Twycross R G
Postgrad Med J. 1973 May;49(571):309-13. doi: 10.1136/pgmj.49.571.309.
Although the centenary of the discovery of diamorphine is soon to be celebrated, much work remains to be done before its mode of action is thoroughly understood. The main stumbling blocks facing the would-be investigator can be summarized as follows: (1) Diamorphine in solution has a limited shalf-life. (2) The potency ratio of diamorphine to morphine is still a matter of dispute. (3) No basic studies appear to have been carried out on the fate of orally administered diamorphine. (4) Current methods of assay are not sensitive enough to detect diamorphine or its metabolites in serum after the administration of the drug when given in therapeutic amounts. (5) The undersirable side-effects of diamorphine may vary according to posture and mobility. (6) As the metabolic handling of the drug may be different in the two sexes, provision for a between-sex comparison should be included in the design of a clinical trial of diamorphine.
尽管二乙酰吗啡的发现即将迎来百年纪念，但在其作用方式被彻底了解之前，仍有许多工作要做。潜在研究者面临的主要障碍可总结如下：(1) 二乙酰吗啡溶液的半衰期有限。(2) 二乙酰吗啡与吗啡的效价比仍存在争议。(3) 似乎尚未对口服二乙酰吗啡的代谢情况进行基础研究。(4) 当前的检测方法不够灵敏，无法在给予治疗剂量的药物后检测出血清中的二乙酰吗啡或其代谢产物。(5) 二乙酰吗啡不良副作用可能因姿势和活动能力而异。(6) 由于该药物在两性中的代谢处理可能不同，在二乙酰吗啡的临床试验设计中应考虑进行性别间比较。
