Tiotropium bromide is a specific anticholinergic with a long-lasting effect that has an affinity for the M1-M5 subtypes of muscarinic receptors. Competitively and reversibly blocking receptors of the M3 subtype in the airways leads to relaxation of the smooth muscles of the bronchi. In vitro and in vivo studies, the bronchodilating effect was dose-dependent and lasted more than 24 hours. This duration of effect is probably due to the very slow release of the drug from its association with M3 receptors, which determines the long half-life and significantly exceeds ipratropium bromide. Being a quaternary ammonium compound, tiotropium bromide exerts a predominantly local effect upon inhalation use, its systemic anticholinergic effects are mild. Dissociation from communication with M2 receptors is faster than from communication with M3in vitro receptors. M3 is more acceptable (kinetically controlled) receptor subtype.
The high efficacy of the drug and the slow dissociation from association with receptors were clinically correlated with significantly pronounced and prolonged bronchodilation in patients with COPD. Bronchodilation after inhalation of tiotropium is primarily a local effect on the respiratory tract, and not a systemic one. The use of the drug Spiriva 1 time per day was accompanied by a significant increase in lung function (increase in forced expiratory volume in the first second and forced vital capacity of the lungs) for 30 minutes after inhalation, the effect lasted 24 hours. The stable pharmacotherapeutic effect is achieved within 1 week from the start of treatment. With daily use, the drug Spiriva significantly increases the morning and evening maximum expiratory flow rate.
Improvement of lung function during treatment is maintained for a long period, signs of the development of drug tolerance are not observed. Bronchodilation lasts over the 24-hour dosing interval compared with placebo. It did not take into account the mode of taking the drug (in the morning or in the evening).
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In long-term studies (throughout the year) it has been established:
- Spiriva significantly reduces shortness of breath; improvement was maintained throughout the entire period of treatment;
- significantly reduces the number of exacerbations of COPD and stops the occurrence of the first exacerbation;
- significantly improves the quality of life; improvement was noted throughout the entire period of treatment;
- significantly reduces the number of hospitalized patients with exacerbation of COPD, with the first hospitalization required later.
In 2 studies it was found that, due to taking the drug Spiriva, the tolerance to physical activity, limited by the symptoms of the disease, significantly increased by 19.7 and 28.3%, respectively.
In the study of the use of 18 and 54 µg (3 times a day, 18 µg each), Spiriva did not show prolongation of the QT interval in terms of ECG for 12 days.
Taking Spiriva does not lead to an increased risk of death
Boehringer Ingelheim and Pfizer unveiled the results of a new analysis of 30 controlled studies that confirm the long-term safety profile of Spiriva (tiotropium bromide). New and expanded data contradict the findings regarding tiotropium bromide, which were published by a group of authors (Singh S., Loke Y.K., Furberg C.D.) in September in the Journal of the American Medical Association (Journal of the American Medical Association).
Thus, the latest data obtained in the analysis of 30 placebo-controlled double-blind randomized studies conducted by Boehringer Ingelheim with 19,545 patients with chronic obstructive pulmonary disease, 10,846 of whom received tiotropium bromide, and 8699 – placebo, indicate the absence increased the risk of death when taking Spiriva.
We strongly disagree with the conclusion obtained in the study of Singh S. et al. We have provided important information to regulators around the world, which is part of a very thorough analysis of our tests. And the results of the analysis, which includes data from the UPLIFT four-year study, confirm the Spiriva safety profile, said Dr. Andreas Barner, vice chairman of the board of managing directors of Boehringer Ingelheim, who is in charge of research, development and medical issues. – Patients and doctors can be sure that Spiriva is safe and effective. In the course of clinical and post-marketing research, we collected extensive safety data, not counting that the volume of Spiriva intake is more than 10 million patient-years.