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Antiemesis
NCCN Guidelines Version 1.2019
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International Manual of Oncology Practice pp 779-804
Chemotherapy-induced nausea
and/ or vomiting (CINV)
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For cisplatin, emesis reaches
Delayed-onset
its max. intensity 48-72 hr
after administration and can
last 6-7 days
Acute-onset
Anticipatory CINV
Before CT
CT
24 hr
48hr
6-7 days
Anticipatory CINV
Acute-onset
Delayed-onset
- Nausea
- 18-57%
- Younger p’t
- Peak: 5-6 hr
- Cisplatin
carboplatin
cyclophosphamide
doxorubicin
Breakthrough CINV
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Corticosteroid antiemetic premedication should be avoid with immune
checkpoint inhibitors when administered without cytotoxic chemotherapy.
(Nivolumab, Pembrolizumab, Atezolizumab, Ipilimumab)
N/V prevention for HEC
4-drug regimen
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N/V prevention for MEC
2-drug regimen
5 mg
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Types of Antiemetic Therapies
• Serotonin (5-HT3 ) Antagonists
• Ondansetron, Granisetron, Dolasetron, Palonosetron
• Acute N/V
• Palonosetron was significantly more effective in preventing acute
and delayed N/V for both HEC and MEC
• Binding affinity 100-fold higher than others
• T1/2 40 hr: preventing delayed N/V
• Side effects
• Heart (prolongation of PR or QT interval), cardiac arrhythmia
• Except, palonosetron, granisetron extended-release inj., granisetron
transdermal patch
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Akynzeo® capsule
(Palonosetron 0.5 mg,
netupitant 300 mg )
• Neurokinin-1-receptor antagonists
• Aprepitant, fosaprepitant, rolapitant, netupitant
• Oral aprepitant
• FDA approved for the prevention of N/V in p’t receiving HEC and
MEC
• 125 mg on day 1, 80 mg on day 2 and 3
• Fosaprepitant inj.
• 150 mg IV on day 1
• Aprepitant injectable emulsion
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• Other antiemetics
• Corticosteroids: dexamethasone
• DM p’t
• Dyspepsia, insomia
• Olanzapine
• Atypical antipsychotic
• EPS: combination with primperan or haloperidol
• Prolongation of QT interval
• Benzodiazepines、Phenothiazines、metoclopramide
• EPS
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健保規範-Antiemetic drugs
• Serotonin antagonists: ondansetron、granisetron
(Otril®3mg/3mL、Sancuso® 3.1mg/24hr/patch)、tropisetron、
ramosetron、palonosetron (Aloxi ® 0.25mg/5ml/vial)
• 中、高致吐性藥品:
• 預防性使用ondansetron 8~32 mg、granisetron 1~3 mg 、tropisetron 5 mg、
ramosetron 0.3 mg
• 嚴重延遲性嘔吐 (≤5 days)
• 血腫病患得依患者接受抗癌藥品實際使用天數使用本類製劑
• Palonosetron限於中、高致吐化學治療之前使用
• 接受腹部放射照射之癌症病人
• 經使用dexamethasone、metoclopramide或prochlorperazine等傳統止吐劑無效，仍
發生嚴重嘔吐之患者
• 穿皮貼片劑限用於無法口服之病患
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• Neurokinin-1 receptor antagonist: aprepitant、fosaprepitant
• 與其他止吐藥劑併用，以防止由高致吐性癌症化療藥物在初次或重
覆使用時所引起的急性或延遲性噁心與嘔吐
• 口服製劑限用三天，每日限用一顆。注射製劑限於化療第一天使用。
• 本品除第一天外，不得併用5-HT3之藥物。
• 若於化療第四天（含）後仍有Grade 2 以上之嘔吐，則於第四天及
第五天可依照7.2.1.規範給予serotonin antagonist。
• 含palonosetron及netupitant之複方製劑(如Akynzeo)
• 限用於防止由高致吐性癌症化療藥物在初次或重覆使用時所引起的
急性或延遲性噁心與嘔吐。
• 每次化療限使用1粒。
• 自使用本案藥品之日起3天內不得併用其他serotonin antagonist或
neurokinin-1 receptor antagonist止吐劑。
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Updates
• Aprepitant injectable emulsion
• Dexamethasone dose for HEC and MEC regimens
• Day 1: 12 mg PO/ IV once
• Day 2-4: 8 mg PO/IV daily
• Can be replaced with olanzapine
• Any NK1 RA could be used in the 4-drug HEC regimen on day 1
(olanzapine/ NK1 RA/ 5-HT3/ dexamethasone)
• 3-drug olanzapine regimen fore HEC and MEC: only
palonosetron should be used (olanzapine/ palonosetron/
dexamethasone)
• NK1 RA+ 5-HT3/dexamethasone regimen( 2-drug regimen)
• MEC therapy, additional risk factors or previous treatment failure
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• Irinotecan (liposomal)-MEC
• Atezolizumab- minimal emetic
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References
• NCCN Guidelines Version 1.2019, Antiemesis
• International Manual of Oncology Practice pp 779-804
• The Journal of Taiwan Pharmacy, vol. 28, No. 2, 2012