Cancer Care Program, Eastern Europe World Health Organization.
Expert Opin Pharmacother. 2014 Dec;15(17):2599-608. doi: 10.1517/14656566.2014.972366. Epub 2014 Oct 17.
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 introduction of 5-hydroxytryptamine-3 (5-HT3) receptor antagonists has been a major factor in the improvement of the prevention of chemotherapy-induced acute and delayed emesis. 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 this drug class.
Palonosetron's chemistry, pharmacodynamics, pharmacokinetics, metabolism, clinical efficacy, including comparison with other antiemetics, role in controlling nausea, potential role in multi-day chemotherapy and bone marrow transplantation, and overall safety are discussed.
The clinical data in the literature have established palonosetron as the 5-HT3 receptor antagonist of choice in terms of efficacy and safety for the prevention of CINV for patients receiving moderately or highly emetogenic chemotherapy. Three international guidelines have listed palonosetron as the preferred 5-HT3 receptor antagonist. Due to its higher efficacy, the use of palonosetron may be more cost effective compared to the generic first-generation 5-HT3 receptor antagonists. Clinical organizations' pharmacy and formulary committees should consider efficacy when making recommendations for agents for the prevention of CINV.
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、重复化疗周期和患者的风险因素都会显著影响 CINV。5-羟色胺 3（5-HT3）受体拮抗剂的引入是改善化疗引起的急性和迟发性呕吐预防的主要因素。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。
帕洛诺司琼的化学、药效学、药代动力学、代谢、临床疗效，包括与其他止吐药的比较、对控制恶心的作用、在多日化疗和骨髓移植中的潜在作用以及总体安全性进行了讨论。
文献中的临床数据表明，帕洛诺司琼在预防中高度致吐性化疗引起的 CINV 方面的疗效和安全性方面是 5-HT3 受体拮抗剂的首选。三个国际指南都将帕洛诺司琼列为首选的 5-HT3 受体拮抗剂。由于其更高的疗效，与通用的第一代 5-HT3 受体拮抗剂相比，帕洛诺司琼的使用可能更具成本效益。临床组织的药剂科和处方委员会在推荐预防 CINV 的药物时应考虑疗效。
