Farm effects Albuterol Inhalation:
Albuterol Inhalation Bronchodilator. At therapeutic doses, has a pronounced stimulatory effect on beta 2-adrenergic receptors of the bronchi, blood vessels and myometrium. Virtually no effect on beta1-adrenergic receptors in heart.
Inhibits the release of mast cell histamine, leukotrienes, PgD2 and other biologically active substances for a long time.
Inhibits early and late bronchial reactivity. It has a pronounced effect of bronchodilators, warning or kupiruya bronchospasm, reduces airway resistance, increases the VC. Positive effect on the mucociliary clearance (with chronic bronchitis increases it by 36%), stimulates mucus secretion, activates the function of ciliated epithelium.
Inhibits the release of inflammatory mediators from mast cells and basophils, in particular anti-IgE-induced release of histamine, which eliminates the suppression antigenzavisimoe mucociliary transport and separation factor of chemotaxis of neutrophils. Prevents the development of allergen-induced bronchospasm.
May cause a reduction in the number of beta-adrenergic receptors, including on lymphocytes. It has a number of metabolic effects: it reduces the concentration of K + in the plasma affects glycogenolysis and insulin release, has hyperglycemic (especially in patients with bronchial asthma) and the lipolytic effect, increases the risk of acidosis.
In the recommended therapeutic doses has no negative effect on the cardiovascular system, causes no increase in blood pressure. To a lesser extent compared with drugs of this group has a positive chronotropic and inotropic effect. Causes dilation of coronary arteries. It has a tocolytic effect – lowers the tone and the contractile activity of myometrium.
After ingestion neprolongirovannogo lekform beginning of the effect – within 30 minutes, maximum – 2 hours while taking the syrup and 2-3 h with the pill, duration – 4-6 hours for a solution. Prolonged forms of the drug by a gradual release of active substances through the membrane tablets provide the necessary plasma concentration to maintain the therapeutic effect within 12-14 hours
Pharmacokinetics of Albuterol Inhalation:
If ingestion absorption – high. Food intake decreases the rate of absorption, but does not affect bioavailability. After a single oral administration of 4 mg tablets or syrup Cmax – 18 ng / ml after ingestion of tablets at a dose of 2 mg every 6 hours, Cmax – 6.7 ng / m, after ingestion of tablets at a dose of 4 mg every 6 hours, Cmax – 14.8 ng / ml after oral administration of prolonged lekform 4 mg every 12 hours, Cmax – 6.5 ng / ml. Relationship to plasma proteins – 10%. Crosses the placenta.
Undergoes first-pass metabolism in the liver and intestinal wall, through fenolsulfotransferazy inactivated by 4-0-sulfate ester. T1 / 2 – 3.8-6 hours
Excreted by the kidneys (69-90%), mainly as an inactive metabolite fenolsulfatnogo (60%) for 72 h and in bile (4%).
Indications Albuterol Inhalation:
Inside – bronhospastichesky syndrome, bronchial asthma (including nocturnal – long-acting forms) – the prevention and relief, COPD.
Parenteral – bronhospastichesky syndrome (mild).
Parenteral (with subsequent transfer to intake): threatening preterm labor with the appearance of contractile activity, isthmic-cervical insufficiency, fetal bradycardia (depending on uterine contractions in the uterine cervix opening times and expulsion); operations on pregnant uterus (the imposition of a circular weld at failure internal uterine os.)
Category of the fetus Albuterol Inhalation:
Category effects on the fetus. C ( Study of Reproduction in animals showed adverse effects on the fetus and adequate and well controlled studies in pregnant women is not held, but the potential benefits associated with the use of drugs in pregnancy, may justify its use, despite the risks.)
Contra Albuterol Inhalation:
Hypersensitivity, pregnancy (when used as a bronchodilator), lactation, infancy (younger than 6 years – for tablets, under 2 years – for oral solution and syrup).
For / in the introduction as a tocolytic agent (optional) – infection of the birth canal, fetal death, fetal malformations, bleeding from placenta previa or premature placental abruption, threatening miscarriage (in I-II trimester of pregnancy).
With caution. Tachyarrhythmias, severe heart failure, hypertension, hyperthyroidism, tachyarrhythmias, pheochromocytoma, pregnancy, lactation, coronary heart disease (angina, myocardial infarction), myocarditis, heart defects, aortic stenosis, diabetes, epilepsy, seizures, gastrointestinal stenosis (including piloroduodenalny).
Dosing Albuterol Inhalation:
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.
Sustained-release 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 hours). Tablets swallowed whole without chewing.
Intravenous – with severe bronchospasm in / bolus over 2-5 minutes with 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 / in the required concentration of 0.01 mg / ml solution of salbutamol 5 mg diluted with 500 ml of solvent (water for injection, 0.9% sodium chloride, 5% dextrose).
As a tocolytic agent – in / drip, 2.5-5 mg (1-2 ampoules) was dissolved in 500 ml 0.9% NaCl or 5% dextrose. Speed in / drip (20-40 drops / min) depends on the intensity of uterine activity and tolerability of (pulse pregnant should not be more 120/min). Further held oral maintenance therapy – 2-4 mg 4-5 times a day. The first tablet is prescribed for 15-30 minutes before the end of infusion. The course of treatment – 14 days.
Side effects: Albuterol Inhalation:
Often – palpitations, tachycardia (during pregnancy – the mother and fetus), headache, tremor, nervousness;
less often – dizziness, insomnia, muscle cramps, nausea, vomiting, sweating;
rare – allergic reactions (hives, skin rash, angioedema, paradoxical bronchospasm, erythema multiforme, Stevens-Johnson syndrome, arrhythmia, chest pain, hypokalemia, neuropsychiatric disorders (including psychomotor agitation, disorientation, impaired memory, aggressiveness, panic, hallucinations, suicide attempts, schizophreniform disorder, delay mochi.Peredozirovka: Symptoms of acute poisoning: angina pectoris, tachycardia (heart rate of 200 beats per minute), tachycardia, arrhythmia, dizziness, dryness of mucous membranes of the mouth, fatigue, headache, hyperglycemia (alternate hypoglycemia), decreased or increased blood pressure, hypokalemia, insomnia, malaise, nausea, nervousness, convulsions, tremor.
Treatment: symptomatic, with an overdose of tablets of the drug forms – gastric lavage, with tachyarrhythmias enter cardioselective beta-blockers (with caution because of the risk of bronchospasm).
Interaction:
Enhances the effect of CNS stimulants, tachycardia in patients with hyperthyroidism and the risk of arrhythmias in patients receiving cardiac glycosides.
One-time use of salbutamol reduces the concentration of digoxin by 16-22% against the 10-day treatment of the latter (the clinical significance has not, should monitor the concentration of digoxin in the blood).
The probable increase in heart rate and blood pressure in patients receiving salbutamol may necessitate a dose adjustment of antihypertensive and antianginal drugs.
Theophylline and other xanthine, while the application increases the risk of tachyarrhythmias; means for inhalation anesthesia, levodopa – serious ventricular arrhythmias.
MAO inhibitors and tricyclic antidepressants increase the effect of salbutamol in the SCA.
Incompatible (pharmacological antagonism) with nonselective beta-blockers (which must also be taken into account in applying eye forms of beta-adorenoblokatorov).
Simultaneous with the appointment of anticholinergic agents (including inhaled) can increase intraocular pressure.
Diuretics and corticosteroids increase the effect of salbutamol gipokaliemicheskoe.
Cautions:
Frequent use of salbutamol may exacerbate bronchospasm, a sudden death, and therefore between taking regular doses of the drug to take breaks in a few hours (6 hours). The reduction of these intervals can only occur in exceptional cases.
If necessary, use during lactation should cease to be careful (not known whether salbutamol in breast milk).
Strictly controlled clinical studies on the teratogenicity of salbutamol is not carried out. In separate studies revealed polydactyly in children at the background of mothers during pregnancy, salbutamol (an unambiguous causal connection of her drug-not installed). In experimental studies have revealed the presence of a teratogenic effect of salbutamol: in mice with s / c infusion (dose, 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 skull.
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 can cause tachycardia and hyperglycemia in the mother (especially if you have diabetes) and the fetus, and cause a delay of a mother in labor, reduction in blood pressure, acute pulmonary edema and NC.
