Ramipril: Difference between revisions

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===Better Known as: Altace===

* Marketed By: King Pharmaceuticals (Now part of Pfizer Inc.)<br />

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===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.

~~Lisinopril~~ binds to the active site of <scene name='~~Lisinopril~~/~~Ace~~/1'>Angiotensin-Converting Enzyme</scene>, ~~utilizing residues like~~ <scene name='~~Lisinopril~~/~~Lisinopril_bound~~/1'>His ~~353, Ala 354 (backbone oxygen), Glue 384~~, Lys ~~511~~, ~~His 513~~, Tyr ~~520~~, Tyr ~~523~~ and ~~Glu 162</scene> as well as van der Waals interactions between~~ the ~~phenylpropyl group and Val 518. <ref>PMID:15236580</ref> Binding by Lisinopril actively inhibits~~ ACE-1 ~~binding and conversion of angiotensin 1 into angiotensin II~~.

Ramipril is quickly metabolized into Ramiprilat, the most active inhibitor 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.

===Pharmacokinetics===

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-<applet   load="" size="480" color="" frame="true"  spin="on" Scene ="Ramipril/Ramiprilat/1" align="right" caption="Ramiprilat, the metabolite of Ramipril, also known as Altace"/>
+<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"/>
 ===Better Known as: Altace===
 * Marketed By: King Pharmaceuticals (Now part of Pfizer Inc.)<br />
@@ Line 10: / Line 10: @@
 ===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.
-Lisinopril binds to the active site of <scene name='Lisinopril/Ace/1'>Angiotensin-Converting Enzyme</scene>, utilizing residues like <scene name='Lisinopril/Lisinopril_bound/1'>His 353, Ala 354 (backbone oxygen), Glue 384, Lys 511, His 513, Tyr 520, Tyr 523 and Glu 162</scene> as well as van der Waals interactions between the phenylpropyl group and Val 518. <ref>PMID:15236580</ref> Binding by Lisinopril actively inhibits ACE-1 binding and conversion of angiotensin 1 into angiotensin II.
+Ramipril is quickly metabolized into Ramiprilat, the most active inhibitor 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.
 ===Pharmacokinetics===