Active substanceAminophyllineAminophylline
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  • Dosage form: & nbspsolution for intravenous administration
    Composition:

    Active substance:

    aminophylline 24.0 mg or theophylline 19.2 mg and ethylenediamine 4.8 mg

    Excipient: water for injection up to 1 ml.

    Description:transparent colorless or slightly colored liquid.
    Pharmacotherapeutic group:bronchodilator.
    ATX: & nbsp

    R.03.D.A.05   Aminophylline

    Pharmacodynamics:

    Bronchodilator, derivative, purine; inhibits phosphodiesterase, increases accumulation in cAMP 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 muscles of the bronchi, increases mucociliary clearance, stimulates the 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 reduces the severity and frequency of episodes of apnea.Normalizing the respiratory function, contributes to the saturation of blood oxygen and reduce the concentration of carbon dioxide.

    Strengthens lung ventilation in hypokalemia.

    Has a stimulating effect on the activity of the heart, increases the strength and heart rate, increases coronary blood flow and the need for myocardium in oxygen. Reduces the tone of blood vessels (mainly vessels of the brain, skin and kidneys). Has peripheral venodilating effect, reduces pulmonary vascular resistance, lowers pressure in the "small" circle of blood circulation. Increases renal blood flow, has a moderate diuretic effect.

    Expands extrahepatic biliary tract.

    Stabilizes the membranes of mast cells, inhibits the release of mediators of allergic reactions.

    It inhibits platelet aggregation (suppresses the platelet activation factor and PgE2 alpha), increases the resistance of erythrocytes to deformation (improves the rheological properties of the blood), reduces thrombus formation and normalizes microcirculation. Has tocolytic effect, increases the acidity of gastric juice.

    When used in large doses has an epileptogenic effect.

    Pharmacokinetics:

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

    Bronchodilator properties aminophylline shows in concentrations of 10-20 μg / ml. Concentration above 20 mg / ml is toxic. Exciting effect on the respiratory center is realized with a lower content of the drug in the blood - 5-10 μg / 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-dimethylurea (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 amounts, with the exception of premature newborns and children younger than 6 months,in which, due to extremely long T1 / 2 caffeine, there is a significant accumulation in the body (up to 30% of that for aminophylline)

    In children older than 3 years and in adults, the phenomenon of caffeine cumulation is absent. Half-life in infants and children up to 6 months - more than 24 hours; in children older than 6 months - 3.7 hours; in adults - 8.7 hours; in "smokers" (20-40 cigarettes per day) - 4-5 hours (after quitting smoking, normalization of pharmacokinetics after 3-4 months); in adults with chronic obstructive pulmonary diseases, pulmonary heart disease and pulmonary heart disease - over 24 hours. It is excreted by the kidneys. In neonates, about 50% of theophylline is excreted unchanged in urine against 10% in adults, which is due to inadequate activity of liver enzymes.

    Indications:

    Asthmatic status (additional therapy), apnea of ​​newborns, cerebral blood flow disorder according to ischemic type (as part of combination therapy), left ventricular failure with bronchospasm and respiratory depression by the type of Cheyne-Stokes, edematous renal genesis (as part of complex therapy).

    Contraindications:

    Hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine), epilepsy, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, and bleeding in the retina of the eye.

    Carefully:

    Severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread atherosclerosis of vessels, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased convulsive alertness, hepatic and / or renal failure, peptic ulcer and duodenal ulcer (in the anamnesis), bleeding from gastrointestinal tract in a recent history, uncontrolled hypothyroidism (the possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, hyper trophism of the prostate gland, pregnancy, lactation, elderly age, children's age.

    Pregnancy and lactation:

    If it is necessary to prescribe the drug during pregnancy and lactation, it is necessary to compare the expected benefit to the mother and the potential risk to the fetus or newborn.

    Dosing and Administration:

    Adults:

    Intravenous slowly (for 4-6 minutes) for 5-10 ml of a 24 mg / ml solution (0.12-0.24 g) is slowly injected into the 10-20 ml isotonic sodium chloride solution.With the appearance of palpitations, dizziness, nausea, the rate of administration slows down or changes to drop introduction, for which 10-20 ml of a 24 mg / ml solution (0.24-0.48 g) is diluted in 100-150 ml of isotonic sodium chloride solution; injected at a rate of 30-50 drops per minute.

    Parenterally enter euphyllin up to 3 times a day, no more than 14 days.

    Higher doses of euphyllin for adults: single-dose 0.25 g, daily - 0.5 g.

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

    When asthmatic status is shown in / in the drip introduction - 720-750 mg.

    For children:

    if necessary, enter eufillin intravenously from the calculation of a single dose of 2-3 mg / kg, preferably drip.

    At the age of 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.

    Higher doses for children intravenously: single dose - 3 mg / kg, daily 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.

    The duration of parenteral administration is no more than 14 days.

    In apnea of ​​newborns, the initial dose (a condition characterized by periods of absence of breath for 15 seconds and accompanied by cyanosis and bradycardia) is 5 mg / kg (per nasogastric tube), maintaining a dose of 2 mg / kg in 2 divided doses. Duration of treatment is several weeks, in rare cases - months.

    You can prescribe rectally in the form of microclysters. The dose for adults is 0.24-0.48 g in 20-25 ml of warm water; children - less, according to age.

    Higher doses for adults rectally - single 0.5 g, daily 1.5 g; in / in - single 0.25 g, daily 0.5 g.

    Higher doses for children rectally - single 7 mg / kg, daily 15 mg / kg; in / in - single 3 mg / kg.

    Side effects:

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

    From the cardiovascular system: palpitations, tachycardia (including the fetus when taking a pregnant woman in the third trimester), arrhythmias, lowering blood pressure, 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 admission - a decrease in appetite.

    Allergic reactions: skin rash, skin itching, fever.

    Other: pain in the chest, tachypnea, sensation of hot flashes to the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

    Side effects decrease with a decrease in the dose of the drug.

    Local reactions: compaction, hyperemia, tenderness at the injection site.

    When rectal administration - proctitis, irritation of the mucous membrane of the rectum.

    Overdose:

    Symptoms: anorexia, diarrhea, nausea, vomiting, epigastric pain, gastrointestinal bleeding, tachycardia, ventricular arrhythmias, tremor, generalized convulsions, hyperventilation, a sharp drop in blood pressure are observed during an overdose.

    Treatment of overdose depends on the clinical picture, includes the abolition of the drug, stimulation of its removal from the body (forced diuresis, hemosorption, plasmosorption, hemodialysis, peritoneal dialysis) and the appointment of symptomatic agents. For cramping seizures applied diazepam (in injections). Do not use barbiturates. At the expressed intoxication (the maintenance of an eufillina more than 50 g / l) the hemodialysis is recommended.

    Interaction:

    Ephedrine, beta-adrenostimulators, caffeine and furosemide increase the effect of the drug. In combination with phenobarbital, diphenin, rifampicin, isoniazid, carbamazepine or sulfinpyrazone, a decrease in the efficacy of euphyllin is observed, which may require an increase in the applied doses of the drug.The clearance of the drug is reduced when it is administered in combination with antibiotics of the macrolide group, lincomycin, allopurinol, cimetidine, isoprenaline, beta-blockers, which may require a dose reduction. Oral estrogen-containing contraceptives, antidiarrheal drugs, intestinal sorbents weaken, and H2-histaminoblockers, slow calcium channel blockers, mexiletine intensify the action (bind to the enzymatic system of cytochrome P450 and slow the metabolism of aminophylline). When used in combination with enoxacin and other fluoroquinolines, the dose of euphyllin is reduced. The drug inhibits the therapeutic effects of lithium carbonate and beta-blockers. The appointment of beta-blockers - prevents the bronchodilating effect of euphyllin and can cause bronchospasm. Eufillin potentiates the action of diuretics by increasing the glomerular filtration and reducing tubular reabsorption. With caution, euphyllin is prescribed concomitantly with anticoagulants, with other theophylline derivatives or purine. It is not recommended to use euphyllin with funds,stimulating the central nervous system (increases neurotoxicity). The drug can not be used with solutions of dextrose, is not compatible with solutions of glucose, fructose and levulose. The pH of the mixed solutions should be taken into account: pharmaceutically incompatible with acid solutions.

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

    In an application with enoxacin, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and may increase, which may require the dose reduction during influenza vaccination intensity aminophylline action.

    Special instructions:

    The drug is administered with caution to patients with severe impairment of liver and kidney function, peptic ulcer of the stomach and duodenum.

    Elderly patients are recommended to reduce the dose of the drug due to delayed excretion from the body.Smoking patients are advised to increase the dose due to accelerated removal of the drug from the body.

    Effect on the ability to drive transp. cf. and fur:

    No information.

    Form release / dosage:

    Solution for intravenous administration is 24 mg / ml.

    Packaging:

    Ampoules of 5 ml or 10 ml. For 10 ampoules with instructions for use and scarifier ampoule in a box of cardboard.

    By 5 or 10 ampoules per contour cell packaging from a polyvinyl chloride film or polyethylene terephthalate tape.

    For 1 or 2 contour packs with instructions for use and a scapegrator ampoule in a pack of cardboard.

    When packing ampoules with a break ring or a break point, the ampoule scaper is not inserted.

    Storage conditions:

    Store in a dark place at a temperature of 15 to 25 ° C. Keep out of the reach of children.

    Shelf life:3 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:P N002436 / 01
    Date of registration:17.07.2008
    The owner of the registration certificate:NOVOSIBHIMFARM, OJSC NOVOSIBHIMFARM, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp06.09.2011
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