Lisinopril: Difference between revisions
David Canner (talk | contribs) New page: <applet load="" size="480" color="" frame="true" spin="on" Scene ="Captopril/Captopril/2" align="right" caption="Captopril, also known as Capoten"/> ===Better Known as: Prinivil=== * Ma... |
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< | <StructureSection load='' size='340' side='right' caption='Lisinopril, also known as Prinivil' scene='Lisinopril/Lisinopril/1'> | ||
===Better Known as: Prinivil=== | ===Better Known as: Prinivil=== | ||
* Marketed By: Merck & Co.<br /> | * Marketed By: Merck & Co.<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): 1988 (2001)<br /> | * Date of FDA Approval (Patent Expiration): 1988 (2001)<br /> | ||
* 1998 Sales: $690 Million | * 1998 Sales: $690 Million | ||
* | * Importance: It is the only [[Angiotensin-Converting Enzyme]] Inhibitor that is not a prodrug and is excreted unchanged in the urine. Was one of the best selling ACE inhibitors in history. | ||
* | * See [[Pharmaceutical Drugs]] for more information about other drugs and diseases. | ||
===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. | ||
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. | |||
</StructureSection> | |||
===Pharmacokinetics=== | |||
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{{:ACE Inhibitor Pharmacokinetics}} | |||
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==References== | ==References== | ||