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Relationship of serum ACE inhibition to oral dose of enalapril in normotensive volunteers
Author(s) -
Rouini M.,
Hamidi M.,
Ghayoumi A.,
Ismailpour A.
Publication year - 2002
Publication title -
journal of clinical pharmacy and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.622
H-Index - 73
eISSN - 1365-2710
pISSN - 0269-4727
DOI - 10.1046/j.1365-2710.2002.00390.x
Subject(s) - enalapril , enalapril maleate , pharmacodynamics , angiotensin converting enzyme , pharmacology , enzyme inhibitor , crossover study , blood pressure , medicine , chemistry , ace inhibitor , pharmacokinetics , endocrinology , enzyme , biochemistry , alternative medicine , placebo , pathology
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 ( E max and AUEC 0→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 ( E max and AUEC 0→24 ). The r 2 values were 0·548 ( F =3·63, P =0·153) and 0·6360 ( F =5·24, P =0·106) for E max and AUEC 0→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.