Katcher M L, Reed C E
J Allergy Clin Immunol. 1980 Sep;66(3):223-6. doi: 10.1016/0091-6749(80)90043-3.
Lodoxamide ethyl, an orally active drug with pharmacologic activity similar to that of cromolyn sodium, blocks passive cutaneous anaphylaxis (PCA) in rats and antigen-induced bronchoconstriction in guinea pigs and monkeys. Its effectiveness in preventing antigen-induced airway obstruction was studied in 12 asymptomatic asthmatic adults with immediate skin test sensitivity to ragweed, Alternaria, or animal dander. The dose required to reduce the forced expiratory volume in 1 sec (FEV1) by 20% (PD20) was determined by dosimeter bronchoprovocation challenge with the appropriate antigen. At 1-wk intervals each subject received either placebo of 1, 3, or 10 mg drug in a randomized, double-blind fashion 30 min prior to starting bronchoprovocation challenge. On average, 1 mg increased the PD20 fivefold, 3 mg about sixfold, and 10 mg about 27-fold. Dose-related side effects began 10 min after drug and lasted up to 40 min. Thus the oral administration of lodoxamide ethyl was effective in preventing antigen-induced bronchoconstriction, and both the beneficial effects and side effects are dose related.
洛度沙胺乙酯是一种口服活性药物，其药理活性与色甘酸钠相似，可阻断大鼠的被动皮肤过敏反应（PCA）以及豚鼠和猴子的抗原诱导的支气管收缩。在12名对豚草、链格孢属或动物皮屑有速发型皮肤试验敏感性的无症状哮喘成年患者中，研究了其预防抗原诱导的气道阻塞的有效性。通过用适当抗原进行剂量计支气管激发试验，确定使1秒用力呼气量（FEV1）降低20%所需的剂量（PD20）。在开始支气管激发试验前30分钟，每个受试者以随机、双盲方式每隔1周接受安慰剂或1、3或10毫克药物。平均而言，1毫克使PD20增加了五倍，3毫克约为六倍，10毫克约为27倍。与剂量相关的副作用在用药后10分钟开始，持续长达40分钟。因此，口服洛度沙胺乙酯可有效预防抗原诱导的支气管收缩，其有益作用和副作用均与剂量相关。
