Aprepitant - Revision history

Chris.Rishel at 20:19, 8 January 2023

2023-01-08T20:19:38Z

← Older revision		Revision as of 13:19, 8 January 2023
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	* Decreases the efficacy of hormonal contraceptives for up to 28 days<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 for up to 28 days<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>
	*Inhibits CYP3A4 and induces CYP2C9<ref>{{Cite journal\|last=Aapro\|first=M. S.\|last2=Walko\|first2=C. M.\|date=2010~~-12~~\|title=Aprepitant: drug-drug interactions in perspective\|url=https://pubmed.ncbi.nlm.nih.gov/20488873/\|journal=Annals of Oncology: Official Journal of the European Society for Medical Oncology\|volume=21\|issue=12\|pages=2316–2323\|doi=10.1093/annonc/mdq149\|issn=1569-8041\|pmid=20488873}}</ref>		*Inhibits CYP3A4 and induces CYP2C9<ref>{{Cite journal\|last=Aapro\|first=M. S.\|last2=Walko\|first2=C. M.\|date=2010\|title=Aprepitant: drug-drug interactions in perspective\|url=https://pubmed.ncbi.nlm.nih.gov/20488873/\|journal=Annals of Oncology: Official Journal of the European Society for Medical Oncology\|volume=21\|issue=12\|pages=2316–2323\|doi=10.1093/annonc/mdq149\|issn=1569-8041\|pmid=20488873}}</ref>
	**Some other drugs may need close monitoring and/or dose adjustment postoperatively (e.g. warfarin)		**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<ref name=":0" />		* Some formulations of IV aprepitant may contain alcohol which should be avoided in pregnant patients<ref name=":0" />

Chris.Rishel: Added antiemetics category

2023-01-08T20:18:31Z

Added antiemetics category

← Older revision		Revision as of 13:18, 8 January 2023
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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]]

Chris.Rishel: Many minor changes

2023-01-08T20:13:33Z

Many minor changes

← Older revision		Revision as of 13:13, 8 January 2023
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	{{Infobox drug reference		{{Infobox drug reference
	\| trade_names = Emend		\| trade_names = Emend
	\| drug_class = ~~Anti-emetic~~		\| drug_class = Antiemetic
	\| drug_class_color =		\| drug_class_color =
	\| uses = Postoperative Nausea and Vomiting		\| uses = Postoperative Nausea and Vomiting
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	125 mg PO followed by 2 days of 80 mg PO for CINV		125 mg PO followed by 2 days of 80 mg PO for CINV
	\| dosage_calculation = aprepitant		\| dosage_calculation = aprepitant
	\| mechanism = Neurokinin 1 receptor antagonist		\| mechanism = Neurokinin-1 receptor antagonist
	\| adverse_effects = ~~Anaphylaxis~~		\| adverse_effects = Decreased efficacy of hormonal contraceptives
			CYP interactions
	\| metabolism = CYP3A4 oxidation		\| metabolism = CYP3A4 oxidation
	\| protein_binding = 95%		\| protein_binding = 95%
	}}		}}

	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.		'''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<!-- 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. --> ==

	* ~~Supplement standard anti-emetic regimen in chemotherapy induced~~ nausea and vomiting		* Prevention of postoperative nausea and vomiting
	* ~~Supplement standard anti~~-~~emetic regimen in post operative~~ nausea and vomiting		*Prevention of chemotherapy-induced nausea and vomiting

	== Contraindications<!-- List contraindications and precautions for use of the drug. --> ==		== Contraindications<!-- List contraindications and precautions for use of the drug. --> ==
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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)~~<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 for up to 28 days<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~~<ref ~~name~~=":0" />		*Inhibits CYP3A4 and induces CYP2C9<ref>{{Cite journal\|last=Aapro\|first=M. S.\|last2=Walko\|first2=C. M.\|date=2010-12\|title=Aprepitant: drug-drug interactions in perspective\|url=https://pubmed.ncbi.nlm.nih.gov/20488873/\|journal=Annals of Oncology: Official Journal of the European Society for Medical Oncology\|volume=21\|issue=12\|pages=2316–2323\|doi=10.1093/annonc/mdq149\|issn=1569-8041\|pmid=20488873}}</ref>
	* ~~Avoid~~ IV aprepitant in pregnant patients ~~as it contains alcohol~~<ref name=":0" />		**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<ref name=":0" />
			**IV fosaprepitant is not prepared with alcohol

	== 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 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.		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<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. --> ====
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	* Metabolized by CYP3A4 via oxidation w minor contribution by CYP1A2 and CYP2C19 <ref name=":0" />		* Metabolized by CYP3A4 via oxidation w minor contribution by CYP1A2 and CYP2C19 <ref name=":0" />
	* Terminal half-life is 9 to 13 hours<ref name=":0" />		* Terminal half-life is 9 to 13 hours<ref name=":0" />
	* ~~Inducer of~~ CYP3A4 and CYP2C9		* Inhibits CYP3A4 and induces CYP2C9

	== Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. --> ==		== Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. --> ==

Cornel.Chiu: References

2023-01-05T22:39:13Z

References

← Older revision		Revision as of 15:39, 5 January 2023
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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 = ~~Substance P/~~Neurokinin 1 receptor antagonist		\| mechanism = Neurokinin 1 receptor antagonist
	\| adverse_effects = Anaphylaxis		\| adverse_effects = Anaphylaxis
	\| metabolism = CYP3A4 oxidation		\| metabolism = CYP3A4 oxidation
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	}}		}}

	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.		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 ~~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.		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. --> ====
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	* 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

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	== 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]]

Cornel.Chiu: Brief summary, Uses, contraindication, precautions, pharmacodynamics, adverse effects, chemistry and formulation

2023-01-04T21:28:18Z

Brief summary, Uses, contraindication, precautions, pharmacodynamics, adverse effects, chemistry and formulation

← Older revision		Revision as of 14:28, 4 January 2023
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	{{Infobox drug reference		{{Infobox drug reference
	\| trade_names =		\| trade_names = Emend
	\| drug_class =		\| drug_class = Anti-emetic
	\| drug_class_color =		\| drug_class_color =
	\| uses =		\| uses = Postoperative Nausea and Vomiting
	\| contraindications =		\| contraindications = Known hypersensitivity
	\| routes =		\| routes = PO or IV
	\| dosage =		\| dosage =
	\| dosage_calculation = aprepitant		\| 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. --> ==		== 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. --> ==		== 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. --> ===		=== 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. --> ===		=== 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 ==		== 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 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. --> ====		==== 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. --> ===		=== 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. --> ==		== 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. --> ==		== History<!-- Describe the historical development of the drug. --> ==

Chris.Rishel: Added embedded dosage calculation

2022-03-30T08:01:19Z

Added embedded dosage calculation

← Older revision		Revision as of 01:01, 30 March 2022
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	\| routes =		\| routes =
	\| dosage =		\| dosage =
			\| dosage_calculation = aprepitant
	}}		}}

Oliviamsutton: Created page with "{{Infobox drug reference | trade_names = | drug_class = | drug_class_color = | uses = | contraindications = | routes = | dosage = }} Provide a brief summary of this dr..."

2021-11-10T17:40:38Z

Created page with "{{Infobox drug reference | trade_names = | drug_class = | drug_class_color = | uses = | contraindications = | routes = | dosage = }} Provide a brief summary of this dr..."

New page

{{Infobox drug reference
| trade_names =
| drug_class =
| drug_class_color =
| uses =
| contraindications =
| routes =
| dosage =
}}

Provide a brief summary of this drug here.

== Uses ==

== Contraindications ==

=== Absolute contraindications ===

=== Precautions ===

== Pharmacology ==

=== Pharmacodynamics ===

==== Mechanism of action ====

==== Adverse effects ====

=== Pharmacokinetics ===

== Chemistry and formulation ==

== History ==

== References ==

[[Category:Drug reference]]