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The pharmacological rationale for combining muscarinic receptor antagonists and beta-adrenoceptor agonists in the treatment of airway and bladder disease

Dale, P. R., Cernecka, H., Schmidt, M., Dowling, M. R., Charlton, S. J., Pieper, M. P. & Michel, M. C., Jun-2014, In : Current Opinion in Pharmacology. 16, p. 31-42 12 p.

Research output: Contribution to journalArticleAcademicpeer-review

  • Philippa R. Dale
  • Hana Cernecka
  • Martina Schmidt
  • Mark R. Dowling
  • Steven J. Charlton
  • Michael P. Pieper
  • Martin C. Michel

Muscarinic receptor antagonists and beta-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 beta-adrenoceptors are physiological antagonists for smooth muscle tone in airways and bladder. Muscarinic agonism may attenuate beta-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 beta(2)-adrenoceptors can enhance neuronal acetylcholine release. Moreover, at least in the airways, muscarinic receptors and beta-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 beta-adrenoceptor agonists, the full value of such combination as compared to monotherapy can only be determined in clinical studies.

Original languageEnglish
Pages (from-to)31-42
Number of pages12
JournalCurrent Opinion in Pharmacology
Volume16
Publication statusPublished - Jun-2014

    Keywords

  • TRACHEAL SMOOTH-MUSCLE, RAT URINARY-BLADDER, PROTEIN-KINASE-C, CYCLIC ADENOSINE-MONOPHOSPHATE, NONNEURONAL CHOLINERGIC SYSTEM, CA2+-ACTIVATED K+ CHANNEL, GUINEA-PIG TRACHEA, ACETYLCHOLINE-RELEASE, AUTORADIOGRAPHIC VISUALIZATION, ADRENERGIC RELAXATION

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