Captopril - Revision history

Alexander Berchansky at 12:50, 10 January 2024

Alexander Berchansky — Wed, 10 Jan 2024 12:50:45 GMT

←Older revision		Revision as of 12:50, 10 January 2024
Line 1:		Line 1:
-	<~~applet~~ load="" size=~~"430" color~~=~~"" frame="true" spin="on" Scene ="Captopril/Captopril/2" align="~~right" caption="Captopril, also known as Capoten"/>	+	<StructureSection load='' size='340' side='right' caption='Captopril, also known as Capoten' scene='Captopril/Captopril/2'>
	===Better Known as: Capoten===		===Better Known as: Capoten===
	* Marketed By: Bristol-Myers Squibb<br />		* Marketed By: Bristol-Myers Squibb<br />
Line 11:		Line 11:
	===Mechanism of Action===		===Mechanism of Action===
	Extensive research has validated a pathological role for Angiotensin II 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 primary degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure. Captopril binds to the ACE-1 binding site of <scene name='Captopril/Ace/1'>Angiotensin-Converting enzyme</scene>, preventing ACE-1 from binding angiotensin. Captopril,<scene name='Captopril/Captopril_binding/1'> binds ACE-1 precisely</scene>, forming electrostatic interactions with His 353, Glu 384, Lys 511, His 513 and Tyr 520, along with zinc cation. <ref>PMID:15236580</ref>		Extensive research has validated a pathological role for Angiotensin II 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 primary degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure. Captopril binds to the ACE-1 binding site of <scene name='Captopril/Ace/1'>Angiotensin-Converting enzyme</scene>, preventing ACE-1 from binding angiotensin. Captopril,<scene name='Captopril/Captopril_binding/1'> binds ACE-1 precisely</scene>, forming electrostatic interactions with His 353, Glu 384, Lys 511, His 513 and Tyr 520, along with zinc cation. <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 09:16, 10 December 2010

David Canner — Fri, 10 Dec 2010 09:16:32 GMT

←Older revision		Revision as of 09:16, 10 December 2010
Line 1:		Line 1:
-	<applet load="" size="~~[450,~~430]" color="" frame="true" spin="on" Scene ="Captopril/Captopril/2" align="right" caption="Captopril, also known as Capoten"/>	+	<applet load="" size="430" color="" frame="true" spin="on" Scene ="Captopril/Captopril/2" align="right" caption="Captopril, also known as Capoten"/>
	===Better Known as: Capoten===		===Better Known as: Capoten===
	* Marketed By: Bristol-Myers Squibb<br />		* Marketed By: Bristol-Myers Squibb<br />

David Canner at 09:16, 10 December 2010

David Canner — Fri, 10 Dec 2010 09:16:11 GMT

←Older revision		Revision as of 09:16, 10 December 2010
Line 1:		Line 1:
-	<applet load="" size="[~~430,~~450]" color="" frame="true" spin="on" Scene ="Captopril/Captopril/2" align="right" caption="Captopril, also known as Capoten"/>	+	<applet load="" size="[450,430]" color="" frame="true" spin="on" Scene ="Captopril/Captopril/2" align="right" caption="Captopril, also known as Capoten"/>
	===Better Known as: Capoten===		===Better Known as: Capoten===
	* Marketed By: Bristol-Myers Squibb<br />		* Marketed By: Bristol-Myers Squibb<br />

David Canner at 09:15, 10 December 2010

David Canner — Fri, 10 Dec 2010 09:15:54 GMT

←Older revision		Revision as of 09:15, 10 December 2010
Line 1:		Line 1:
-	<applet load="" size="450" color="" frame="true" spin="on" Scene ="Captopril/Captopril/2" align="right" caption="Captopril, also known as Capoten"/>	+	<applet load="" size="[430,450]" color="" frame="true" spin="on" Scene ="Captopril/Captopril/2" align="right" caption="Captopril, also known as Capoten"/>
	===Better Known as: Capoten===		===Better Known as: Capoten===
	* Marketed By: Bristol-Myers Squibb<br />		* Marketed By: Bristol-Myers Squibb<br />
Line 22:		Line 22:
	</tr>		</tr>
	</table>		</table>
-

	==References==		==References==

David Canner at 09:15, 10 December 2010

David Canner — Fri, 10 Dec 2010 09:15:25 GMT

←Older revision		Revision as of 09:15, 10 December 2010
Line 1:		Line 1:
-	<applet load="" size="~~480~~" color="" frame="true" spin="on" Scene ="Captopril/Captopril/2" align="right" caption="Captopril, also known as Capoten"/>	+	<applet load="" size="450" color="" frame="true" spin="on" Scene ="Captopril/Captopril/2" align="right" caption="Captopril, also known as Capoten"/>
	===Better Known as: Capoten===		===Better Known as: Capoten===
	* Marketed By: Bristol-Myers Squibb<br />		* Marketed By: Bristol-Myers Squibb<br />

David Canner at 09:14, 10 December 2010

David Canner — Fri, 10 Dec 2010 09:14:54 GMT

←Older revision		Revision as of 09:14, 10 December 2010
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 11:20, 9 December 2010

David Canner — Thu, 09 Dec 2010 11:20:36 GMT

←Older revision		Revision as of 11:20, 9 December 2010
Line 7:		Line 7:
	* 2009 Sales: N/A		* 2009 Sales: N/A
	* Importance: It was the first [[Angiotensin-Converting Enzyme]] Inhibitor. Was one of the earliest successes of Structure-Based drug design paving the way for future discoveries.		* Importance: It was the first [[Angiotensin-Converting Enzyme]] Inhibitor. Was one of the earliest successes of Structure-Based drug design paving the way for future discoveries.
-	* ~~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===
Line 15:		Line 15:
	{\| 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 12:28:42 GMT

←Older revision		Revision as of 12:28, 1 December 2010
Line 6:		Line 6:
	* Date of FDA Approval (Patent Expiration): 1981 (1996)<br />		* Date of FDA Approval (Patent Expiration): 1981 (1996)<br />
	* 2009 Sales: N/A		* 2009 Sales: N/A
-	* ~~Why You Should Care~~: It was the first [[Angiotensin-Converting Enzyme]] Inhibitor. Was one of the earliest successes of Structure-Based drug design paving the way for future discoveries.	+	* Importance: It was the first [[Angiotensin-Converting Enzyme]] Inhibitor. Was one of the earliest successes of Structure-Based drug design paving the way for future discoveries.
	* 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===
	Extensive research has validated a pathological role for Angiotensin II 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 primary degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure. Captopril binds to the ACE-1 binding site of <scene name='Captopril/Ace/1'>Angiotensin-Converting enzyme</scene>, preventing ACE-1 from binding angiotensin. Captopril,<scene name='Captopril/Captopril_binding/1'> binds ACE-1 precisely</scene>, forming electrostatic interactions with His 353, Glu 384, Lys 511, His 513 and Tyr 520, along with zinc cation. <ref>PMID:15236580</ref>		Extensive research has validated a pathological role for Angiotensin II 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 primary degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure. Captopril binds to the ACE-1 binding site of <scene name='Captopril/Ace/1'>Angiotensin-Converting enzyme</scene>, preventing ACE-1 from binding angiotensin. Captopril,<scene name='Captopril/Captopril_binding/1'> binds ACE-1 precisely</scene>, forming electrostatic interactions with His 353, Glu 384, Lys 511, His 513 and Tyr 520, along with zinc cation. <ref>PMID:15236580</ref>

David Canner at 13:30, 29 November 2010

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

←Older revision		Revision as of 13:30, 29 November 2010
Line 14:		Line 14:
	{\| 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 11:40, 29 November 2010

David Canner — Mon, 29 Nov 2010 11:40:39 GMT

←Older revision		Revision as of 11:40, 29 November 2010
Line 2:		Line 2:
	===Better Known as: Capoten===		===Better Known as: Capoten===
	* Marketed By: Bristol-Myers Squibb<br />		* Marketed By: Bristol-Myers Squibb<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): 1981 (1996)<br />		* Date of FDA Approval (Patent Expiration): 1981 (1996)<br />