Benazepril

spinqualitylabelsall models Benazepril, also known as Lotensin Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Better Known as: Lotensin (Lotrel when combined with Amlodipine) Marketed By: Novartis International AG Major Indication: Hypertension & Congestive Heart Failure Drug Class: ACE Inhibitor Date of FDA Approval (Patent Expiration): 1991 (2003) 2002 Sales (Lotrel 2005 Sales): $300 Million ($1.2 Billion) Importance: One of the earliest and best selling Angiotensin-Converting Enzyme Inhibitors of all time. 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. 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.

Pharmacokinetics

ACE-Inhibitor Hypertension & Congestive Heart Failure Comparison at Equivalent Dosages Parameter ACE Angiotensin-Converting Enzyme Pharmaceutical Drugs ACE-1 Benazepril Perindopril Trandolapril Tmax (hr) .98 6.5 .67 1.06 .5 .75 .72 Cmax (ng/ml) 1210 79 16.4 314 149 105 1.68 Bioavailability (%) 72 25 28 60 97 24 10 Protein Binding (%) 97 0 73 20 97 20 80 T1/2 (hr) .56 10.1 1.93 1.6 10 .9 .68 AUC (ng/ml/hr) 1673 1016 21.9 450 140 182 1.86 IC50 (nM) 1.1 5.5 5.0 5.4 1.7 2.4 2.5 Dosage (mg) 10 20 5 20 10 4 2 Metabolism Hepatic (CYP2D6) None Hepatic Hepatic (CYP3A4) Hepatic Hepatic Hepatic (CYP2D6 & CYP2C9) For Pharmacokinetic Data References, See: References

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