Ramipril: Difference between revisions

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<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="Ramipril/Rama/1" align="right" caption="Ramiprilat, the metabolite of Ramipril, also known as Altace"/>
<StructureSection load='' size='340' side='right' caption='Ramiprilat, the metabolite of Ramipril, also known as Altace' scene='Ramipril/Rama/1'>
===Better Known as: Altace or Ramipro===
===Better Known as: Altace or Ramipro===
* Marketed By: King Pharmaceuticals (Now part of Pfizer Inc.)<br />
* Marketed By: King Pharmaceuticals (Now part of Pfizer Inc.)<br />
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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.  
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.  
Ramipril is quickly metabolized into Ramiprilat, the most active metabolite of Ramipril. Ramiprilat binds to the active site of <scene name='Ramipril/Angio/1'>Angiotensin-Converting Enzyme</scene>, actively inhibiting ACE-1 from binding and converting Angiotensin I into Angiotensin II. ACE-1 <scene name='Ramipril/Ramiprilat_binding/1'> binds Ramiprilat</scene> using residues Glu 395, His 497, Lys 495, Gln 265, Tyr 504, Tyr 496 and Tyr 507, tightly affixing the inhibitor to the active site of ACE-1.  
Ramipril is quickly metabolized into Ramiprilat, the most active metabolite of Ramipril. Ramiprilat binds to the active site of <scene name='Ramipril/Angio/1'>Angiotensin-Converting Enzyme</scene>, actively inhibiting ACE-1 from binding and converting Angiotensin I into Angiotensin II. ACE-1 <scene name='Ramipril/Ramiprilat_binding/1'> binds Ramiprilat</scene> using residues Glu 395, His 497, Lys 495, Gln 265, Tyr 504, Tyr 496 and Tyr 507, tightly affixing the inhibitor to the active site of ACE-1.  
 
</StructureSection>
===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==

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

David Canner, Alexander Berchansky