Benazepril - Revision history

Alexander Berchansky at 12:52, 10 January 2024

Alexander Berchansky — Wed, 10 Jan 2024 12:52:46 GMT

←Older revision		Revision as of 12:52, 10 January 2024
Line 1:		Line 1:
-	<~~applet~~ load="" size=~~"430" color~~=~~"" frame="true" spin="on" Scene ="Benazepril/Benazepril/1" align="~~right" caption="Benazepril, also known as Lotensin"/>	+	<StructureSection load='' size='340' side='right' caption='Benazepril, also known as Lotensin' scene='Benazepril/Benazepril/1'>
	===Better Known as: Lotensin (Lotrel when combined with Amlodipine)===		===Better Known as: Lotensin (Lotrel when combined with Amlodipine)===
	* Marketed By: Novartis International AG<br />		* Marketed By: Novartis International AG<br />
Line 11:		Line 11:
	===Mechanism of Action===		===Mechanism of Action===
	Angiotensin II has been implicated in cardiac, renal and vascular diseases. <ref>PMID:17083068</ref> Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since [[ACE\|ACE-1]] is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure.<ref>PMID:15236580</ref>		Angiotensin II has been implicated in cardiac, renal and vascular diseases. <ref>PMID:17083068</ref> Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since [[ACE\|ACE-1]] is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure.<ref>PMID:15236580</ref>
-		+	</StructureSection>
	===Pharmacokinetics===		===Pharmacokinetics===
	<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%">		<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%">

David Canner at 09:18, 10 December 2010

David Canner — Fri, 10 Dec 2010 09:18:01 GMT

←Older revision		Revision as of 09:18, 10 December 2010
Line 1:		Line 1:
-	<applet load="" size="~~480~~" color="" frame="true" spin="on" Scene ="Benazepril/Benazepril/1" align="right" caption="Benazepril, also known as Lotensin"/>	+	<applet load="" size="430" color="" frame="true" spin="on" Scene ="Benazepril/Benazepril/1" align="right" caption="Benazepril, also known as Lotensin"/>
	===Better Known as: Lotensin (Lotrel when combined with Amlodipine)===		===Better Known as: Lotensin (Lotrel when combined with Amlodipine)===
	* Marketed By: Novartis International AG<br />		* Marketed By: Novartis International AG<br />
Line 13:		Line 13:

	===Pharmacokinetics===		===Pharmacokinetics===
-	~~{\| class~~="~~wikitable~~" ~~border~~="1" width="50%" style="~~text~~-align:~~center"~~	+	<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%">
-	\|-	+	<tr>
-	~~! colspan="8" align="center"\| ACE~~-~~Inhibitor [[Pharmacokinetics]] Comparison at Equivalent Dosages <ref>PMID~~: ~~7867683</ref~~><~~ref>DOI~~: ~~10.1111/j.1365-2710.2005.00646.x</ref><ref>PMID~~: ~~16075412</ref~~>~~<ref>PMID~~:~~7527101</ref>~~	+	<td style="width:100%; vertical-align:top;border-width:0px; border-style:inset">
-	\|-	+	<div style="height:100%; width: 100%">
-	~~! Parameter~~	+	{{:ACE Inhibitor Pharmacokinetics}}
-	~~! [[Captopril]]~~	+	</div>
-	~~! [[Lisinopril]]~~	+	</td>
-	~~! [[Ramipril]]~~	+	</tr>
-	~~! [[Enalapril]]~~	+	</table>
-	~~! [[Benazepril]]~~	+
-	~~! [[Perindopril]]~~	+
-	~~! [[Trandolapril]]~~	+
-	\|-	+
-	~~! [[Pharmacokinetics#Tmax\|T<sub>max~~</~~sub~~>~~]] (hr)~~	+
-	~~! .98~~	+
-	~~! 6.5~~	+
-	~~! .67~~	+
-	~~! 1.06~~	+
-	~~! .5~~	+
-	~~! .75~~	+
-	~~! .72~~	+
-	\|-	+
-	~~! [[Pharmacokinetics#Cmax\|C<sub>max~~</~~sub~~>~~]] (ng/ml)~~	+
-	~~! 1210~~	+
-	~~! 79~~	+
-	~~! 16.4~~	+
-	~~! 314~~	+
-	~~! 149~~	+
-	~~! 105~~	+
-	~~! 1.68~~	+
-	\|-	+
-	~~! [[Pharmacokinetics#Bioavailability_.28F.29\|Bioavailability]] (%)~~	+
-	~~! 72~~	+
-	~~! 25~~	+
-	~~! 28~~	+
-	~~! 60~~	+
-	~~! 97~~	+
-	~~! 24~~	+
-	~~! 10~~	+
-	\|-	+
-	~~! [[Pharmacokinetics#Protein_Binding\|Protein Binding]] (%)~~	+
-	~~! 97~~	+
-	~~! 0~~	+
-	~~! 73~~	+
-	~~! 20~~	+
-	~~! 97~~	+
-	~~! 20~~	+
-	~~! 80~~	+
-	\|-	+
-	~~! [[Pharmacokinetics#Half_Life_.28T1.2F2.29\|T~~<~~sub>1~~/~~2</sub~~>~~]] (hr)~~	+
-	~~! .56~~	+
-	~~! 10.1~~	+
-	~~! 1.93~~	+
-	~~! 1.6~~	+
-	~~! 10~~	+
-	~~! .9~~	+
-	~~! .68~~	+
-	\|-	+
-	~~! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29\|AUC]] (ng/ml/hr)~~	+
-	~~! 1673~~	+
-	~~! 1016~~	+
-	~~! 21.9~~	+
-	~~! 450~~	+
-	~~! 140~~	+
-	~~! 182~~	+
-	~~! 1.86~~	+
-	\|-	+
-	~~! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29\|IC<sub>50~~</~~sub~~>~~]] (nM)~~	+
-	~~! 1.1~~	+
-	~~! 5.5~~	+
-	~~! 5.0~~	+
-	~~! 5.4~~	+
-	~~! 1.7~~	+
-	~~! 2.4~~	+
-	~~! 2.5~~	+
-	\|-	+
-	~~! Dosage (mg)~~	+
-	~~! 10~~	+
-	~~! 20~~	+
-	~~! 5~~	+
-	~~! 20~~	+
-	~~! 10~~	+
-	~~! 4~~	+
-	~~! 2~~	+
-	\|-	+
-	~~! Metabolism~~	+
-	~~! Hepatic (CYP2D6)~~	+
-	~~! None~~	+
-	~~! Hepatic~~	+
-	~~! Hepatic (CYP3A4)~~	+
-	~~! Hepatic~~	+
-	~~! Hepatic~~	+
-	~~! Hepatic (CYP2D6 & CYP2C9)~~	+
-	\|}	+

	==References==		==References==

David Canner at 11:21, 9 December 2010

David Canner — Thu, 09 Dec 2010 11:21:17 GMT

←Older revision		Revision as of 11:21, 9 December 2010
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	* 2002 Sales (Lotrel 2005 Sales): $300 Million ($1.2 Billion)		* 2002 Sales (Lotrel 2005 Sales): $300 Million ($1.2 Billion)
	* Importance: One of the earliest and best selling [[Angiotensin-Converting Enzyme]] Inhibitors of all time.		* Importance: One of the earliest and best selling [[Angiotensin-Converting Enzyme]] Inhibitors of all time.
-	* ~~The following is a list of Pharmacokinetic Parameters.~~ See: [[Pharmaceutical Drugs]] for more information	+	* See [[Pharmaceutical Drugs]] for more information about other drugs and diseases.

	===Mechanism of Action===		===Mechanism of Action===
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	{\| class="wikitable" border="1" width="50%" style="text-align:center"		{\| class="wikitable" border="1" width="50%" style="text-align:center"
	\|-		\|-
-	! colspan="8" align="center"\| ACE-Inhibitor [[~~Pharmaceutical_Drugs#Pharmacokinetics_Translated\|~~Pharmacokinetics]] Comparison at Equivalent Dosages <ref>PMID: 7867683</ref><ref>DOI: 10.1111/j.1365-2710.2005.00646.x</ref><ref>PMID: 16075412</ref><ref>PMID:7527101</ref>	+	! colspan="8" align="center"\| ACE-Inhibitor [[Pharmacokinetics]] Comparison at Equivalent Dosages <ref>PMID: 7867683</ref><ref>DOI: 10.1111/j.1365-2710.2005.00646.x</ref><ref>PMID: 16075412</ref><ref>PMID:7527101</ref>
	\|-		\|-
	! Parameter		! Parameter
Line 26:		Line 26:
	! [[Trandolapril]]		! [[Trandolapril]]
	\|-		\|-
-	! [[~~Pharmaceutical_Drugs~~#Tmax\|T<sub>max</sub>]] (hr)	+	! [[Pharmacokinetics#Tmax\|T<sub>max</sub>]] (hr)
	! .98		! .98
	! 6.5		! 6.5
Line 35:		Line 35:
	! .72		! .72
	\|-		\|-
-	! [[~~Pharmaceutical_Drugs~~#Cmax\|C<sub>max</sub>]] (ng/ml)	+	! [[Pharmacokinetics#Cmax\|C<sub>max</sub>]] (ng/ml)
	! 1210		! 1210
	! 79		! 79
Line 44:		Line 44:
	! 1.68		! 1.68
	\|-		\|-
-	! [[~~Pharmaceutical_Drugs~~#Bioavailability_.28F.29\|Bioavailability]] (%)	+	! [[Pharmacokinetics#Bioavailability_.28F.29\|Bioavailability]] (%)
	! 72		! 72
	! 25		! 25
Line 53:		Line 53:
	! 10		! 10
	\|-		\|-
-	! [[~~Pharmaceutical_Drugs~~#Protein_Binding\|Protein Binding]] (%)	+	! [[Pharmacokinetics#Protein_Binding\|Protein Binding]] (%)
	! 97		! 97
	! 0		! 0
Line 62:		Line 62:
	! 80		! 80
	\|-		\|-
-	! [[~~Pharmaceutical_Drugs~~#Half_Life_.28T1.2F2.29\|T<sub>1/2</sub>]] (hr)	+	! [[Pharmacokinetics#Half_Life_.28T1.2F2.29\|T<sub>1/2</sub>]] (hr)
	! .56		! .56
	! 10.1		! 10.1
Line 71:		Line 71:
	! .68		! .68
	\|-		\|-
-	! [[~~Pharmaceutical_Drugs~~#Area_Under_the_Curve_.28AUC.29\|AUC]] (ng/ml/hr)	+	! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29\|AUC]] (ng/ml/hr)
	! 1673		! 1673
	! 1016		! 1016
Line 80:		Line 80:
	! 1.86		! 1.86
	\|-		\|-
-	! [[~~Pharmaceutical_Drugs~~#Inhibitory_Concentration_.28IC50.29\|IC<sub>50</sub>]] (nM)	+	! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29\|IC<sub>50</sub>]] (nM)
	! 1.1		! 1.1
	! 5.5		! 5.5

David Canner at 12:28, 1 December 2010

David Canner — Wed, 01 Dec 2010 12:28:53 GMT

←Older revision		Revision as of 12:28, 1 December 2010
Line 6:		Line 6:
	* Date of FDA Approval (Patent Expiration): 1991 (2003)<br />		* Date of FDA Approval (Patent Expiration): 1991 (2003)<br />
	* 2002 Sales (Lotrel 2005 Sales): $300 Million ($1.2 Billion)		* 2002 Sales (Lotrel 2005 Sales): $300 Million ($1.2 Billion)
-	* ~~Why You Should Care~~: One of the earliest and best selling [[Angiotensin-Converting Enzyme]] Inhibitors of all time.	+	* Importance: One of the earliest and best selling [[Angiotensin-Converting Enzyme]] Inhibitors of all time.
	* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information		* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information
		+
	===Mechanism of Action===		===Mechanism of Action===
	Angiotensin II has been implicated in cardiac, renal and vascular diseases. <ref>PMID:17083068</ref> Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since [[ACE\|ACE-1]] is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure.<ref>PMID:15236580</ref>		Angiotensin II has been implicated in cardiac, renal and vascular diseases. <ref>PMID:17083068</ref> Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since [[ACE\|ACE-1]] is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure.<ref>PMID:15236580</ref>

David Canner at 13:30, 29 November 2010

David Canner — Mon, 29 Nov 2010 13:30:20 GMT

←Older revision		Revision as of 13:30, 29 November 2010
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	{\| class="wikitable" border="1" width="50%" style="text-align:center"		{\| class="wikitable" border="1" width="50%" style="text-align:center"
	\|-		\|-
-	! colspan="8" align="center"\| ACE-Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated\|Pharmacokinetics]] Comparison at Equivalent Dosages <ref>PMID: 7867683</ref><ref>DOI: 10.1111/j.1365-2710.2005.00646.x~~</ref><ref>PMID: 15985045~~</ref><ref>PMID: 16075412</ref><ref>PMID:7527101</ref>	+	! colspan="8" align="center"\| ACE-Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated\|Pharmacokinetics]] Comparison at Equivalent Dosages <ref>PMID: 7867683</ref><ref>DOI: 10.1111/j.1365-2710.2005.00646.x</ref><ref>PMID: 16075412</ref><ref>PMID:7527101</ref>
	\|-		\|-
	! Parameter		! Parameter

David Canner at 12:15, 29 November 2010

David Canner — Mon, 29 Nov 2010 12:15:10 GMT

←Older revision		Revision as of 12:15, 29 November 2010
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	<applet load="" size="480" color="" frame="true" spin="on" Scene ="Benazepril/Benazepril/1" align="right" caption="Benazepril, also known as Lotensin"/>		<applet load="" size="480" color="" frame="true" spin="on" Scene ="Benazepril/Benazepril/1" align="right" caption="Benazepril, also known as Lotensin"/>
-	===Better Known as: Lotensin===	+	===Better Known as: Lotensin (Lotrel when combined with Amlodipine)===
	* Marketed By: Novartis International AG<br />		* Marketed By: Novartis International AG<br />
	* Major Indication: [[Hypertension & Congestive Heart Failure]]<br />		* Major Indication: [[Hypertension & Congestive Heart Failure]]<br />
	* Drug Class: [[ACE]] Inhibitor		* Drug Class: [[ACE]] Inhibitor
	* Date of FDA Approval (Patent Expiration): 1991 (2003)<br />		* Date of FDA Approval (Patent Expiration): 1991 (2003)<br />
-	* 2002 Sales: $300 Million	+	* 2002 Sales (Lotrel 2005 Sales): $300 Million ($1.2 Billion)
	* Why You Should Care: One of the earliest and best selling [[Angiotensin-Converting Enzyme]] Inhibitors of all time.		* Why You Should Care: One of the earliest and best selling [[Angiotensin-Converting Enzyme]] Inhibitors of all time.
	* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information		* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information

David Canner at 11:40, 29 November 2010

David Canner — Mon, 29 Nov 2010 11:40:57 GMT

←Older revision		Revision as of 11:40, 29 November 2010
Line 2:		Line 2:
	===Better Known as: Lotensin===		===Better Known as: Lotensin===
	* Marketed By: Novartis International AG<br />		* Marketed By: Novartis International AG<br />
-	* Major Indication: Hypertension & Congestive Heart Failure<br />	+	* Major Indication: [[Hypertension & Congestive Heart Failure]]<br />
	* Drug Class: [[ACE]] Inhibitor		* Drug Class: [[ACE]] Inhibitor
	* Date of FDA Approval (Patent Expiration): 1991 (2003)<br />		* Date of FDA Approval (Patent Expiration): 1991 (2003)<br />

David Canner at 11:21, 29 November 2010

David Canner — Mon, 29 Nov 2010 11:21:43 GMT

←Older revision		Revision as of 11:21, 29 November 2010
Line 9:		Line 9:
	* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information		* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information
	===Mechanism of Action===		===Mechanism of Action===
-	Angiotensin II has been implicated in cardiac, renal and vascular diseases. <ref>PMID:17083068</ref> Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since ACE-1 is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure.<ref>PMID:15236580</ref>	+	Angiotensin II has been implicated in cardiac, renal and vascular diseases. <ref>PMID:17083068</ref> Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since [[ACE\|ACE-1]] is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure.<ref>PMID:15236580</ref>

	===Pharmacokinetics===		===Pharmacokinetics===

David Canner at 11:20, 29 November 2010

David Canner — Mon, 29 Nov 2010 11:20:51 GMT

←Older revision		Revision as of 11:20, 29 November 2010
Line 1:		Line 1:
-	<applet load="" size="480" color="" frame="true" spin="on" Scene ="~~Enalapril~~/~~Enal~~/1" align="right" caption="~~Enalaprilat, the metabolite of Enalapril~~, also known as ~~Vasotec~~"/>	+	<applet load="" size="480" color="" frame="true" spin="on" Scene ="Benazepril/Benazepril/1" align="right" caption="Benazepril, also known as Lotensin"/>
	===Better Known as: Lotensin===		===Better Known as: Lotensin===
	* Marketed By: Novartis International AG<br />		* Marketed By: Novartis International AG<br />
Line 9:		Line 9:
	* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information		* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information
	===Mechanism of Action===		===Mechanism of Action===
-	Angiotensin II has been implicated in cardiac, renal and vascular diseases. <ref>PMID:17083068</ref> Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since ACE-1 is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure. Enalapril is quickly metabolized into Enalaprilat, the more active metabolite of Enalapril predominantly by the Hepatic enzyme CYP3A4. Enalaprilat binds to the active site of <scene name='Enalapril/Ace/1'>Angiotensin-Converting Enzyme</scene>, preventing ACE-1 from binding and converting Angiotensin I into Angiotensin II. <scene name='Enalapril/Enalalprilat/2'>Enalaprilat is bound </scene>to ACE-1 via electrostatic interactions with His 353, Ala 354 (Backbone oxygen), Glue 384, Lys 511, His 513, Tyr 520 and Tyr 523 along with the zinc cation. <ref>PMID:15236580</ref>	+	Angiotensin II has been implicated in cardiac, renal and vascular diseases. <ref>PMID:17083068</ref> Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since ACE-1 is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure.<ref>PMID:15236580</ref>

	===Pharmacokinetics===		===Pharmacokinetics===

David Canner at 11:18, 29 November 2010

David Canner — Mon, 29 Nov 2010 11:18:05 GMT

←Older revision		Revision as of 11:18, 29 November 2010
Line 1:		Line 1:
	<applet load="" size="480" color="" frame="true" spin="on" Scene ="Enalapril/Enal/1" align="right" caption="Enalaprilat, the metabolite of Enalapril, also known as Vasotec"/>		<applet load="" size="480" color="" frame="true" spin="on" Scene ="Enalapril/Enal/1" align="right" caption="Enalaprilat, the metabolite of Enalapril, also known as Vasotec"/>
-	===Better Known as: ~~Vasotec~~===	+	===Better Known as: Lotensin===
-	* Marketed By: ~~Merck & Co.~~<br />	+	* Marketed By: Novartis International AG<br />
	* Major Indication: Hypertension & Congestive Heart Failure<br />		* Major Indication: Hypertension & Congestive Heart Failure<br />
	* Drug Class: [[ACE]] Inhibitor		* Drug Class: [[ACE]] Inhibitor
-	* Date of FDA Approval (Patent Expiration): ~~1985~~ (~~2000~~)<br />	+	* Date of FDA Approval (Patent Expiration): 1991 (2003)<br />
-	* ~~1996 Peak~~ Sales: $~~2.5 Billion~~	+	* 2002 Sales: $300 Million
-	* Why You Should Care: One of the best selling [[Angiotensin-Converting Enzyme]] Inhibitors of all time~~. Was developed by Merck as a replacement for [[Captopril]] with a better side effect profile~~.	+	* Why You Should Care: One of the earliest and best selling [[Angiotensin-Converting Enzyme]] Inhibitors of all time.
	* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information		* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information
	===Mechanism of Action===		===Mechanism of Action===