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Pharmacological effects of tiotropium bromide(136310-93-5) for the long-term anticholinergic drugs, its five choline receptors (M1-M5) have similar affinity. Through the smooth muscle and M3 receptor binding on bronchial smooth muscle expansion. This effect is competitive and reversible. In vivo and in vitro studies have shown that this product has a dose-dependent, sustainable 24h inhibition of methacholine-induced bronchoconstriction. The goods on the role of bronchial expansion with outstanding positioning selectivity. 

Tiotropium bromide(136310-93-5) toxicological studies:

Reproductive toxicity: rat inhalation dose of 1.689mg /kg /d (according to body surface area, about 760 times the recommended daily dose), no effect on fertility. Rats inhalation dose of 0.078mg /kg /d (according to body surface area of about 35 times the recommended daily dose), abortion, the number of live births and the average fetal weight reduction, delayed fetal sexual maturity; Dose of 0.4mg /kg /d (according to body surface area, about 360 times the recommended clinical dose), increase the loss after implantation. But in rats and rabbits inhaled doses of 0.009 and 0.088 mg /kg /d (according to body surface area, about clinically recommended daily dose of 4 and 80 times), no such effect. 

Genetic toxicity: This product bacterial gene mutation test, V79 Chinese hamster lung cell chromosome aberration test, human lymphocyte chromosomal aberration test, mouse micronucleus test, rat hepatocyte extracellular DNA synthesis test results were negative. 

Carcinogenicity: Inhalation of this product dose of 0.059mg /kg /d (according to body surface area, the equivalent of clinically recommended daily dose of 25 times) 104 weeks, female mice inhaled the dose of 0.145mg /kg /d The body dose of 0.002mg /kg /d (according to body surface area, the equivalent of 0.5 times the recommended daily dose of clinical) for 101 weeks, the male mice inhaled this dose of 0.002mg /kg /d (according to body surface area, equivalent to 0.5 times the clinical day recommended dose) , No carcinogenic effect was observed.

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