1.1. Adults
Aprepitant is FDA-approved for prevention of CINV due to high and moderate emetogenic agents including high dose cisplatin, as well as prevention for PONV1-4. When used to prevent CINV with highly emetogenic chemotherapy, aprepitant and rolapitant are prescribed as triple or quadruple therapy in combination with a 5-HT3 receptor antagonist, dexamethasone, and olanzapine based on product labeling, clinical trial data, as well as data from available published antiemetic guidelines8,9. Rolapitant is indicated to manage delayed CINV seen with initial and repeat courses of chemotherapy, including, but not limited to, highly emetogenic chemotherapy1,2,6. Netupitant (substance P/NK1 receptor antagonist) and palonosetron (selective 5-HT3 receptor antagonist), as combination therapy, are FDA-approved to prevent acute and delayed CINV seen with initial and repeat courses of chemotherapy, including, but not limited to, highly emetogenic chemotherapy1,2,7. Maximum recommended adult dosages for substance P/NK1 receptor antagonists are summarized in Tables 1 and 2. Dosages exceeding those listed in Tables 1 and 2 will be reviewed.
| Drug Name | Dosage Form/Strength | Treatment Indication | Maximum Recommended Dosage |
|---|---|---|---|
| aprepitant (Emend®) | 40 mg, 80 mg, 125 mg capsules 125 mg/5 ml oral suspension |
preventing CINV: highly or moderately emetogenic chemotherapy: day 1 (one hour before chemotherapy) |
125 mg/day (as capsule or suspension)*! |
| preventing CINV: highly or moderately emetogenic chemotherapy: days 2 and 3 |
80 mg/day (as capsule or suspension)+@ ¥α | ||
| PONV: within 3 hours of anesthesia induction |
40 mg as a single dose (as capsule) | ||
| rolapitant (Varubi®) | 90 mg tablet | preventing delayed CINV seen with highly emetogenic chemotherapy | 180 mg as a single dose 1 to 2 hours before chemotherapy on day 1 (2 x 90 mg tablets)^!@ |
| preventing delayed CINV seen with non-highly emetogenic chemotherapy and combinations of anthracycline and cyclophosphamide | 180 mg as a single dose 1 to 2 hours before chemotherapy on day 1 (2 x 90 mg tablets)#**α |
Legend:
- * for high and moderate emetic risk regimens, use in conjunction with a 5-HT3 receptor antagonist plus dexamethasone on day 1 (product labeling)
- ! for high emetic risk regimens, use in conjunction with a 5-HT3 receptor antagonist, dexamethasone, and olanzapine on day 1 (guideline recommendation)8,9
- + for high emetic risk regimens, use in conjunction with dexamethasone on days 2-3; dexamethasone monotherapy is given on day 4 (product labeling)
- @ for high emetic risk regimens, administer dexamethasone and olanzapine on days 2-4 (guideline recommendation)8,9
- ¥ for high emetic risk regimens containing an anthracycline combined with cyclophosphamide, dexamethasone should not be continued on days 2-4 (guideline recommendation)8,9
- α for moderate emetic risk regimens with a known risk for delayed nausea and vomiting such as cyclophosphamide, doxorubicin, or oxaliplatin; continue dexamethasone through day 3 (guideline recommendation)8,9
- ^ in conjunction with dexamethasone and a 5-HT3 receptor antagonist on day 1, and dexamethasone on days 2-4 (product labeling)
- # for moderate emetic risk regimens, use in conjunction with dexamethasone and a 5-HT3 receptor antagonist on day 1. Continue 5-HT3 receptor antagonist therapy on days 2-4 (product labeling).
- ** for high emetic risk regimens containing an anthracycline combined with cyclophosphamide, use in conjunction with a 5-HT3 receptor antagonist, dexamethasone, and olanzapine on day 1. Olanzapine monotherapy is given on days 2-4 (guideline recommendation)8,9
- PONV = postoperative nausea and vomiting
- CINV = chemotherapy-induced nausea and vomiting
- PONV = postoperative nausea and vomiting
| Drug Name | Treatment Indication | Dosage Form/Strength | Maximum Recommended Dosage |
|---|---|---|---|
| netupitant/palonosetron (Akynzeo®) | preventing acute and delayed CINV seen with chemotherapy (highly emetogenic) | 300 mg netupitant/ 0.5 mg palonosetron capsules | 1 capsule on day 1 (one hour before chemotherapy)**#! |
| preventing acute and delayed CINV seen with chemotherapy (NOT highly emetogenic) | 300 mg netupitant/ 0.5 mg palonosetron capsules | 1 capsule on day 1 (one hour before chemotherapy)++ α |
Legend:
- ** in conjunction with dexamethasone 30 minutes before chemotherapy on day 1, and dexamethasone once daily on days 2-4 (product labeling)
- # for high emetic risk regimens, use in conjunction with dexamethasone and olanzapine on day 1. Continue dexamethasone and olanzapine on days 2-4 (guideline recommendation)8,9
- ! for high emetic risk regimens containing an anthracycline combined with cyclophosphamide, use in conjunction with dexamethasone and olanzapine on day 1. Olanzapine monotherapy is given on days 2-4 (guideline recommendation)8,9
- ++ for regimens that are not considered high emetic risk, use in conjunction with dexamethasone 30 minutes before chemotherapy on day 1 (product labeling)
- α for moderate emetic risk regimens with a known risk for delayed nausea and vomiting such as cyclophosphamide, doxorubicin, or oxaliplatin; continue dexamethasone through day 3 (guideline recommendation)8,9
- CINV = chemotherapy-induced nausea and vomiting