Lisinopril: Difference between revisions
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* 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. | * 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. | ||
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{| class="wikitable" border="1" width="50%" style="text-align:center" | {| class="wikitable" border="1" width="50%" style="text-align:center" | ||
|- | |- | ||
! colspan="8" align="center"| ACE-Inhibitor [[ | ! colspan="8" align="center"| ACE-Inhibitor [[Pharmacokinetics]] Comparison at Equivalent Dosages <ref>PMID: 7867683</ref><ref>DOI: 10.1111/j.1365-2710.2005.00646.x</ref><ref>PMID: 16075412</ref><ref>PMID:7527101</ref> | ||
|- | |- | ||
! Parameter | ! Parameter | ||
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! [[Trandolapril]] | ! [[Trandolapril]] | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr) | ||
! .98 | ! .98 | ||
! 6.5 | ! 6.5 | ||
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! .72 | ! .72 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml) | ||
! 1210 | ! 1210 | ||
! 79 | ! 79 | ||
| Line 44: | Line 45: | ||
! 1.68 | ! 1.68 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%) | ||
! 72 | ! 72 | ||
! 25 | ! 25 | ||
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! 10 | ! 10 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%) | ||
! 97 | ! 97 | ||
! 0 | ! 0 | ||
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! 80 | ! 80 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ||
! .56 | ! .56 | ||
! 10.1 | ! 10.1 | ||
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! .68 | ! .68 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ||
! 1673 | ! 1673 | ||
! 1016 | ! 1016 | ||
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! 1.86 | ! 1.86 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM) | ||
! 1.1 | ! 1.1 | ||
! 5.5 | ! 5.5 | ||