Indiana University School of Medicine, 1234 Notre Dame Avenue, South Bend, IN 46617, USA.
Drugs. 2013 Mar;73(3):249-62. doi: 10.1007/s40265-013-0019-1.
Chemotherapy-induced nausea and vomiting (CINV) is associated with a significant deterioration in quality of life. The emetogenicity of the chemotherapeutic agents, repeated chemotherapy cycles, and patient risk factors significantly influence CINV. The use of a combination of a serotonin 5-HT3 receptor antagonist, dexamethasone and a neurokinin 1 (NK1) receptor antagonist has significantly improved the control of acute and delayed emesis in single-day chemotherapy. Palonosetron, a second-generation 5-HT3 receptor antagonist with a different half-life, a different binding capacity and a different mechanism of action than the first-generation 5-HT3 receptor antagonists appears to be the most effective agent in its class. Aprepitant, the first and only agent clinically available in the NK1 receptor antagonist drug class has been used effectively as an additive agent to the 5-HT3 receptor antagonists and dexamethasone to control CINV. Rolapitant and netupitant are other NK1 receptor antagonists that are currently in phase III clinical trials. Despite the control of emesis, nausea has not been well controlled by current agents. Olanzapine, a US-FDA approved antipsychotic, has emerged in recent trials as an effective preventative agent for CINV, as well as a very effective agent for the treatment of breakthrough emesis and nausea. Clinical trials using gabapentin, cannabinoids and ginger have not been definitive regarding their efficacy in the prevention of CINV. Additional studies are necessary for the control of nausea and for the control of CINV in the clinical settings of multiple-day chemotherapy and bone marrow transplantation.
化疗引起的恶心和呕吐（CINV）与生活质量的显著恶化有关。化疗药物的致吐性、重复的化疗周期和患者的风险因素都会显著影响 CINV。联合使用 5-羟色胺 3 受体拮抗剂、地塞米松和神经激肽 1（NK1）受体拮抗剂可显著改善单日化疗中急性和迟发性呕吐的控制。帕洛诺司琼是一种第二代 5-HT3 受体拮抗剂，与第一代 5-HT3 受体拮抗剂相比，其半衰期、结合能力和作用机制不同，似乎是该类药物中最有效的药物。阿瑞匹坦是 NK1 受体拮抗剂类药物中首个也是唯一的临床应用药物，已作为添加剂与 5-HT3 受体拮抗剂和地塞米松联合用于控制 CINV。拉洛昔芬和奈妥匹坦是其他正在进行 III 期临床试验的 NK1 受体拮抗剂。尽管呕吐得到了控制，但目前的药物并不能很好地控制恶心。奥氮平是一种获得美国食品和药物管理局（FDA）批准的抗精神病药物，在最近的试验中作为 CINV 的有效预防药物，以及治疗突破性呕吐和恶心的非常有效药物出现。加巴喷丁、大麻素和姜黄在预防 CINV 方面的临床试验结果并不明确。需要进一步的研究来控制恶心和 CINV，特别是在多日化疗和骨髓移植的临床环境中。
