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布地奈德、丙酸倍氯米松和泼尼松龙在人体中的局部及全身糖皮质激素效力

Topical and systemic glucocorticoid potencies of budesonide, beclomethasone dipropionate and prednisolone in man.

作者信息

Johansson S A, Andersson K E, Brattsand R, Gruvstad E, Hedner P

出版信息

Eur J Respir Dis Suppl. 1982;122:74-82.

PMID:6958496
Abstract

Topical anti-inflammatory ('intracutaneous vasoconstriction') and systemic glucocorticoid potencies (depression of plasma cortisol) were compared in human volunteers after administration of the glucocorticoids budesonide, beclomethasone dipropionate (BDP) and prednisolone. After topical application budesonide was about twice as potent as BDP and more than 1 000 times more potent than prednisolone and hydrocortisone in inducing 'vasoconstriction'. After oral administration, on the other hand, budesonide was one half to one third as potent as BDP in depressing plasma cortisol. After inhalation budesonide was only half as potent as BDP. When inhaled budesonide was compared to oral prednisolone budesonide 1 600 micrograms and prednisolone 5 mg were shown to have the same effect on plasma cortisol. The improved ratio between the topical and the systemic glucocorticoid effect of budesonide, makes the drug a promising alternative for aerosol treatment in asthma.

摘要

在人类志愿者中,给予糖皮质激素布地奈德、二丙酸倍氯米松(BDP)和泼尼松龙后,比较了局部抗炎作用(“皮内血管收缩”)和全身糖皮质激素效力(血浆皮质醇降低)。局部应用后,布地奈德在诱导“血管收缩”方面的效力约为BDP的两倍,比泼尼松龙和氢化可的松强1000多倍。另一方面,口服后,布地奈德在降低血浆皮质醇方面的效力仅为BDP的二分之一至三分之一。吸入后,布地奈德的效力仅为BDP的一半。当将吸入布地奈德与口服泼尼松龙进行比较时,显示1600微克布地奈德和5毫克泼尼松龙对血浆皮质醇具有相同的作用。布地奈德局部和全身糖皮质激素作用之间改善的比率,使其成为哮喘气雾剂治疗的有前途的替代药物。

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