Tiotropium Bromide

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Application and synthesis of Tiotropium Bromide:

Tiotropium bromide, also known as tiotropine bromide, is a new type of bronchodilator, a long-acting anticholinergic drug, which has a selective inhibitory effect on M3 receptors, and has a long-lasting blood drug concentration. Small and other advantages, the efficacy of tiotropium bromide for the treatment of chronic obstructive pulmonary disease (COPD) is equivalent to that of ipratropium bromide, but its advantage is that it only needs to be administered once a day, while the latter needs to be administered once a day4 Second-rate. Recent studies have shown that long-acting β2-adrenoceptor agonists (eg, formoterol) are equally effective at dilating the bronchi compared with short-acting ones. Both formoterol and tiotropium bromide can significantly increase the forced expiratory volume in the first second (FEV1), forced vital capacity (FVC) and deep inspiratory capacity (IC) at rest, and the combination of the two is more effective than single use Improvement in lung function was even more pronounced.

Pharmacological action of Tiotropium Bromide:

Tiotropium bromide, a quaternary ammonium derivative, is a highly selective anticholinergic drug that has the same affinity for five types of muscarinic receptors, M1-M5. In the human airway, this product has a high affinity to receptors, and dissociates slowly from muscarinic M1 and M3 receptors, and can block the contraction of bronchial smooth muscle mediated by cholinergic nerves for a long time. However, this product dissociates from muscarinic M2 receptors quite quickly, thus showing unique kinetic selectivity for M1 and M3 receptors.

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