Van Berkel Megan A, Elefritz Jessica L
Department of Pharmacy, Erlanger Health System, Chattanooga, TN
Department of Pharmacy, Wexner Medical Center, Ohio State University, Columbus, OH.
Am J Health Syst Pharm. 2018 Apr 15;75(8):524-531. doi: 10.2146/ajhp170279.
Current off-label uses of acetazolamide in hospitalized patients are reviewed.
Acetazolamide is a carbonic anhydrase inhibitor typically used for indications including epilepsy, glaucoma, edema, and altitude sickness but it may be prescribed in hospitalized patients for off-label indications. It inhibits carbonic anhydrase, which leads to reduced hydrogen ion secretion in the proximal renal tubule, resulting in increased bicarbonate and cation excretion and causing urinary alkalization and diuresis. In addition, acetazolamide decreases the production of cerebrospinal fluid (CSF) and aqueous humor, reducing intracranial pressure (ICP) and intraocular pressure. This allows acetazolamide to be used for treatment of idiopathic intracranial hypertension and elevated ICP due to CSF leaks to avoid invasive procedures. It is a sulfonamide derivative, with dosages ranging from 250 to 4,000 mg daily divided every 6-12 hours. The plasma half-life is 4-8 hours, though the pharmacologic effects of acetazolamide last longer. Acetazolamide is highly protein bound and primarily eliminated by the kidneys, so administration should not be more frequent than every 12 hours if creatinine clearance is less than 50 mL/min. Limited literature exists describing the optimal patients to receive acetazolamide therapy.
The potential benefits of acetazolamide include ventilator weaning for chronic obstructive pulmonary disease patients, avoidance of invasive procedures in patients with a CSF leak or elevated ICP, and prevention of high-dose methotrexate toxicity and contrast-induced nephropathy. Uncertainty remains regarding the selection of patients who would best benefit from acetazolamide use.
回顾乙酰唑胺在住院患者中的当前非适应证使用情况。
乙酰唑胺是一种碳酸酐酶抑制剂，通常用于癫痫、青光眼、水肿和高原病等适应证，但在住院患者中可能会因非适应证而被处方。它抑制碳酸酐酶，导致近端肾小管中氢离子分泌减少，从而使碳酸氢盐和阳离子排泄增加，引起尿液碱化和利尿。此外，乙酰唑胺可减少脑脊液（CSF）和房水的生成，降低颅内压（ICP）和眼压。这使得乙酰唑胺可用于治疗特发性颅内高压以及因脑脊液漏导致的颅内压升高，以避免侵入性操作。它是一种磺胺衍生物，剂量范围为每日250至4000毫克，每6 - 12小时分服。血浆半衰期为4 - 8小时，不过乙酰唑胺的药理作用持续时间更长。乙酰唑胺与蛋白质高度结合，主要经肾脏排泄，因此如果肌酐清除率低于50毫升/分钟，给药频率不应超过每12小时一次。描述接受乙酰唑胺治疗的最佳患者的文献有限。
乙酰唑胺的潜在益处包括用于慢性阻塞性肺疾病患者的呼吸机撤机、避免脑脊液漏或颅内压升高患者的侵入性操作，以及预防大剂量甲氨蝶呤毒性和造影剂诱导的肾病。对于哪些患者最能从使用乙酰唑胺中获益的选择仍存在不确定性。
