. Maintenance therapy with Eufillin is aimed at maintaining the results achieved by injections, as well as achieving stable remission and preventing repeated episodes of severe, life-threatening bronchospasm.
Maintenance therapy begins with taking the minimum dosage of Eufillin tablets, which can be increased by 25% every three days, until the maximum allowable amount of drug use is reached. The duration of therapy is determined by the rate of onset of stable remission with the absence of episodes of bronchospasm.
So, for adults, the minimum maintenance dosage is as follows – 1 tablet every 6 hours (that is, take 1 tablet 4 times a day). After three days, the dosage can be increased by 25%, that is, by 1 tablet and take not 4, but 5 tablets per day. This fifth tablet can be divided into four parts and taken 1 + 1/4 tablets 4 times a day. But you can take one additional tablet as a whole in one of four daily doses. For example, take 2 tablets at once in the morning, and one tablet at a time during the remaining three doses. The maximum daily dosage for adults for maintenance treatment is 900 mg, which corresponds to 6 tablets.
For children, the initial dosage of maintenance therapy is calculated based on body weight at a ratio of 16 mg per 1 kg. The calculated amount of the drug is divided into 3 to 4 doses per day. If necessary, as for adults, every 3 days you can increase the daily dosage by 25% until the maximum permissible values are reached. The maximum daily dosage for maintenance treatment in children is determined by age and is as follows:
- Children under 1 year– dosage is calculated using the formula: 0.3*age in weeks + 8;
- Children 1 – 9 years old– the maximum permissible daily dosage is 22 mg per 1 kg;
- Children 9 – 12 years old– 20 mg per 1 kg;
- Children 12 – 16 years old– 18 mg per 1 kg.
- Children from 0 to 6 months – dosage is calculated using the formula: 0.07 * age in weeks + 1.7. The calculated amount of Euphyllin is given to the child every 8 hours (3 times a day).
- Children 6 – 12 months – calculated using the formula: 0.05*age in weeks + 1.25. The calculated amount of the drug is given to the child every 6 hours (4 times a day).
- Children 1 – 9 years old– 5 mg per 1 kg every 6 hours.
- Children 9 – 12 years old
- Children 12 – 16 years old
- Adults who do not smoke or have liver disease – 3 mg per 1 kg every 6 hours.
- Adults smoking – 4 mg per 1 kg every 6 hours.
- Adults with liver disease – 2 mg per 1 kg every 8 hours.
Eufillin ampoules - instructions for use
The ampoules may contain a solution of Eufillin of different concentrations, intended, respectively, for intravenous or intramuscular administration. If the ampoule indicates a concentration of 2.4% or 2%, then this is a solution for intravenous administration. And if the concentration of the solution is 24%, then it is intended for intramuscular administration. That is, the difference in the concentration of solutions for intravenous and intramuscular injections is 10 times. These solutions are not interchangeable, so before performing an injection you should always look carefully at the ampoule and read the concentration of this particular drug. Intravenous administration of Eufillin is used only in emergency conditions, when it is necessary to quickly relieve life-threatening bronchospasm. When the acute condition is relieved, they switch to maintenance use of Eufillin tablets or intramuscular injections. Wherein the best option are tablets, and intramuscular injections are used only in cases where a person for some reason cannot take tablets orally (for example, stomach diseases, etc.). However, at the first opportunity it is recommended to switch from intramuscular injections to taking tablets.
So, in acute emergency conditions, Eufillin is administered intravenously (a “dropper” is placed). The dosage is calculated or determined individually depending on the age and weight of the person:
- Adults and teenagers over 16 years of age – 6 mg per 1 kg of weight;
- Infants up to 3 months – administer 30–60 mg per day;
- Children 4 – 12 months – administer 60–90 mg per day;
- Children 2 – 3 years old– administer 90–120 mg per day;
- Children 4 – 7 years old– administer 120–140 mg per day;
- Children 8 – 16 years old– administer 250–500 mg per day.
For status asthmaticus, regardless of weight, 720–750 mg of Eufillin is administered intravenously (30–32 ml of solution from ampoules is diluted in 250 ml of physiological solution) for 1–2 hours.
Intramuscularly at various states For adults, Eufillin is administered at 100–500 mg per day, and for children, the dosage is calculated individually according to the ratio of 15 mg per 1 kg. Moreover, the daily dosage is divided into 3 - 4 equal parts and, accordingly, 3 - 4 injections are given per day.
Intramuscular and intravenous use of Eufillin should be as short as possible, and at the first opportunity it is necessary to switch to taking tablets. The maximum permissible duration of injection administration of Eufillin solutions is 14 days.
Gynecologists prescribe Eufillin in the complex treatment of gestosis and edema in pregnant women, placental insufficiency, as well as other conditions that require immediate use of the drug due to a threat to the life of the mother. Thus, Eufillin is not a completely safe drug, but the degree of its “harmlessness” is quite sufficient for use during pregnancy if indicated.
Therefore, if a doctor has prescribed Eufillin to a pregnant woman, she can take it, strictly observing the prescribed dosage and duration of therapy. But if any signs that worry a woman appear, you should not use the drug on your own.
Eufillin for children
For children under 3 months of age, Eufillin in injections and tablets is prescribed only for health reasons. Even at older ages, intravenous and intramuscular injections of the drug are carried out only in emergency conditions, since Eufillin has a pronounced effect on the child’s cardiovascular system, as a result of which, after each administration of the solution, the baby should be under the supervision of a doctor.And at older ages, tablets are quite widely used in the practice of pediatricians, who prescribe them for the treatment of bronchospasms, which often develop in children suffering from bronchitis. In tablet form, this is the main use of Eufillin. However, pediatricians for the treatment of bronchitis prefer to prescribe Eufillin not in tablets, but in the form of inhalations, for the production of which a 2.4% solution is used.
In infancy (up to one year), Eufillin is used to relieve muscle hypertonicity, reduce intracranial pressure, and also to eliminate developmental delays associated with cerebrovascular accidents. However, in infants, Eufillin is used, as a rule, during the physiotherapeutic procedure of electrophoresis, since it allows the medicine to be administered directly to the areas where it is needed. That is, administration of the drug during electrophoresis allows one to avoid pronounced systemic effects on blood vessels, bronchi, bile ducts and kidneys, as well as possible irritation of the stomach and intestines, and at the same time create the necessary concentration of Euphyllin in the affected tissues.
Dosages of aminophylline for electrophoresis, inhalation and oral administration are determined by the doctor. Typically, the dosage of Eufillin tablets for a child is calculated according to the ratio of 7–10 mg per 1 kg, after which the resulting value is divided into 3–4 doses per day.
Use for cough
Eufillin expands the bronchi, as a result of which sputum is more easily removed, and a person can breathe normally without whistling, wheezing and painful coughing attacks. If an adult or child is not bothered by attacks of painful coughing, during which he literally suffocates, then there is no need to use Eufillin. In such situations, expectorant medications are quite sufficient. But if an adult or child coughs heavily and painfully, he develops entire attacks that prevent him from breathing and literally has a suffocating effect, then it is recommended to take Eufillin 3 times a day. Adults are recommended to take 1 tablet, and children – 1/4 - 1/3 tablet. As the cough decreases, you should switch to taking only one dose of Eufillin (1 tablet for adults and 1/4 - 1/3 for children) at night so that you can sleep peacefully without coughing attacks, which quite often occur with transition from vertical to horizontal position. A minimum of 6-hour interval should be maintained between taking tablets.
For the purpose of a speedy recovery, 10–15 minutes after taking the Eufillin tablet, it is recommended to inhale ordinary mineral water or saline solution. This will speed up the removal of sputum and, accordingly, the recovery process will be faster.
Eufillin for inhalation
Inhalations with Eufillin are prescribed for obstructive bronchitis, since the drug dilates the bronchi, relieving spasm, and facilitates the removal of sputum. However, the drug has all these effects only once it enters the systemic bloodstream, that is, when taken orally or by injection.Inhalation use of Eufillin belongs to the category of so-called off-label-prescription, that is, use not according to instructions. Unfortunately, such inhalations are used quite widely, although their effectiveness is very low, since when it comes into contact with the mucous membrane, Eufillin has practically no significant effect. After all, to achieve a therapeutic effect, the drug must reach the blood.
In such situations, relaxation of the bronchi and removal of mucus occurs due to the fact that water vapor enters the respiratory tract during inhalation. That is, inhalation with Eufillin is comparable in effectiveness to inhalation with plain water. Therefore, in order to treat obstructive bronchitis or relieve an attack of suffocation, it is not recommended to use inhalations with Eufillin.
Electrophoresis with Eufillin (infants, children, adults)
Electrophoresis with Eufillin in people of any age is carried out to relieve muscle hypertonicity, reduce intracranial pressure, treat hip dysplasia, osteochondrosis and arthrosis. In other words, electrophoresis with Eufillin is recommended for conditions when it is necessary to increase blood flow in a particular area. For example, with hypertonicity of the legs, Eufillin electrophoresis is performed on the lumbar region, with increased intracranial pressure or cerebral circulatory failure - on the cervical vertebrae, etc. This physiotherapeutic procedure allows you to create a concentration of the drug directly in the affected tissues, due to which it acts locally without causing systemic effects. It is precisely due to the absence of these systemic effects that electrophoresis with Eufillin can be used in
Catad_pgroup Antiasthmatic drugs
Eufillin solution - instructions for use
INSTRUCTIONS medical use drug
Registration number:
Tradename:
Eufillin
INN:
AminophyllineDosage form:
solution for intravenous administration
Compound:
1 ml contains:Active substance:
aminophylline for injection (aminophylline) - 24.0 mg;
Excipient:
water for injection - up to 1 ml
Description:
clear, colorless or slightly colored liquidPharmacotherapeutic group:
bronchodilatorATX Code:
R03DA05Pharmacological properties
Pharmacodynamics
The drug inhibits phosphodiesterase, increases the accumulation of cyclic adenosine monophosphate in tissues, blocks adenosine (purine) receptors, reduces the flow of calcium ions through cell membrane channels, and 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 the strength and frequency 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 lowers pressure in the pulmonary circulation. Increases renal blood flow, enhances the release of adrenaline by the adrenal glands. Has a moderate diuretic effect. Expands extrahepatic biliary tract. Inhibits platelet aggregation (suppresses platelet activating factor and prostaglandin E2 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
Bioavailability of the drug is 90-100%.
The maximum concentration (7 mcg/ml) with intravenous administration of 300 mg is achieved after 15 minutes.
The volume of distribution is in the range of 300-700 ml/kg (30-70% of “ideal” body weight), with an average of 450 ml/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 blood 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 in the body occurs (up to 30% of that for aminophylline).
In children over 3 years of age and in adults, the phenomenon of caffeine accumulation is absent.
The half-life in newborns and children under 6 months is 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, normalization of pharmacokinetics occurs for 3-4 months); in adults with chronic obstructive pulmonary disease (COPD), 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 liver enzymes.
Indications for use:
Broncho-obstructive syndrome of any origin: bronchial asthma (the drug of choice in patients with bronchial asthma of physical exertion and as an additional remedy for other forms), chronic obstructive pulmonary disease, emphysema, chronic obstructive bronchitis, hypertension in the pulmonary circulation, night apnea. Ischemic cerebrovascular accident (as part of combination therapy to reduce intracranial pressure).Left ventricular heart failure (as part of complex therapy).
Contraindications
Hypersensitivity to the drug, as well as to xanthine derivatives: caffeine, pentoxifylline, theobromine. Severe arterial hypotension or hypertension, paroxysmal tachycardia, extrasystole, myocardial infarction with cardiac arrhythmias, epilepsy, increased convulsive readiness, hypertrophic obstructive cardiomyopathy, thyrotoxicosis, pulmonary edema, severe coronary insufficiency, hepatic and/or renal failure, hemorrhagic stroke, retinal hemorrhage eyes, recent history of bleeding.Carefully
Sepsis, peptic ulcer of the stomach and duodenum (history), old age (over 55 years), uncontrolled hypothyroidism (possibility of cumulation), widespread vascular atherosclerosis, prostatic hyperplasia, children under 14 years of age (due to possible side effects).
Pregnancy and lactation
If it is necessary to use the drug during pregnancy, the expected benefit to the mother should be compared with the potential risk to the fetus.If it is necessary to use the drug during breastfeeding, breastfeeding should be discontinued.
Directions for use and doses
Method of administration: intravenously.Adults are administered slowly (over 4-6 minutes) 5-10 ml of the drug (0.12-0.24 g), which is pre-diluted in 10-20 ml of 0.9% sodium chloride solution.
If a feeling of palpitations, dizziness, or nausea occurs, the rate of administration is slowed down or switched to drip administration, for which 10-20 ml of the drug (0.24-0.48 g) is diluted in 100-150 ml of 0.9% sodium chloride solution; administered at a rate of 30-50 drops per minute.
Before parenteral administration, the solution must be warmed to body temperature. Aminophylline is administered parenterally up to 3 times a day, for no more than 14 days. Higher doses of aminophylline for adults when administered intravenously: single - 0.25 g, daily - 0.5 g.
If necessary, children are administered aminophylline intravenously by drip at a single dose of 2-3 mg/kg. Higher doses for children with intravenous administration: single - 3 mg/kg, daily - at the age of up to 3 months - 0.03-0.06 g, from 4 to 12 months - 0.06-0.09 g, from 2 to 3 years - 0.09-0.12 g, from 4 to 7 years - 0.12-0.24 g, from 8 to 18 years - 0.25-0.5 g.
Side effect
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 peptic ulcer, diarrhea, with long-term use - decreased appetite.
Allergic reactions: skin rash, skin itching, exfoliative dermatitis, fever.
Others: chest pain, tachypnea, feeling of “hot flashes” in the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.
Side effects decrease when the dose of the drug is reduced, when the method of administration is changed (from jet to drip).
Local reactions: compaction, hyperemia, pain at the injection site.
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 convulsions 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, forced diuresis, hemosorption, plasma sorption, hemodialysis (low efficiency, peritoneal dialysis is ineffective), symptomatic therapy (including intravenous metoclopramide for vomiting). If convulsions occur, maintain airway patency and administer oxygen therapy. To relieve seizures, administer diazepam 0.1-0.3 mg/kg intravenously (but not more than 10 mg).
Interaction with other drugs
Pharmaceutically incompatible with acid solutions.Increases the likelihood of developing side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), drugs for general anesthesia (increases the risk of ventricular arrhythmias), drugs that excite the central nervous system. nervous system(increases neurotoxicity).
Antidiarrheal drugs and oral estrogen-containing contraceptives weaken the effect of aminophylline (they bind to the cytochrome P450 enzymatic system and change the metabolism of aminophylline).
Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine and moracizine, being inducers of microsomal oxidation, increase the clearance of aminophylline, which may require an increase in its dose.
When used simultaneously with macrolide antibiotics, lincomycin, allopurinol, cimetidine, isoprenaline, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon alpha, 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.
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.
Prescribe with caution simultaneously with anticoagulants.
special instructions
Use caution when consuming large amounts of caffeine-containing foods or drinks during treatment.Before use, the drug solution must be warmed to body temperature.
Effect on ability to drive vehicles, mechanisms and engaging in other activities that require concentration and speed of psychomotor reactions.
During treatment with the drug, it is not recommended to drive vehicles, machinery, or engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Release form:
Solution for intravenous administration 24 mg/ml.5 or 10 ml in neutral glass ampoules. 10 ampoules each along with instructions for use and an ampoule scarifier in a cardboard box.
5 ampoules per blister pack. 2 blister packs each, along with instructions for use and an ampoule scarifier in a cardboard pack.
When using ampoules with a notch, a point or a break ring, do not insert a scarifier.
Storage conditions:
In a place protected from light at a temperature of 2 to 25 ° C.Keep out of the reach of children.
Best before date:
3 years.Do not use after the expiration date stated on the package.
Vacation conditions
Prescription release.Manufacturer's address/
Organization accepting complaints:
st. Bolshiye Kamenschiki, 9, Moscow, 115172
Place of production
JSC "Moskhimfarmpreparaty" named after. N.A. Semashko"
1. st. Sergius of Radonezh, 15-17, Moscow. 107120;
2. st. B. Kamenshchiki, 9, Moscow. 115172.
In this article you can read the instructions for use of the drug Eufillin. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Eufillin in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Eufillin in the presence of existing structural analogues. Use for the treatment of status asthmaticus and bronchial obstruction in adults, children, as well as during pregnancy and lactation.
Eufillin- bronchodilator, xanthine derivative. Inhibits phosphodiesterase, increases the accumulation of cyclic adenosine monophosphate in tissues, blocks adenosine (purine) receptors; reduces the flow of calcium ions through the channels of cell membranes, reduces the contractile activity of smooth muscles.
Relaxes the bronchial muscles, increases mucociliary clearance, stimulates contraction of the diaphragm, improves the function of the respiratory and intercostal muscles, stimulates the respiratory center, increases its sensitivity to carbon dioxide and improves alveolar ventilation, which ultimately leads to a decrease in the severity and frequency of apnea episodes. By normalizing respiratory function, it helps saturate the blood with oxygen and reduce the concentration of carbon dioxide.
It has a stimulating effect on the activity of the heart, increases the strength and number of heart contractions, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly those of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, and reduces pressure in the pulmonary circulation. Increases renal blood flow and has a moderate diuretic effect.
Expands extrahepatic bile ducts.
Inhibits platelet aggregation (suppresses platelet activating factor and PgE2 alpha), increases the resistance of red blood cells to deformation (improves the rheological properties of blood), reduces thrombus formation and normalizes microcirculation.
It has a tocolytic effect, increases the acidity of gastric juice.
When used in large doses, it has an enileptogenic effect.
Pharmacokinetics
In the body, aminophylline (the active substance of the drug Euphyllin) is metabolized at physiological pH values with the release of free theophylline. Bronchodilating properties appear at plasma theophylline concentrations of 10-20 mcg/ml. Concentrations above 20 mg/ml are toxic. The stimulating effect on the respiratory center is realized at a lower concentration - 5-10 mcg/ml. Penetrates the placental barrier (the concentration in the fetal blood serum is slightly higher than in the maternal serum). Stands out with breast milk. 10% is excreted unchanged in adults. In newborns, a significant portion is excreted in the form of caffeine (due to the immaturity of the pathways for its further metabolism), unchanged - 50%.
Indications
- status asthmaticus (additional therapy);
- apnea of newborns;
- ischemic cerebrovascular accident (as part of combination therapy);
- left ventricular failure with bronchospasm and Cheyne-Stokes type breathing disorder;
- edematous syndrome of renal origin (as part of complex therapy);
- acute and chronic heart failure (as part of combination therapy);
- broncho-obstructive syndrome of various origins (including bronchial asthma, COPD, including pulmonary emphysema, chronic obstructive bronchitis);
- hypertension in the pulmonary circulation;
- "pulmonary" heart;
- night apnea.
Release forms
Tablets 150 mg.
Solution for intravenous administration 24 mg/ml (injections in ampoules, in droppers).
Solution for intramuscular administration 240 mg/ml (injections in injection ampoules).
Instructions for use and dosage
Pills
Orally, adults should be prescribed 150 mg per dose 1-3 times a day after meals. Children should be prescribed orally at the rate of 7-10 mg/kg per day in 4 divided doses. The duration of the course of treatment is from several days to several months, depending on the course of the disease and tolerability of the drug.
Higher doses of aminophylline for adults orally: single - 0.5 g, daily - 1.5 g. Higher doses for children orally: single - 7 mg/kg, daily - 15 mg/kg.
Injection
Individual, depending on the indications, age, clinical situation, route and scheme of administration (intravenously, intramuscularly, through a drip), nicotine addiction.
Side effect
- dizziness;
- headache;
- insomnia;
- excitation;
- anxiety;
- irritability;
- tremor;
- heartbeat;
- tachycardia (including in the fetus when taken by a pregnant woman in the 3rd trimester);
- chest pain;
- decreased blood pressure;
- abdominal pain;
- nausea, vomiting;
- heartburn;
- exacerbation of peptic ulcer;
- diarrhea;
- decreased appetite;
- skin rash;
- fever;
- feeling of flushing in the face;
- hematuria;
- increased diuresis;
- increased sweating.
Contraindications
- hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine);
- epilepsy;
- peptic ulcer of the stomach and duodenum (in the acute stage);
- gastritis with high acidity;
- severe arterial hyper- or hypotension;
- tachyarrhythmias;
- hemorrhagic stroke;
- retinal hemorrhage;
- children's age (up to 3 years).
Use during pregnancy and breastfeeding
Be careful during pregnancy and lactation.
special instructions
Use caution when consuming large amounts of caffeine-containing foods or drinks during treatment.
Impact on the ability to drive vehicles and operate machinery
It is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Drug interactions
Increases the likelihood of developing side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), general anesthesia (increases the risk of ventricular arrhythmias), xanthines and drugs that excite the central nervous system (increases neurotoxicity), beta-agonists.
Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline.
Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracizine, being inducers of microsomal liver enzymes, increase the clearance of aminophylline, which may require an increase in its dose.
With the simultaneous use of macrolides with antibiotics, lincomicin, allopurinol, tsimetidine, isoprenaline, ennoxacin, small doses of ethanol (alcohol), disulfiram, fluoroquinolones, recombinant interferon-alpha, methotrexate, propaphenone, thiabendazol, sore thylopidisol, sore thylopidisol, sore thylopidisol, sore thylopidisol, sore thylopidisol Verapamil and when vaccinating against influenza the intensity of action of Eufillin may increase, which may require a reduction in its dose.
Enhances the effect of beta-adrenergic stimulants and diuretics (including by increasing glomerular filtration), reduces the effectiveness of lithium preparations and beta-blockers. Compatible with antispasmodics, do not use in combination with other xanthine derivatives.
Analogues of the drug Eufillin
Structural analogues of the active substance:
- Aminophylline;
- Aminophylline-Eskom;
- Eufillin-Darnitsa;
- Eufillin solution for injection 2.4%;
- Eufillin injection solution 24%.
If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.
