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Published online by Cambridge University Press: 06 October 2020
THERAPEUTICS
Brands
• Akynzeo
Generic?
• No
Class
• Antiemetic
Commonly Prescribed for
(FDA approved in bold)
• Prevention of chemotherapy-induced nausea and vomiting (CINV)
• Nausea and vomiting (gastroenteritis, postoperative)
• Pruritus
How the Drug Works
• Netupitant: selectively inhibits substance P (vomit inducer) at neurokinin 1 (NK1) receptors with long-lasting brain receptor (brainstem, area postrema) saturation after single dose
• Palonosetron: second-generation 5-HT3 antagonist with higher binding affinity and longer plasma half-life. It may trigger 5-HT3 receptor internalization and prolong receptor inhibition
How Long Until It Works
• Typically less than an hour
If It Works
• Use at lowest effective dose
If It Doesn't Work
• Increase dose, or discontinue and change to another agent
Best Augmenting Combos for Partial Response or Treatment-Resistance
• May add D2 antagonist, antihistamine, benzodiazepine, or corticosteroid
Tests
• None required
ADVERSE EFFECTS (AEs)
How the Drug Causes AEs
• Not known
Notable AEs
• Headache, asthenia, dyspepsia, fatigue, constipation, and erythema
Life-Threatening or Dangerous AEs
• Serotonin syndrome
• Hypersensitivity reactions such as angioedema and Stevens-Johnson syndrome have been reported
Weight Gain
• Unusua
Sedation
• Unusual
What to Do About AEs
• Reduce dose or discontinuation
Best Augmenting Agents to Reduce AEs
• Symptomatic management
DOSING AND USE
Usual Dosage Range
• 1 capsule
Dosage Forms
• Capsule: 300mg netupitant and 0.5mg palonosetron
How to Dose
• One capsule 1 hour and dexamethasone 12mg 30 minutes prior to chemotherapy on day 1. Dexamethasone 8mg orally once daily on days 2 to 4 if under highly emetogenic chemotherapy (cisplatin)
Dosing Tips
• Can be taken with or without food. Only for short-term use
Overdose
• May develop drowsiness or headache
Long-Term Use
• Not been studied
Habit Forming
• No
How to Stop
• No need to taper
Pharmacokinetics
• Netupitant: Tmax: 5 hours. Half-life: 80 hours. > 99.5% protein bound. Metabolized by CYP3A4 and inhibits CYP3A4
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