Pharmacogenetic differences in the inhibitory effect of cimetidine on the metabolism of antipyrine
The relationship between acetylator phenotype and the inhibitory effect of cimetidine on the hepatic metabolism of antipyrine has been studied in 20 subjects. Cimetidine, 1,0 g/day resulted in a significant decrease in the metabolic clearance rate of antipyrine, but only in slow acetylators, as fast...
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| Veröffentlicht in: | European journal of clinical pharmacology 1987-01, Vol.31 (5), p.613-615 |
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| container_end_page | 615 |
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| container_title | European journal of clinical pharmacology |
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| creator | GACHALYI, B VAS, A CSILLAG, K NAGY, B KOCSIS, F KALDOR, A |
| description | The relationship between acetylator phenotype and the inhibitory effect of cimetidine on the hepatic metabolism of antipyrine has been studied in 20 subjects. Cimetidine, 1,0 g/day resulted in a significant decrease in the metabolic clearance rate of antipyrine, but only in slow acetylators, as fast acetylators were less affected. No sex difference was observed. No major change occurred in the urinary excretion of D-glucaric acid, which means that cimetidine had not-affected that Phase II reaction. It did significantly decrease the urinary partial clearance rate of norantipyrine, leaving that of antipyrine and 4-OH-antipyrine unchanged, which suggests that cimetidine had preferentially inhibited the P450 isozyme that catalyses norantipyrine formation. |
| doi_str_mv | 10.1007/BF00606641 |
| format | Article |
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Cimetidine, 1,0 g/day resulted in a significant decrease in the metabolic clearance rate of antipyrine, but only in slow acetylators, as fast acetylators were less affected. No sex difference was observed. No major change occurred in the urinary excretion of D-glucaric acid, which means that cimetidine had not-affected that Phase II reaction. It did significantly decrease the urinary partial clearance rate of norantipyrine, leaving that of antipyrine and 4-OH-antipyrine unchanged, which suggests that cimetidine had preferentially inhibited the P450 isozyme that catalyses norantipyrine formation.</description><identifier>ISSN: 0031-6970</identifier><identifier>EISSN: 1432-1041</identifier><identifier>DOI: 10.1007/BF00606641</identifier><identifier>PMID: 3830247</identifier><language>eng</language><publisher>Heidelberg: Springer</publisher><subject>Acetylation ; Adult ; Antipyrine - analogs & derivatives ; Antipyrine - antagonists & inhibitors ; Antipyrine - metabolism ; Biological and medical sciences ; Cimetidine - pharmacology ; Edaravone ; Female ; General pharmacology ; Glucaric Acid - urine ; Humans ; Male ; Medical sciences ; Metabolic Clearance Rate - drug effects ; Microsomes, Liver - metabolism ; Middle Aged ; Pharmacogenetics ; Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions ; Pharmacology. 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Cimetidine, 1,0 g/day resulted in a significant decrease in the metabolic clearance rate of antipyrine, but only in slow acetylators, as fast acetylators were less affected. No sex difference was observed. No major change occurred in the urinary excretion of D-glucaric acid, which means that cimetidine had not-affected that Phase II reaction. It did significantly decrease the urinary partial clearance rate of norantipyrine, leaving that of antipyrine and 4-OH-antipyrine unchanged, which suggests that cimetidine had preferentially inhibited the P450 isozyme that catalyses norantipyrine formation.</description><subject>Acetylation</subject><subject>Adult</subject><subject>Antipyrine - analogs & derivatives</subject><subject>Antipyrine - antagonists & inhibitors</subject><subject>Antipyrine - metabolism</subject><subject>Biological and medical sciences</subject><subject>Cimetidine - pharmacology</subject><subject>Edaravone</subject><subject>Female</subject><subject>General pharmacology</subject><subject>Glucaric Acid - urine</subject><subject>Humans</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Metabolic Clearance Rate - drug effects</subject><subject>Microsomes, Liver - metabolism</subject><subject>Middle Aged</subject><subject>Pharmacogenetics</subject><subject>Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions</subject><subject>Pharmacology. Drug treatments</subject><subject>Phenotype</subject><issn>0031-6970</issn><issn>1432-1041</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkE1Lw0AQhhdRaq1evAs5iAchOvuVTY5arAoFPeg5bDazdiXJ1t300H_vSkudy8vwPMzAS8glhTsKoO4fFwAFFIWgR2RKBWc5BUGPyRSA07yoFJySsxi_AaisgE_IhJccmFBT0ryvdOi18V844OhM1jprMeBgMGZuyMYVpli5xo0-bDNM0IyZt5lxffJbN2Dmd1radeM7F_s_rofRrbch8XNyYnUX8WKfM_K5ePqYv-TLt-fX-cMyN5zSMeclk2hRqpZbriqFTHFG0ztUWjEhrQZbSlq1ylLe2FKjKlqwUlihy1JWfEZudnfXwf9sMI5176LBrtMD-k2slRIC0iTxdiea4GMMaOt1cL0O25pC_Vdo_V9okq_2VzdNj-1B3TeY-PWe62h0Z4MejIsHrWRccsb5Lym_fX4</recordid><startdate>19870101</startdate><enddate>19870101</enddate><creator>GACHALYI, B</creator><creator>VAS, A</creator><creator>CSILLAG, K</creator><creator>NAGY, B</creator><creator>KOCSIS, F</creator><creator>KALDOR, A</creator><general>Springer</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>7X8</scope></search><sort><creationdate>19870101</creationdate><title>Pharmacogenetic differences in the inhibitory effect of cimetidine on the metabolism of antipyrine</title><author>GACHALYI, B ; VAS, A ; CSILLAG, K ; NAGY, B ; KOCSIS, F ; KALDOR, A</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c311t-3825efe57d3f3797e27321fece7a7245fa0f8519d7f13bf8ae76d0f54f4a88593</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Acetylation</topic><topic>Adult</topic><topic>Antipyrine - analogs & derivatives</topic><topic>Antipyrine - antagonists & inhibitors</topic><topic>Antipyrine - metabolism</topic><topic>Biological and medical sciences</topic><topic>Cimetidine - pharmacology</topic><topic>Edaravone</topic><topic>Female</topic><topic>General pharmacology</topic><topic>Glucaric Acid - urine</topic><topic>Humans</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Metabolic Clearance Rate - drug effects</topic><topic>Microsomes, Liver - metabolism</topic><topic>Middle Aged</topic><topic>Pharmacogenetics</topic><topic>Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions</topic><topic>Pharmacology. Drug treatments</topic><topic>Phenotype</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>GACHALYI, B</creatorcontrib><creatorcontrib>VAS, A</creatorcontrib><creatorcontrib>CSILLAG, K</creatorcontrib><creatorcontrib>NAGY, B</creatorcontrib><creatorcontrib>KOCSIS, F</creatorcontrib><creatorcontrib>KALDOR, A</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>MEDLINE - Academic</collection><jtitle>European journal of clinical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>GACHALYI, B</au><au>VAS, A</au><au>CSILLAG, K</au><au>NAGY, B</au><au>KOCSIS, F</au><au>KALDOR, A</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacogenetic differences in the inhibitory effect of cimetidine on the metabolism of antipyrine</atitle><jtitle>European journal of clinical pharmacology</jtitle><addtitle>Eur J Clin Pharmacol</addtitle><date>1987-01-01</date><risdate>1987</risdate><volume>31</volume><issue>5</issue><spage>613</spage><epage>615</epage><pages>613-615</pages><issn>0031-6970</issn><eissn>1432-1041</eissn><abstract>The relationship between acetylator phenotype and the inhibitory effect of cimetidine on the hepatic metabolism of antipyrine has been studied in 20 subjects. Cimetidine, 1,0 g/day resulted in a significant decrease in the metabolic clearance rate of antipyrine, but only in slow acetylators, as fast acetylators were less affected. No sex difference was observed. No major change occurred in the urinary excretion of D-glucaric acid, which means that cimetidine had not-affected that Phase II reaction. It did significantly decrease the urinary partial clearance rate of norantipyrine, leaving that of antipyrine and 4-OH-antipyrine unchanged, which suggests that cimetidine had preferentially inhibited the P450 isozyme that catalyses norantipyrine formation.</abstract><cop>Heidelberg</cop><cop>Berlin</cop><pub>Springer</pub><pmid>3830247</pmid><doi>10.1007/BF00606641</doi><tpages>3</tpages></addata></record> |
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| issn | 0031-6970 1432-1041 |
| language | eng |
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| subjects | Acetylation Adult Antipyrine - analogs & derivatives Antipyrine - antagonists & inhibitors Antipyrine - metabolism Biological and medical sciences Cimetidine - pharmacology Edaravone Female General pharmacology Glucaric Acid - urine Humans Male Medical sciences Metabolic Clearance Rate - drug effects Microsomes, Liver - metabolism Middle Aged Pharmacogenetics Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions Pharmacology. Drug treatments Phenotype |
| title | Pharmacogenetic differences in the inhibitory effect of cimetidine on the metabolism of antipyrine |
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