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  • Title: Relationship of serum ACE inhibition to oral dose of enalapril in normotensive volunteers.
    Author: Rouini M, Hamidi M, Ghayoumi A, Ismailpour A.
    Journal: J Clin Pharm Ther; 2002 Apr; 27(2):121-6. PubMed ID: 11975696.
    Abstract:
    OBJECTIVES: To determine the relationship between oral dose of enalapril and parameters describing serum angiotensin converting enzyme (ACE) inhibition. METHODS: Four different oral doses of enalapril maleate (2.5, 5, 10 and 20 mg) were administered to six healthy normotensive volunteers, in a four-period crossover study. Serum ACE inhibition profiles were determined in each case using a synthetic substrate, hippuryl-histidyl-leucine (HHL). Pharmacodynamic parameters of the drug (Emax and AUEC0-->24) were calculated and their relationship to oral doses investigated using linear regression analysis. RESULTS: There was no significant relationship between drug dose and the two pharmacodynamic parameters (Emax and AUEC0-->24). The r2 values were 0.548 (F=3.63, P=0.153) and 0.6360 (F=5.24, P=0.106) for Emax and AUEC0-->24, respectively. CONCLUSION: The extent of serum ACE inhibition, as the main determinant of the blood pressure lowering effect of enalapril, is not dose-dependent within the single dose range of 2.5-20 mg.
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