Findlay J W
Department of Medicinal Biochemistry, Burroughs Wellcome Co., Research Triangle Park, NC 27709.
J Clin Pharm Ther. 1988 Feb;13(1):5-17. doi: 10.1111/j.1365-2710.1988.tb00502.x.
Pholcodine has antitussive activity similar to, or somewhat greater than, that of codeine in animal test systems. The drug, which has been formulated in many combination medications (45)--some rational and some quite irrational pharmacologically--also appears to be active in man, although the clear-cut demonstrations, unfortunately, are in artificially-induced cough models. Additional efficacy studies are needed. Preclinical toxicity studies demonstrate a generally safer profile for pholcodine than codeine, although pholcodine appears to have greater depressant effects on the respiratory and cardiovascular systems in animals. These effects have not been observed in man after administration of therapeutic doses. Pholcodine appears to be devoid of addiction liability in man. In contrast to codeine, pholcodine is not metabolised to morphine in man, a fact which may contribute to its more favourable toxicity profile, and it is metabolised and eliminated much more slowly than codeine.
在动物试验系统中，福尔可定具有与可待因相似或略强的镇咳活性。该药物已被制成多种复方制剂（45）——有些在药理学上是合理的，有些则不然——尽管遗憾的是，明确的证据来自人工诱导咳嗽模型，但它在人体中似乎也有活性。还需要进行更多的疗效研究。临床前毒性研究表明，福尔可定总体上比可待因更安全，尽管福尔可定在动物中对呼吸系统和心血管系统的抑制作用似乎更强。在给予治疗剂量后，人体中未观察到这些作用。福尔可定在人体中似乎没有成瘾倾向。与可待因不同，福尔可定在人体中不会代谢为吗啡，这一事实可能有助于其更有利的毒性特征，而且它的代谢和消除比可待因要慢得多。
