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Steroid Hormone Powder:

Pharmacological effects

To beta 2 receptor has high selectivity, airway smooth muscle to catechu oxygen methyl transformation of the enzymes and monoamine oxidation resistance increases, the duration extension, of the excitation of the heart is very small. In vitro experiments, the selectivity index of salbutamol was 250, terbutaline 138, and supradenin of isoproteradrenal gland 1.4. Comparison of FEV1 and heart rate changes between intravenous salbutamol and supradrenal gland isoproterenol in 1 second forced expiratory volume (FEV1) showed that lower salbutamol dose of 0.1μg/kg per minute could significantly increase FEV1. With the increase of dose, heart rate was accelerated, indicating high selectivity. However, supradenin of isoproteradrenal gland can accelerate heart rate when increasing the dose of FEV1, with poor selectivity.

pharmacokinetics

Since salbutamol is not easily destroyed by sulfatase in the digestive tract and catechol-oxo-methyltransferase in the tissue, it is effective when taken orally and lasts for a long time. Oral bioavailability was 30%, the effect was 15-30min after administration, the peak time of plasma concentration was 2-4h, and the effect lasted more than 6h. The elimination half-life is 2.7 ~ 5h. 90% of salbutamol 8mg controlled release tablets were released at a steady rate of 0.8mg/h after repeated administration in healthy volunteers. Constant release of the drug avoids fluctuations in blood concentration. The drug release rate was not affected by ph, gastrointestinal motility and food quantity. During aerosol inhalation, most of the inhaled dose is swallowed and then absorbed by the gastrointestinal tract. The bioavailability of aerosol is 10%, effective 1 ~ 5min after inhalation, and peak 1h. Most salbutamol is metabolized in the intestinal wall and liver, with less than 20% of the original drug entering the bloodstream. 80% of salbutamol is excreted in urine within 3 days of oral or inhalation.

indications

Used for various types of bronchial asthma and bronchial and lung diseases with bronchial spasm; Obstetrics is used to prevent premature birth and relieve placental vasospasm and increase blood flow to the placenta. For sinus bradycardia, sinus arrest, sinus atrial block, atrioventricular block and other chronic arrhythmias and heart failure.

contraindications

Contraindicated for those allergic to salbutamol.