Metabolism of tienilic acid (ticrynafen) in man. Pharmacokinetic and mass spectrometric studies
| العنوان: | Metabolism of tienilic acid (ticrynafen) in man. Pharmacokinetic and mass spectrometric studies |
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| المؤلفون: | Guy Lemieux, Joanne Paquin, Michel J. Bertrand, André Gougoux, Patrick Vinay |
| المصدر: | European Journal of Drug Metabolism and Pharmacokinetics. 5:113-125 |
| بيانات النشر: | Springer Science and Business Media LLC, 1980. |
| سنة النشر: | 1980 |
| مصطلحات موضوعية: | Adult, Chromatography, Gas, Time Factors, Uricosuric, Ticrynafen, Urine, Pharmacology, Hydroxylation, Mass Spectrometry, Excretion, Pharmacokinetics, medicine, Bile, Humans, Pharmacology (medical), Volume of distribution, Chromatography, Chemistry, Blood Proteins, Glycolates, Uric Acid, Kinetics, Tienilic acid, Liver function, medicine.drug |
| الوصف: | The pharmacokinetics and metabolism of tienilic acid (ticrynafen) a new diuretic with uricosuric properties, were studied in human volunteers following single ingestion of 250, 500 or 1000 mg. Tienilic acid was found to be extentively (more than 98%) bound to plasma proteins but not to displace the fraction of urate bound to plasma proteins at the usual therapeutic dosage (250 to 500 mg). The uricosuric and natriuretic effects of the drug lasted 8 to 12 hours. A peak concentration of 2.5, 4.5 or 10.1 mg/dl was noted in the plasma 2 hours following ingestion of each dose. The apparent volume of distribution of the drug was close to that of plasma volume. Tienilic acid disappeared rapidly from the plasma according to a first order kinetics and the plasma half-life ranged from 1.6 to 2.4 hours. Gas chromatography and mass spectrometric studies revealed that 21% of the ingested tienilic acid is excreted as such in the urine over 24 hours. Three major metabolites of the drug were identified in the urine: a monohydroxylated, a dihydroxylated and a diacid product. Including metabolites, 36 to 47% of the drug was excreted in the urine within 24 hours. No significant glucuro or sulfoconjugation of the drug or its metabolites could be detected in the urine. Excretion of the drug and its metabolites was also noted in the bile. It is concluded that tienilic acid is rapidly metabolized and excreted in humans with normal kidney and liver function. |
| تدمد: | 2107-0180 0378-7966 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db5fe079817a6e554db1d785823fad9dTest https://doi.org/10.1007/bf03189454Test |
| حقوق: | CLOSED |
| رقم الانضمام: | edsair.doi.dedup.....db5fe079817a6e554db1d785823fad9d |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 21070180 03787966 |
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