The instruction for medical use of ASKORIL EKSPEKTORANT medicine the Trade name Askoril Expektorant the International unlicensed name Is not present the Dosage form Oral solution, 100 ml Structure of 10 ml of solution contain active agents: salbutamol sulfate of 2.4 mg (it is equivalent to salbutamol of 2.00 mg) Bromhexine a hydrochloride of 4.00 mg gvayfenezin 100.00 mg, excipients: Natrium benzoicum, sodium chloride, sodium citrate, a sucralose, citric acid monohydrate, fragrance ID20158 blackcurrant, fragrance pineapple, menthol (left menthol), the water purified. Description Colourless or yellowish solution. Pharmacotherapeutic group Drugs for treatment of obstructive respiratory diseases. Sympathomimetics for system use. Sympathomimetics in a combination with other drugs for treatment of obstructive respiratory diseases. The ATX R03CK code the Pharmacological Pharmacokinetics Salbutamol properties is well soaked up in digestive tract with bioavailability of 50% – 85%. Peak plasma concentration (Cmax) come in 1 – 4 hour (Tmax) after oral administration of salbutamol. Meal does not influence bioavailability of salbutamol. Linking with proteins of plasma makes 10%. Volume of distribution (Vd) 156 +/-38 of liters. Salbutamol is metabolized in a liver in an active metabolite – ester 4-O-sulfate. Salbutamol with urine – 64% and with bile is removed. Elimination half-life of salbutamol makes 3 – 6.5 h. Bromhexine is well soaked up from digestive tract. Maximum concentration in plasma (Cmax) it is observed in 1 hour after oral administration. Bromhexine is metabolized in a liver in an active metabolite Ambroxol. Bromhexine is excreted mainly with urine in the form of metabolites. Only a small amount is removed in an invariable look. Elimination half-life (T ½) Bromhexine makes 6.5 hours. Gvayfenezin is well soaked up from digestive tract. 60% of a gvay-fenezin are hydrolyzed in blood within 7 hours with forming of ß-2-of metoksifenol-lactic acid. Gvayfenezin is excreted with urine in the form of metabolites. Elimination half-life (T ½) makes 1 hour. A pharmacodynamics Askoril Expektorant – the combined drug with bronkho-dilatiruyushchy, mucolytic and expectorant action. Thanks to a rational combination of salbutamol, Bromhexine of a hydrochloride, the gvayfenezina effectively and quickly decreases expressiveness of functional disturbances from a respiratory system. Salbutamol — selection agonist β2-адренорецепторов, has broncholitic effect, stops a bronchospasm. Stimulates beta adrenoceptors of bronchial tubes, myometrium and blood vessels. The action mechanism – elimination of spasms of bronchial tubes, increasing at the same time the vital capacity of lungs. Salbutamol – a direct sympathomimetic which selectively works on β2-adrenoceptors, stimulating an adeniltsilaza – enzyme which catalyzes forming cyclic 3, 5-adenosine of monophosphate (cyclic AMF) from adenosine of triphosphate (ATP). Increase in level cyclic ATP causes relaxation of bronchial muscles and slows down release of mediators from mast cells and improves transport mechanisms of a ciliate epithelium. Bromhexine the hydrochloride has mucolytic effect. Bromhexine – derivative benzylamine, derivative a vazitsin and adatoidny acid – the alkaloids received from plant Adatoda vascular. Reduces viscosity of a bronchial secret due to depolarization of acid mucopolysaccharides and stimulation of secretory cells of mucous membranes of bronchial tubes. Bromhexine activates cilia of a ciliary epithelium of a mucous trachea and bronchial tubes, normalizes the broken ratio between the making phlegm components, increasing its serous component, and as a result of it its viscosity decreases and volume increases that improves an otkhozhdeniye and expectoration of a phlegm. Bromhexine also increases secretion of excretory glands and stimulates production of pulmonary surfactant. Gvayfenezin reduces surface intention and adhesive properties of a phlegm, promotes expectoration. This mucolytic means which activates secretory cells of a ciliary epithelium of a mucous membrane of bronchial tubes which produce neutral polysaccharides, depolimeriziruya acid mucopolysaccharides. As a result of it the viscosity of a phlegm decreases, the tsiliarny device of bronchial tubes is activated, and the otkhozhde-niya of a phlegm leads to simplification and promotes change of unproductive cough on productive. Indications – the cough connected with a bronchospasm in respiratory diseases (acute and chronic bronchitis, pneumonia, the chronic obstructive pulmonary disease (COPD), bronchial asthma, emphysema of lungs and others) as a part of complex therapy the Route of administration and doses Inside. Adults and children are more senior than 12 years – on 10 ml (2 teaspoons) 3 times a day. Children from 6 to 12 years – on 5 ml (1 teaspoon) 3 times a day, Children from 2 to 5 years – on 2.5 ml (1/2 teaspoons) 3 times a day, are not recommended to children 2 years are younger. Duration of treatment is defined individually. The maximum course of treatment – 10 days. Side effects Often – nausea, vomiting, the dispepsichesky phenomena, diarrhea, exacerbation of a peptic ulcer of a stomach and duodenum, it is rare – passing expansion of peripheral vessels, a lowering of arterial pressure, increase in arterial blood pressure, collapse, a headache, dizziness, moderate tachycardia – the increased nervous irritability, irritability, concern – a tremor, muscular spasms, a sleep disorder, insomnia, drowsiness – allergic reactions, including a Quincke’s disease, skin rash, nettles – Nice, a paradoxical bronchospasm – a hypopotassemia – coloring of urine in pink color – unpleasant feelings in a breast – dryness of an oral cavity, unusual taste – epigastric pains Very seldom – increase in activity of transaminases of a liver – difficulty at urination – the Contraindication urolithiasis – hypersensitivity to active and to excipients of drug – simultaneous use of antibechics, non-selective blockers of beta adrenoceptors, monoamine oxidase inhibitors, cardiac glycosides – tachycardia, myocarditis, heart diseases – a peptic ulcer of a stomach and duodenum (in a stage obostre-a niya) – gastric bleeding – a hyperthyroidism – glaucoma – hereditary intolerance of fructose, a glyukozo-galaktozny malyabsorbtsionny syndrome, deficit sukrazy-isomaltases – dekompensirovanny diabetes – a liver and/or renal failure – pregnancy, the lactation period – children’s up to 2 years Medicinal interactions Other beta2-adrenomimetichesky means and theophylline strengthen effect of salbutamol and increase the probability of emergence of side effects. It is not recommended to use drug along with such non-selective blockers of beta adrenoceptors as propranolol. The salbutamol which is a part of the drug Askoril Expektorant is not recommended to patients who receive monoaminooxidase inhibitors. Diuretics and drugs of glucocorticosteroids strengthen a gipokaliyemiches-cue effect of salbutamol. Co-administration with the antibechic drugs Askorila Expektorant complicates an otkhozhdeniye of the diluted phlegm therefore it is not recommended to take these drugs together. Salbutamol increases risk of intoxication glycosides at joint use. Salbutamol reduces anti-anginal effect of nitrates. Bromhexine is not compatible to alkaline solutions. The special instructions Being a part of drug Bromhexine promotes penetration of antibiotics (erythromycin, cefalexin, Oxytetracyclinum) into pulmonary fabric. It is not recommended to accept alkaline drink along with drug. Gvayfenezin paints urine in pink color. According to the recommendations of the Joint advisory council about foodstuff and the Joint committee on FAO/BO3 nutritional supplements, the daily dose of consumption of a sucralose should not exceed 15 mg/kg of body weight. The sucralose has no energy value as it is not metabolized in an organism. It can be used by all people, including the pregnant women feeding women and children of any age. This sweetener does not influence the level of glucose and insulin of blood as it is not split in an organism, unlike sucrose therefore can without fears be applied in diabetes (N. Mezitis et al., 1994.1997). Studying influence of a sucralose on various physiological indicators at experimental animals and people (more than 100 researches for 20 years) was shown by its safety and harmlessness. It is proved that the sucralose has no damaging effect on enamel of teeth, does not cause genetic and immunospecific injurys, has no cancerogenic and teratogenic properties. As drug is multicomponent and contains sodium chloride and sodium citrate and fragrances, it is necessary to appoint with care the patient with disturbance of secretory function of kidneys, at a hypopotassemia, to the persons keeping to a saltless diet. Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms Considering that at sensitive patients at use can arise tachycardia, the tremor of hands, muscular spasms for the period of administration of drug is better to refrain from the control of vehicles and mechanisms, performance of work demanding concentration of attention. Overdose Symptoms – tachycardia, excitement, a tremor, a hypopotassemia, a hyperpotassemia, nausea, vomiting, an urolithiasis. Treatment is symptomatic. A form of release and packing On 100 ml of solution in a bottle from dark plastic. On 1 bottle together with the instruction for medical use in the state and Russian languages put in a pack from cardboard. To Store storage conditions in the dry, protected from light place at a temperature not above 25ºС. Not to freeze! To store out of children’s reach! A period of storage 2 years the use Period after opening of a bottle – 45 days. Not to use after expiry date. Prescription status According to the prescription of Proizvoditel Glenmark Pharmasyyutikalz Ltd, Villedzh Kishanpura, Baddi-Nalagarkh Road Tekhsil Buddy, Distt. Solana, Naymikel of Pradish-173205, India. The owner of the registration certificate of Glenmark Pharmasyyutikalz Ltd, India the Address of the organization accepting in the territory of the Republic of Kazakhstan claims on quality of products from consumers of Predstavitelstvo Glenmark Pharmasyyutikalz LTD in RK, 050005, Almaty, Al-Farabi Avenue, 7, business center of “Nurla Tau”, block 4 A, office 7.