吸入性皮质类固醇类药物治疗哮喘：这些药物一样吗？
2009/03/24
目的：评价现在已有的治疗哮喘的吸入性皮质类固醇类药物（ICS）的相同之处和差别，特别强调可能影响这些药物相对安全性的因素。
方法：检索PubMed中相关的综述类文章和原始研究论文。综合这些研究中的信息，并严格评价。
结果：皮质类固醇的剂型和转运系统的差异会引起疗效发生变化。不同皮质类固醇类药物的化学特性也可能影响其相对安全性。环索奈德和倍氯美松双丙酸酯作为肺内而不是口咽部的酶类激活的前药给药。这样可以避免口咽部皮质类固醇引发的特异性不良反应，尽管还可能有剂型特异性不良反应。一旦药物进入体循环，所有的ICS都会被肝脏迅速代谢。ICS（如氟替卡松、环索奈德和莫美他松）的口服生物利用度最小，因为这些药物主要经过肝脏的首过代谢消除。环索奈德还要经过肝外代谢，使得药物的消除更加迅速。此外，环索奈德和莫美他松与血清蛋白的结合力极强，这使这些药物对肺外糖皮质激素受体的刺激能力下降。
结论：不管是否通过相似机制起作用，目前已有的ICS及其转运系统不同，可能影响其在个别患者中的安全性和疗效。
（陈欣 审校）
Baptist AP, Reddy RC.J Clin Pharm Ther. 2009 Feb;34(1):1-12
Baptist AP, Reddy RC.J Clin Pharm Ther. 2009 Feb;34(1):1-12. Links
Inhaled corticosteroids for asthma: are they all the same?
OBJECTIVES: To assess similarities and differences among currently available inhaled corticosteroids (ICS) for treatment of asthma, with special emphasis on factors that may affect the relative safety of these medications.
METHODS: PubMed was searched for relevant reviews and original articles. Information from these studies was synthesized and critically assessed.
RESULTS: Differences in corticosteroid formulations and delivery systems can create variations in therapeutic efficacy. Chemical properties of the various corticosteroids may also affect their relative safety. Ciclesonide and beclomethasone dipropionate are administered as prodrugs activated by enzymes present in the lungs but not the oropharynx. Corticosteroid-specific adverse effects in the oropharynx are thus avoided, although formulation-specific effects may remain. Other adverse effects require systemic availability, either via the gastrointestinal tract or the lung. Once they enter the systemic circulation, all ICS are rapidly metabolized by the liver. Oral bioavailability of ICS such as fluticasone, ciclesonide and mometasone is minimal, as a result of their essentially complete first-pass metabolism in the liver. Ciclesonide also undergoes extrahepatic metabolism that eliminates it even more rapidly. Additionally, ciclesonide and mometasone exhibit very high levels of binding to serum proteins that reduces their ability to stimulate glucocorticoid receptors outside the lung.
CONCLUSIONS: Despite acting by similar mechanisms, currently available ICS and their delivery systems differ in ways that can potentially affect both safety and therapeutic effectiveness for individual patients.
方法：检索PubMed中相关的综述类文章和原始研究论文。综合这些研究中的信息，并严格评价。
结果：皮质类固醇的剂型和转运系统的差异会引起疗效发生变化。不同皮质类固醇类药物的化学特性也可能影响其相对安全性。环索奈德和倍氯美松双丙酸酯作为肺内而不是口咽部的酶类激活的前药给药。这样可以避免口咽部皮质类固醇引发的特异性不良反应，尽管还可能有剂型特异性不良反应。一旦药物进入体循环，所有的ICS都会被肝脏迅速代谢。ICS（如氟替卡松、环索奈德和莫美他松）的口服生物利用度最小，因为这些药物主要经过肝脏的首过代谢消除。环索奈德还要经过肝外代谢，使得药物的消除更加迅速。此外，环索奈德和莫美他松与血清蛋白的结合力极强，这使这些药物对肺外糖皮质激素受体的刺激能力下降。
结论：不管是否通过相似机制起作用，目前已有的ICS及其转运系统不同，可能影响其在个别患者中的安全性和疗效。
（陈欣 审校）
Baptist AP, Reddy RC.J Clin Pharm Ther. 2009 Feb;34(1):1-12
Baptist AP, Reddy RC.J Clin Pharm Ther. 2009 Feb;34(1):1-12. Links
Inhaled corticosteroids for asthma: are they all the same?
OBJECTIVES: To assess similarities and differences among currently available inhaled corticosteroids (ICS) for treatment of asthma, with special emphasis on factors that may affect the relative safety of these medications.
METHODS: PubMed was searched for relevant reviews and original articles. Information from these studies was synthesized and critically assessed.
RESULTS: Differences in corticosteroid formulations and delivery systems can create variations in therapeutic efficacy. Chemical properties of the various corticosteroids may also affect their relative safety. Ciclesonide and beclomethasone dipropionate are administered as prodrugs activated by enzymes present in the lungs but not the oropharynx. Corticosteroid-specific adverse effects in the oropharynx are thus avoided, although formulation-specific effects may remain. Other adverse effects require systemic availability, either via the gastrointestinal tract or the lung. Once they enter the systemic circulation, all ICS are rapidly metabolized by the liver. Oral bioavailability of ICS such as fluticasone, ciclesonide and mometasone is minimal, as a result of their essentially complete first-pass metabolism in the liver. Ciclesonide also undergoes extrahepatic metabolism that eliminates it even more rapidly. Additionally, ciclesonide and mometasone exhibit very high levels of binding to serum proteins that reduces their ability to stimulate glucocorticoid receptors outside the lung.
CONCLUSIONS: Despite acting by similar mechanisms, currently available ICS and their delivery systems differ in ways that can potentially affect both safety and therapeutic effectiveness for individual patients.
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