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Euphyllin official instruction. What helps children with Euphyllin in ampoules: instructions for use. "Euphyllin" from cellulite |
Preparations containing Aminophylline (Aminophylline, ATC code R03DA05):
Euphyllin and edema during pregnancy - a review of a cardiologist:There is a fairly stable opinion on the Internet that with edema of the legs in pregnant women, it is imperative to start taking aminophylline. Let me disagree with this. Euphyllin is a rather serious drug, it has side effects that are not consistent with the interests of the mother and the unborn baby. For example, it causes an increase in the pulse rate (tachycardia), and during pregnancy, the pulse is already accelerated, often to exorbitant values. Therefore, aminophylline can lead to a decrease in the efficiency of the heart, including the blood supply to the placenta and, accordingly, to the fetus. Euphyllin can only be prescribed by a doctor, and self-administration of aminophylline for the treatment of edema remains entirely on the conscience of the expectant mother. There is a certain substance that is equally beloved by obstetricians-gynecologists and cardiologists, it can reduce swelling in pregnant women, lower the pulse rate and eliminate cramps in the calf muscles, while having practically no side effects. Euphyllin - instructions for use. Prescription drug, information is intended only for healthcare professionals!Clinical and pharmacological group:Bronchodilator - phosphodiesterase inhibitor pharmachologic effectBronchodilator, 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 diaphragm contraction, 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 the respiratory function, it contributes to the saturation of blood with oxygen and a decrease in 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 the vessels of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, reduces pressure in the "small" circle of blood circulation. Increases renal blood flow, has a moderate diuretic effect. Expands the extrahepatic biliary tract. It inhibits platelet aggregation (inhibits platelet activation factor and PgE2 alpha), increases the resistance of erythrocytes to deformation (improves the rheological properties of blood), reduces thrombus formation and normalizes microcirculation. Has a tocolytic effect, increases the acidity of gastric juice. When used in large doses, it has an enileptogenic effect. PharmacokineticsAfter oral administration, it is rapidly and completely absorbed, bioavailability is 90-100%. Food reduces the rate of absorption without affecting its value (large volumes of liquid and proteins accelerate the process). The higher the dose taken, the lower the rate of absorption. The time to reach Cmax is 1-2 hours. Vd is in the range of 0.3-0.7 l / kg (30-70% of the “ideal” body weight), on average 0.45 l / kg. Communication with plasma proteins in adults - 60%, in patients with liver cirrhosis - 36%. Penetrates into breast milk (10% of the dose taken), through the placental barrier (the concentration in the fetal serum is slightly higher than in the mother's serum). Aminophylline exhibits bronchodilating properties at concentrations of 10-20 μg / ml. Concentrations over 20 mg / ml are toxic. The stimulating effect on the respiratory center is realized at a lower content of the drug in the blood of 5-10 μg / ml. It is 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-dimethyl uric acid (45-55%) is formed, which has pharmacological activity, but is 1-5 times inferior to theophylline. Caffeine is an active metabolite and is produced in small amounts. In children over 3 years of age and in adults (as opposed to younger children), the phenomenon of caffeine accumulation is absent. T1 / 2 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, the pharmacokinetics are normalized after 3-4 months); in adults with chronic obstructive pulmonary disease, pulmonary heart disease and pulmonary heart disease - over 24 hours. It is excreted by the kidneys. Indications for the use of the drug EuphillinBroncho-obstructive syndrome of any genesis: bronchial asthma (the drug of choice in patients with asthma of physical exertion and as an additional remedy for other forms), chronic obstructive pulmonary disease, pulmonary emphysema, chronic obstructive bronchitis, pulmonary hypertension, pulmonary heart, sleep apnea, apnea newborns (a condition characterized by periods of lack of breathing for 15 s and accompanied by cyanosis and bradycardia), Cheyne-Stokes respiration. It is also recommended for arresting cerebral vascular crises of atherosclerotic origin and improving cerebral circulation, reducing intracranial pressure and cerebral edema in ischemic strokes, as well as in chronic cerebrovascular accident. The drug improves renal blood flow and can be used if indicated. Dosage regimenAssign aminophylline inside, intramuscularly, intravenously and in microclysters. Aminophylline solutions are not injected under the skin, as they cause tissue irritation. The route of administration depends on the characteristics of the case: in acute attacks of bronchial asthma and strokes, it is administered intravenously, in less severe cases - intramuscularly or orally. Inside, adults take 0.15 g after meals 1 to 3 times a day after meals. Children are given inside 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 the tolerability of the drug. Into a vein, adults are injected slowly (within 4 - 6 minutes) at 0.12 - 0.24 g (5 - 10 ml of a 2.4% solution), which are preliminarily diluted in 10 - 20 ml of isotonic sodium chloride solution. When palpitations, dizziness, nausea appear, the rate of administration is slowed down or switched to drip, for which 10 - 20 ml of a 2.4% solution (0.24 - 0.48 g) is diluted in 1OO - 150 ml of isotonic sodium chloride solution; injected at a rate of 30-50 drops per minute. If it is impossible to inject into a vein, 1 ml of a 24% solution is injected intramuscularly. Aminophylline is parenterally administered up to 3 times a day for no more than 14 days. Children are injected intravenously at the rate of a single dose of 2 - 3 mg / kg. The drug is not recommended for children under 14 years of age (due to possible side effects). You can prescribe aminophylline rectally in the form of microclysters. Dose for adults 1O - 20 ml of a 2.4% solution in 20 - 25 ml of warm water; children are smaller according to age. Higher doses of aminophylline for adults inside, intramuscularly and rectally: single 0.5 g, daily 1.5 g; in a vein: single 0.25 g, daily 0.5 g. Higher doses for children orally, intramuscularly and rectally: single 7 mg / kg, daily 15 mg / kg; intravenously: single - 3 mg / kg. When taking aminophylline inside (especially when taken on an empty stomach), dyspeptic symptoms associated with the irritating effect of the drug are possible; with rapid intravenous administration, dizziness, headache, palpitations, nausea, vomiting, convulsions, a sharp decrease in blood pressure are possible. Intravenous administration should be carried out under close supervision of the indicators of blood circulation, respiration and the general well-being of the patient. Side effectFrom the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor. From the side of the cardiovascular system: palpitations, tachycardia (including in the fetus when taken by a pregnant woman in the third trimester), arrhythmias, cardialgia, decreased blood pressure, increased frequency of angina attacks. From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer disease, diarrhea, with prolonged use - decreased appetite. Allergic reactions: skin rash, itching, fever. Others: chest pain, tachypnea, flushing, albuminuria, hematuria, hypoglycemia, increased urine output, increased sweating. Contraindications to the use of the drug EuphillinHypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine), epilepsy, gastric ulcer and duodenal ulcer (in the acute stage), gastritis with high acidity, severe arterial hyper- or hypotension, tachyarrhythmias, hemorrhagic stroke into the retina of the eye, children (up to 3 years). Carefully. Severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread vascular atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular premature beats, increased convulsive readiness, hepatic and / or renal failure, gastric ulcer and 12 duodenal ulcer (duodenal ulcer) a recent history of the gastrointestinal tract, uncontrolled hypothyroidism (the possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hyperplasia, pregnancy, lactation, old age, childhood. Prescribed simultaneously with anticoagulants. Use of the drug Euphillin during pregnancy and lactationWith caution during pregnancy and lactation. Application for violations of liver functionWith caution in liver failure. Application for impaired renal functionWith caution in renal failure. special instructionsExercise caution when consuming large amounts of caffeinated foods or drinks during treatment, you must refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions. OverdoseSymptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, facial flushing, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremors, convulsions. In severe poisoning, epileptoid seizures may develop (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, skeletal muscle necrosis, confusion, renal failure with myoglobinuria. Treatment: drug withdrawal, gastric lavage, use of activated charcoal, laxatives, intestinal lavage with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasma sorption, hemodialysis (efficiency is not high, peritoneal dialysis is not effective), symptomatic therapy (including metoclopramide and ondansetron - with vomiting). If seizures occur, maintain airway patency and oxygen therapy. To stop the seizure - intravenous diazepam 0.1-0.3 mg / kg (but not more than 10 mg). For severe nausea and vomiting, metoclopramide or ondansetron (IV). Drug interactionsIncreases the likelihood of developing side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), agents for general anesthesia (the risk of ventricular arrhythmias increases), xanthines and drugs that excite the central nervous system (increases neurotoxicity), beta-adrenostimulants. Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline. Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracizin, being inducers of liver microsomal enzymes, increase the clearance of aminophylline, which may require an increase in its dose. With simultaneous use with antibiotics of the macrolide group, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon-alpha, methotrexate, mexiletine, propafenone, thilopendazole, vaccine, verapamino may increase, which may require a decrease in its dose. It enhances the effect of beta-adrenostimulants and diuretics (including by increasing glomerular filtration), reduces the effectiveness of lithium preparations and beta-blockers. Compatible with antispasmodics, not used in conjunction with other xanthine derivatives. Terms of dispensing from pharmaciesThe drug is available with a prescription. Storage conditions and periodsIn a dry, dark place at a temperature not exceeding 20 ° C. Keep out of the reach of children. Shelf life. 5 years. Do not use after the expiration date. The Euphyllin dropper in ampoules is used to treat pathologies that are accompanied by airway obstruction and other diseases with smooth muscle spasms. It contains the active ingredient theophylline. Release form: solution with different concentrations of this ingredient, packaged in glass ampoules. The medicine is used for intramuscular administration. When the drug is diluted in water, intravenous injections can be given with it. The dosage and duration of treatment is prescribed by the attending physician. What is this drug?Euphyllin is an antispasmodic that helps to relax the smooth muscles of the uterus, bronchi, and biliary tract. After application, the drug eliminates spasm and muscle contractions. For example, in case of diseases of the bronchi, it reduces spasm, and in case of a threat of miscarriage, it eliminates unnecessary contractions of the uterus. The drug Euphyllin is produced by several manufacturers. The brand name may differ as pharmaceutical factories seek to register their own brand. These are Euphyllin-Darnitsa and UBF. But the composition of the solution does not change. It is produced using the same formula that was patented many years ago. Release formThe drug is available in the form of a solution for injection and tablets. There are two types of solutions:
Additionally, the solution contains water and a preservative. The preservative is determined by the formula of the manufacturing plant. Action on the bodyWhen using aminophylline, the work of the muscles between the ribs and ventilation of the alveolar space improves. The drug enhances the local immune defense of the mucous membranes from aggressive pathogenic agents (viruses, bacteria). It expands the lumen of blood vessels, relieving the tension of their walls, and reduces the pressure of blood flow in the lungs. The medicine improves the work of the heart muscle, enhances the production of adrenaline, and has a diuretic effect. The dropper prevents blood clots from forming and prolongs the life of red blood cells in the body. It relaxes the walls of the uterus during muscle contractions that threaten premature birth and termination of pregnancy. Indications for treatmentEuphyllin is recommended if the patient has chronic obstructive pulmonary disease, asthma, bronchitis, and apnea. It is used to reduce high intracranial pressure, to eliminate asthma attacks, with impaired blood circulation in the brain, which develops during strokes and its edema. Injections of aminophylline intravenously are prescribed if the patient develops acute or chronic heart failure. Such injections lower the pressure in the vessels of the lungs, relieve edema in case of kidney disease. The medicine for neuralgia helps (like Milgamma and its substitutes). It is used in gynecology when there is a risk of premature birth or a threat of miscarriage. It has a relaxing effect on the smooth muscles of the uterus and relieves spasms. Do not recommend a drip at home. Contraindications of the drugEuphyllin has a synthetic nature and a number of contraindications, in which it should not be used:
Doctors recommend using it with caution to treat children under 14 years of age, elderly patients. The risk group also includes breastfeeding mothers, pregnant women, people suffering from atherosclerosis. Such treatment is carried out only under the supervision of the attending physician, for any side effects or deterioration in health, the medicine is canceled. Instructions for useThe dosage of the drug and the duration of the course of treatment are determined based on the diagnosed disease, age, weight of the patient and other factors:
Euphyllin side effectsAfter taking the medicine, patients may experience anxiety, insomnia. They feel dizzy, their limbs cramp, tremors in the muscles begin. At the same time, the work of the heart muscle is disrupted, and heart palpitations begin. After the injections, a migraine occurs, the patient is agitated, quickly irritated. If a woman is pregnant, heart palpitations and arrhythmias may occur when taking medication in the last months of the term. In addition, angina pectoris develops, blood pressure rises. With a long course of treatment with aminophylline, appetite may decrease, nausea occurs, and there are bouts of vomiting. Sometimes the drug provokes diarrhea or the development of stomach and duodenal ulcers.
Overdose: symptoms and patient careAfter the introduction of too large a dose of the drug, appetite worsens, diarrhea develops, there is vomiting of blood, nausea. After an overdose, tachycardia may begin, internal gastric bleeding develops. Sleep problems may occur, convulsions and tremors in the limbs begin, photophobia and tachycardia develop. When the dose is increased, the patient may be agitated, he has epileptic seizures, hypokalemia develops, and blood pressure drops. A person often begins to have confusion and kidney failure. To stop the symptoms and improve the condition, the drug must be canceled. The patient is washed stomach, given laxatives and activated charcoal. And also symptomatic treatment is carried out with metoclopramide and ondansetron if the patient vomits. For seizures, oxygen therapy with airway support is recommended. In case of epileptic seizures, it is necessary to give the patient an intravenous injection of diazepam. If a person vomits violently, then intravenous injections of metoclopramide, ondansetron should be administered. Application nuancesThe medicine should be used with caution in heart attacks, angina pectoris, atherosclerosis. Under the supervision of a physician, treatment is carried out for renal and hepatic insufficiency, for stomach or gastrointestinal ulcers. Treatment should be monitored for hypothyroidism, thyrotoxicosis, and prostatic hypertrophy. The drug should be used with caution to treat the elderly and children. This is especially true for taking pills. A decrease in dosage may be necessary in case of impaired liver function, in chronic alcohol dependence, if a person has a fever, in acute respiratory disease. Dose reduction is possible when treatment is prescribed to an elderly person. If a medicine with the same active substance is chosen, then regular tests should be carried out to determine its concentration in the blood.
Medicine during pregnancyThe instructions for use state that its use at this time may threaten the health of the child. In the blood of a newborn, doctors often reveal a high concentration of caffeine and aminophylline. If the mother is undergoing a course of injections with this drug, but the children are monitored after birth by doctors to exclude intoxication with xanthines. When taking aminophylline, doctors assess the risks and possible consequences. The medicine is prescribed for extreme vital signs. Why are pregnant women prescribed euphyllin?Indications during gestation:
Pregnancy in the annotation is prescribed as a contraindication, therefore there is no clear treatment regimen. The doctor prescribes the dosage and the schedule of admission, based on the woman's diagnosis, her state of health. In pregnant women, during the course of treatment, a strong heartbeat may begin, weakness is observed. Electrophoresis with drugThis procedure is performed for people of any age to relax muscles and reduce intracranial pressure. It is used in complex therapy for joint diseases. Electrophoresis is used to improve blood supply to specific areas (neck, lower back). It acts pointwise, without exerting a systemic effect. Therefore, the procedure is applied even for infants and is well tolerated by all groups of patients. For the procedure, a piece of gauze is moistened in the medicine (at a concentration of 2.4%), electrodes are applied to the desired area. During the procedure, the patient feels warmth or tingling sensation. The course of treatment is 10 sessions, 10-15 minutes each. The procedure is done every other day, then a break is needed. Euphyllin and alcoholic beveragesThe drug is not combined with alcohol, because it increases the toxic effect on the body, enhancing the effects of the drug. Against this background, pressure drops, suffocation begins, heart rate increases, arrhythmia and tachycardia develop. Due to the relaxation of the muscles of the lungs, sometimes there is a complete cessation of breathing, with weakened vessels of the brain, hemorrhages are possible. In rare cases, taking alcohol and aminophylline at the same time provokes death. Storage conditions, vacation conditionsThe medicine is available with a prescription. Its cost depends on the form of release and varies from 11 to 94 rubles per package.
- a phosphodiesterase inhibitor. It helps to reduce the level of calcium ions and, as a result, reduce the contractility of smooth muscles. Basically, the drug is used as a bronchodilator, vasodilator, diuretic. Composition of the preparationThe main active ingredient is Aminophylline... It is he who has all the pharmacological actions that will be described below. If the drug is in ampoules, then injection water is also contained with Aminophylline. If this is a tablet form, then the composition will include povidone, magnesium stearate, potato starch. Pharmacological group - adenosinergic substances. Mechanism of actionBy blocking phosphodiesterase, it reduces the concentration of Ca ions. Low calcium levels impair smooth muscle contractility. All this is manifested by relaxation of the muscles: bronchi, blood vessels; relieves bronchospasm, improves the work of the respiratory muscles. The oxygen filling of the blood increases, the frequency of apnea attacks decreases, and the respiratory center is stimulated. Acting on the receptors of blood vessels, reduces their tone, promoting expansion. Increases blood flow in the kidneys, which accelerates the excretion of urine, and hence urine output. Improves blood flow in the heart arteries, increasing the heart rate and strength of the heart. By acting on the cells of the immune system (mast cells), it reduces the release of substances that cause inflammation, thereby reducing allergic manifestations. Release form: Euphyllin is produced and sold in powders, tablets or ampoules. Powder in sachets is rarely used. In the form of tablets: 1 tablet contains 0.15 g of the substance. There are usually 10 tablets in a blister, and in a package there are 3 blisters. Another form is a solution in ampoules of 12%, 2 ml each. This dose is universal for both subcutaneous and intravenous and intramuscular injections. Ampoules with 2.4% x 10 ml are used purely for intravenous injections. You need to store Euphyllin at a temperature of 25 degrees or less. AnalogsIf pronounced side effects from Euphyllin develop or there is no means in the public domain, it is possible to replace it with a group of drugs with a similar effect:
It is impossible to independently cancel the prescribed remedy and replace it with another, despite the fact that they have similar properties. Only a specialist can replace the remedy, since only he will be able to take into account all the side effects and the risk of their development in a particular patient. Indications for useWhat does the drug help from:
Some women choose to use Euphyllin to combat cellulite by adding it to their moisturizer or anti-cellulite cream. But so far there are no reliable sources, conducted studies on the effect of the drug on the elimination of cellulite, so we cannot talk about effectiveness. As such, this method of application will not bring harm if there is no allergy to the substance. Contraindications
Side effectsThe main side effects are:
If you look from the side of the heart, then it is possible:
Method of administration and dosageEuphyllin tablets are drunk after meals. 1-3 times a day, 1 tablet 0.15 g, for children - 4 times. The frequency of admission, the duration, how much to drink the drug in days is determined only by the doctor. If Euphyllin is prescribed in ampoules, then the solution is injected 1-3 times / day intravenously, with the calculation of 10 mg / 1 kg of body weight. How to dilute the drug in ampoules? The frequency of administration and the dose is determined by the attending physician. Usually, in the first injections, a small concentration of the substance is used, diluting it before use in saline under pressure control, because Euphyllin is able to change it. For adults, a 2.4% solution with a volume of 15 ml is diluted in 100 ml of 0.9% sodium chloride. It is forbidden to dilute Euphyllin on your own without determining the dosage and concentration of a specialist. Especially when it comes to children. Enter slowly. For children under 18 years of age or infants, the ratio of the solution is lower and is regulated by a pediatrician. OverdoseIf the dose is exceeded above the therapeutic dose, symptoms associated with an overdose occur. This is manifested by a decrease in appetite, nausea, vomiting, tachycardia, insomnia, and anxiety. Perhaps the appearance of bleeding in the gastrointestinal tract, convulsions, epileptic seizures are also signs of an overdose. A drop in pressure, kidney failure also develop when the dose is exceeded. If these symptoms develop, or at least some of them, the first step is to stop taking the drug. When vomiting occurs, metoclopramide is taken, seizures - oxygen therapy, and if an epileptic seizure develops, diazepam is administered intravenously at a rate of 0.2 mg / 1 kg of weight. Forced diuresis and hemosorption are recommended. A warningDuring the use of Euphyllin, you should seriously monitor your diet. It is necessary to limit the use of coffee and caffeinated foods and drinks. People with a long smoking history need to increase the concentration of the injected drug, because nicotine interferes with its absorption. Euphyllin with cervical osteochondrosisTaking into account all the effects that a drug has on a person as a whole, one can understand such a widespread prevalence of it as a means for the treatment of cervical osteochondrosis. Exhibiting a relaxing effect on spasmodic cervical muscles, a vasodilating effect, it normalizes blood circulation and nutrition of these muscles, which also improves the nutrition of the cartilage of the cervical spine. For the treatment of cervical osteochondrosis, the optimal solution is intravenous administration. In this case, the drug is better absorbed and has a greater therapeutic effect. Electrophoresis of the cervical spine with euphyllinFor better penetration of the substance into the deep structures of the neck, electrophoresis with Euphyllin on the cervical spine can be used. It is used in case of detection of hernias, osteochondrosis. Electrophoresis is also effective for infants. What is the electrophoresis technique? Several electrodes are applied to the cervical spine, on which there is the necessary dosage of Euphyllin. A small discharge current is applied. The drug applied to the electrodes moves under the action of an electric field and penetrates into the necessary structures, in particular the skin. The very effect of electric current already has a positive therapeutic effect, it is especially effective in relieving edema, and when combined with the introduction of Euphyllin, this effect is enhanced. A significant advantage of the introduction of Euphyllin using electrophoresis is that the drug does not affect other organs, but acts locally at the site of application and penetration, where its maximum concentration is created. Instructions for use: Euphyllin is a bronchodilator. Pharmacological propertiesEuphyllin belongs to the xanthine group. It contains the main active ingredient - theophylline. The drug has an expanding effect on the bronchi, relaxing their smooth muscles and eliminating spasms. In addition, it improves the functioning of the cilia of the epithelium of the respiratory tract, improves the contraction of the diaphragmatic, intercostal and other respiratory muscles. Eufillin stimulates the respiratory center in the medulla oblongata, improves pulmonary ventilation, oxygen saturation of the blood and reduces the content of carbon dioxide in it, that is, normalizes the respiratory function. The mechanism of action of Euphyllin consists in inhibition of the phosphodiesterase enzyme, due to which cAMP accumulates in the tissues, the entry of calcium ions into the cells, which are responsible for muscle contraction, decreases, and this relaxes the muscles of the bronchi. According to the instructions, Euphyllin stimulates cardiac activity, increasing the frequency and strength of myocardial contraction. It is able to reduce the tone of blood vessels, mainly of the skin, kidneys and brain. Providing a relaxing effect on the venous walls in the pulmonary circulation, the drug reduces the pressure in it. The use of Euphyllin improves the blood supply to the kidneys, thereby increasing the formation and excretion of urine. The drug slows down platelet aggregation and makes red blood cells more resistant to damage, that is, improves the rheological properties of blood. It is known about the tocolytic effect of Euphyllin on the uterus, it also increases the acidity of gastric juice. The agent is well absorbed from the digestive tract, its bioavailability reaches 100%. When taken simultaneously with food, absorption slows down somewhat. It passes into breast milk and through the placenta. Euphyllin's metabolism occurs in the liver, its excretion from the body occurs in the urine. Release formAccording to the instructions, Euphyllin is released in tablets of 150 mg, in ampoules in the form of a 2.4% and 24% solution. IndicationsThe drug is used to relieve attacks of bronchial asthma, heart failure, angina pectoris, pulmonary edema and other conditions associated with congestion. According to reviews, Euphyllin effectively reduces blood pressure in hypertensive crises. It is used in the complex therapy of stroke and other ischemic conditions of the brain, in the treatment of apnea in newborns. ContraindicationsThe use of Euphyllin is contraindicated in case of its intolerance, in the acute period of myocardial infarction, with collapse, paroxysmal tachycardia, extrasystole, epilepsy, hyperthyroidism, peptic ulcer, abnormalities in the functioning of the liver and kidneys, with prostate adenoma, diarrhea. It is not recommended to use the drug in tablets under the age of 6 years. Instructions for the use of EuphyllinIn the form of a solution, the drug is administered intravenously and intramuscularly, parenteral use is justified in the treatment of emergency and urgent conditions. In this case, the dosage is calculated individually, depending on the severity of the condition and the weight of the patient. For adults in emergency situations, the dose of Euphyllin, according to the instructions, is selected at the rate of 6 mg / kg, it is diluted in 20 ml of saline sodium chloride solution, and injected intravenously slowly for at least 5 minutes. Status asthmaticus requires infusion of the drug in the amount of 720 - 750 mg. Parenteral administration of Euphyllin is not recommended for longer than 14 days. To alleviate the condition in chronic obstructive pulmonary diseases in the acute phase, begin with a dose of 5-6 mg / kg of the drug. If necessary, it should be increased very carefully, under the control of its content in the blood. In tablets, Euphyllin is taken 0.15 g from 1 to 3 times a day, after a meal. The course of admission can last from several days to several months. With apnea of newborns, when respiratory arrest lasts from 15 seconds with a simultaneous decrease in heart rate, the initial dose of this drug for newborns is 5 mg / kg / day in 2 divided doses. The drug is administered via a nasogastric tube. When the condition is stabilized, they switch to a maintenance dose of 2 mg / kg / day in 2 divided doses. The duration of use can range from several weeks to several months. Depending on the severity of the condition and indications for Euphyllin in children, the daily dose varies from 6 to 15 mg / kg. For elderly patients, caution should be exercised in drug treatment. According to reviews, Euphyllin enhances the side effects of glucocorticoids, mineralocorticoids and adrenostimulants. Do not use this agent simultaneously with other xanthine derivatives. Side effects of EuphyllinAccording to reviews, Euphyllin is capable of causing such undesirable effects as insomnia, dizziness, agitation, headaches, tremors, increased heart rate, arrhythmias, heart pain, decreased blood pressure, abdominal pain, nausea, heartburn, vomiting, diarrhea, allergic reactions, increased sweating, decreased blood glucose, changes in urine tests.
ATX code: Respiratory system (R)> Drugs for the treatment of bronchial asthma (R03)> Other drugs for the treatment of bronchial asthma for systemic use (R03D)> Xanthine derivatives (R03DA)> Aminophylline (R03DA05) Release form, composition and packagingsolution for intravenous administration 24 mg / ml: 5 ml amp. 10 pieces.Reg. No: 19/03/566 from 30.05.2018 - The validity period of the reg. beats is not limited Solution for intravenous administration colorless or slightly yellowish, transparent. Excipients: water d / i. 5 ml - ampoules (10) - cardboard boxes. Description of the medicinal product Euphillin solution created in 2013 on the basis of instructions posted on the official website of the Ministry of Health of the Republic of Belarus. Updated date: 23.01.2014 The action of aminophylline is primarily due to the content of theophylline in it. Ethylenediamine enhances antispasmodic (spasm relieving) activity and promotes drug dissolution. Important features of aminophylline are its solubility in water and the possibility of its intravenous administration. Euphyllin relaxes the muscles of the bronchi, lowers the resistance of the blood vessels, dilates the coronary (cardiac) vessels, lowers the pressure in the pulmonary artery system, increases renal blood flow, has a diuretic (diuretic) effect, associated mainly with a decrease in canalic reabsorption (reabsorption of water in the renal tubules), causes an increase in urinary excretion of water and electrolytes, especially sodium and chlorine ions. The drug strongly inhibits platelet aggregation (adhesion). Blocks adenosine receptors, inhibits phosphodiesterase activity, increases the level of cyclic AMP, reduces the level of ionized calcium in smooth muscle cells.
Aminophylline for injection 24 mg / ml is intended for slow intravenous administration. The solution should be injected very slowly over 4-6 minutes, 5-10 ml of the drug (0.12-0.24 g), which is previously diluted with a small volume (5-10 ml) of 5% dextrose or 0.9% sodium chloride solution for injection. Supportive therapy can be achieved by administering large volumes of infusion solutions, the rate of administration is adjusted so as to provide the required amount of the drug every hour. Usually, with dropwise administration, 10-20 ml of the drug (0.24-0.48 g) is diluted in 100-150 ml of 0.9% sodium chloride solution and injected at a rate of 30-50 drops per minute. Before parenteral administration, the solution must be heated to body temperature. Aminophylline is administered parenterally up to 3 times / day, no more than 14 days. Higher doses of aminophylline for adults with intravenous administration:
Theophylline therapeutic plasma concentration is considered to be in the range of 5 to 20 μg / ml, and levels above 20 μg / ml are most likely associated with toxic effects. There is also individual patient variation in the dosage required to achieve a plasma theophylline concentration within the desired therapeutic range. During therapy, patients should be closely monitored for toxicity and, where possible, theophylline content should also be monitored, doses should be calculated based on ideal body weight, the drug is not recommended for children under 6 months of age due to significant fluctuations in theophylline metabolism in young children. Patients not receiving theophylline preparations A. A loading dose of aminophylline 6 mg / kg body weight can be given IV 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:
Patients already receiving theophylline The loading dose can be calculated on the basis that every 0.5 mg / kg of theophylline given as a loading dose may lead to an increase of 1 μg / ml 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 a dose of 3.1 mg / kg of aminophylline (equivalent to 2.5 mg / kg of anhydrous theophylline) is administered on the grounds that this can lead to an increase in the concentration of theophylline in serum by about 5 μg / ml when administered as a loading dose. Aminophylline can irritate the gastrointestinal tract, stimulate the central nervous system, and affect the cardiovascular system. Hypotension, arrhythmias, and seizures may follow IV injections, especially if the injection is given too quickly. There were also reports of sudden death. Severe toxicity can occur without prior precursor symptoms. The immune system: allergic reactions. Metabolic and nutritional disorders: metabolic disorders such as hypokalemia, hypophosphatemia, hyponatremia. Mental disorders: anxiety, insomnia. Higher doses can lead to manic behavior and delirium. Nervous system disorders: headache, confusion, anxiety, hyperventilation, dizziness, and tremors. Higher doses can lead to seizures. Disorders of the organ of vision: visual impairment. Heart Disorders: palpitations, tachycardia, cardiac arrhythmias, arterial hypotension. Gastrointestinal Disorders: nausea, vomiting, abdominal pain, diarrhea, gastroesophageal reflux, gastrointestinal bleeding. Diseases of the skin and subcutaneous tissue: rash, maculopapular rash, redness, itching, urticaria, exfoliative dermatitis. General violations: IM injections are painful, pain lasts several hours. Higher doses can lead to hyperthermia and thirst.
Reproductive studies in animals have not been performed with theophylline. It is not known whether theophylline can cause fetal harm when administered to pregnant women. Despite this, the safe use of theophylline during pregnancy has not been established regarding the potential risk to the fetus; theophylline has been used during pregnancy without teratogenic 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 doctor decides on the use of aminophylline during pregnancy. 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. 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. Aminophylline has a narrow therapeutic index and serum concentration should be monitored regularly, especially during initiation of therapy. Aminophylline for injection should be administered cautiously in patients over 55 years of age. Elderly patients with heart or hepatic disease should be closely monitored for signs of theophylline toxicity. Children are especially susceptible to the effects of theophylline and caution is required when prescribing aminophylline in children. There have been reports of seizures in children who were prescribed theophylline at a plasma concentration of the latter within the accepted therapeutic range. Alternative treatment should be considered in patients with a history of seizure activity, and if Aminophylline for injection is used in such patients, they should be carefully evaluated for possible signs of CNS hyperstimulation. Due to the fact that the average T 1/2 of theophylline is shorter in smokers than in non-smokers, the first group may require large doses of aminophylline. Caution should be exercised in patients who have undergone influenza immunization or who have an active influenza infection or acute febrile illness. Aminophylline should be prescribed with caution in patients with heart failure, chronic obstructive pulmonary disease, renal or hepatic dysfunction, and in chronic alcoholism, since the clearance of Aminophylline decreases. Serum potassium levels should be monitored during regular therapy. This is very important in combination therapy with beta-2 agonists, corticosteroids or diuretics, or in the presence of hypoxia. Aminophylline should be used with caution in patients with peptic ulcer disease, hyperthyroidism, glaucoma, diabetes mellitus, severe hypoxemia, arterial hypertension, and impaired cardiac function or circulation, as these conditions may be aggravated. Methylxanthines can increase gastric acidity and appropriate measures should be taken if they are used in patients with a history of peptic ulcer disease. Aminophylline should not be administered concurrently with other xanthine-containing drugs. There is no information on the effect on the ability to drive and operate machinery. Aminophylline has a narrow therapeutic index. Theophylline toxicity is most likely to occur at serum concentrations in excess of 20 μg / ml and becomes progressively more severe at high serum concentrations. Doses over 3 g may be serious in adults (40 mg / kg in a child). The lethal dose may be as little as 4.5 g in adults (60 mg / kg in a child), but it is generally higher. Death in adults can occur with the introduction of IV Aminophylline in high doses in patients with renal, hepatic or cardiovascular complications, or if the injection was made quickly. Symptoms: tachycardia, in the absence of hypoxia, fever, or with co-administration of sympathomimetic drugs, may be a sign of theophylline toxicity. Gastrointestinal symptoms: anorexia, nausea, vomiting, diarrhea, vomiting of blood. Neurological symptoms: anxiety, insomnia, irritability, headache, agitation, hallucinations, intense thirst, mild fever, dilated pupils, and tinnitus. Seizures can occur even without prior symptoms of toxicity and are often fatal. Coma can develop in very severe cases. Cardiovascular symptoms: palpitations, arrhythmias, arterial hypotension, supraventricular and ventricular arrhythmias. Metabolic symptoms: hypokalemia can develop quickly and can be severe. Hyperglycemia, albuminuria, pyrexia, hypomagnesemia, hypophosphatemia, hypercalcemia, respiratory alkalosis, metabolic acidosis, and rhabdomyolysis can also occur. Treatment: overdose treatment is supportive and symptomatic. Serum levels of theophylline and potassium should be monitored. Repeated oral administration of activated charcoal helps to eliminate theophylline from the body even after intravenous administration. Aggressive antiemetic therapy may be required to enable oral administration of activated charcoal. Convulsions can be stopped by intravenous injection 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 given IV to reverse tachycardia, hypokalemia, and hyperglycemia, provided the patient is not suffering from asthma. In general, theophylline is rapidly metabolized and hemodiadesis is not warranted. In patients with congestive heart failure or liver disease, hemodialysis can double theophylline clearance. Hemosorption should be considered if:
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