Aapro Matti
Clinique de Genolier, 1 Route du Muids, CH-1272 Genolier, Switzerland.
Oncologist. 2004;9(6):673-86. doi: 10.1634/theoncologist.9-6-673.
Nausea and vomiting are typical side effects of cytotoxic therapy and some surgical procedures. These symptoms can represent a major therapeutic challenge and, if inadequately controlled by antiemetic treatment, will result in increased mortality, morbidity, and health care costs. However, the management of nausea and vomiting has improved greatly in recent years following the introduction of the 5-HT3-receptor antagonists, known as 'setrons.' In light of recent developments in antiemetic care, including the approval of the first neurokinin-1-receptor antagonist aprepitant (Emend; Merck and Company, Inc.; West Point, PA) and a new 5-HT3 receptor antagonist palonosetron (Aloxi; MGI Pharma; Minneapolis, MN), this article provides an update on the clinical experience gained with the 5-HT3-receptor antagonist granisetron (Kytril; Roche Laboratories, Inc.; Nutley, NJ) for the management of chemotherapy-induced, radiation-induced, and postoperative nausea and vomiting, and also reviews its use in special patient populations. Granisetron is a potent and highly selective 5-HT3-receptor antagonist that has little or no affinity for other receptors, a characteristic that is thought to underlie the favorable side-effect and safety profiles of this agent. Extensive clinical trial data have shown granisetron to be an effective and well-tolerated agent for the treatment of nausea and vomiting in the oncology and surgical settings. Granisetron has also been shown to be effective and well tolerated in special populations, such as patients refractory to antiemetic treatment, patients with hepatic or renal impairment, and children. Data also suggest that its safety profile and minimal potential for drug-drug interactions would make it an antiemetic agent of choice for elderly cancer patients.
恶心和呕吐是细胞毒性疗法及一些外科手术的典型副作用。这些症状可能构成一项重大的治疗挑战,若抗呕吐治疗控制不当,将会导致死亡率、发病率上升以及医疗费用增加。然而,自被称为“司琼类”的5-羟色胺3(5-HT3)受体拮抗剂问世以来,近年来恶心和呕吐的治疗有了很大改善。鉴于抗呕吐护理方面的最新进展,包括首个神经激肽-1受体拮抗剂阿瑞吡坦(意美;默克公司;宾夕法尼亚州西点)及新型5-HT3受体拮抗剂帕洛诺司琼( Aloxi;MGI制药公司;明尼苏达州明尼阿波利斯)获批,本文提供了关于5-HT3受体拮抗剂格拉司琼(凯特瑞;罗氏实验室;新泽西州纳特利)用于治疗化疗引起的、放疗引起的及术后恶心和呕吐的临床经验的最新情况,并对其在特殊患者群体中的应用进行了综述。格拉司琼是一种强效且高度选择性的5-HT3受体拮抗剂,对其他受体几乎没有或没有亲和力,这一特性被认为是该药物良好的副作用和安全性特征的基础。大量临床试验数据表明,格拉司琼在肿瘤学和外科手术环境中是治疗恶心和呕吐的一种有效且耐受性良好的药物。格拉司琼在特殊人群中,如对抗呕吐治疗难治的患者、肝或肾功能损害患者以及儿童中,也已被证明是有效且耐受性良好的。数据还表明,其安全性特征及极小的药物相互作用可能性使其成为老年癌症患者的首选抗呕吐药物。