Eufillin - instructions for use, dose, side effects, contraindications

Inhibits phosphodiesterase, increases accumulation in tissues of cyclic adenosine monophosphate, 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 muscles of the bronchi, stops bronchospasm, 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 leads to a reduction in the severity and frequency of episodes of apnea. Normalizes the respiratory function, promotes the saturation of blood with oxygen and a decrease in 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 myocardial oxygen demand. 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. It inhibits platelet aggregation (suppresses the platelet and prostaglandin E2 alpha activation factor), increases the resistance of erythrocytes to deformation (improves rheological properties of 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 for liquid dosage forms is 90-100%. Maximum Concentration (7 μg / ml) with intravenous administration of 300 mg is achieved after 15 minutes. 60% of aminophylline (in healthy adults), 36% (in newborns) binds to plasma proteins and is distributed in the blood, extracellular fluid and muscle tissue. Penetrates into breast milk (10% of the dose), through the placental barrier (the concentration in the fetal serum is slightly higher than in the mother's blood serum). 90 % the drug is metabolized in the liver. Metabolites are excreted by the kidneys, 7-13% of the drug is excreted unchanged. The half-life is for non-smokers from 5 to 10 hours, for children over 10 months from 2.5 to 5 hours. Smoking, alcohol significantly affect the metabolism and excretion of the drug, in particular among smokers this period is significantly reduced and ranges from 4 to 5 hours. Elimination of the drug is prolonged in patients with respiratory failure, with renal and heart failure, with viral infections and hyperthermia.

Indications:

Bronchoobstructive syndrome in bronchial asthma, bronchitis, pulmonary emphysema (in mainly for relief of seizures); hypertension in the "small" circle of the circulation.

Violation of cerebral circulation by ischemic type (as part of combination therapy to reduce intracranial pressure). Left ventricular heart insufficiency with bronchospasm and respiratory depression by the type of Cheyne-Stokes (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 heart rhythm disturbances, epilepsy, increased convulsive alertness, hypertrophic obstructive cardiomyopathy, thyrotoxicosis, pulmonary edema, severe coronary insufficiency, hepatic and / or renal insufficiency, hemorrhagic stroke, retinal hemorrhage eyes, bleeding in a recent medical history, acute porphyria, the period of breastfeeding.

Carefully:

Pregnancy, neonatal period, age over 55 years and uncontrolled hypothyroidism (the possibility of cumulation), widespread atherosclerosis of vessels, sepsis, prolonged hyperthermia,gastroesophageal reflux, peptic ulcer of the stomach and duodenum (in the anamnesis), hyperplasia of the prostate. The drug is administered with caution to patients with severe impairment of liver function and nights.

Children under 14 years of age (due to possible side effects).

With caution appoint simultaneously with antiplatelet agents (ticlopidine).

Pregnancy and lactation:

If you need to use the drug during pregnancy, you should compare the expected benefit to the mother and the potential risk to the fetus.

Dosing and Administration:

Intravenously. Adults inject slowly (for 4-6 minutes) to 5-10 ml of solution 24 mg / ml (0.12-0.24 g), which is previously diluted in 10-20 ml of a 0.9% solution of sodium chloride. When there is a palpitation, dizziness, nausea - speed injections are slowed down or switched to drip administration, for which 10-20 ml solution 24 mg / ml (0.24-0.48 g) is diluted in 100-150 ml of a 0.9% solution of sodium chloride; introduced with speed of 30-50 drops per minute. Parenterally administered aminophylline up to 3 times a day, no more than 14 days. Higher doses of aminophylline for adults with intravenous administration: single-dose 0.25 g, dovecia-0.5 g. If necessary, children are given aminophylline intravenously drip from the calculation of a single dose of 2-3 mg / kg.Higher doses for children with intravenous administration: single dose - 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 effects:

From the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor; convulsions, nausea, vomiting.

From the cardiovascular system: heart palpitations, tachycardia (including fetus when taking a pregnant woman in the third trimester), arrhythmias, lowering blood pressure right up to collapse - with rapid intravenous injection, cardialgia, an increase in the frequency of angina attacks.

From the digestive system: gastroesophageal reflux, heartburn, exacerbation of peptic ulcer of the stomach and duodenum.

Allergic reactions: skin rash, itchy skin, fever.

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

Local reactions: compaction, hyperemia, tenderness at the site of administration.

Overdose:

Symptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (incl.with blood), gastrointestinal bleeding, tachypnea, hyperemia of the facial skin, tachycardia, ventricular arrhythmias, insomnia, motor excitement, anxiety, photophobia, tremor, convulsions. In severe poisoning, epileptic seizures may develop (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, lowering blood pressure, necrosis of skeletal muscles, confusion, renal insufficiency with myoglobinuria.

Treatment: cancellation of the drug, forced diuresis, hemosorption, plasmosorption, hemodialysis (efficacy is low, peritoneal dialysis is ineffective), symptomatic therapy (incl. metoclopramide and ondansetron - when vomiting). When the occurrence of convulsions to maintain airway patency and conduct oxygen therapy. For seizure seizure - in / in diazepam, 0.1-0.3 mg / kg, but not more than 10 mg). With severe nausea and vomiting - metoclopramide or ondansetron (w / w).

Interaction:

The drug is incompatible with a solution 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 (increases the risk of ventricular arrhythmias), drugs that excite the central nervous system (increases neurotoxicity).

Doxapram with simultaneous use with aminophylline increases the stimulation of respiratory centers in the central nervous system.

Aminophylline shows a synergistic toxicity with ephedrine and other sympathomimetics. When they are combined, the risk of arrhythmias increases.

The combined use of aminophylline and xanthine derivatives, including pentoxifylline, is contraindicated due to the risk of development of toxicity.

Enoxacin reduces the excretion of aminophylline due to inhibition of cytochrome P450 1A2; with the effect of aminophylline increasing by 300%, which leads to an increased risk of convulsions.

The combined use of aminophylline and fluvoxamine should be avoided. If their joint use is necessary, patients should reduce the dose of aminophylline by half and closely monitor the concentration of aminophylline in the blood plasma.

Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracisin, as inducers of microsomal oxidation, increase the clearance of aminophylline, which may require an increase in its dose.

With simultaneous use with antibiotics from the group of macrolides, lincomycin, with fluoroquinolones, small doses of ethanol, allopurinol, beta adrenoblockers, cimetidine, disulfiram, hormonal contraceptives for ingestion, recombinant interferon alpha, isoprenaline, viloxazine, methotrexate, propafenone, verapamil and for vaccination against influenza, the intensity of action of aminophylline may increase, which may require a reduction in its dose.

Strengthens the action of beta-adrenoblockers and diuretics (including by increasing the glomerular filtration), reduces the effectiveness of lithium and beta-blockers. Compatible with antispasmodics. With caution appoint simultaneously with antiplatelet agents (ticlopidine).

Special instructions:

Before use, the drug solution must be heated to body temperature.

The drug is administered with caution to patients with severe impairment of liver and kidney function, peptic ulcer disease of the stomach and duodenum. Elderly patients are advised to reduce the dose of the drug due to delayed excretion of it from the body. Smoking patients are advised to increase the dose due to accelerated removal of the drug from the body.

Avoid using large amounts of caffeinated foods or drinks during the treatment period.

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

During drug treatment, it is not recommended to drive vehicles, mechanisms, and engage in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions, as the drug may cause dizziness and other side effects that may affect these abilities.

Form release / dosage:

Solution for intravenous administration is 24 mg / ml.

Packaging:

By 5 or 10 ml into ampoules of colorless neutral glass type I by ISO 9187 with color a fracture ring or with a color dot and a notch or without a fault ring, a colored dot and incisions.One, two or three color rings and / or a two-dimensional bar code and / or alphanumeric coding, or without additional color rings, a two-dimensional bar code, alphanumeric encoding.

5 ampoules per circuit cell packaging made of polyvinylchloride film and aluminum foil foil or polymer film or without foil and without film. Or 5 ampoules are placed in a prefabricated form (tray) made of cardboard with cells for laying ampoules.

One or two contour squares or cardboard trays, together with the instruction for use and the ampoule ampoule or ampoule scarifier or ampoule ampoule and ampoule scarifier, are placed in a cardboard package.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

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:LP-002938

Date of registration:01.04.2015 / 15.02.2016

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZON PHARM, LLC Russia

Information update date: & nbsp01.04.2015

Illustrated instructions

Instructions

Eufillin (Euphyllin)