Department of Pharmacology and Medicine, Division of Clinical Pharmacology, Rush University, Chicago, IL, USA.
Am J Ther. 2009 Jan-Feb;16(1):102-4. doi: 10.1097/MJT.0b013e3181961264.
Ethacrynic acid (EC), an effective loop diuretic especially in patients allergic to sulfa-containing drugs, possesses a number of potentially useful actions in addition to the inhibition of the Na⁺-K⁺-2Cl⁻ kidney symport. Inhibition of the enzyme glutathione S-transferase plays an important role in reducing chemotherapy drug resistance. Chemical modifications of EC increase inhibition of glutathione S-transferase and reduce toxicity due to diuretic action (hypotension and hypovolemia). This work may lead to effective therapies in reducing chemotherapy resistance in cancer chemotherapeutics. In addition, EC or conjurers may be a radiation enhancer, an anti-inflammatory agent, or a treatment for glaucoma.
依他尼酸(EC)是一种有效的袢利尿剂,尤其适用于对含磺胺类药物过敏的患者,除了抑制 Na⁺-K⁺-2Cl⁻肾脏协同转运外,它还具有许多潜在的有用作用。抑制谷胱甘肽 S-转移酶的活性在降低化疗药物耐药性方面起着重要作用。EC 的化学修饰增加了对谷胱甘肽 S-转移酶的抑制作用,并降低了利尿作用(低血压和血容量不足)的毒性。这项工作可能会导致在癌症化疗中降低化疗耐药性的有效治疗方法。此外,EC 或 conjurers 可能是一种辐射增强剂、一种抗炎剂或治疗青光眼的药物。