Ipraterol-native solution Inh. 0.25mg / mL + 0.5mg / mL 20ml

$5.64

Ipraterol-native solution Inh. 0.25mg / mL + 0.5mg / mL 20ml

Quantity:

Description

Composition
Active substance:
Ipratropium bromide monohydrate 0.261 mg (calculated as ipratropium bromide 0.25 mg)
Fenoterol hydrobromide 0.5 mg.
Excipients:
Sodium benzoate 0.5 mg
Disodium edetate dihydrate 0.554 mg
Citric acid monohydrate 1.5 mg
Sodium hydroxide to pH 3,2
Purified water to 1.0 ml.
Description:
Transparent colorless or yellowish white with a weak liquid.
Product form:
Solution for inhalation 0.25 mg + 0.5 mg / ml. 20 ml of the product in dark glass vials with a polyethylene dropper and a polypropylene screw cap.
1 bottle with instructions for use placed in a cardboard box.
Contraindications
• Hypersensitivity to fenoterol, ipratropium bromide (as well as other drugs atropine) and the auxiliary components within the preparation. • Hypertrophic obstructive cardiomyopathy. • Tachyarrhythmia.
Carefully
Preparation Ipraterol-native should be used with caution in patients with diseases such as the angle-closure glaucoma, hypertension, diabetes, recent myocardial infarction (within the last 3 months), heart and vascular diseases, such as chronic heart failure, coronary heart disease , arrhythmias, aortic stenosis, marked the defeat of cerebral and peripheral artery disease, hyperthyroidism, pheochromocytoma, prostatic hyperplasia, bladder neck obstruction, mukovi stsidoz, II and III trimesters of pregnancy, lactation, children under 6 years.
Dosage
0.25 mg + 0.5 mg / ml
Indications
Chronic obstructive pulmonary disease (COPD), chronic bronchitis, emphysema, bronchial asthma (mild and moderate).
Interaction with other drugs
Prolonged simultaneous use of the drug Ipraterol-native with other anticholinergic drugs is not recommended due to lack of data.
The simultaneous use of other beta-adrenomimeticheskih and anticholinergic drugs, including systemic effects, and xanthine derivatives (e.g., theophylline) may enhance bronchodilatory drug action Ipraterol-native and lead to increased unwanted reactions.
Perhaps a significant weakening of bronchodilator action Ipraterol- native drug with concomitant administration of beta-blockers.
Hypokalemia associated with beta-agonists, can be enhanced while appointment xanthine derivatives, glucocorticoids, and diuretics. This fact should be given special attention in the treatment of patients with severe obstructive airways disease. Hypokalemia may increase the risk of arrhythmias in patients receiving digoxin. Additionally, hypoxia may exacerbate the negative effect of hypokalaemia on cardiac rhythm. In such cases, it is recommended to carry out monitoring of the concentration of potassium in the blood serum.
It should be used with caution beta2-adrenergic drugs patients receiving monoamine oxidase inhibitors, and tricyclic antidepressants, since these drugs can enhance the effect of beta-adrenergic agents.
Inhalation agents for general anesthesia such as a halogenated hydrocarbon anesthetics (halothane, trichlorethylene, enflurane), may enhance the adverse effect of beta-adrenergic agents to the cardiovascular system.
The combined use of the drug with the native-Ipraterol cromoglicic acid and / or increases the efficiency of therapy with glucocorticosteroids.
Overdose
symptoms
Overdose symptoms typically associated with the action of fenoterol. Perhaps the appearance of symptoms caused by excessive stimulation of beta-adrenergic receptors. The most likely occurrence of tachycardia, palpitations, tremor, hypertension or hypotension, increasing the difference between systolic and diastolic blood pressure, angina, arrhythmias, and a sense of “tides” of blood to the face, metabolic acidosis, hypokalemia, a feeling of heaviness in the chest, increased bronchial obstruction. Possible overdose symptoms of ipratropium bromide (such as dry mouth, accommodation disturbance Eye), considering the great breadth of therapeutic action of the drug and the local way of application, generally mild and transient in nature are.
Treatment
It is necessary to stop the use of Ipraterol-native drug. Should take into account monitoring data of acid-base balance of blood. It recommended the appointment of sedative drugs, anxiolytic drugs (tranquilizers), in severe cases – intensive care.
As a specific antidote possible use of beta-blockers, preferably selective beta1-adrenergic blockers. However, be aware of the possible strengthening of bronchial obstruction under the influence of beta-blockers and carefully select a dose for patients with asthma or chronic obstructive pulmonary disease because of the risk of severe bronchospasm, which can be fatal.
pharmachologic effect
Pharmacological group:
Bronchodilatory agent combined (selective beta2- adrenoagonists + m-holinoblokator).
Pharmacodynamics:
The drug-native Ipraterol comprises two components having bronchodilating activity: ipratropium bromide – m-holinoblokator and fenoterol – beta2-agonists.
Bronchodilation when inhaled ipratropium bromide is mainly due to local rather than systemic anticholinergic effects.
Ipratropium bromide is a quaternary ammonium derivatives having anticholinergic (parasympatholytic) properties. Ipratropium bromide inhibits the reflexes caused by the vagus nerve, counteracting the influence of acetylcholine – a mediator released from the nerve endings of the vagus.
Anticholinergics prevent the increase in intracellular calcium ion concentration that occurs due to the interaction with muscarinic acetylcholine receptors of bronchial smooth muscle. The release of calcium ions is mediated by the system of secondary mediators, which include inositol triphosphate (ITP) and diacylglycerol (DAG).
In patients with bronchospasm associated with chronic obstructive pulmonary disease (chronic bronchitis and emphysema), significant improvements in lung function (increase in forced expiratory volume in 1 second (FEV1) and peak expiratory flow rate (PSV) of 15% or more) is marked for 15 minutes, the maximum effect is achieved after 1-2 hours and lasts until the majority of patients 6 hours after administration.
Ipratropium bromide has no adverse effect on mucus secretion in airway mucociliary clearance and gas exchange.
Fenoterol selectively stimulates beta2-adrenergic receptors in the therapeutic dose.
Stimulation of the beta1-adrenergic receptor occurs at high doses. Beta adrenergic (beta-adrenoceptor stimulating) effect of the drug on cardiac activity, such as increased frequency and severity of cardiac contractions, due to the action of vascular fenoterol, beta2-adrenergic stimulation of the heart, and at doses exceeding therapeutic, beta1-adrenoceptor stimulation.
As with other beta-adrenergic drugs is marked prolongation of the interval QTc at high doses. When using fenoterol via aerosol metered dose inhalers (MDIs), this effect was unstable and was observed in the case of doses exceeding recommended. However, after application via a nebulizer fenoterol (solution in vials for inhalation unit dose) systemic exposure may be higher than when using the drug by MDI at recommended doses. The clinical relevance of these observations has not been established.
Fenoterol relaxes the smooth muscles of bronchi and vessels and prevents the development of bronchospastic reactions, caused by histamine, methacholine, cold air and allergens (immediate hypersensitivity reaction).
Immediately after application fenoterol blocks the release of mediators of inflammation and bronchoconstriction from mast cells. Furthermore, when using fenoterol at doses of 0.6 mg marked enhancement of mucociliary clearance.
Tremor is the most common adverse effect with beta-adrenoceptor agonists. In contrast to the effects on the bronchial smooth muscle to systemic effects agonists, beta-blockers may develop a tolerance, but the clinical significance of this phenomenon is not revealed.
When the joint application of ipratropium bromide and fenoterol bronchodilatory (bronchodilation) effect is achieved by acting on different pharmacological targets. These active substances complement each other, resulting in enhanced spasmolytic effect on the bronchial muscle and provides greater latitude therapeutic action in bronchopulmonary diseases accompanied by airway obstruction. The complementary action is such that to achieve the desired effect requires a lower dose of beta-adrenergic component that enables individually choose an effective dose in the substantial absence of undesired reactions.
In acute bronchoconstriction effect of the drug is rapidly developing, it can be used for acute attacks of bronchospasm.
Pharmacokinetics:
There is no evidence that the pharmacokinetics combined preparation comprising ipratropium bromide and fenoterol, differs from that of each of the individual components.
Suction
Inhalation administration route for ipratropium bromide is characterized by very low absorption from the respiratory tract mucosa. The concentration of ipratropium bromide in blood plasma is at the lower boundary definition, and it can be measured only at high doses of active ingredient. After inhalation to the lung is usually misses (depending upon the dosage form and the method of inhalation) 10-30% of the administered dose of ipratropium bromide. Most of the dose is swallowed and enters the gastrointestinal tract.
Part dose ipratropium bromide, entering the lungs rapidly reaches the systemic circulation (within several minutes). The total systemic bioavailability of ipratropium bromide, used by inhalation, is 7-28%.
Depending on the method used by inhalation and inhalation system of about 10-30% of fenoterol reaches the lower airways, and the remainder is deposited in the upper airways and is swallowed. As a result, a certain amount of inhaled fenoterol enters the gastrointestinal tract. Suction is biphasic – 30% of fenoterol is rapidly absorbed with a half-life (T1 / 2) 11 minutes and 70% slowly absorbed from T1 / 2 – 120 minutes. There is no correlation between the concentrations of fenoterol in blood plasma is achieved after inhalation, and pharmacodynamic curve “time effect”. Long (3-5 hours) bronchodilatory effect after inhalation of the drug that is comparable with the respective effects achieved after intravenous administration, is not supported fenoterol high concentrations in the systemic circulation. After oral administration absorbed about 60% of fenoterol. Time of maximum plasma concentration is 2 hour.
Distribution
Ipratropium bromide, a quaternary amine which is poorly soluble in fats and weakly penetrates through biological membranes. Not accumulates. Ipratropium bromide binds to plasma proteins to a minimum extent (less than 20%). No information about the possibility of penetration of ipratropium bromide through the placental barrier and into breast milk.
Fenoterol is distributed rapidly to organs and tissues. Communication with the plasma proteins is 40-55%. Fenoterol unaltered cross the placental barrier and is excreted in breast milk.
Metabolism
Ipratropium bromide is metabolized by oxidation primarily in the liver.
It is known to 8 ipratropium bromide metabolites, which are poorly bind to muscarinic receptors and are considered inactive.
Fenoterol metabolized in the liver. After 24 hours 60% of the intravenously administered dose and 35% of an oral dose is excreted in the urine. This fraction fenoterol biotransformation due to “first-pass” effect through the liver, resulting in drug bioavailability after oral administration of drops to about 1.5%. This explains the fact that the amount of drug swallowed virtually no effect on the concentration of the active substance in the blood plasma is reached after inhalation. Biotransformation of fenoterol in man occurs principally by conjugation with sulphates in the intestinal wall.
breeding
Ipratropium bromide is derived mainly through the intestine and through the kidneys.
About 25% is excreted unchanged in the rest – in the form of metabolites.
Fenoterol excreted by the kidneys and in bile as inactive sulfate conjugates. In parenteral administration, fenoterol respectively output three-phase model with half-lives – 0.42 minutes, 14.3 minutes and 3.2 hours.
Pharmacokinetics in specific patient groups
Pharmacokinetics combined preparation comprising ipratropium bromide and fenoterol, patients with diabetes, patients of advanced age and older and children, and in patients with impaired hepatic and renal function was not studied.
Pregnancy and breast-feeding
These pre-clinical studies and the current clinical experience with the combination of fenoterol and ipratropium bromide showed that the active ingredients that make up the combination product, no adverse effects during pregnancy. It is necessary to consider the possibility of an inhibitory action of fenoterol on uterine activity. The drug is contraindicated Ipraterol-native in the I trimester of pregnancy. It should be used with caution in drug Ipraterol-native in the II and III trimester of pregnancy (possible weakening of labor).
Fenoterol passes into breast milk. Data confirming that ipratropium bromide penetrates into breast milk, are not obtained. Safety of the drug during breast-feeding has not been established. In this regard, use of the drug Ipraterol- native breastfeeding period is possible only when the potential risk to the child’s potential benefit to the mother.
Conditions of supply of pharmacies
Prescription.
side effects
Determination of the frequency: very often (> 1/10), often (1/100 to 1/10) infrequently (from 1/1000 to 1/100), rare (from 1/000 to 1/10000), very seldom (
From the nervous system: often – a fine tremor of skeletal muscles, nervousness; rarely – headache, dizziness, rarely – change of mentality.
With the cardiovascular system: often – tachycardia, including supraventricular tachycardia; palpitations (especially in patients with aggravating factors); rarely (if used in high doses) – decrease in diastolic blood pressure, systolic blood pressure, arrhythmias (including atrial fibrillation..).
The respiratory system: rarely – cough, local irritation of the respiratory tract, pharyngitis; very rarely – paradoxical bronchospasm, laryngospasm.
Gastro-intestinal tract: often – dry mouth; infrequently – a violation of motility of the gastrointestinal tract, vomiting, constipation, diarrhea (especially in patients with cystic fibrosis).
From a sight organ: If the product enters the eye – mydriasis, increased intraocular pressure, glaucoma, pain in the eyeball; sometimes observed in the treatment of drug reversible accommodation disturbances and glaucoma.
Pain in the eyeball or discomfort, blurred vision, feeling ghosting or color spots before the eyes, combined with conjunctival hyperemia and corneal edema may be signs of acute glaucoma. Constricts the pupil should be used drops and immediately contact an ophthalmologist.
Allergic reactions: seldom – skin rash, angioedema swelling of the tongue, lips and face, urticaria.
Other: urinary retention, increased sweating, hypokalemia, a sense of general weakness, myalgia.
special instructions
In the event of an unexpected rapid amplification of dyspnea (difficulty breathing) should seek medical advice immediately.
In children, the drug Ipraterol-native should be used only on a doctor’s prescription and under supervision of an adult.
Hypersensitivity
After the drug-native Ipraterol may arise immediate hypersensitivity reactions, features which in rare cases can be: urticaria, angioedema, skin rashes, bronchospasm, oropharyngeal edema, anaphylactic shock.
paradoxical bronchospasm
Preparation Ipraterol native-like and other inhalable medicaments can cause paradoxical bronchospasm, which can be life threatening. In the case of paradoxical bronchospasm drug application Ipraterol-native should be discontinued immediately and switch to an alternative therapy.
Prolonged use in patients suffering from bronchial asthma, drug-Ipraterol native should be used only when necessary; in patients with COPD, mild symptomatic treatment may be preferable to regular use; – patients with bronchial asthma patients should be aware of the need for strengthening or anti-inflammatory therapy to control airway inflammation and the disease process.
Регулярное применение возрастающих доз лекарственных средств, содержащих бета2-адреномиметики, таких как препарат Ипратерол-натив, для купирования бронхиальной обструкции может вызвать неконтролируемое ухудшение течения заболевания. В случае усиления бронхиальной обструкции увеличение дозы бета2-адреномиметиков, в том числе препарата Ипратерол-натив, больше рекомендуемой в течение длительного времени не только не оправдано, но и опасно. Для предотвращения угрожающего жизни ухудшения течения заболевания следует рассмотреть вопрос о пересмотре плана лечения пациента и адекватной противовоспалительной терапии ингаляционными глюкокортикостероидами.
Другие симпатомиметические бронходилататоры следует назначать одновременно с препаратом Ипратерол-натив только под медицинским наблюдением.
Disorders of the gastrointestinal tract
У пациентов, имеющих в анамнезе муковисцидоз, возможны нарушения моторики желудочно-кишечного тракта.
Violations by the organ of vision
Препарат Ипратерол-натив должен применяться с осторожностью у пациентов, предрасположенных к закрытоугольной глаукоме. Известны отдельные сообщения об осложнениях со стороны органа зрения (например, повышение внутриглазного давления, мидриаз, закрытоугольная глаукома, боль в глазах), развившихся при попадании ингаляционного ипратропия бромида (или ипратропия бромида в сочетании с бета2-адреномиметиками) в глаза. Симптомами острой закрытоугольной глаукомы могут быть боль или дискомфорт в глазах, затуманивание зрения, появление ореола вокруг предметов и цветных пятен перед глазами в сочетании с отеком роговицы и покраснением глаз вследствие гиперемии конъюнктивы. Если развивается любая совокупность этих симптомов, показаны применение глазных капель, снижающих внутриглазное давление, и немедленная консультация специалиста. Пациенты должны быть проинструктированы о правильном применении ингаляционного препарата Ипратерол-натив. Для предупреждения попадания раствора в глаза рекомендуется, чтобы раствор, используемый с помощью небулайзера, вдыхался через мундштук. При отсутствии мундштука должна использоваться плотно прилегающая к лицу маска. Особенно тщательно должны заботиться о защите глаз пациенты, предрасположенные к развитию глаукомы.
Системные эффекты
При таких заболеваниях, как недавно перенесенный инфаркт миокарда, сахарный диабет с неадекватным гликемическим контролем, тяжело протекающие органические заболевания сердца и сосудов, гипертиреоз, феохромоцитома или обструкция мочеиспускательных путей (например, при гиперплазии предстательной железы или обструкции шейки мочевого пузыря) препарат Ипратерол-натив должен применяться только после тщательной оценки риск/польза, особенно при использовании доз, превышающих рекомендуемые.
Влияние на сердечно-сосудистую систему
Отмечались редкие случаи возникновения ишемии миокарда при приеме бета2- адреномиметиков. Пациентов с сопутствующими серьезными заболеваниями сердца (например, ишемической болезнью сердца, аритмиями или выраженной сердечной недостаточностью), получающих препарат Ипратерол-натив, следует предупреждать о необходимости обращения к врачу в случае появления болей в сердце или других симптомов, указывающих на ухудшение заболевания сердца. Необходимо обращать внимание на такие симптомы, как одышка и боль в груди, так как они могут быть как сердечной, так и легочной этиологии.
Гипокалиемия
При применении бета2-адреномиметиков может возникать гипокалиемия (см. раздел «Передозировка»).
У спортсменов применение препарата Ипратерол-натив в связи с наличием в его составе фенотерола может приводить к положительным результатам тестов на допинг.
Effect on the ability to drive mechanisms and
Исследований влияния комбинированного препарата, содержащего ипратропия бромид и фенотерол, на способность к управлению транспортными средствами и механизмами не проводилось. Однако, поскольку при применении препарата возможно развитие таких нежелательных реакций, как головокружение, нервозность, тремор, нарушение аккомодации глаз, мидриаз и затуманивание зрения, следует соблюдать осторожность при управлении транспортными средствами и механизмами, а также при занятиях другими потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций.
Storage conditions
In the dark place at a temperature not higher than 25 ° C.
Do not freeze.
Keep out of the reach of children.
Dosing and Administration
Во время проведения терапии требуется медицинское наблюдение (например, в условиях стационара). Лечение в домашних условиях возможно только после консультации с врачом в тех случаях, когда быстродействующий бета-агонист в низкой дозе недостаточно эффективен. Так же раствор для ингаляций может быть рекомендован пациентам в случае, когда аэрозоль для ингаляций не может использоваться или при необходимости применения более высоких доз.
Доза должна подбираться индивидуально в зависимости от остроты приступа. Лечение обычно должно начинаться с наименьшей рекомендуемой дозы и прекращаться после того как достигнуто достаточное уменьшение симптомов. The recommended dose:
У взрослых (включая пациентов пожилого и старшего возрастов) и подростков старше 12 лет
Острые приступы бронхиальной астмы
В зависимости от тяжести приступа дозы могут варьировать от 1 мл (1 мл = 20 капель) до 2,5 мл (2,5 мл = 50 капель). В особо тяжелых случаях возможно применение доз, достигающих 4 мл (4 мл = 80 капель).
У детей в возрасте 6-12 лет
Острые приступы бронхиальной астмы
В зависимости от тяжести приступа дозы могут варьировать от 0,5 мл (0,5 мл = 10 капель) до 2 мл (2 мл = 40 капель).
У детей в возрасте младше 6 лет (масса тела которых составляет менее 22 кг)
В связи с тем, что информация о применении препарата в этой возрастной группе ограничена, рекомендуется использование следующей дозы (только при условии медицинского наблюдения): около 25 мкг ипратропия бромида и 50 мкг фенотерола гидробромида = 0,1 мл (2 капли) на кг массы тела (на одну дозу), но не более 0,5 мл (10 капель) (на одну дозу).
Раствор для ингаляций следует использовать только для ингаляций (с подходящим небулайзером) и не применять перорально.
Лечение следует обычно начинать с наименьшей рекомендуемой дозы.
Рекомендуемая доза должна разводиться 0,9 % раствором натрия хлорида до конечного объема, составляющего 3-4 мл, и применяться (полностью) с помощью небулайзера.
Препарат Ипратерол-натив для ингаляций не должен разводиться дистиллированной водой.
Разведение раствора должно осуществляться каждый раз перед применением, остатки разведенного раствора следует уничтожать.
Разведенный раствор следует использовать сразу после приготовления.
The duration of inhalation can be controlled by spending diluted volume.
Препарат Ипратерол-натив для ингаляций может применяться с использованием различных коммерческих моделей небулайзеров. Доза, достигающая легких, и системная доза зависят от типа используемого небулайзера и могут быть выше, чем соответствующие дозы при использовании дозированного аэрозоля. В тех случаях, когда имеется настенный кислород, раствор лучше всего применять при скорости потока 6 – 8 литров в минуту.
Необходимо следовать инструкции по применению, обслуживанию и чистке прибора, поставляемой совместно с небулайзером.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg
Manufacturer

FT SYNTHESIS

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