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二丙酸倍氯米松吸入器:其药理学、治疗价值及不良反应综述。I:哮喘

Beclomethasone dipropionate inhaler: a review of its pharmacology, therapeutic value and adverse effects. I: Asthma.

作者信息

Brogden R N, Pinder R M, Sawyer P R, Speight T M, Avery G S

出版信息

Drugs. 1975;10(3):166-210. doi: 10.2165/00003495-197510030-00002.

Abstract

Beclomethasone dipropionate is a topically active corticosteroid used as an adjuvant in the control of chronic asthma when given by inhalation as an aerosol. It is not intended for treatment of acute attacks. It appears that the main difference between beclomethasone dipropionate and other corticosteroids previously used by inhalation is its high topical activity together with a lower systemic activity due to metabolic inactivation of the swallowed portion of the dose. Clinical experience has shown that at doses of 200 to 600mug daily, beclomethasone dipropionate inhaler is preferable to oral corticosteroids, because of lack of side-effects, when adult patients and children who are inadequately controlled by full doses of sodium cromoglycate and bronchodilators, are first considered to need maintenance corticosteroids. Inhaled beclomethasone dipropionate can allow a worthwhile reduction in maintenance doses of systemic corticosteroids in many patients already receiving these drugs and can replace systemic steroids entirely in some patients, particularly when their initial dose of steroids is less than 10mg daily of prednisone or its equivalent. Substitution should be attempted when the patient's asthma is well controlled on their usual doses of systemic steroids and full doses of other adjuvant therapy. Withdrawal of systemic corticosteroids should be performed slowly and carefully. Because recovery from impaired adrenocortical function caused by prolonged systemic steroid therapy is usually slow, special care is necessary for 9 to 12 months after transfer to beclomethasone dipropionate aerosol until the hypothalamo-pituitary-adrenal axis has sufficiently recovered to cope with emergencies such as trauma, surgery, severe infections or an acute attack of asthma. It is essential that additional therapy including high doses of systemic corticosteroids be used immediately to control any acute exacerbation of asthma which occurs during maintenance therapy with beclomethasone dipropionate aerosol. Tests of adrenal function suggest that beclomethasone dipropionate at dosages of 400 to 800 mug daily has little or no adverse effect. The most common side-effect associated with the continuous use of beclomethasone dipropionate inhaler has been oropharyngeal candidiasis, which appears to be dose-related and more common in women than in men. Systemic steroid withdrawal effects, like being generally unwell, and exacerbation of underlying allergic diseases such as allergic rhinitis, have been reported after substitution of beclomethasone dipropionate inhaler for systemic steroids. However, systemic withdrawal effects seldom occur if systemic steroids are withdrawn slowly.

摘要

二丙酸倍氯米松是一种局部活性皮质类固醇,通过气雾剂吸入给药时用作控制慢性哮喘的佐剂。它不适用于治疗急性发作。二丙酸倍氯米松与先前吸入使用的其他皮质类固醇之间的主要区别似乎在于其高局部活性以及由于剂量的吞咽部分代谢失活导致的较低全身活性。临床经验表明,对于成年患者和使用全剂量色甘酸钠和支气管扩张剂控制不佳、首次被认为需要维持性皮质类固醇治疗的儿童,每日剂量为200至600μg时,二丙酸倍氯米松吸入器优于口服皮质类固醇,因为它没有副作用。吸入二丙酸倍氯米松可使许多已经在接受这些药物治疗的患者的全身皮质类固醇维持剂量显著降低,并且在一些患者中可完全替代全身类固醇,特别是当他们最初的类固醇剂量低于每日10mg泼尼松或其等效剂量时。当患者的哮喘在其通常剂量的全身类固醇和全剂量的其他辅助治疗下得到良好控制时,应尝试进行替代。全身皮质类固醇的撤药应缓慢而谨慎地进行。由于长期全身类固醇治疗引起的肾上腺皮质功能受损的恢复通常较慢,在改用二丙酸倍氯米松气雾剂后的9至12个月内需要特别小心,直到下丘脑 - 垂体 - 肾上腺轴充分恢复以应对诸如创伤、手术、严重感染或哮喘急性发作等紧急情况。在用二丙酸倍氯米松气雾剂维持治疗期间发生任何哮喘急性加重时,必须立即使用包括高剂量全身皮质类固醇在内的额外治疗来控制。肾上腺功能测试表明,每日剂量为400至800μg的二丙酸倍氯米松几乎没有或没有不良反应。与持续使用二丙酸倍氯米松吸入器相关的最常见副作用是口咽念珠菌病,这似乎与剂量有关,并且在女性中比在男性中更常见。在用二丙酸倍氯米松吸入器替代全身类固醇后,已报告有全身类固醇撤药效应,如全身不适,以及潜在过敏性疾病如过敏性鼻炎的加重。然而,如果全身类固醇缓慢撤药,全身撤药效应很少发生。

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