کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5825993 | 1558132 | 2014 | 12 صفحه PDF | دانلود رایگان |
- Muscarinic receptors increase smooth muscle tone in airways and urinary bladder.
- β-Adrenoceptors relax smooth muscle tone and oppose muscarinic contraction.
- Opposition involves transmitter release, signal transduction and receptor expression.
- This supports the combined use of muscarinic antagonists and β-adrenoceptor agonists.
Muscarinic receptor antagonists and β-adrenoceptor agonists are used in the treatment of obstructive airway disease and overactive bladder syndrome. Here we review the pharmacological rationale for their combination. Muscarinic receptors and β-adrenoceptors are physiological antagonists for smooth muscle tone in airways and bladder. Muscarinic agonism may attenuate β-adrenoceptor-mediated relaxation more than other contractile stimuli. Chronic treatment with one drug class may regulate expression of the target receptor but also that of the opposing receptor. Prejunctional β2-adrenoceptors can enhance neuronal acetylcholine release. Moreover, at least in the airways, muscarinic receptors and β-adrenoceptors are expressed in different locations, indicating that only a combined modulation of both systems may cause dilatation along the entire bronchial tree. While all of these factors contribute to a rationale for a combination of muscarinic receptor antagonists and β-adrenoceptor agonists, the full value of such combination as compared to monotherapy can only be determined in clinical studies.
Journal: Current Opinion in Pharmacology - Volume 16, June 2014, Pages 31-42