Oral beta 2-selective adrenergic bronchodilators.
Oral beta 2-selective adrenergic bronchodilators.
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口服β2-选择性肾上腺素能支气管扩张剂。
DOI：
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发表时间：
1986
期刊：
影响因子：
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通讯作者：
C. Tantucci
中科院分区：
文献类型：
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作者：
V. Grassi;S. Daniotti;M. Schiassi;M. Dottorini;C. Tantucci
口服β2受体激动剂(卡布特罗、吡布特罗、丙卡特罗、比妥特罗、克伦特罗)是广泛用作支气管扩张剂的药物。支气管扩张剂药物的疗效和选择性取决于其固有的药理学特性和给药途径。该口服途径具有使用方便、剂量准确、疗效确切等特点。因此，缺点(起效延迟，副作用更频繁)和适应症(严重的慢性呼吸道阻塞患者，夜间哮喘发作，以及儿童和老年受试者)明显。最新的β2-激动剂具有有效和持久的支气管扩张作用，并有众所周知的副作用。为了在大量人群中控制药物效率，并确定不良反应的类型和程度，计划对克伦特罗进行上市后监测研究。现有的结果证实，长期口服克伦特罗是一种有效和安全的治疗方法。在长期治疗过程中，会出现快速反应(一种反应减弱)。这一复杂的生物学现象可以通过几个方面进行研究，即靶器官的功能反应、适当的生化代谢指标以及体外细胞β受体的功能评估。此外，根据对血清环核苷酸(环腺苷和一磷酸鸟苷)水平的评估，似乎快速反应的临床重要性是轻微的，在选定的患者中使用β2激动剂进行慢性治疗是安全和有效的。
Oral beta 2-agonists (carbuterol, pirbuterol, procaterol, bitolterol, clenbuterol) are drugs widely used as bronchodilators. The efficacy and selectivity of bronchodilators drugs depend on their intrinsic pharmacological properties and on the route of administration. The characteristics of the oral route are easy usage, precise dosage and assured effects. Consequently, disadvantages (delayed onset of action, more frequent side-effects) and the indications, (patients with severe chronic airways obstruction, nocturnal asthmatic attacks, and children and elderly subjects) are clearly evident. The most recent beta 2-agonists have an efficient and prolonged bronchodilating action with well-known side-effects. In order to control drug efficiency in a large population and identify type and degree of adverse reactions, a post-marketing surveillance study was programmed for clenbuterol. The results available confirms that long-term treatment with oral clenbuterol is an effective and safe therapeutical approach. During long-term treatment, tachyphylaxis (a diminished responsiveness) develops. This complex biological phenomenon can be studied, in several ways i.e. functional response of target-organ, appropriate biochemical-metabolical indices, and functional evaluation of the cellular beta-receptors in vitro. Also in the light of evaluation of serum levels of cyclic nucleotides (cyclic adenosine and guanosine monophosphates) it appears that the clinical importance of tachyphylaxis is mild and that chronic therapy with beta 2-agonists is safe and effective when used in selected patients.