阿瑞吡坦是第一种可帮助患者避免恶心及呕吐-通常在患者接受极易引起呕吐的化疗法治疗后第一天即发生，并可持续几天-这种症状持续发生的药物
靶 点:
为P/神经激肽受体拮抗剂。
作用机制:
为P/神经激肽受体拮抗剂，它是由FDA批准的第一种可帮助患者避免恶心及呕吐-通常在患者接受极易引起呕吐的化疗法治疗后第一天即发生，并可持续几天-这种症状持续发生的药物
临床阶段:2003年3月美国FDA批准上市
EMEND
Generic Name for EMEND
Aprepitant 40mg, 80mg, 125mg; caps.
Legal Classification:
Rx
Pharmacological Class for EMEND
Substance P/neurokinin 1 receptor antagonist.
Manufacturer of EMEND
Merck & Co., Inc.
Indications for EMEND
In combination with other antiemetic agents to prevent acute and delayed nausea and vomiting associated with initial and repeat courses of moderately to highly emetogenic cancer chemotherapy, including high-dose cisplatin. Prevention of post-op nausea and vomiting.
Adult dose for EMEND
≥18yrs: Chemotherapy: Give with corticosteroid and 5-HT3 antagonist. Day 1 of chemotherapy cycle: 125mg 1 hour before chemotherapy; Days 2 and 3: 80mg once daily in the AM. Post-op prophylaxis: 40mg within 3hrs prior to anesthesia.
Children's dosing for EMEND
<18yrs: not recommended.
Also:
EMEND INJECTION
Contraindications for EMEND
Concomitant pimozide, cisapride.
Warnings/Precautions for EMEND
Not for chronic continuous use. Severe hepatic insufficiency. Pregnancy (Cat.B). Nursing mothers: not recommended.
Interactions for EMEND
See Contraindications. Monitor, and caution with, CYP3A4 substrates, including chemotherapy agents (eg, ifosfamide, vinblastine, vincristine); CYP3A4 inhibitors (eg, azole antifungals, macrolides, nefazodone, ritonavir, nelfinavir, diltiazem); and with CYP3A4 inducers (eg, carbamazepine, phenytoin, rifampin). Potentiates dexamethasone (reduce its dose by 50%), methylprednisolone (reduce its IV dose by 25% and its oral dose by 50%), midazolam, alprazolam, triazolam. May antagonize warfarin (closely monitor INR for 2 weeks after starting each regimen); phenytoin, tolbutamide, other CYP2C9 substrates; paroxetine, oral contraceptives (use alternative or backup method during and for 1 month after last dose).
Adverse Reactions for EMEND
Asthenia, fatigue, hiccups, diarrhea, constipation, anorexia, dyspepsia. Injection: inj site pain, headache.
How is EMEND supplied?
Caps 125mg—30
40mg—1
Bi-fold pack (2 x 80mg)—1
Tri-fold pack (1 x 125mg + 2 x 80mg)—1
Vial—1
阿瑞吡坦可预防术后恶心呕吐
美国杜克大学医学中心麻醉科Gan医师报告,NK-1受体拮抗剂阿瑞吡坦(aprepitant)较之常用的镇吐药物昂丹司琼(枢复宁)对减少患者术后呕吐更有效。
该多中心临床试-验纳入805例因腹部手术而接受全身麻醉的住院患者。这些患者随机分成三组:口服阿瑞吡坦125 mg(1组)和阿瑞吡垣40 mg组(2组),以及静脉注射昂丹司琼4 mg组(3组)。均为术前单次给药,并采用双盲法。
术后最初48小时内,患者在麻醉复苏室接受持续监测,多时点记录呕吐次数,补救治疗恶心或呕吐的次数,以及恶心的严重程度。主要观察终点为术后0~24小时内完全有效(无呕吐及补救治疗)。次要观察终点包括0~24小时内无呕吐、无补救治疗以及0~48小时无呕吐。通过报告的不良事件、体格及实验室检查、苏醒时间以及麻醉后的恢复时间评估耐受性。
结果显示,阿瑞吡坦1组95%和2组90%的患者术后24小时没有发生呕吐,而3组只有74 %的患者没有发生呕吐(P<0.001)。相应的术后48小时呕吐发生率分别为93%、85%和67%。三组患者的耐受性差别无显著性,患者对阿瑞吡坦40 mg和125 mg均有良好的耐受性。该结果表明阿瑞吡垣预防术后呕吐的作用显著好于昂丹司琼,较大剂量的阿瑞吡坦效果更佳。
Gan医师认为,这个结果非常重要。他说,很多患者都害怕呕吐超过术后疼痛。这是第一次有一种镇吐药可以使超过90%的患者获得持久的镇吐效果。