Materson B J
Am Heart J. 1983 Jul;106(1 Pt 2):188-208. doi: 10.1016/0002-8703(83)90117-5.
Effective diuresis requires both sufficient glomerular filtrate and adequate delivery of the diuretic drug to the lumen of the renal tubule. Diuretics will not "force open" the kidney. Diuretics that work primarily in the proximal tubule include osmotic diuretics (e.g., mannitol), diuretics that interfere with the adenyl cyclase system (e.g., xanthines), and those which inhibit carbonic anhydrase (e.g., acetazolamide). Some thiazide and thiazide-like diuretics have a secondary site of action in the proximal tubule based on either carbonic anhydrase inhibition or other mechanisms, such as inhibition of sodium phosphate reabsorption. The diuretics that work primarily in the medullary diluting segment of the loop of Henle, furosemide and ethacrynic acid, block the active reabsorption of chloride and interfere with the tubular reabsorption of free water. The exact mechanism remains unknown. These diuretics tend to have a "high ceiling," to be potent and rapidly acting, and to have a short duration of effect. They are excellent for the treatment of severe fluid overload or pulmonary edema but are not ideal for the treatment of uncomplicated hypertension. Furosemide is a sulfonamide derivative; ethacrynic acid can be used in patients who are allergic to sulfa drugs. Diuretics that work primarily in the cortical diluting segment include the thiazides and thiazide-like drugs. They inhibit sodium transport by an undetermined mechanism. Most of them seem to reach a dose-response plateau beyond which little additional effect is gained by increasing the dose. Most of them appear to lose efficacy as the glomerular filtration rate decreases, except for metolazone and indapamide. The thiazides are most commonly used to treat hypertension. Diuretics that work primarily in the distal tubule and collecting tubule include the aldosterone inhibitor spironolactone and two drugs that impair tubular reabsorption of sodium by direct action, triamterene and amiloride. These drugs are primarily used for their potassium-sparing effect.
有效的利尿作用既需要足够的肾小球滤过液，也需要将利尿药充分输送到肾小管腔。利尿剂不会“强行打开”肾脏。主要作用于近端小管的利尿剂包括渗透性利尿剂（如甘露醇）、干扰腺苷酸环化酶系统的利尿剂（如黄嘌呤类）以及抑制碳酸酐酶的利尿剂（如乙酰唑胺）。一些噻嗪类和类噻嗪类利尿剂基于碳酸酐酶抑制作用或其他机制（如抑制磷酸钠重吸收）在近端小管有次要作用位点。主要作用于髓袢髓质稀释段的利尿剂，呋塞米和依他尼酸，可阻断氯离子的主动重吸收并干扰游离水的肾小管重吸收。确切机制尚不清楚。这些利尿剂往往有“高效能”，作用强效且起效迅速，作用持续时间短。它们是治疗严重液体超负荷或肺水肿的理想药物，但并非治疗单纯性高血压的理想药物。呋塞米是一种磺胺衍生物；依他尼酸可用于对磺胺类药物过敏的患者。主要作用于皮质稀释段的利尿剂包括噻嗪类和类噻嗪类药物。它们通过一种未明机制抑制钠转运。它们中的大多数似乎会达到剂量反应平台期，超过此阶段增加剂量几乎不会有额外效果。随着肾小球滤过率降低，它们中的大多数似乎会失去疗效，但美托拉宗和吲达帕胺除外。噻嗪类最常用于治疗高血压。主要作用于远端小管和集合小管的利尿剂包括醛固酮抑制剂螺内酯以及两种通过直接作用损害肾小管钠重吸收的药物，氨苯蝶啶和阿米洛利。这些药物主要因其保钾作用而被使用。
