Pharm
Neurokinin-1 Receptor Antagonist
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Neurokinin-1 Receptor Antagonist
, NK1 Receptor Antagonist, Netupitant
See Also
Aprepitant
Rolapitant
Antiemetic
Chemotherapy Induced Nausea and Vomiting
Indications
Prevention of
Nausea
,
Vomiting
with highly emetogenic
Chemotherapy
Typically used in combination with
5-HT3 Antagonist
s and
Dexamethasone
20 mg daily
Mechanism
Blocks the neurokinin-1 receptor (a tachykinin)
Cross the blood brain barrier to inhibit CNS substance-P activity
Effects
Antiemetic
(synergistic with
5-HT3 Antagonist
s)
Anxiolysis and
Antidepressant
properties
Dosing
Aprepitant
Typically administered with
5-HT3 Antagonist
s and
Dexamethasone
before
Chemotherapy
Oral (
Emend
) before
Chemotherapy
Adult: 125 mg orally 1 hour before
Chemotherapy
, then 80 mg orally daily in AM on days 2 and 3
Child (age >6 months): 3 mg/kg (up to 125 mg), then 2 mg/kg (up to 80 mg) orally daily in AM on days 2 and 3
Oral (
Emend
) post-op
Vomiting
prophylaxis
Adult: 40 mg orally given 3 hours or less prior to
Anesthesia
IV before
Chemotherapy
Fosaprepitant
(
Aprepitant
prodrug)
Adult: 150 mg infused over 20 to 30 minutes
Child: 3 mg/kg (up to 125 mg) IV over 20 to 30 minutes, followed by oral
Emend
on days 2, 3 (see dose above)
Cinvanti
Adult: 130 mg IV over 2 minutes (or infused over 30 min) OR 100 mg IV followed by oral
Emend
on days 2, 3
Dosing
Rolapitant
(
Varubi
)
Typically administered with
5-HT3 Antagonist
s and
Dexamethasone
before
Chemotherapy
Take 180 mg orally 1 to 2 hours prior to
Chemotherapy
Dosing
Netupitant/
Palonosetron
(
Akynzeo
)
See
Akynzeo
Combined 5HT-3
Antagonist
(
Palonosetron
) with the NK1
Antagon
ist Netupitant
Contraindicated in severe renal disease (including
ESRD
) and severe hepatic disease
Oral: Take 1 capsule orally one hour before
Chemotherapy
IV: Give one injectable vial diluted in 50 ml over 30 min prior to
Chemotherapy
Adverse Effects
Asthenia
or
Fatigue
Hiccup
s
Drug Interactions
See
Aprepitant
(
Emend
,
Fosaprepitant
,
Cinvanti
)
See
Rolapitant
(
Varubi
)
Resources
NK1 Receptor Antagonist (Wikipedia)
https://en.wikipedia.org/wiki/NK1_receptor_antagonist
Antiemetic
Neurokinin-1 Receptor Blockers (Stat Pearls)
https://www.ncbi.nlm.nih.gov/books/NBK470394
Aprepitant
-
Emend
(DailyMed)
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f58b8944-93ee-4be1-a238-cc0061ddd93a
Aprepitant
-
Cinvanti
(DailyMed)
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4c218d3a-a508-4abc-9ed8-a6e8e191d1b4
Rolapitant
(DailyMed)
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a52896cd-4a98-49b8-82db-bf1985a64d97
References
Hamilton (2020) Tarascon Pocket Pharmacopoeia
(2003) Med Lett Drugs Ther 45(W1162B): 62-4 [PubMed]
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