Butchers P R, Fullarton J R, Skidmore I F, Thompson L E, Vardey C J, Wheeldon A
Br J Pharmacol. 1979 Sep;67(1):23-32.
1 Salbutamol and disodium cromoglycate were compared for anti-anaphylactic activity against passive anaphylaxis in rat skin and peritoneum in vivo and in rat mast cells and human lung fragments in vitro.2 Salbutamol administered intravenously to rats inhibited cutaneous anaphylaxis, but also inhibited cutaneous responses to histamine and 5-hydroxytryptamine. Salbutamol administered intraperitoneally inhibited the release of slow reacting substance of anaphylaxis (SRS-A) but not the release of histamine in the peritoneum. It was a very weak inhibitor of histamine release from rat mast cells in vitro.3 Disodium cromoglycate administered intravenously to rats inhibited cutaneous anaphylaxis. Disodium cromoglycate administered intraperitoneally to rats inhibited the release of histamine and, to a lesser extent, SRS-A in the peritoneum. It was an effective but short-acting inhibitor of histamine release from rat mast cells in vitro.4 Salbutamol was a potent inhibitor of the anaphylactic release of histamine and SRS-A from fragments of human lung.5 Disodium cromoglycate was a weak inhibitor of the anaphylactic release of histamine and SRS-A from fragments of human lung. The inhibition was variable and not dose-related.6 The concentration of salbutamol required to inhibit anaphylaxis in human lung is of the same order as that required to relax human bronchial muscle. It is suggested that salbutamol may be more effective in allergic asthma if given in a prophylactic regimen.
对沙丁胺醇和色甘酸钠在大鼠皮肤和腹膜被动过敏反应中的体内抗过敏活性以及在大鼠肥大细胞和人肺组织碎片中的体外抗过敏活性进行了比较。
静脉注射给大鼠的沙丁胺醇可抑制皮肤过敏反应,但也会抑制皮肤对组胺和5-羟色胺的反应。腹腔注射的沙丁胺醇可抑制过敏反应慢反应物质(SRS-A)的释放,但不抑制腹膜中组胺的释放。在体外,它是大鼠肥大细胞组胺释放的非常弱的抑制剂。
静脉注射给大鼠的色甘酸钠可抑制皮肤过敏反应。腹腔注射给大鼠的色甘酸钠可抑制腹膜中组胺的释放,并在较小程度上抑制SRS-A的释放。在体外,它是大鼠肥大细胞组胺释放的有效但短效的抑制剂。
沙丁胺醇是从人肺组织碎片中过敏反应性释放组胺和SRS-A的有效抑制剂。
色甘酸钠是从人肺组织碎片中过敏反应性释放组胺和SRS-A的弱抑制剂。这种抑制作用是可变的,且与剂量无关。
抑制人肺过敏反应所需的沙丁胺醇浓度与舒张人支气管肌肉所需的浓度相当。有人提出,如果采用预防性给药方案,沙丁胺醇在过敏性哮喘中可能更有效。