Difference between revisions of "Aprepitant"

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
	Pharmacodynamics
Mechanism of action	Substance P/Neurokinin 1 receptor antagonist
Adverse effects	Anaphylaxis
	Pharmacokinetics
Metabolism	CYP3A4 oxidation
Protein binding	95%
	Physical and chemical data
	Article quality
Editor rating	Comprehensive
User likes	0

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Revision as of 13:28, 4 January 2023

Aprepitant is a selective substance P neurokinin 1 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)
Decreases the efficacy of hormonal contraceptives
Avoid IV aprepitant in pregnant patients as it contains alcohol

Pharmacology

Pharmacodynamics

Mechanism of action

Antagonism of substance P/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. 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
Metabolized by CYP3A4 via oxidation w minor contribution by CYP1A2 and CYP2C19
Terminal half-life is 9 to 13 hours
Inducer of CYP3A4 and CYP2C9

Chemistry and formulation

Aprepitant is administered orally and intravenously. Fosaprepitant, a prodrug of aprepitant, is administered intravenously.

History

References

Top contributors: Cornel Chiu, Olivia Sutton and Chris Rishel

@@ Line 1: / Line 1: @@
 {{Infobox drug reference
-| trade_names =
+| trade_names = Emend
-| drug_class =
+| drug_class = Anti-emetic
 | drug_class_color =
-| uses =
+| uses = Postoperative Nausea and Vomiting
-| contraindications =
+| contraindications = Known hypersensitivity
-| routes =
+| routes = PO or IV
 | dosage =
 | dosage_calculation = aprepitant
+| mechanism = Substance P/Neurokinin 1 receptor antagonist
+| adverse_effects = Anaphylaxis
+| metabolism = CYP3A4 oxidation
+| protein_binding = 95%
 }}
-Provide a brief summary of this drug here.
+Aprepitant is a selective substance P neurokinin 1 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. --> ==
+* Supplement standard anti-emetic regimen in chemotherapy induced nausea and vomiting
+* Supplement standard anti-emetic regimen in post operative nausea and vomiting
 == Contraindications<!-- List contraindications and precautions for use of the drug. --> ==
 === Absolute contraindications<!-- List absolute contraindications for use of the drug. If none, this section may be removed. --> ===
+* Known hypersensitivity
 === 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)
+* Decreases the efficacy of hormonal contraceptives
+* Avoid IV aprepitant in pregnant patients as it contains alcohol
 == Pharmacology ==
@@ Line 25: / Line 38: @@
 ==== Mechanism of action<!-- Describe the mechanism of action for the primary uses of the drug. --> ====
+Antagonism of substance P/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. 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. --> ====
+* Anaphylactic reaction
+* Angioedema
+* Urticaria
+* Toxic epidermal necrolysis
+* Acne vulgaris
+* Photosensitivity
+* Oily skin
+* Skin lesion
+* Headache
+* Dizziness
+* Fatigue
 === Pharmacokinetics<!-- Describe the pharmacokinetics of the drug. --> ===
+* 95% is bound to plasma proteins
+* Crosses the blood brain barrier
+* Metabolized by CYP3A4 via oxidation w minor contribution by CYP1A2 and CYP2C19
+* Terminal half-life is 9 to 13 hours
+* Inducer of CYP3A4 and CYP2C9
 == Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. --> ==
+Aprepitant is administered orally and intravenously. Fosaprepitant, a prodrug of aprepitant, is administered intravenously.
 == History<!-- Describe the historical development of the drug. --> ==