Yang Lily P H, Scott Lesley J
Adis, North Shore, Auckland, New Zealand.
Drugs. 2009 Nov 12;69(16):2257-78. doi: 10.2165/11200980-000000000-00000.
Palonosetron is a second-generation serotonin 5-HT3 receptor antagonist, with a distinct pharmacological profile that differs from first-generation 5-HT3 receptor antagonists. Intravenous palonosetron is widely indicated for the prevention of chemotherapy-induced nausea and vomiting (CINV) in the acute and delayed phases following moderately emetogenic chemotherapy (MEC) and the prevention of CINV in the acute phase following highly emetogenic chemotherapy (HEC). In the US, oral palonosetron is approved for the prevention of CINV in the acute phase following MEC (although this formulation is not currently available), and intravenous palonosetron is indicated for the prevention of postoperative nausea and vomiting (PONV) in the first 24 hours following surgery. All indications are currently limited to adult patients. Intravenous palonosetron was noninferior to intravenous ondansetron (with statistically greater efficacy than ondansetron) or dolasetron in preventing CINV following MEC, or to intravenous ondansetron or granisetron in preventing CINV following HEC, in the acute phase. Statistically greater efficacy was seen with intravenous palonosetron than ondansetron or dolasetron in preventing CINV following MEC in the delayed phase. Oral palonosetron was noninferior to intravenous palonosetron in preventing CINV in the acute phase in patients receiving MEC. Intravenous palonosetron was superior to placebo in preventing PONV in the first 24 hours following surgery. Palonosetron was generally well tolerated in clinical trials. Intravenous palonosetron is a valuable option in the prevention of acute- and delayed-phase CINV in adult patients receiving MEC, and of acute-phase CINV in patients receiving HEC. Oral palonosetron is likely to be a useful addition to oral formulations of other 5-HT3 receptor antagonists in preventing CINV in patients receiving MEC. Intravenous palonosetron is a useful alternative to currently recommended agents in PONV prevention.
帕洛诺司琼是第二代5-羟色胺5-HT3受体拮抗剂，具有与第一代5-HT3受体拮抗剂不同的独特药理学特性。静脉注射帕洛诺司琼广泛用于预防中度致吐性化疗（MEC）后急性期和延迟期的化疗引起的恶心和呕吐（CINV），以及预防高度致吐性化疗（HEC）后急性期的CINV。在美国，口服帕洛诺司琼被批准用于预防MEC后急性期的CINV（尽管目前该剂型不可用），静脉注射帕洛诺司琼用于预防手术后最初24小时内的术后恶心和呕吐（PONV）。目前所有适应症均限于成年患者。在预防MEC后急性期的CINV方面，静脉注射帕洛诺司琼不劣于静脉注射昂丹司琼（统计学上疗效高于昂丹司琼）或多拉司琼，在预防HEC后急性期的CINV方面，不劣于静脉注射昂丹司琼或格拉司琼。在预防MEC后延迟期的CINV方面，静脉注射帕洛诺司琼的疗效在统计学上高于昂丹司琼或多拉司琼。在接受MEC的患者中，口服帕洛诺司琼在预防急性期CINV方面不劣于静脉注射帕洛诺司琼。静脉注射帕洛诺司琼在预防术后最初24小时内的PONV方面优于安慰剂。帕洛诺司琼在临床试验中一般耐受性良好。静脉注射帕洛诺司琼是预防接受MEC的成年患者急性期和延迟期CINV以及接受HEC患者急性期CINV的有价值选择。口服帕洛诺司琼可能是预防接受MEC患者CINV的其他5-HT3受体拮抗剂口服制剂的有用补充。静脉注射帕洛诺司琼是预防PONV目前推荐药物的有用替代药物。
