Aprepitant
| Trade names |
Emend |
|---|---|
| Clinical data | |
| Drug class |
Anti-emetic |
| Uses |
Postoperative Nausea and Vomiting |
| Contraindications |
Known hypersensitivity |
| Routes of administration |
PO or IV |
| Dosage |
40 mg PO for PONV 125 mg PO followed by 2 days of 80 mg PO for CINV |
| Dosage | |
| Pharmacodynamics | |
| Mechanism of action |
Neurokinin 1 receptor antagonist |
| Adverse effects |
Anaphylaxis |
| Pharmacokinetics | |
| Metabolism |
CYP3A4 oxidation |
| Protein binding |
95% |
| Physical and chemical data | |
| Article quality | |
| Editor rating | |
| User likes | 0 |
Aprepitant is a neurokinin 1 (NK1) antagonist that is used in combination with standard anti-emetic regimen to prevent acute and delayed chemotherapy induced nausea and vomiting as well as prevention of post-operative nausea and vomiting.
Uses
- Supplement standard anti-emetic regimen in chemotherapy induced nausea and vomiting
- Supplement standard anti-emetic regimen in post operative nausea and vomiting
Contraindications
Absolute contraindications
- Known hypersensitivity
Precautions
- Coadministration with warfarin may result in a clinically significant decrease in International Normalized Ratio (INR)[1]
- Decreases the efficacy of hormonal contraceptives[1]
- Avoid IV aprepitant in pregnant patients as it contains alcohol[1]
Pharmacology
Pharmacodynamics
Mechanism of action
Antagonism of neurokinin-1 (NK1) receptors centrally (requires > 95% blockade to have maximum efficacy) and peripherally (located in the gut). NK1 receptor antagonists exert their main anti-emetic action by depressing the neural activity of the nucleus tracts solitaires lying ventrally to the to the area postrema[1]. Peripherally, the blockade of receptors in the gut may decrease the intensity of the emetic afferent signal to the central emetic structures.
Adverse effects
- Anaphylactic reaction
- Angioedema
- Urticaria
- Toxic epidermal necrolysis
- Acne vulgaris
- Photosensitivity
- Oily skin
- Skin lesion
- Headache
- Dizziness
- Fatigue
Pharmacokinetics
- 95% is bound to plasma proteins
- Crosses the blood brain barrier[1]
- Metabolized by CYP3A4 via oxidation w minor contribution by CYP1A2 and CYP2C19 [1]
- Terminal half-life is 9 to 13 hours[1]
- Inducer of CYP3A4 and CYP2C9
Chemistry and formulation
Aprepitant is administered orally and intravenously. Fosaprepitant, a prodrug of aprepitant, is administered intravenously.
History
References
Zabirowicz, Eric S.; Gan, Tong J. (2019), "Pharmacology of Postoperative Nausea and Vomiting", Pharmacology and Physiology for Anesthesia, Elsevier, pp. 671–692, retrieved 2023-01-05[1]
Top contributors: Cornel Chiu, Olivia Sutton and Chris Rishel