Difference between revisions of "Aprepitant"
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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<ref name=":0" /> | 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<ref name=":0" /> | ||
[[Category:Drug reference]] | [[Category:Drug reference]] | ||
<references /> | |||
[[Category:Antiemetics]] | |||
Revision as of 12:18, 8 January 2023
| Trade names |
Emend |
|---|---|
| Clinical data | |
| Drug class |
Antiemetic |
| 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 |
Decreased efficacy of hormonal contraceptives CYP interactions |
| 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 antiemetic regimen to prevent postoperative nausea and vomiting, as well as prevention of acute and delayed chemotherapy-induced nausea and vomiting.
Uses
- Prevention of postoperative nausea and vomiting
- Prevention of chemotherapy-induced nausea and vomiting
Contraindications
Absolute contraindications
- Known hypersensitivity
Precautions
- Decreases the efficacy of hormonal contraceptives for up to 28 days[1]
- Inhibits CYP3A4 and induces CYP2C9[2]
- Some other drugs may need close monitoring and/or dose adjustment postoperatively (e.g. warfarin)
- Some formulations of IV aprepitant may contain alcohol which should be avoided in pregnant patients[1]
- IV fosaprepitant is not prepared with alcohol
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 antiemetic 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]
- Inhibits CYP3A4 and induces 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]
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 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
- ↑ Aapro, M. S.; Walko, C. M. (2010-12). "Aprepitant: drug-drug interactions in perspective". Annals of Oncology: Official Journal of the European Society for Medical Oncology. 21 (12): 2316–2323. doi:10.1093/annonc/mdq149. ISSN 1569-8041. PMID 20488873. Check date values in:
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