Aprepitant
- Atc Codes:A04AD12
- CAS Codes:170729-80-3
- PHARMGKB ID:170729-80-3
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Emend; Belgium: Emend; Bulgaria: Emend; Cyprus: Emend; Czech Republic: Emend; Denmark: Emend; Estonia: Emend; Finland: Emend; France: Emend; Germany: Emend; Greece: Emend; Hungary: Emend; Ireland: Emend; Italy: Emend; Latvia: Emend; Lithuania: Emend; Luxembourg: Emend; Malta: Emend; Netherlands: Emend; Poland: Emend; Portugal: Emend; Romania: Emend; Slovakia: Emend; Slovenia: Emend; Spain: Emend; Sweden: Emend; UK: Emend.
North America
Canada: Emend; USA: Emend.
Latin America
Argentina: Emend.
Drug combinations
Chemistry
Aprepitant: C~23~H~21~F~7~N~4~O~3~. Mw: 534.43. (1) 3H-1,2,4-Triazol-3-one, 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-; (2) 3-[[(2R,3S)-3-(p-Fluorophenyl)-2-[[(αR)-α-methyl-3,5-bis(trifluoromethyl)benzyl]oxy]morpholino]methyl]-Δ^2^-1,2,4-triazolin-5-one. CAS-170729-80-3 (2000).
Pharmacologic Category
Antiemetics, Miscellaneous; Substance P/Neurokinin-1 Receptor Antagonist. (ATC-Code: A04AD12).
Mechanism of action
Inhibits the substance P/neurokinin-1 (NK~1~) receptor. Augments the antiemetic activity of the 5-HT~3~ receptor antagonist and corticosteroid activity and inhibits both acute and delayed phases of chemotherapy-induced emesis.
Therapeutic use
Prevention of acute and delayed nausea and vomiting associated with emetogenic chemotherapy. Prevention of postoperative nausea and vomiting.
Pregnancy and lactiation implications
Teratogenic effects were not observed in animal studies. There are no adequate and well-controlled studies in pregnant women; use only if clearly needed. Not recommended for use during lactation.
Unlabeled use
Contraindications
Hypersensitivity to aprepitant or any component of the formulation. Use with cisapride or pimozide.
Warnings and precautions
Use with caution in hepatic impairment. Not for treatment of existing nausea and vomiting or for chronic continuous therapy. Potential for CYP-mediated interactions exists.