Captopril: Difference between revisions
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< | <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 /> | ||
* 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 /> | ||
* 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. | ||
* | * See [[Pharmaceutical Drugs]] for more information about other drugs and diseases | ||
===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> | |||
</StructureSection> | |||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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{{:ACE Inhibitor Pharmacokinetics}} | |||
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==References== | |||
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