The effects of age on the pharmacokinetics and pharmacodynamics of single oral doses of benazepril and enalapril

1. Eighteen healthy, normotensive subjects (nine young and nine elderly) participated in a double‐blind, 3‐way, crossover study to compare aspects of the pharmacokinetics and pharmacodynamics of single oral doses of 10 mg benazepril, 10 mg enalapril and placebo. 2. The hypotensive effect was similar...

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Veröffentlicht in:British journal of clinical pharmacology 1993-09, Vol.36 (3), p.205-209
Hauptverfasser: Macdonald, NJ, Sioufi, A, Howie, CA, Wade, JR, Elliott, HL
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container_issue 3
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container_title British journal of clinical pharmacology
container_volume 36
creator Macdonald, NJ
Sioufi, A
Howie, CA
Wade, JR
Elliott, HL
description 1. Eighteen healthy, normotensive subjects (nine young and nine elderly) participated in a double‐blind, 3‐way, crossover study to compare aspects of the pharmacokinetics and pharmacodynamics of single oral doses of 10 mg benazepril, 10 mg enalapril and placebo. 2. The hypotensive effect was similar after both drugs but the absolute reductions were greater in the elderly who had higher initial levels of blood pressure. 3. The AUCs for both benazeprilat and enalaprilat were higher in the elderly but by a significantly greater amount for enalaprilat (+ 113% vs 40%; P < 0.01). 4. The AUCs for both drugs tended to be highest in subjects with the lowest creatinine clearance. 5. The changes in kinetics and dynamics observed in the elderly after benazepril are qualitatively similar to those with other ACE inhibitors. The clinical significance of the quantitative differences requires further investigation.
doi_str_mv 10.1111/j.1365-2125.1993.tb04218.x
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Eighteen healthy, normotensive subjects (nine young and nine elderly) participated in a double‐blind, 3‐way, crossover study to compare aspects of the pharmacokinetics and pharmacodynamics of single oral doses of 10 mg benazepril, 10 mg enalapril and placebo. 2. The hypotensive effect was similar after both drugs but the absolute reductions were greater in the elderly who had higher initial levels of blood pressure. 3. The AUCs for both benazeprilat and enalaprilat were higher in the elderly but by a significantly greater amount for enalaprilat (+ 113% vs 40%; P &lt; 0.01). 4. The AUCs for both drugs tended to be highest in subjects with the lowest creatinine clearance. 5. The changes in kinetics and dynamics observed in the elderly after benazepril are qualitatively similar to those with other ACE inhibitors. 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Eighteen healthy, normotensive subjects (nine young and nine elderly) participated in a double‐blind, 3‐way, crossover study to compare aspects of the pharmacokinetics and pharmacodynamics of single oral doses of 10 mg benazepril, 10 mg enalapril and placebo. 2. The hypotensive effect was similar after both drugs but the absolute reductions were greater in the elderly who had higher initial levels of blood pressure. 3. The AUCs for both benazeprilat and enalaprilat were higher in the elderly but by a significantly greater amount for enalaprilat (+ 113% vs 40%; P &lt; 0.01). 4. The AUCs for both drugs tended to be highest in subjects with the lowest creatinine clearance. 5. The changes in kinetics and dynamics observed in the elderly after benazepril are qualitatively similar to those with other ACE inhibitors. The clinical significance of the quantitative differences requires further investigation.</description><subject>Administration, Oral</subject><subject>Adolescent</subject><subject>Age</subject><subject>Aged</subject><subject>Aging - metabolism</subject><subject>Angiotensin-Converting Enzyme Inhibitors - administration &amp; dosage</subject><subject>Angiotensin-Converting Enzyme Inhibitors - adverse effects</subject><subject>Angiotensin-Converting Enzyme Inhibitors - pharmacokinetics</subject><subject>Angiotensin-Converting Enzyme Inhibitors - pharmacology</subject><subject>Antihypertensive Agents - administration &amp; dosage</subject><subject>Antihypertensive Agents - adverse effects</subject><subject>Antihypertensive Agents - pharmacokinetics</subject><subject>Antihypertensive Agents - pharmacology</subject><subject>Benzazepines - administration &amp; dosage</subject><subject>Benzazepines - adverse effects</subject><subject>Benzazepines - pharmacokinetics</subject><subject>Benzazepines - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Blood pressure</subject><subject>Blood Pressure - drug effects</subject><subject>Blood Proteins - metabolism</subject><subject>Cardiovascular system</subject><subject>Clinical trials</subject><subject>Creatinine</subject><subject>Cross-Over Studies</subject><subject>Dose-Response Relationship, Drug</subject><subject>Double-Blind Method</subject><subject>Drugs</subject><subject>Enalapril - administration &amp; dosage</subject><subject>Enalapril - pharmacokinetics</subject><subject>Enalapril - pharmacology</subject><subject>Female</subject><subject>Geriatrics</subject><subject>Humans</subject><subject>Kinetics</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Miscellaneous</subject><subject>Peptidyl-Dipeptidase A - blood</subject><subject>Pharmacodynamics</subject><subject>Pharmacokinetics</subject><subject>Pharmacology. 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Drug treatments</topic><topic>Protein Binding</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Macdonald, NJ</creatorcontrib><creatorcontrib>Sioufi, A</creatorcontrib><creatorcontrib>Howie, CA</creatorcontrib><creatorcontrib>Wade, JR</creatorcontrib><creatorcontrib>Elliott, HL</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Toxicology Abstracts</collection><collection>Environmental Sciences and Pollution Management</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>British journal of clinical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Macdonald, NJ</au><au>Sioufi, A</au><au>Howie, CA</au><au>Wade, JR</au><au>Elliott, HL</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The effects of age on the pharmacokinetics and pharmacodynamics of single oral doses of benazepril and enalapril</atitle><jtitle>British journal of clinical pharmacology</jtitle><addtitle>Br J Clin Pharmacol</addtitle><date>1993-09</date><risdate>1993</risdate><volume>36</volume><issue>3</issue><spage>205</spage><epage>209</epage><pages>205-209</pages><issn>0306-5251</issn><eissn>1365-2125</eissn><coden>BCPHBM</coden><abstract>1. Eighteen healthy, normotensive subjects (nine young and nine elderly) participated in a double‐blind, 3‐way, crossover study to compare aspects of the pharmacokinetics and pharmacodynamics of single oral doses of 10 mg benazepril, 10 mg enalapril and placebo. 2. The hypotensive effect was similar after both drugs but the absolute reductions were greater in the elderly who had higher initial levels of blood pressure. 3. The AUCs for both benazeprilat and enalaprilat were higher in the elderly but by a significantly greater amount for enalaprilat (+ 113% vs 40%; P &lt; 0.01). 4. The AUCs for both drugs tended to be highest in subjects with the lowest creatinine clearance. 5. The changes in kinetics and dynamics observed in the elderly after benazepril are qualitatively similar to those with other ACE inhibitors. The clinical significance of the quantitative differences requires further investigation.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>9114905</pmid><doi>10.1111/j.1365-2125.1993.tb04218.x</doi><tpages>5</tpages><oa>free_for_read</oa></addata></record>
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subjects Administration, Oral
Adolescent
Age
Aged
Aging - metabolism
Angiotensin-Converting Enzyme Inhibitors - administration & dosage
Angiotensin-Converting Enzyme Inhibitors - adverse effects
Angiotensin-Converting Enzyme Inhibitors - pharmacokinetics
Angiotensin-Converting Enzyme Inhibitors - pharmacology
Antihypertensive Agents - administration & dosage
Antihypertensive Agents - adverse effects
Antihypertensive Agents - pharmacokinetics
Antihypertensive Agents - pharmacology
Benzazepines - administration & dosage
Benzazepines - adverse effects
Benzazepines - pharmacokinetics
Benzazepines - pharmacology
Biological and medical sciences
Blood pressure
Blood Pressure - drug effects
Blood Proteins - metabolism
Cardiovascular system
Clinical trials
Creatinine
Cross-Over Studies
Dose-Response Relationship, Drug
Double-Blind Method
Drugs
Enalapril - administration & dosage
Enalapril - pharmacokinetics
Enalapril - pharmacology
Female
Geriatrics
Humans
Kinetics
Male
Medical sciences
Miscellaneous
Peptidyl-Dipeptidase A - blood
Pharmacodynamics
Pharmacokinetics
Pharmacology. Drug treatments
Protein Binding
title The effects of age on the pharmacokinetics and pharmacodynamics of single oral doses of benazepril and enalapril
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