Influence of Various Steroids on the Specific Binding of Cortisol

Demoor, P; Deckx, R; Steeno, Omer

doi:10.1677/joe.0.0270355

Cited by 37 publications

(5 citation statements)

References 1 publication

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“…Prednisolone, on the other hand, has an affinity for transcortin that is similar to that of cortisol 11 , . 12 During medication with prednisolone in patients, an apparent lowering (up to 30%) of the transcortin binding capacity was found. This is probably due to competition from the exogenous steroid for the binding site on transcortin 13 .…”

Section: Discussionmentioning

confidence: 99%

A cortisol suppression dose–response comparison of budesonide in controlled ileal release capsules with prednisolone

Edsbäcker

Nilsson²,

Larsson³

1999

Aliment Pharmacol Ther

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Aim: To assess the systemic effect of oral budesonide, given as Entocort controlled ileal release capsules, over a dose range of 3–15 mg/day, compared with that of a moderate dose (20 mg/day) of prednisolone. Methods: Twenty four healthy subjects were given 3, 9 or 15 mg budesonide or 20 mg prednisolone once daily, or 4.5 mg budesonide b.d., or placebo for 5 days in a randomized, double‐blind crossover study. The area under the curve (AUC) of plasma cortisol concentration and the amount of cortisol excreted in the urine were monitored. Results: Both plasma and urine cortisol suppression showed a dose‐response for the daily doses of budesonide. Prednisolone, 20 mg, suppressed plasma cortisol (AUC) statistically significantly more than 15 mg budesonide (P = 0.014), and 3 mg budesonide statistically significantly more than placebo (P = 0.010). No difference in AUC was detected between 9 mg and 4.5 mg budesonide b.d. Similar results for budesonide vs. placebo were obtained from urine cortisol excretion data. However, prednisolone affected urine cortisol less than it affected plasma cortisol. Conclusion After 5 days of administration, budesonide controlled ileal release capsules, in both clinical (9 mg/day) and high doses (15 mg/day), affected plasma cortisol less than a moderate (20 mg/day) dose of prednisolone.

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Section: Discussionmentioning

confidence: 99%

A cortisol suppression dose–response comparison of budesonide in controlled ileal release capsules with prednisolone

Edsbäcker

Nilsson²,

Larsson³

1999

Aliment Pharmacol Ther

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“…Furthermore, additional affinity is endowed by the presence of hydroxyl groups in the 1 I/?, 17a and 21 positions. The configuration of the oxygen at position 11 is important as neither cortisone (the 1 I-ketone) nor the 1 I alpha-isomer of cortisol is bound as strongly as cortisol itself (Daughaday, 1958a;De Moor et a/., 1963, Sandberg et al, 1960.…”

Section: Binding Ofsteroids Other Than Cortisol 10 Cbgmentioning

confidence: 99%

“…Tetrahydro compounds and most synthetic steroids (with the exception of prednisone and prednisolone) appear to possess little cross-reactivity (De Moor et a/., 1963;Murphy, 1967;Fiorelli et al, 1972).…”

Section: Binding Ofsteroids Other Than Cortisol 10 Cbgmentioning

confidence: 99%

“…The compounds with the greatest degree of competition with cortisol for binding sites on human CBG are cortisone, corticosterone, deoxycorticosterone, 1 1-deoxycortisol and progesterone. Tetrahydro compounds and most synthetic steroids (with the exception of prednisone and prednisolone) appear to possess little cross-reactivity (De Moor et a/., 1963;Murphy, 1967;Fiorelli et al, 1972).…”

Section: Biosynthesis Of Cbgmentioning

confidence: 99%

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Human Corticosteroid Binding Globulin

Brien

1981

Clinical Endocrinology

181

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SUMMARY The literature on corticosteroid binding globulin (transcortin) in the human is reviewed under the following headings: physicochemical properties, biosynthesis, measurement, and physiological, pharmacological and pathological variations with particular emphasis of the effects of pregnancy and oral contraceptives. Finally, the physiological implications of corticosteroid binding globulin are discussed.

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“…l4 Some studies required that a standard be formulated in each subject's predose plasma to correct for endogenous interferences3 and most RIA studies used dexamethasone to suppress the synthesis of plasma cortisol concentrations which interfere with the RIA assay for predni~olone.l-~ The effects of dexamethasone and its suppression of cortisol synthesis on the normal absorption and disposition of prednisolone are not kn0wn.l The possibility exists that dexamethasone may decrease the clearance of prednisolone because cortisol will no longer occupy high affinity binding sites on corticosteroid binding globulin (CBG). 15 The net effect may mimic the decreased clearance of cortisol that is associated with the administration of betamethasone.l8 Our studies do not require the suppression of cortisol. The HPLC assay is specific, accurate, and sensitive enough to characterize the absorption and disposition kinetics of a 5 mg prednisone d0se.l'…”

Section: Discussionmentioning

confidence: 90%

Bioavailability and disposition of prednisone and prednisolone from prednisone tablets

Rose

Yurchak

Nsko

et al. 1980

Biopharm & Drug Disp

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SUMMARYThe relative bioavailability of two 50 mg prednisone tablet formulations was determined in 18 healthy male volunteers who were not pretreated with dexamethasone. Plasma and urine samples were collected over a 24-h period and their concentrations of prednisone and prednisolone were assayed by a specific and sensitive high pressure liquid chromatography (HPLC) method. Bioavailability was assessed by comparing the areas under the plasma concentration-time curves and by the relative amounts of prednisone and prednisolone in urine. There were no significant differences between the bioavailability of the film-coated and standard 50 mg tablets. Eight subjects subsequently received a 40 mg equivalent intravenous dose of prednisolone as prednisolone succinate to provide plasma concentrations of prednisolone similar to concentrations found after oral doses of prednisone. The systemic bioavailability of prednisolone, the active metabolite generated from film-coated and standard prednisone tablets, was estimated to be 0.77k0.15 and 0.80+ 0.11, respectively. The nonlinear distribution, the interconversion, and the simultaneous elimination of these drugs, however, complicate any assessment of their relative and absolute bioavailability.

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Influence of Various Steroids on the Specific Binding of Cortisol

Cited by 37 publications

References 1 publication

A cortisol suppression dose–response comparison of budesonide in controlled ileal release capsules with prednisolone

A cortisol suppression dose–response comparison of budesonide in controlled ileal release capsules with prednisolone

Human Corticosteroid Binding Globulin

Bioavailability and disposition of prednisone and prednisolone from prednisone tablets

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