Enalapril: Difference between revisions
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<applet load="" size="480" color="" frame="true" spin="on" Scene =" | <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: Vasotec=== | ||
* Marketed By: Merck & Co.<br /> | * Marketed By: Merck & Co.<br /> | ||
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* Drug Class: [[ACE]] Inhibitor | * Drug Class: [[ACE]] Inhibitor | ||
* Date of FDA Approval (Patent Expiration): 1985 (2000)<br /> | * Date of FDA Approval (Patent Expiration): 1985 (2000)<br /> | ||
* | * 1996 Peak Sales: $2.5 Billion | ||
* Why You Should Care: One of the best selling [[Angiotensin-Converting Enzyme]] Inhibitors of all time. | * 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. | ||
* 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. | 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 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. | 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. | ||
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<scene name='Enalapril/Ace/1'>TextToBeDisplayed</scene> | |||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
{| class="wikitable" border="1" width="50%" style="text-align:center" | {| class="wikitable" border="1" width="50%" style="text-align:center" | ||