Department of Molecular Pharmacology, Rappaport Faculty of Medicine, Technion, Haifa, Israel.
Int Rev Neurobiol. 2011;100:169-90. doi: 10.1016/B978-0-12-386467-3.00009-1.
Potentiation of the cardiovascular and other effects of dietary tyramine by monoamine oxidase (MAO) inhibitors (cheese effect) has been a major limitation to clinical use of these drugs. The discovery that MAO exists in two distinct isoforms, MAO-A and MAO-B, together with the development of selective inhibitors of each isoform, enabled the understanding that selective inhibition of MAO-A, or inhibition of both isoforms, will cause cheese effect, but selective inhibition of MAO-B can be elicited without dangerous pressor reaction. This development has permitted the introduction of selective MAO-B inhibitors to clinical medicine for treatment of Parkinson's disease. This review describes the basic mechanisms involved in cheese effect, as well as providing information on tyramine levels in a variety of foodstuff, and surveys clinical information from tyramine pressor testing with the selective MAO-B inhibitors, selegiline and rasagiline.
饮食中的酪胺（tyramine）在体内会被单胺氧化酶（monoamine oxidase，MAO）代谢，而 MAO 抑制剂会增强这种代谢，从而导致心血管等方面的不良反应（所谓“奶酪效应”），这一现象严重限制了这些药物的临床应用。后来发现 MAO 存在两种不同的同工酶形式，即 MAO-A 和 MAO-B，而且针对每种同工酶都开发出了选择性抑制剂。这一发现使人们认识到，选择性抑制 MAO-A 或同时抑制两种同工酶都会引发“奶酪效应”，但选择性抑制 MAO-B 则不会引起血压升高的危险反应。这一发现使选择性 MAO-B 抑制剂得以问世，并应用于治疗帕金森病。本文介绍了“奶酪效应”的基本机制，以及各种食物中酪胺的含量信息，并综述了选择性 MAO-B 抑制剂司来吉兰（selegiline）和雷沙吉兰（rasagiline）在进行酪胺升压试验时的临床信息。
