论文部分内容阅读
氨茶碱用于治疗哮喘至少已有50年历史。近10年来随着对氨茶碱疗效和血清中毒浓度关系的了解、氨茶碱检测技术的发展,以及基础药物动力学的理论在临床中的应用,致使氨茶碱在急、慢性哮喘的治疗中成为主要的药物。作用机制传统的观点是,氨茶碱主要通过抑制磷酸二酯酶,提高3′5′-cAMP的浓度,而引起支气管扩张。Dolson等首先对上述理论提出异议,证实氨茶碱在一般治疗量时,组织内的浓度对磷酸二酯酶的抑制作用不大,最高20%。用狗的支气管实验证明,氨茶碱对磷酸二酯酶抑制所需浓度要比其松弛平滑肌高5倍。
Aminophylline is used to treat asthma for at least 50 years. In the past 10 years, with the understanding of the relationship between the theophylline efficacy and serum concentration, the development of aminophylline detection technology, and the application of the theory of basic pharmacokinetics in the clinic led to the treatment of acute and chronic asthma Become the main drug. The mechanism of action The traditional view is that aminophylline mainly by inhibiting phosphodiesterase, increased 3’5’-cAMP concentration, causing bronchiectasis. Dolson and other first proposed the above theory objections, confirmed that aminophylline in the general treatment, the concentration within the organization of phosphodiesterase inhibition is not up to 20%. Bronchial experiments with dogs demonstrated that aminophylline required phosphodiesterase inhibition at concentrations five times higher than its relaxed smooth muscle.