Johnson A G, Day R O
St Vincents Hospital, Sydney, Australia.
Drugs Aging. 1991 Mar;1(2):130-43. doi: 10.2165/00002512-199101020-00005.
Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most commonly prescribed drugs worldwide when grouped by generic categories and account for 3 to 9% of total prescription numbers in various countries. While NSAIDs are responsible for approximately 25% of all reported adverse drug reactions, aging may substantially increase the risk of NSAID-induced reactions. Several factors may contribute to NSAID-related toxicity in the elderly. The increase in morbidity associated with aging may result in consumption of a wide range of potent drugs, while inappropriate drug therapy and aberrant compliance are also capable of contributing to adverse drug reactions in geriatric patients. Age-related alterations in pharmacokinetics may influence the handling of NSAIDs in the elderly; in particular, dosage reduction is appropriate for azapropazone (apazone), naproxen, ketoprofen and salicylates administered to healthy aged patients, whereas the presence of renal disease may also necessitate dosage reduction of diflunisal, indomethacin, sulindac and mefenamic acid. Changes in NSAID pharmacodynamics with aging, such as increased CNS sensitivity to NSAIDs and impaired homeostasis, also predispose the elderly to NSAID-related adverse effects. It is undisputed that gastrointestinal toxicity due to NSAID therapy is a class effect. A significant association has been found between aspirin and uncomplicated gastric, but not uncomplicated duodenal ulcer, while nonaspirin NSAIDs are significantly associated with both uncomplicated gastric and duodenal ulceration. The use of NSAIDs is accompanied by a 2- to 5-fold risk of serious complications of peptic ulcer disease, i.e. haemorrhage or perforation, which increases in the elderly, particularly women. A broad range of renal side effects has been ascribed to NSAIDs, of which acute renal impairment is the most common in the elderly. Although most NSAIDs have been reported to cause hepatotoxicity, serious abnormalities of liver function are rare and are largely unpredictable. Other adverse effects due to NSAIDs have also been described, some of which (e.g. cardiovascular, CNS and haematological effects) may be more common in the elderly.
按通用类别分组时,非甾体抗炎药(NSAIDs)是全球处方量最多的药物,在各国处方总量中占3%至9%。虽然NSAIDs约占所有报告药物不良反应的25%,但衰老可能会大幅增加NSAID引起反应的风险。有几个因素可能导致老年人NSAID相关毒性。与衰老相关的发病率增加可能导致服用多种强效药物,而不适当的药物治疗和依从性异常也会导致老年患者出现药物不良反应。药代动力学方面与年龄相关的改变可能会影响老年人对NSAIDs的处理;特别是,对于给健康老年患者服用的阿扎丙宗(阿扎酮)、萘普生、酮洛芬和水杨酸盐,适当减少剂量,而存在肾脏疾病时可能也需要减少双氟芬酸、吲哚美辛、舒林酸和甲芬那酸的剂量。随着年龄增长,NSAIDs药效学的变化,如中枢神经系统对NSAIDs的敏感性增加和体内稳态受损,也使老年人更容易出现NSAID相关不良反应。NSAID治疗导致的胃肠道毒性是一种类效应,这一点无可争议。已发现阿司匹林与单纯性胃溃疡有显著关联,但与单纯性十二指肠溃疡无关联,而非阿司匹林NSAIDs与单纯性胃溃疡和十二指肠溃疡均有显著关联。使用NSAIDs会使消化性溃疡疾病严重并发症(即出血或穿孔)的风险增加2至5倍,这种风险在老年人中,尤其是女性中会增加。NSAIDs有广泛的肾脏副作用,其中急性肾功能损害在老年人中最为常见。虽然大多数NSAIDs据报道会引起肝毒性,但严重肝功能异常很少见且在很大程度上不可预测。还描述了NSAIDs的其他不良反应,其中一些(如心血管、中枢神经系统和血液学影响)在老年人中可能更常见。