Chronic obstructive pulmonary disease (COPD) is a chronic bronchitis and/or emphysema characterized by airflow obstruction, which can further develop into common chronic diseases. Chronic obstructive pulmonary disease (COPD) is a partially irreversible chronic disease that affects approximately 384 million individuals globally. There are several approved classes of maintenance therapy medications for stable COPD treatment, including β2 agonists, anticholinergic agents, and their combination agents. Over the past two decades, only one COPD medication with a new target (PDE-4), roflumilast, has been approved.
Tiotropium, the first approved LAMA, inhibits smooth muscle cell contraction by inhibiting the binding of acetylcholine to M3 muscarinic receptors. Its structural features contribute significantly to its efficacy in COPD treatment. It also has shown more significant efficacy when used in combination with olodaterol hydrochloride (LABA). Therefore, this blog discusses data on the bronchodilator (tiotropium) and the combination drug (olodaterol hydrochloride) to illustrate the pharmacokinetics (PK) of inhaled bronchodilator medications.
Tiotropium and olodaterol hydrochloride act on the M3 muscarinic receptors and β2 receptors on the airway smooth muscles, respectively, achieving bronchodilatory. They have similar PK profiles, including poor oral absorption, low systemic exposure, and rapid clearance. When the combination of tiotropium and olodaterol hydrochloride is administered by inhalation, the PK parameters of each component are similar to those observed with individual administration.
Using the example of tiotropium inhalation formulation and tiotropium bromide/olodaterol hydrochloride combination inhalation formulation, the PK profiles of inhaled COPD medications were summarized as follows:
Given the widespread prevalence of patients with COPD worldwide, the market prospects for inhaled COPD drugs are promising. Therefore, developing strategies for PK studies on COPD drugs needs more effort in the future.
If you want to learn more details about the PK profiles of inhaled medications, please read the article now.
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