Abstract：
:We studied the pharmacokinetics of moguisteine, a racemic non-narcotic peripheral antitussive drug, in 12 healthy male subjects after a single oral administration of 200 mg. The unchanged drug was absent in plasma and urine of all subjects. Moguisteine was immediately and completely hydrolyzed to its main active metabolite, the free carboxylic acid M1. Therefore, we evaluated the kinetic profiles of M1, of its enantiomers R(+)-M1 and S(-)-M1, and of M1 sulfoxide optical isomers M2/I and M2/II by conventional and stereospecific HPLC. Maximum plasma concentrations for M1 (2.83 mg/l), M2/I (0.26 mg/l) and M2/II (0.40 mg/l), were respectively reached at 1.3, 1.6 and 1.5 h after moguisteine administration. Plasma concentrations declined after the peak with mean apparent terminal half-lives of 0.65 h (M1), 0.88 h (M2/I) and 0.84 h (M2/II). Most of the administered dose was recovered in urine within 6 h from moguisteine treatment. The systemic and renal clearance values indicated high renal extraction ratio for all moguisteine metabolites, and particularly for M1 sulfoxide optical isomers. Plasma concentration-time profiles and urinary excretion patterns for M1 enantiomers R(+)-M1 and S(-)-M1 were quite similar. Thus, for later moguisteine pharmacokinetic evaluations the investigation of the plasma concentration-time curve and the urinary excretion of the sole racemic M1 through non-stereospecific analytical methods may suffice in most cases.
journal_name
Eur J Drug Metab Pharmacokinetjournal_title
European journal of drug metabolism and pharmacokineticsauthors
Bernareggi A,Crema A,Carlesi RM,Castoldi D,Ratti E,Renoldi MI,Ratti D,Ceserani R,Tognella Sdoi
10.1007/BF03190242subject
Has Abstractpub_date
1995-10-01 00:00:00pages
263-70issue
4eissn
0378-7966issn
2107-0180journal_volume
20pub_type
杂志文章abstract：:The kinetics of the nootropic drug oxiracetam was studied in 6 elderly female patients (age range 69-96 years) in good physical condition. After a single oral dose (800 mg), serum oxiracetam levels reached a peak (25 +/- 6 micrograms/ml) within 1-3 h and declined thereafter with a half-life of 3 to 6 h. Eighty-four pe...
journal_title：European journal of drug metabolism and pharmacokinetics
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更新日期：1987-04-01 00:00:00
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journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
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journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190109
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journal_title：European journal of drug metabolism and pharmacokinetics
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更新日期：1987-01-01 00:00:00
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pub_type： 杂志文章
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更新日期：2015-06-01 00:00:00
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journal_title：European journal of drug metabolism and pharmacokinetics
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abstract：:The disposition of the gonadotropin-releasing hormone (GnRH) agonist buserelin was studied in male rats under conditions of long-term administration. Rats were continuously infused with about 30 pmole [3H]-buserelin/24 h subcutaneously by osmotic minipumps for 4-7 days. After killing the rats, the 3H-activity of the t...
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journal_title：European journal of drug metabolism and pharmacokinetics
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更新日期：2001-10-01 00:00:00
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pub_type： 杂志文章
doi：10.1007/BF03188728
更新日期：1982-01-01 00:00:00
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journal_title：European journal of drug metabolism and pharmacokinetics
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doi：10.1007/BF03189539
更新日期：1982-01-01 00:00:00
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journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190057
更新日期：2000-01-01 00:00:00
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journal_title：European journal of drug metabolism and pharmacokinetics
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更新日期：1991-01-01 00:00:00
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journal_title：European journal of drug metabolism and pharmacokinetics
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doi：10.1007/BF03190149
更新日期：1992-07-01 00:00:00
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doi：10.1007/s13318-011-0049-6
更新日期：2011-12-01 00:00:00
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journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,多中心研究
doi：10.1007/s13318-013-0153-x
更新日期：2014-09-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Previous studies reported that tapentadol-sulfate represented one of the major metabolites of tapentadol excreted in urine. The current study aimed to identify the human cytosolic sulfotransferases (SULTs) that is(are) capable of sulfating tapentadol and to examine whether human cells and huma...
journal_title：European journal of drug metabolism and pharmacokinetics
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更新日期：2017-10-01 00:00:00
