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The assessment of ACE activity in man following angiotensin I challenges: a comparison of cilazapril, captopril and enalapril.
Author(s) -
Essig J,
Belz GG,
Wellstein A
Publication year - 1989
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1989.tb03485.x
Subject(s) - cilazapril , enalapril , captopril , angiotensin converting enzyme , angiotensin ii , pharmacology , ace inhibitor , blood pressure , chemistry , medicine , endocrinology
1. The aim of the studies was to develop a new methodology to estimate the pharmacodynamic properties and potency of angiotensin converting enzyme (ACE) inhibitors in man. 2. Angiotensin I dose‐response curves were derived by continuous infusion of angiotensin I in increasing dose steps; steady state was reached within 3 min. 3. Interaction between angiotensin I (agonist) and ACE inhibitors (antagonist) was characterized according to Schild‐plot methodology by measuring agonist dose‐response curves using diastolic blood pressure in the absence and the presence of varying doses of the antagonist. 4. Cilazapril shifted the angiotensin I dose‐response curves to the right. A twofold shift (apparent Ki‐dose) was observed with approximately 0.6 mg cilazapril. 5. The effect of angiotensin I on diastolic blood pressure was determined before and up to 36 h after administration of 25 mg captopril, 10 mg enalapril, 4 mg cilazapril and a placebo orally. The pharmacodynamic half‐life of captopril was about 2 h, whereas the effect of enalapril and cilazapril was about 4 h. 6. Angiotensin I dose‐ response curves are useful methods of investigating the pharmacodynamic properties of ACE‐inhibitors in man.