Metabolism of Hydrocortisone 21-Sulfate in Man

Nakada, Fujinori; Fukushima, David K.; Bradlow, H. Leon; Hellman, Louis M.; Gallagher, T. F.

doi:10.1210/jcem-29-10-1330

Cited by 8 publications

(1 citation statement)

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“…Pare, Bush and Roberts 1970). The finding of elevated 11oxo-17 -ketosteroids in patients with a high risk of myocardial infarction is in accordance with the high excretion of cortisol sulfate in patients with P V D. In adult subjects a great portion of these three metabolites is formed from exogenously administered cortisol sulfate (Nakada. Fukushima, Bradlow, Hel/man and Gallagher 1969;Hall and Giroud 1970).…”

Section: Discussionsupporting

confidence: 55%

The Excretion of Free Cortisol, Cortisone, Cortisol Sulfate and Cortisone Sulfate in Peripheral Vascular Disease, Diabetes Mellitus and Hyperthyroidism

et al. 1978

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In four groups of persons, l/healthy individuals, 2/ patients with diabetes mellitus, 3/ patients with peripheral vascular disease, and 4/ patients with hyperthyroidism, the urinary excretion of frce cortisol, cortisone, cortisol sulfate and cortisone sulfate was estimated. In groups 2 and 3 the excretion of all four substances was elevated. In hyperthyroidism a preponderance of free cortisone over cortisol was registered. The ratias of the followed substances suggest in patients with peripheral vascular disease a detoriation in the normal excretion of the followed corticoids, based on a preponderance of ll-OH-corticosteroids over their II-oxo-denvatives. This observation could be implicated in the mild hyperglycemia or decreased glucose tolerance, tha t is often found in atherosclerotic disease.

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Section: Discussionsupporting

confidence: 55%

The Excretion of Free Cortisol, Cortisone, Cortisol Sulfate and Cortisone Sulfate in Peripheral Vascular Disease, Diabetes Mellitus and Hyperthyroidism

et al. 1978

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A comparison of the bioavailability and potency of dexamethasone phosphate and sulphate in man

Miyabo

Nakamura

Kuwazima

et al. 1981

Eur J Clin Pharmacol

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The metabolic fate and ACTH-suppressant activity of two injectable dexamethasone esters, 21-phosphate and 21-sulphate, were studied in healthy men. After i.v. injection of 20mg free steroid alcohol, dexamethasone phosphate was efficiently hydrolyzed to free dexamethasone, reaching its peak plasma concentration within 5 min. About 9% of the administered dose appeared in the urine as free dexamethasone. By contrast, virtually no free dexamethasone was found in plasma and urine after injection of dexamethasone sulphate. Pharmacokinetic analysis showed that dexamethasone sulphate had a shorter plasma half-life and a higher metabolic clearance rate than free dexamethasone. A larger fraction (60%) of dexamethasone sulphate was rapidly excreted unmetabolized in urine. The plasma cortisol level was significantly suppressed for more than 24h after dexamethasone phosphate, while the plasma cortisol profile after dexamethasone sulphate merely showed physiological circadian variations. When the steroid esters were injected after pretreatment with metyrapone, a definite suppression of plasma ACTH was noted after dexamethasone phosphate, but again, dexamethasone sulphate was ineffective. These results cast serious doubt on the clinical value of dexamethasone sulphate as an injectable glucocorticoid, and critical reevaluation of this preparation is needed.

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Diagnostica Radioimmunologica. ModalitÀ operative per la determinazione dei valori basali e per l’effettuazione degli stimoli farmacodinamici

Dotti¹

1973

La Ricerca Clin. Lab.

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Metabolism of Hydrocortisone 21-Sulfate in Man

Cited by 8 publications

References 0 publications

The Excretion of Free Cortisol, Cortisone, Cortisol Sulfate and Cortisone Sulfate in Peripheral Vascular Disease, Diabetes Mellitus and Hyperthyroidism

The Excretion of Free Cortisol, Cortisone, Cortisol Sulfate and Cortisone Sulfate in Peripheral Vascular Disease, Diabetes Mellitus and Hyperthyroidism

A comparison of the bioavailability and potency of dexamethasone phosphate and sulphate in man

Diagnostica Radioimmunologica. ModalitÀ operative per la determinazione dei valori basali e per l’effettuazione degli stimoli farmacodinamici

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