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Euphyllin - a bronchodilator, PDE inhibitor. It is theophylline ethylene diamine salt (which facilitates solubility and increases absorption). It has a bronchodilator effect, apparently due to a direct relaxing effect on the smooth muscles of the respiratory tract and blood vessels of the lungs. It is believed that this action is caused by the selective inhibition of the activity of specific PDEs, which leads to an increase in the intracellular concentration of cAMP. The results of experimental studies in vitro show that the main role seems to be played by isoenzymes of types III and IV. Suppression of the activity of these isoenzymes may also cause some side effects of aminophylline (theophylline), including vomiting, hypotension and tachycardia. Blocks adenosine (purine) receptors, which may be one of the factors of action on the bronchi.
Reduces airway hyperreactivity associated with the late phase of the reaction caused by inhalation of allergens through an unknown mechanism that does not relate to the inhibition of PDE or to the blockade of adenosine action. There are reports that aminophylline increases the number and activity of T-suppressors in peripheral blood.
It 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 episodes of apnea. Normalizing the respiratory function, helps to saturate the blood with oxygen and reduce the concentration of carbon dioxide. Strengthens ventilation of the lungs in the conditions of a hypokalemia.
It has a stimulating effect on heart activity, increases strength and heart rate, increases coronary blood flow and increases myocardial oxygen demand. Reduces the tone of blood vessels (mainly vessels of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, lowers the pressure in the pulmonary circulation. Increases renal blood flow, has a moderate diuretic effect. Expands extrahepatic biliary tract. Stabilizes the membranes of mast cells, inhibits the release of mediators of allergic reactions. It inhibits platelet aggregation (inhibits platelet activating factor and PgE2α), increases erythrocyte resistance to deformation (improves blood rheology), reduces blood clot formation and normalizes microcirculation. It has a tocolytic effect, increases the acidity of gastric juice. In high doses, it has an epileptogenic effect.
In the body, aminophylline is metabolized at physiological pH values with the release of free theophylline. Bronchodilating properties appear at plasma concentrations of theophylline 10–20 mcg / ml. Concentration over 20 mg / ml is toxic. The stimulating effect on the respiratory center is realized at a lower concentration - 5-10 μg / ml.
Binding of theophylline to plasma proteins is approximately 40%; in newborns, as well as in adults with diseases, the binding is reduced. Plasma protein binding is about 60% in adults, 36% in newborns, and 36% in patients with liver cirrhosis. Gets through a placental barrier (concentration in blood serum of a fruit is slightly higher, than in serum of mother). It is excreted in breast milk.
Theophylline is metabolized in the liver with the participation of several cytochrome P450 isoenzymes, the most important of which is CYP1A2. In the process of metabolism 1,3-dimethyl uric acid, 1-methyl uric acid and 3 methylxanthine are formed. These metabolites are excreted in the urine. Unchanged in adults is 10%. In newborns, a significant part is excreted in the form of caffeine (due to the immaturity of the pathways of its further metabolism), unchanged - 50%.
Significant individual differences in the rate of hepatic metabolism of theophylline are the reason for the pronounced variability of clearance values, plasma concentrations, and half-life. The hepatic metabolism is influenced by such factors as age, addiction to tobacco smoking, diet, diseases, simultaneously conducted drug therapy.
T1 / 2 of theophylline in non-smoking patients with asthma with virtually no pathological changes from other organs and systems is 6-12 hours, in smokers - 4-5 hours, in children - 1-5 hours, in newborns and premature babies - 10- 45 hours
Theophylline T1 / 2 is increased in the elderly and in patients with heart failure or liver disease.
Clearance decreases with heart failure, abnormal liver function, chronic alcoholism, pulmonary edema, chronic obstructive pulmonary disease.
Ethylenediamine does not affect theophylline pharmacokinetics.
- asthmatic status (adjunctive therapy),
- newborn apnea,
- violation of cerebral circulation in ischemic type (as part of combination therapy),
- left ventricular failure with bronchospasm and Cheyne-Stokes-type breathing disorder,
- edematous syndrome of renal genesis (as part of complex therapy);
- acute and chronic heart failure (as part of combination therapy).
1 mlintravenous solution contains:
active substance: aminophylline 24 mg.
Aminophylline is marketed under different brands and generic names, and comes in different dosage forms:
|Brand name||Manufacturer||Country||Dosage form|
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Dosage and Administration
The dose of the drug is set individually.
If necessary, the dose of the drug can be increased with an interval of 2-3 days to achieve the optimal therapeutic effect.
Duration of treatment from several days to several months.
Intravenous administration of the drug should be carried out carefully and slowly, at least for 5 minutes. The dose of the drug is chosen individually, given the possibility of different rates of excretion in different patients.
From the side of the central nervous system: dizziness, sleep disturbance, anxiety, tremor, convulsions.
Since the cardiovascular system: feeling of heartbeat, disturbances of a heart rhythm; with rapid on / in the introduction - the appearance of pain in the heart, lowering blood pressure, tachycardia (including the fetus when taken in the third trimester of pregnancy), arrhythmias, blood pressure reduction, cardialgia, an increase in the frequency of angina attacks.
From the digestive system: nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea; with prolonged ingestion - anorexia.
From the urinary system: albuminuria, hematuria.
Allergic reactions: skin rash, itching, fever.
Metabolism: rarely - hypoglycemia.
Local reactions: induration, hyperemia, soreness at the injection site; with rectal use, irritation of the rectal mucosa, proctitis.
Other: chest pain, tachypnea, sensation of hot flashes to the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.
- hypersensitivity to aminophylline and theophylline.
- severe hypertension or hypotension,
- stomach ulcer and duodenal ulcer in the acute phase,
- hyperacid gastritis,
- severe violations of the liver and / or kidneys,
- hemorrhagic stroke,
- retinal hemorrhage
- simultaneous use with ephedrine in children
- children's age (up to 12 years).
With simultaneous use with sympathomimetics, mutual reinforcement of action occurs; with beta-blockers and lithium preparations - the action is mutually reduced. The intensity of the action of aminophylline may decrease (due to an increase in its clearance), while being used with phenobarbital, rifampicin, isoniazid, carbamazepine, sulfinpyrazone, phenytoin, and also in smokers.
The intensity of the action of aminophylline can increase (due to a decrease in its clearance) with simultaneous use with macrolide antibiotics, lincomycin, quinolones, allopurinol, beta-adrenergic blockers, cimetidine, disulfiram, fluvoxamine, hormonal contraceptives for inhalation, ioprenylamino, hormonal contraceptives for inhalation, ipoprostinamine, hormonal contraceptives for inhalation, ioprenamide, hormonal contraceptives, for example, for example, for example, for adherents the flu.
Xanthine derivatives can potentiate hypokalemia caused by the action of β2-adrenoreceptor stimulants, corticosteroids and diuretics.
Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline.
Pharmaceutically incompatible with acid solutions.
Pregnancy and Lactation
Theophylline penetrates the placental barrier. The use of aminophylline during pregnancy can lead to the creation of potentially dangerous concentrations of theophylline and caffeine in the plasma of the newborn. Newborns whose mothers were given aminophylline during pregnancy (especially in trimester III) need medical supervision to control the possible symptoms of theophylline intoxication.
Theophylline is excreted in breast milk. When aminophylline is used in a nursing mother during lactation, irritability of the baby may occur.
Thus, the use of aminophylline during pregnancy and lactation (breastfeeding) is possible in cases where the intended benefit of therapy for the mother outweighs the potential risk to the fetus or child.
Use with caution in severe coronary insufficiency (acute phase of myocardial infarction, angina), advanced atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased convulsive readiness, in case of hepatic and / or renal failure, ulcers of the stomach and increased congestion, in case of hepatic and / or renal failure, ulcers of the stomach and increased congestion, in case of hepatic and / or renal failure, ulcers of the stomach and increased congestion, in case of hepatic and / or renal failure, ulcers of the stomach and increased congestion, in case of hepatic and / or renal insufficiency, ulcers of the stomach, and increased convulsive readiness, in case of hepatic and / or renal insufficiency, gastric ulcer, and increased convulsive readiness, in case of hepatic and / or renal insufficiency, ulcers of the stomach and increased congestion, in case of hepatic and / or renal insufficiency, gastric ulcer, and increased convulsive readiness; with recent bleeding from the gastrointestinal tract, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, with prolonged hyperthermia, gastroesophageal At reflux, prostatic hypertrophy, in patients in the elderly, in children (especially orally).
Correction of the dosing regimen of aminophylline may be required for heart failure, abnormal liver function, chronic alcoholism, fever, acute respiratory disease.
Elderly patients may require a dose reduction.
When replacing the used dosage form of aminophylline with another, clinical observation and control of theophylline concentration in the blood plasma is necessary.
Aminophylline is not used simultaneously with other xanthine derivatives. During treatment, you should avoid eating foods containing xanthine derivatives (strong coffee, tea).
With caution used simultaneously with anticoagulants, with other derivatives of theophylline or purine.
Avoid simultaneous use with beta-blockers.
Aminophylline should not be used simultaneously with glucose solution.
In case of overdose observed facial flushing, insomnia, motor agitation, anxiety, photophobia, anorexia, diarrhea, nausea, vomiting, epigastric pain, gastrointestinal bleeding, tachycardia, ventricular arrhythmias, tremors, generalized convulsions, hyperventilation, a sharp drop in blood pressure . In severe poisoning, epileptoid seizures may develop (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, skeletal muscle necrosis, confusion, renal failure with myoglobinuria.
Treatment of overdose depends on the clinical picture, includes the abolition of the drug, stimulation of its removal from the body (forced diuresis, hemosorption, plasma sorption, hemodialysis, peritoneal dialysis) and the appointment of symptomatic agents. Diazepam (injections) is used to relieve seizures. Do not use barbiturates. In severe intoxication (eufillin content more than 50 g / l) hemodialysis is recommended.
- Brand name: Euphyllin for injections
- Active ingredient: Aminophylline
- Dosage form: Solution for intravenous administration.
- Manufacturer: Novosibkhimpharm
- Country of Origin: Russia
- Treatment of acute cerebral ischemia with intravenous aminophylline
- Combined treatment with terbutaline and aminophylline inhibits experimental amyloidosis in mice
- Studies on aminophylline disposition I. A rapid and sensitive HPLC assay for ethylenediamine in plasma and urine
- Effects of water deprivation on the pharmacokinetics of theophylline and one of its metabolites, 1,3-dimethyluric acid, after intravenous and oral administration of aminophylline to rats
- Lack of interaction of MDL 257 and isoproterenol: Comparison with aminophylline
- Effects of BRL38227, salbutamol, and aminophylline, alone and in combination, on plasma potassium and on the heart
- Intravenous aminophylline for acute severe asthma in children over two years receiving inhaled bronchodilators
- Summary of ‘Intravenous aminophylline for acute severe asthma in children over two years receiving inhaled bronchodilators’
- Commentary on ‘Intravenous aminophylline for acute severe asthma in children over two years receiving inhaled bronchodilators’
- Application of absorbancy ratios to the analysis of pharmaceuticals III. Simultaneous analysis of aminophylline and phenobarbital
- Nonaqueous titrimetric analysis of aminophylline
- Determination of aminophylline and phenobarbital combinations
- Effect of some nonionic surfactants on the rate of absorption of aminophylline from suppositories in rabbits
- UV spectrophotometric determination of aminophylline, amobarbital, and ephedrine hydrochloride in an antiasthma capsule preparation
- Decomposition of aminophylline in suppository formulations
- Ion-pair high-performance liquid chromatography of terbutaline and catecholamines with aminophylline in intravenous solutions
- Preparation of spherically agglomerated crystals of aminophylline
- Estimation of theophylline clearance during intravenous aminophylline infusions
- Circadian rhythm in theophylline disposition during a constant-rate intravenous infusion of aminophylline in the dog
- Preliminary evaluation of the correlation between in vitro release and in vivo bioavailability of two aminophylline slow-release tablets
- The potentiometric titration of aminophylline and aminophylline-phenobarbital mixtures
- Notes on the determination of theophylline, alone and in combinations, by the U. S. P. aminophylline method
- Assay of aminophylline-vinbarbital solutions
- Reversal of neurologic disturbances related to high-dose methotrexate by aminophylline