Medical Department , Chiesi Farmaceutici , Parma , Italy.
Expert Opin Drug Discov. 2011 Nov;6(11):1203-14. doi: 10.1517/17460441.2011.629646. Epub 2011 Oct 25.
Mucoactive drugs are currently used to cleanse the respiratory tract following disturbance of the normal mucociliary clearance due to mucous hyperproduction and/or modification of its physicochemical characteristics. However, in addition to possessing the ability to perform specific actions on airway secretion, these compounds have the capability to modulate the mechanisms involved in abnormal secretions. Indeed, over the years, in the postmarketing phase, a large number of studies have been published showing interesting pharmacological activities in addition to their secretagogue activity.
This article collates available data on ambroxol (2-amino-3,5-dibromo-N-[trans-4-hydroxycyclohexyl]benzylamine), a metabolite of bromhexine, used as a secretagogue in the treatment of childhood airway diseases. This article goes beyond the mucoactive aspects of the drug covering its multiple pharmacological properties.
The non-mucoactive functions exhibited by the compound may provide beneficial effects on airway structure and function in health and disease. Beyond the mucokinetic and secretagogue effects, ambroxol showed great antioxidant, anti-inflammatory, local anesthetic and surfactant synthesis stimulatory activities. Moreover, some antiviral and antibacterial activities were shown. These findings may better explain the clinical results observed in a variety of airway disorders and suggest additional therapeutic potential. Further studies are needed to better define the clinical relevance of these non-mucolytic activities.
黏液活性药物目前被用于治疗由于黏液过度产生和/或其理化特性改变而导致的正常黏液纤毛清除功能障碍后的呼吸道清洁。然而,除了对气道分泌物具有特定作用的能力外,这些化合物还能够调节异常分泌所涉及的机制。事实上,多年来,在上市后阶段,大量的研究已经发表,除了其分泌作用外,还显示出有趣的药理学活性。
本文汇集了氨溴索(2-氨基-3,5-二溴-N-[反式-4-羟基环己基]苯甲胺)的现有数据,氨溴索是溴己新的代谢物,用于治疗儿童气道疾病。本文超越了药物的黏液活性方面,涵盖了其多种药理学特性。
该化合物表现出的非黏液活性功能可能会对健康和疾病状态下的气道结构和功能产生有益影响。除了黏液动力学和分泌作用外,氨溴索还表现出很强的抗氧化、抗炎、局部麻醉和表面活性剂合成刺激活性。此外,还表现出一些抗病毒和抗菌活性。这些发现可能更好地解释了在各种气道疾病中观察到的临床结果,并提示了额外的治疗潜力。需要进一步的研究来更好地确定这些非黏液溶解活性的临床相关性。