Pharm
Aprepitant
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Aprepitant
, Emend, Cinvanti, Fosaprepitant, Aponvie
See Also
Neurokinin-1 Receptor Antagonist
Rolapitant
Antiemetic
Chemotherapy Induced Nausea and Vomiting
Postoperative 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
Chemotherapy Induced Nausea and Vomiting
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
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
Postoperative Nausea and Vomiting
Prophylaxis
Consider with
Dexamethasone
prior to neurosurgery
Post-op
Vomiting
prophylaxis
Oral (Emend): 40 mg orally given 3 hours or less prior to
Anesthesia
IV (Aponvie): 32 mg IV at
Anesthesia
induction
Pharmacokinetics
Terminal
Half-Life
: 9 to 13 hours after oral dose
Absorption is not affected by food
Hepatic Metabolism by
CYP3A4
,
CYP1A2
,
CYP2C19
Excretion in urine and stool
Adverse Effects
See
Neurokinin-1 Receptor Antagonist
Headache
Dizziness
Safety
Pregnancy Category B
Unknown safety in
Lactation
Drug Interactions
May affect drugs metabolized by
CYP3A4
CYP2C9 Inducer
Pimozide
Avoid with
NK1 Receptor Antagonist
Oral Contraceptive
s (OCP)
Aprepitant may reduce OCP efficacy (use second form of
Contraception
)
Warfarin
Aprepitant may affect INR
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
References
(2023)
Postoperative Nausea and Vomiting
Management, Presc Lett, #390431
Hamilton (2020) Tarascon Pocket Pharmacopoeia
(2003) Med Lett Drugs Ther 45(W1162B): 62-4 [PubMed]
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