Difference between revisions of "Aprepitant"
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Cornel Chiu (talk | contribs) (Brief summary, Uses, contraindication, precautions, pharmacodynamics, adverse effects, chemistry and formulation) |
Cornel Chiu (talk | contribs) (References) |
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| contraindications = Known hypersensitivity | | contraindications = Known hypersensitivity | ||
| routes = PO or IV | | routes = PO or IV | ||
| dosage = | | dosage = 40 mg PO for PONV | ||
125 mg PO followed by 2 days of 80 mg PO for CINV | |||
| dosage_calculation = aprepitant | | dosage_calculation = aprepitant | ||
| mechanism = | | mechanism = Neurokinin 1 receptor antagonist | ||
| adverse_effects = Anaphylaxis | | adverse_effects = Anaphylaxis | ||
| metabolism = CYP3A4 oxidation | | metabolism = CYP3A4 oxidation | ||
| Line 14: | Line 15: | ||
}} | }} | ||
Aprepitant is a | 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<!-- Describe uses of the drug. If appropriate, add subsections for each indication. --> == | == Uses<!-- Describe uses of the drug. If appropriate, add subsections for each indication. --> == | ||
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=== Precautions<!-- List precautions for use of the drug. If none, this section may be removed. --> === | === Precautions<!-- List precautions for use of the drug. If none, this section may be removed. --> === | ||
* Coadministration with warfarin may result in a clinically significant decrease in International Normalized Ratio (INR) | * Coadministration with warfarin may result in a clinically significant decrease in International Normalized Ratio (INR)<ref name=":0">{{Citation|last=Zabirowicz|first=Eric S.|title=Pharmacology of Postoperative Nausea and Vomiting|date=2019|url=http://dx.doi.org/10.1016/b978-0-323-48110-6.00034-x|work=Pharmacology and Physiology for Anesthesia|pages=671–692|publisher=Elsevier|access-date=2023-01-05|last2=Gan|first2=Tong J.}}</ref> | ||
* Decreases the efficacy of hormonal contraceptives | * Decreases the efficacy of hormonal contraceptives<ref name=":0" /> | ||
* Avoid IV aprepitant in pregnant patients as it contains alcohol | * Avoid IV aprepitant in pregnant patients as it contains alcohol<ref name=":0" /> | ||
== Pharmacology == | == Pharmacology == | ||
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==== Mechanism of action<!-- Describe the mechanism of action for the primary uses of the drug. --> ==== | ==== Mechanism of action<!-- Describe the mechanism of action for the primary uses of the drug. --> ==== | ||
Antagonism of | 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<ref name=":0" />. Peripherally, the blockade of receptors in the gut may decrease the intensity of the emetic afferent signal to the central emetic structures. | ||
==== Adverse effects<!-- Describe any potential adverse effects of the drug. --> ==== | ==== Adverse effects<!-- Describe any potential adverse effects of the drug. --> ==== | ||
| Line 57: | Line 58: | ||
* 95% is bound to plasma proteins | * 95% is bound to plasma proteins | ||
* Crosses the blood brain barrier | * Crosses the blood brain barrier<ref name=":0" /> | ||
* Metabolized by CYP3A4 via oxidation w minor contribution by CYP1A2 and CYP2C19 | * Metabolized by CYP3A4 via oxidation w minor contribution by CYP1A2 and CYP2C19 <ref name=":0" /> | ||
* Terminal half-life is 9 to 13 hours | * Terminal half-life is 9 to 13 hours<ref name=":0" /> | ||
* Inducer of CYP3A4 and CYP2C9 | * Inducer of CYP3A4 and CYP2C9 | ||
| Line 68: | Line 69: | ||
== References == | == 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<ref name=":0" /> | |||
[[Category:Drug reference]] | [[Category:Drug reference]] | ||
Revision as of 14:39, 5 January 2023
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