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Airway parasympathetic activation can promote bronchial smooth muscle contraction, airway mucus secretion and ciliary movement. This pharmacological effect is achieved by regulating the M1 and M3 receptors located in the large airway smooth muscle. While the M2 receptor is located in the parasympathetic ganglion post-fiber, inhibition of acetylcholine release. Thus, ideally the parasympathetic inhibitor selectively antagonizes the M1 and M3 receptors and does not affect M2 receptors. Tiotropium bromide(136310-93-5) binds to three M receptors, binds to the M3 receptor for 35 hours, and is easily isolated from the M2 receptor, both in animals and in human tissues, so its potency is greater and its duration is longer long.

Inhalation of a single dose of tiotropium bromide(136310-93-5), the first second forced expiratory volume (FEV1) increased steadily, 1 ~ 3h peak, peak after a longer period of plateau. Within the range of 10 ~ 80μg, there was only slight difference in each dose group, but there was a significant increase in FEV1 in each group within 32 hours after the administration compared with the control group. Due to the circadian rhythm of airway function, FEV1 decreased after administration 16 ~ 24 hours, and this effect can not be completely antagonized by tiotropium bromide.

A more rigorous trial studied the duration of tiotropium diastole. Subjects with 12 patients with hereditary allergies in male asthma patients, given tiotropium bromide(136310-93-5) 10 ~ 80μg, 48h can completely antagonize the excitation of acetylcholine. Experiments show that, tiotropium bromide on the airway relaxation can last 48h or longer. After repeated use of tiotropium bromide, the FEV1 baseline increased on day 2 compared with day 1. FEV1 reached a trough 23 to 24 hours after the first administration (before the next administration), and this value increased after several days of continuous administration. Vannoord et al found that FEV1 trough increased by 0119 L (18% higher than baseline) after 8 days of dosing, and almost all improvement occurred on day 2. The forced vital capacity (FVC) trough continued to increase daily during the first week of administration and increased to 0167 L (27% higher than the baseline) at day 8. Increased trough value has important clinical significance, it shows that the daily administration of the law, the role of relaxation will be maintained for 24 hours, repeated administration is better than a single dose.


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