Sulfinpyrazone kinetics after intravenous and oral administration

Lecaillon, J. B.; Souppart, C.; Schoeller, Jean-Paul; Humbert, G.; Massias, P

doi:10.1002/cpt1979265611

Cited by 20 publications

(10 citation statements)

References 3 publications

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“…Shorter half-lives, 2.2 and 2.7 h, were found in two normal males given radiolabelled sulphinpyrazone by Dieterle et al (1975). The estimated AUCs were also comparable with the data of Lecaillon et al (1979) who found 89.2 + 23.0 ug ml-1 h for a 200 mg oral dose and 204.3 + 113 ,ug ml-' h for 400 mg. The ratio of the AUCs at the two doses was overall 2.4 (c.f.…”

Section: Discussionsupporting

confidence: 83%

“…Shorter half-lives, 2.2 and 2.7 h, were found in two normal males given radiolabelled sulphinpyrazone by Dieterle et al (1975). The estimated AUCs were also comparable with the data of Lecaillon et al (1979) Lecaillon et al, 1979). However, the wider interindividual variation will be noted.…”

Section: Resultssupporting

confidence: 73%

“…of sulphinpyrazone found in our subjects may be compared with the Ty, values of 3.9 + 0.7 (s.d.) h and 3.8 + 0.6 h derived by Lecaillon et al (1979) for single oral doses of 200 mg and 400 mg in normal volunteers. Other published estimates of the plasma T½.…”

Section: Discussionmentioning

confidence: 99%

“…trast to the analysis of data following intravenous injection of sulphinpyrazone by Lecaillon et al, 1979).…”

Section: Pharmacokinetic Analysismentioning

confidence: 99%

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Pharmacokinetics of single doses of sulphinpyrazone and its major metabolites in plasma and urine.

Bradbrook¹,

John²,

Morrison³

et al. 1982

Brit J Clinical Pharma

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3 Plasma concentrations of the sulphone were low and peaked before those of the sulphide; its mean half-life was 3.1 h. The sulphide, which may be the sulphinpyrazone metabolite with activity on platelets, was eliminated with a mean half-life of 13.4 h. The AUC increases with dose of both metabolites suggested non-linearity. 4 Approximately 45-50% of the administered dose was eliminated in the urine as unchanged drug or as sulphone or p-hydroxy-sulphinpyrazone. The sulphide metabolite was not detected in the urine. The renal clearance of sulphinpyrazone was approximately 18 ml min-and that for the sulphone was similar. Sigma minus plots of the urinary excretion yielded half-lives of 3.5 h for the sulphone and 1 h for p-hydroxy-sulphinpyrazone.

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Section: Discussionsupporting

confidence: 83%

“…Shorter half-lives, 2.2 and 2.7 h, were found in two normal males given radiolabelled sulphinpyrazone by Dieterle et al (1975). The estimated AUCs were also comparable with the data of Lecaillon et al (1979) Lecaillon et al, 1979). However, the wider interindividual variation will be noted.…”

Section: Resultssupporting

confidence: 73%

Section: Discussionmentioning

confidence: 99%

“…trast to the analysis of data following intravenous injection of sulphinpyrazone by Lecaillon et al, 1979).…”

Section: Pharmacokinetic Analysismentioning

confidence: 99%

See 2 more Smart Citations

Pharmacokinetics of single doses of sulphinpyrazone and its major metabolites in plasma and urine.

Bradbrook¹,

John²,

Morrison³

et al. 1982

Brit J Clinical Pharma

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show abstract

“…Both values are comparable to those of sulphinpyrazone. Lecaillon, Souppart, Schoeller, Humbert & Massias (1979) reported the plasma half-life of sulphinpyrazone to be about 3.8 h and the distribution volume to be 60 ml kg-'. Having these data in mind, the reductive pathway seems to be of major quantitative importance in the elimination of sulphinpyrazone during long-term therapy.…”

Section: Discussionmentioning

confidence: 99%

Sulphinpyrazone metabolism during long‐term therapy.

Ak¹,

Jakobsen²

1981

Brit J Clinical Pharma

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1 The plasma concentrations of sulphinpyrazone and four of its metabolites are reported together with the amounts excreted in urine. Eight insulin-requiring diabetics were investigated, all treated with sulphinpyrazone 600-800 mg day-for 2.5 years or more. 2 Blood samples were drawn before the first morning dose and 2 h later. The mean plasma concentrations were (t = 0 h -t = 2 h): sulphinpyrazone 7.1-16.0>gml-'; sulphide 2.8-4.3 gigml-1; sulphone 1.7-4.8 pgmlm'; p-OH-sulphide 0.67-0.89 Fg ml-; p-OH-sulphinpyrazone 0. 10-0.16 pg ml-'. Statistically significant correlations were found between the plasma concentrations at t = 0 of the sulphide and the p-OH-sulphide and that of sulphinpyrazone. 3 In urine, a very wide range in excretion of unconjugated compounds was observed. Sulphinpyrazone were excreted in amounts corresponding to 1-30% of the daily dose. The metabolites were generally excreted in amounts corresponding to less than 1 % of the daily dose; however, up to 3% was found as the sulphone. 4 Increases of the concentrations of all compounds in urine were found after treatment with f-glucuronidase indicating 0-conjugation with glucuronic acid. 5 Since both the sulphide and the sulphone were found more active as inhibitors of platelet function in vitro than their parent compound, they may together constitute the major part of the platelet inhibitory drug activity in plasma during long-term therapy with sulphinpyrazone.

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S

Seyffart¹

1991

Drug Dosage in Renal Insufficiency

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Sulfinpyrazone kinetics after intravenous and oral administration

Cited by 20 publications

References 3 publications

Pharmacokinetics of single doses of sulphinpyrazone and its major metabolites in plasma and urine.

Pharmacokinetics of single doses of sulphinpyrazone and its major metabolites in plasma and urine.

Sulphinpyrazone metabolism during long‐term therapy.

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