Effect of age and gender on the pharmacokinetics of eprosartan
Aims To compare the pharmacokinetics of eprosartan between young (18–45 years) and elderly (65 years) men and between young men and young, premenopausal women (18–45 years). Methods Twenty‐four subjects (eight subjects/group) received a single 200 mg eprosartan oral dose followed by serial blood s...
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| Veröffentlicht in: | British journal of clinical pharmacology 1998-09, Vol.46 (3), p.267-270 |
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| creator | Tenero, David M. Martin, David E. Miller, Ann K. Ilson, Bernard Boike, Steven C. Zariffa, Névine Jorkasky, Diane K. |
| description | Aims
To compare the pharmacokinetics of eprosartan between young (18–45 years) and elderly (65 years) men and between young men and young, premenopausal women (18–45 years).
Methods
Twenty‐four subjects (eight subjects/group) received a single 200 mg eprosartan oral dose followed by serial blood sampling over 24 h.
Results
Eprosartan was safe and well tolerated. There were no apparent differences in the pharmacokinetics of eprosartan between young females and young males or in the plasma protein binding of eprosartan (≈98%) for the three groups. On average, AUC (0,∞) and Cmax values were ≈2‐fold higher in elderly men than young men [AUC (0,∞) 95% CI: 1.22, 4.34; Cmax 95% CI: 0.98, 4.00]. Similarly, unbound AUC (0,∞) and Cmax values were, on average, ≈2‐fold higher in elderly men than young men [unbound AUC (0,∞) 95% CI: 1.29, 4.44; unbound Cmax 95% CI: 1.02, 4.12]. tmax was delayed in the elderly men compared with young men, with a median difference of 2.5 h (95% CI: 1.00, 3.01 h).
Conclusions
No gender differences were observed in the pharmacokinetics of eprosartan. There were ≈ two fold higher AUC and Cmax values for eprosartan observed in elderly men as compared with young men, most likely due to increased bioavailability of eprosartan in the elderly. Based on the excellent safety profile in the elderly in Phase III clinical trials (doses up to 1200 mg eprosartan) eprosartan can be safely administered to elderly hypertensive patients without an initial dose adjustment. Subsequently, the dose of eprosartan, as for other antihypertensive agents, may be individualized based on tolerability/response. |
| doi_str_mv | 10.1046/j.1365-2125.1998.00778.x |
| format | Article |
| fullrecord | <record><control><sourceid>wiley_pubme</sourceid><recordid>TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_1873684</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>BCP778</sourcerecordid><originalsourceid>FETCH-LOGICAL-c4978-2e1802dd780a4aaefcd63bdf8dcc177283454bf19277b7a1a568c8c6f17a1653</originalsourceid><addsrcrecordid>eNqNkFtLwzAUx4Moc04_gtAHX1uTtE1SkIGOeQFBH_YeTnPZOru0pFW3b2-7jaJvPp0c_pcTfggFBEcEJ-x2HZGYpSElNI1IlokIY85FtD1B40E4RWMcYxamNCXn6KJp1hiTmLB0hEYZZ0nGsjGazq01qg0qG8DSBOB0sDROGx9ULmhXJqhX4Degqo_CmbZQTe80ta8a8C24S3RmoWzM1XFO0OJxvpg9h69vTy-z-9dQJRkXITVEYKo1FxgSAGOVZnGurdBKEc6piJM0yS3JKOc5BwIpE0ooZkm3sDSeoOmhtv7MN0Yr41oPpax9sQG_kxUU8q_iipVcVl-SCB4zkXQF4lCgup833tghS7Dsicq17MHJHpzsico9Ubntote_bw_BI8JOvznq0CgorQenimaw0QRTsrfdHWzfRWl2_z4vH2bv3SP-AXiHkmA</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Effect of age and gender on the pharmacokinetics of eprosartan</title><source>MEDLINE</source><source>Access via Wiley Online Library</source><source>EZB-FREE-00999 freely available EZB journals</source><source>Wiley Online Library (Open Access Collection)</source><creator>Tenero, David M. ; Martin, David E. ; Miller, Ann K. ; Ilson, Bernard ; Boike, Steven C. ; Zariffa, Névine ; Jorkasky, Diane K.</creator><creatorcontrib>Tenero, David M. ; Martin, David E. ; Miller, Ann K. ; Ilson, Bernard ; Boike, Steven C. ; Zariffa, Névine ; Jorkasky, Diane K.</creatorcontrib><description>Aims
To compare the pharmacokinetics of eprosartan between young (18–45 years) and elderly (65 years) men and between young men and young, premenopausal women (18–45 years).
Methods
Twenty‐four subjects (eight subjects/group) received a single 200 mg eprosartan oral dose followed by serial blood sampling over 24 h.
Results
Eprosartan was safe and well tolerated. There were no apparent differences in the pharmacokinetics of eprosartan between young females and young males or in the plasma protein binding of eprosartan (≈98%) for the three groups. On average, AUC (0,∞) and Cmax values were ≈2‐fold higher in elderly men than young men [AUC (0,∞) 95% CI: 1.22, 4.34; Cmax 95% CI: 0.98, 4.00]. Similarly, unbound AUC (0,∞) and Cmax values were, on average, ≈2‐fold higher in elderly men than young men [unbound AUC (0,∞) 95% CI: 1.29, 4.44; unbound Cmax 95% CI: 1.02, 4.12]. tmax was delayed in the elderly men compared with young men, with a median difference of 2.5 h (95% CI: 1.00, 3.01 h).
Conclusions
No gender differences were observed in the pharmacokinetics of eprosartan. There were ≈ two fold higher AUC and Cmax values for eprosartan observed in elderly men as compared with young men, most likely due to increased bioavailability of eprosartan in the elderly. Based on the excellent safety profile in the elderly in Phase III clinical trials (doses up to 1200 mg eprosartan) eprosartan can be safely administered to elderly hypertensive patients without an initial dose adjustment. Subsequently, the dose of eprosartan, as for other antihypertensive agents, may be individualized based on tolerability/response.</description><identifier>ISSN: 0306-5251</identifier><identifier>EISSN: 1365-2125</identifier><identifier>DOI: 10.1046/j.1365-2125.1998.00778.x</identifier><identifier>PMID: 9764969</identifier><identifier>CODEN: BCPHBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Science Ltd</publisher><subject>Acrylates - metabolism ; Acrylates - pharmacokinetics ; Adult ; age ; Aged ; Aging - metabolism ; angiotensin II receptor antagonist ; Antihypertensive agents ; Antihypertensive Agents - metabolism ; Antihypertensive Agents - pharmacokinetics ; Area Under Curve ; Biological and medical sciences ; Cardiovascular system ; eprosartan ; Female ; gender ; Half-Life ; Humans ; Imidazoles - metabolism ; Imidazoles - pharmacokinetics ; Male ; Medical sciences ; Middle Aged ; pharmacokinetics ; Pharmacology. Drug treatments ; Premenopause ; Protein Binding ; Sex Factors ; Short Report ; Thiophenes</subject><ispartof>British journal of clinical pharmacology, 1998-09, Vol.46 (3), p.267-270</ispartof><rights>1998 INIST-CNRS</rights><rights>1998 Blackwell Science Ltd 1998</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4978-2e1802dd780a4aaefcd63bdf8dcc177283454bf19277b7a1a568c8c6f17a1653</citedby><cites>FETCH-LOGICAL-c4978-2e1802dd780a4aaefcd63bdf8dcc177283454bf19277b7a1a568c8c6f17a1653</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1046%2Fj.1365-2125.1998.00778.x$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1046%2Fj.1365-2125.1998.00778.x$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>230,309,310,314,780,784,789,790,885,1417,1433,23930,23931,25140,27924,27925,45574,45575,46409,46833</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2402169$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9764969$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Tenero, David M.</creatorcontrib><creatorcontrib>Martin, David E.</creatorcontrib><creatorcontrib>Miller, Ann K.</creatorcontrib><creatorcontrib>Ilson, Bernard</creatorcontrib><creatorcontrib>Boike, Steven C.</creatorcontrib><creatorcontrib>Zariffa, Névine</creatorcontrib><creatorcontrib>Jorkasky, Diane K.</creatorcontrib><title>Effect of age and gender on the pharmacokinetics of eprosartan</title><title>British journal of clinical pharmacology</title><addtitle>Br J Clin Pharmacol</addtitle><description>Aims
To compare the pharmacokinetics of eprosartan between young (18–45 years) and elderly (65 years) men and between young men and young, premenopausal women (18–45 years).
Methods
Twenty‐four subjects (eight subjects/group) received a single 200 mg eprosartan oral dose followed by serial blood sampling over 24 h.
Results
Eprosartan was safe and well tolerated. There were no apparent differences in the pharmacokinetics of eprosartan between young females and young males or in the plasma protein binding of eprosartan (≈98%) for the three groups. On average, AUC (0,∞) and Cmax values were ≈2‐fold higher in elderly men than young men [AUC (0,∞) 95% CI: 1.22, 4.34; Cmax 95% CI: 0.98, 4.00]. Similarly, unbound AUC (0,∞) and Cmax values were, on average, ≈2‐fold higher in elderly men than young men [unbound AUC (0,∞) 95% CI: 1.29, 4.44; unbound Cmax 95% CI: 1.02, 4.12]. tmax was delayed in the elderly men compared with young men, with a median difference of 2.5 h (95% CI: 1.00, 3.01 h).
Conclusions
No gender differences were observed in the pharmacokinetics of eprosartan. There were ≈ two fold higher AUC and Cmax values for eprosartan observed in elderly men as compared with young men, most likely due to increased bioavailability of eprosartan in the elderly. Based on the excellent safety profile in the elderly in Phase III clinical trials (doses up to 1200 mg eprosartan) eprosartan can be safely administered to elderly hypertensive patients without an initial dose adjustment. Subsequently, the dose of eprosartan, as for other antihypertensive agents, may be individualized based on tolerability/response.</description><subject>Acrylates - metabolism</subject><subject>Acrylates - pharmacokinetics</subject><subject>Adult</subject><subject>age</subject><subject>Aged</subject><subject>Aging - metabolism</subject><subject>angiotensin II receptor antagonist</subject><subject>Antihypertensive agents</subject><subject>Antihypertensive Agents - metabolism</subject><subject>Antihypertensive Agents - pharmacokinetics</subject><subject>Area Under Curve</subject><subject>Biological and medical sciences</subject><subject>Cardiovascular system</subject><subject>eprosartan</subject><subject>Female</subject><subject>gender</subject><subject>Half-Life</subject><subject>Humans</subject><subject>Imidazoles - metabolism</subject><subject>Imidazoles - pharmacokinetics</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Middle Aged</subject><subject>pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>Premenopause</subject><subject>Protein Binding</subject><subject>Sex Factors</subject><subject>Short Report</subject><subject>Thiophenes</subject><issn>0306-5251</issn><issn>1365-2125</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkFtLwzAUx4Moc04_gtAHX1uTtE1SkIGOeQFBH_YeTnPZOru0pFW3b2-7jaJvPp0c_pcTfggFBEcEJ-x2HZGYpSElNI1IlokIY85FtD1B40E4RWMcYxamNCXn6KJp1hiTmLB0hEYZZ0nGsjGazq01qg0qG8DSBOB0sDROGx9ULmhXJqhX4Degqo_CmbZQTe80ta8a8C24S3RmoWzM1XFO0OJxvpg9h69vTy-z-9dQJRkXITVEYKo1FxgSAGOVZnGurdBKEc6piJM0yS3JKOc5BwIpE0ooZkm3sDSeoOmhtv7MN0Yr41oPpax9sQG_kxUU8q_iipVcVl-SCB4zkXQF4lCgup833tghS7Dsicq17MHJHpzsico9Ubntote_bw_BI8JOvznq0CgorQenimaw0QRTsrfdHWzfRWl2_z4vH2bv3SP-AXiHkmA</recordid><startdate>199809</startdate><enddate>199809</enddate><creator>Tenero, David M.</creator><creator>Martin, David E.</creator><creator>Miller, Ann K.</creator><creator>Ilson, Bernard</creator><creator>Boike, Steven C.</creator><creator>Zariffa, Névine</creator><creator>Jorkasky, Diane K.</creator><general>Blackwell Science Ltd</general><general>Blackwell Science</general><general>Blackwell Science Inc</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>5PM</scope></search><sort><creationdate>199809</creationdate><title>Effect of age and gender on the pharmacokinetics of eprosartan</title><author>Tenero, David M. ; Martin, David E. ; Miller, Ann K. ; Ilson, Bernard ; Boike, Steven C. ; Zariffa, Névine ; Jorkasky, Diane K.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4978-2e1802dd780a4aaefcd63bdf8dcc177283454bf19277b7a1a568c8c6f17a1653</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Acrylates - metabolism</topic><topic>Acrylates - pharmacokinetics</topic><topic>Adult</topic><topic>age</topic><topic>Aged</topic><topic>Aging - metabolism</topic><topic>angiotensin II receptor antagonist</topic><topic>Antihypertensive agents</topic><topic>Antihypertensive Agents - metabolism</topic><topic>Antihypertensive Agents - pharmacokinetics</topic><topic>Area Under Curve</topic><topic>Biological and medical sciences</topic><topic>Cardiovascular system</topic><topic>eprosartan</topic><topic>Female</topic><topic>gender</topic><topic>Half-Life</topic><topic>Humans</topic><topic>Imidazoles - metabolism</topic><topic>Imidazoles - pharmacokinetics</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Middle Aged</topic><topic>pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>Premenopause</topic><topic>Protein Binding</topic><topic>Sex Factors</topic><topic>Short Report</topic><topic>Thiophenes</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Tenero, David M.</creatorcontrib><creatorcontrib>Martin, David E.</creatorcontrib><creatorcontrib>Miller, Ann K.</creatorcontrib><creatorcontrib>Ilson, Bernard</creatorcontrib><creatorcontrib>Boike, Steven C.</creatorcontrib><creatorcontrib>Zariffa, Névine</creatorcontrib><creatorcontrib>Jorkasky, Diane K.</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>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>Tenero, David M.</au><au>Martin, David E.</au><au>Miller, Ann K.</au><au>Ilson, Bernard</au><au>Boike, Steven C.</au><au>Zariffa, Névine</au><au>Jorkasky, Diane K.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of age and gender on the pharmacokinetics of eprosartan</atitle><jtitle>British journal of clinical pharmacology</jtitle><addtitle>Br J Clin Pharmacol</addtitle><date>1998-09</date><risdate>1998</risdate><volume>46</volume><issue>3</issue><spage>267</spage><epage>270</epage><pages>267-270</pages><issn>0306-5251</issn><eissn>1365-2125</eissn><coden>BCPHBM</coden><abstract>Aims
To compare the pharmacokinetics of eprosartan between young (18–45 years) and elderly (65 years) men and between young men and young, premenopausal women (18–45 years).
Methods
Twenty‐four subjects (eight subjects/group) received a single 200 mg eprosartan oral dose followed by serial blood sampling over 24 h.
Results
Eprosartan was safe and well tolerated. There were no apparent differences in the pharmacokinetics of eprosartan between young females and young males or in the plasma protein binding of eprosartan (≈98%) for the three groups. On average, AUC (0,∞) and Cmax values were ≈2‐fold higher in elderly men than young men [AUC (0,∞) 95% CI: 1.22, 4.34; Cmax 95% CI: 0.98, 4.00]. Similarly, unbound AUC (0,∞) and Cmax values were, on average, ≈2‐fold higher in elderly men than young men [unbound AUC (0,∞) 95% CI: 1.29, 4.44; unbound Cmax 95% CI: 1.02, 4.12]. tmax was delayed in the elderly men compared with young men, with a median difference of 2.5 h (95% CI: 1.00, 3.01 h).
Conclusions
No gender differences were observed in the pharmacokinetics of eprosartan. There were ≈ two fold higher AUC and Cmax values for eprosartan observed in elderly men as compared with young men, most likely due to increased bioavailability of eprosartan in the elderly. Based on the excellent safety profile in the elderly in Phase III clinical trials (doses up to 1200 mg eprosartan) eprosartan can be safely administered to elderly hypertensive patients without an initial dose adjustment. Subsequently, the dose of eprosartan, as for other antihypertensive agents, may be individualized based on tolerability/response.</abstract><cop>Oxford, UK</cop><pub>Blackwell Science Ltd</pub><pmid>9764969</pmid><doi>10.1046/j.1365-2125.1998.00778.x</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Acrylates - metabolism Acrylates - pharmacokinetics Adult age Aged Aging - metabolism angiotensin II receptor antagonist Antihypertensive agents Antihypertensive Agents - metabolism Antihypertensive Agents - pharmacokinetics Area Under Curve Biological and medical sciences Cardiovascular system eprosartan Female gender Half-Life Humans Imidazoles - metabolism Imidazoles - pharmacokinetics Male Medical sciences Middle Aged pharmacokinetics Pharmacology. Drug treatments Premenopause Protein Binding Sex Factors Short Report Thiophenes |
| title | Effect of age and gender on the pharmacokinetics of eprosartan |
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