Lisinopril: Difference between revisions
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<applet load="" size=" | <applet load="" size="430" color="" frame="true" spin="on" Scene ="Lisinopril/Lisinopril/1" align="right" caption="Lisinopril, also known as Prinivil"/> | ||
===Better Known as: Prinivil=== | ===Better Known as: Prinivil=== | ||
* Marketed By: Merck & Co.<br /> | * Marketed By: Merck & Co.<br /> | ||
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===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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{{:ACE Inhibitor Pharmacokinetics}} | |||
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==References== | ==References== | ||
Revision as of 12:17, 10 December 2010
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Better Known as: Prinivil
- Marketed By: Merck & Co.
- Major Indication: Hypertension & Congestive Heart Failure
- Drug Class: ACE Inhibitor
- Date of FDA Approval (Patent Expiration): 1988 (2001)
- 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
Angiotensin II has been implicated in cardiac, renal and vascular diseases. [1] 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 , utilizing residues like as well as van der Waals interactions between the phenylpropyl group and Val 518. [2] Binding by Lisinopril actively inhibits ACE-1 binding and conversion of angiotensin 1 into angiotensin II.
Pharmacokinetics
For Pharmacokinetic Data References, See: References |
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References
- ↑ Ferrario CM. Role of angiotensin II in cardiovascular disease therapeutic implications of more than a century of research. J Renin Angiotensin Aldosterone Syst. 2006 Mar;7(1):3-14. PMID:17083068
- ↑ Natesh R, Schwager SL, Evans HR, Sturrock ED, Acharya KR. Structural details on the binding of antihypertensive drugs captopril and enalaprilat to human testicular angiotensin I-converting enzyme. Biochemistry. 2004 Jul 13;43(27):8718-24. PMID:15236580 doi:10.1021/bi049480n