Albuterol (Generic)
Dosage form:
Concentrate for solution for infusion, syrup, tablets, coated tablets, tablets long-acting, long-acting tablets albuterol sulfate.
Pharmacological Effects:
Bronchodilator. In therapeutic doses has a pronounced stimulatory effect on beta2-adrenergic receptors of the bronchi, blood vessels and myometrium. Virtually no effect on beta1-adrenergic receptors of the heart. Inhibits release of mast cell histamine, leukotrienes, PgD2 and other biologically active substances in a long time. Inhibits early and late bronchial reactivity. Has a pronounced effect of bronchodilators, warning or kupiruya bronchial spasms, reduces the resistance in the airways, increases the vital capacity. Positive effect on mucociliar clearance (in case of chronic bronchitis increases it by 36%), stimulates mucus secretion, activates the function of the ciliated albuterol inhaler. Inhibits the release of inflammatory mediators from mast cells and basophils, in particular anti-IgE-induced release of histamine, eliminates antigenzavisimoe suppression mucociliary transport and the allocation of neutrophil chemotactic factor. Prevents the development of allergen-induced bronchospasm. Can cause reduction in the number of beta-adrenergic receptors, including on lymphocytes. Has a number of metabolic effects: reduces the concentration of K + in the plasma affects glycogenolysis and insulin release, has a hyperglycemic (especially in patients with bronchial asthma) and the lipolytic effect, increases the risk of acidosis. The recommended therapeutic doses has no negative effect on the cardiovascular system, does not cause increase blood pressure. To a albuterol side effects extent compared with LS in this group, has a positive chrono-and inotropic effects. Causes dilation of coronary arteries. Has tocolytic effect – reduces tone and contractile activity of myometrium. After ingestion neprolongirovannyh lekform beginning effect – within 30 minutes, maximum – 2 hours at the reception syrup and 2-3 h while taking pills, duration – 4-6 hours for a solution. Prolonged forms of the drug by gradually releasing the active ingredient through the shell tablets provide the necessary concentration in plasma to maintain the therapeutic effect within 12-14 hours
Indications:
Inside – bronchospastic syndrome, bronchial asthma (including night – prolonged form) – prevention and cupping, COPD (including chronic bronchitis, emphysema). Parenteral – bronchospastic syndrome (docking). Parenteral followed by transfer to intake): threatening preterm labor with the appearance of contractile activity; isthmic-cervical insufficiency, fetal bradycardia (depending on uterine contractions during periods of disclosure and the is albuterol a steroid of the uterine cervix) operation on the pregnant uterus (the imposition of a circular weld at failure of internal uterine throat).
Contraindications:
Hypersensitivity, pregnancy (when used as a bronchodilator), lactation period, children’s age (under 6 years – for tablets, under 2 years – for a solution for oral administration and syrup). In order to / in the introduction as Tocolytic (optional) – infection of the birth canal, intrauterine fetal death, fetal malformation, bleeding with albuterol meter dose inhaler previa or premature placental abruption, threatening miscarriage (in I-II trimester of pregnancy). C care. Tachyarrhythmia, severe heart failure, hypertension, thyrotoxicosis, tachyarrhythmia, pheochromocytoma, pregnancy, lactation, coronary heart disease (angina, myocardial infarction), myocarditis, heart defects, aortic stenosis, diabetes, epilepsy, convulsions, stenosis of the digestive tract (including piloroduodenalny)
Side effects:
Often – palpitations, tachycardia (in pregnancy – the mother and fetus), headache, tremor, nervous tension, less often – dizziness, insomnia, muscle cramps, nausea, vomiting, sweating, rarely – Allergic reactions (urticaria, rash, angioneurotic swelling, paradoxical bronchospasm, erythema multiforme, Stevens-Johnson bronchospasm albuterol atrovent racemic epinephrine, arrhythmia, chest pain, hypokalemia, neuropsychiatric disorders (including psychomotor agitation, disorientation, impaired memory, aggressiveness, panic, hallucinations, suicide attempts, schizophrenia-like disorders delay mochi.Peredozirovka. Symptoms of acute poisoning: angina pectoris, tachycardia (a heart rate of 200 beats per minute), heart rate, arrhythmia, dizziness, dry mouth, fatigue, headache, hyperglycemia (replaced by hypoglycemia), decreased or increased blood pressure, hypokalemia, insomnia, malaise, nausea, nervous tension, spasms, tremors. Treatment: symptomatic, with an overdose of tablets forms of the drug – a gastric lavage, with tachyarrhythmias enter cardioselective beta-blockers (with caution because of the risk of bronchospasm).
Dosage and administration:
Inside: adults and children over 12 years – 2-4 mg 3-4 times a day, if necessary, may increase the dose to 8 mg 4 times a day. The maximum daily dose – 32 mg. Children 6-12 years – 2 mg 3-4 times per day, maximum dose – 24 mg / day, 2-6 years – 1-2 mg (0.1 mg / kg) 3-4 times per day. Prolonged Action Tablets: Adults and children over 12 years – 4-8 mg every 12 hours, maximum dose – 32 mg / day (16 mg every 12 hours) for children 6-12 years of 4 mg every 12 hours, the maximum dose – 24 mg / day (12 mg every 12 h). Swallow tablets whole, without chewing. Intravenous – in severe bronchospasm in / in bolus over 2-5 minutes by 0.25 mg (4 mg / kg) if necessary, every 15 minutes or infusion, at 0.005 mg / min with increasing dose if necessary after 15-30 min intervals until 0.01-0.02 mg / min. To prepare the solution for i / in the introduction of the necessary concentration of 0.01 mg / ml of 5 mg albuterol nebulizer solution diluted with 500 ml of solvent (water for injection, 0.9% sodium chloride solution, 5% dextrose solution). As tocolytic means – in / drip, 2.5-5 mg (1-2 ampoules) was dissolved in 500 ml 0.9% NaCl solution or 5% dextrose solution. Speed w / drip (20-40 cps / min) depends on the intensity of uterine activity and tolerability of the drug (pulse pregnant should not be more 120/min). Then held oral maintenance therapy – at 2-4 mg 4-5 times a day. The first tablet prescribed for 15-30 minutes before the end of infusion. Course of treatment – 14 days.
Cautions:
Frequent use of salbutamol may lead to increased bronchoconstriction, sudden cardiac death, and therefore between-meal regular doses of the drug to take breaks in a few hours (6 h). Reduction of these intervals can occur only in exceptional cases. If necessary, the appointment during lactation should cease to be nebulizer albuterol (not known whether salbutamol in breast milk). Strictly controlled clinical studies on the teratogenicity of salbutamol is not held. In separate studies found Polydactyly in children while taking their mothers during pregnancy, salbutamol (an unambiguous causal connection with its emergence taking this medication is not installed). In experimental studies revealed the presence of a teratogenic effect of salbutamol: in mice with the s / c infusion (dose of 11.5-115 times the maximum recommended in humans for inhalation) noted the development of cleft palate, in rabbits at oral assignment (the dose of 2315 times exceeding the maximum for inhalation) – cleft the skull bones. Adrenergic bronchodilators may be used during pregnancy because the potential risk to the fetus placental hypoxemia on the background of uncontrolled asthma is much greater than the risk associated with their use. However, their use during pregnancy should be careful because it may cause albuterol inhalers and hyperglycemia in the mother (especially in the presence of diabetes), and the fetus and the mother cause delay generic activity, lower blood pressure, acute pulmonary edema, and NC.
Interaction:
Enhances the effect of CNS stimulants, tachycardia in patients with thyrotoxicosis and the likelihood of arrhythmia while taking cardiac glycosides. One-time use of salbutamol reduces the concentration of digoxin at 16-22% against the 10-day treatment of the latter (clinical significance is not should monitor the concentration of digoxin in the blood). Likely increase in heart rate and blood pressure while taking salbutamol may necessitate a dose adjustment of antihypertensive and antianginal drugs. Theophylline and other xanthine, while the application increases the risk of what is albuterol sulfate; means for inhalation anesthesia, levodopa – serious ventricular arrhythmias. MAO inhibitors and tricyclic antidepressants, increasing the effect of salbutamol, may lead to a sharp decline in AD. Incompatible (pharmacological antagonism) with a nonselective beta-blockers (which must also be considered when applying eye forms of beta-adorenoblokatorov). Concurrent administration of anticholinergic agents (including inhalants) can increase intraocular pressure. Diuretics and GMP reinforce gipokaliemicheskoe effect of albuterol and pregnancy.
