Plasma cortisol delivery from oral cortisol and cortisone acetate: relative bioavailability.

Heazelwood, VJ; Galligan, JP; Cannell, GR; Bochner, Felix; Mortimer, Robin H.

doi:10.1111/j.1365-2125.1984.tb04999.x

Cited by 39 publications

(17 citation statements)

References 13 publications

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“…Both HC and CA have anti-inflammatory activity and mineralocorticoid effects and are short-acting (8 to 12 h), especially HC, which has a serum elimination half-life of 1.7 h and very high bioavailability [25]. The mean bioavailability of CA is about 80% that of HC, with a high correlation between the two steroids (r = 0.87) [26]. Prednisolone (P) is another analogue and it has an intermediate duration of action and more anti-inflammatory effect than mineralocorticoid activity.…”

Section: Gc Replacement Therapymentioning

confidence: 99%

Long-Acting Hydrocortisone for Glucocorticoid Replacement Therapy

Johannsson

Filipsson²,

Bergthorsdottir³

et al. 2007

Horm Res Paediatr

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Background: Glucocorticoid (GC) deficiency is a consequence of various disorders that are by themselves rare. Because of this low prevalence, the low cost of GC replacement therapy and the belief that existing outcomes are good, there has been little interest in development of new and improved pharmaceutical products for treatment of GC deficiency. However, GC replacement therapy is complex: diurnal variation of endogenous cortisol must be replicated, GC needs may change during times of physical and psychological stress and there is no biomarker of its action that can be used to monitor individual dose response. Current Limitations: Recent data suggest that the outcome of established long-term GC replacement therapy may not be as good as previously believed. Short-acting GCs such as hydrocortisone (HC) and cortisone acetate for replacement therapy require 2 to 3 administrations per day. Developing Alternatives: Drug delivery system technologies are now available that could permit design and manufacture of a formulation that could accommodate once-daily administration of HC. Such a formulation would enable more physiological serum cortisol-time profiles than are possible with currently available formulations. This short review provides some background on GC replacement therapy, along with recent data on the outcome of patient groups with GC insufficiency, and briefly discusses some general principles for a controlled-release (‘long-acting’) HC formulation.

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Section: Gc Replacement Therapymentioning

confidence: 99%

Long-Acting Hydrocortisone for Glucocorticoid Replacement Therapy

Johannsson

Filipsson²,

Bergthorsdottir³

et al. 2007

Horm Res Paediatr

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“…We do not recommend cortisone acetate or prednisone for glucocorticoid substitution therapy in CAH because of its lower and variable bioavailability (26). Both need to be converted by 11β-hydroxysteroid dehydrogenase to be biologically active; cortisone acetate needs to be converted to cortisol and prednisone to prednisolone.…”

Section: Accepted Manuscriptmentioning

confidence: 97%

Substitution therapy in adult patients with congenital adrenal hyperplasia

Reisch¹

2015

Best Practice & Research Clinical Endocrinology & Metab

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“…Utilizamos em nosso hospital o acetato de cortisona para tratamento das crianças com HSRC-21OH. O acetato de cortisona apresenta 80% da biodisponibilidade da hidrocortisona (16) e aproximadamente 70% de sua potência (17). Além disso, desde que a cortisona, deve ser convertida ao cortisol para ser biologicamente ativa, a redução da atividade da 11β-hidroxiesteróide desidrogenase, que ocorre no período puberal, pode reduzir a eficácia dessa droga, havendo necessidade do aumento da dose (18).…”

Section: Figura 1 Esquema De Tratamento Pré-natal Da Hsrc-21ohunclassified

Tratamento da hiperplasia supra-renal congênita por deficiência da 21-hidroxilase

Bachega

Madureira

Brenlha

et al. 2001

Arq Bras Endocrinol Metab

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Arq Bras Endocrinol Metab vol 45 nº 1 Fevereiro 2001 64 RESUMOO tratamento da hiperplasia supra-renal congênita por deficiência da 21-hidroxilase (HSRC-21OH) tem como objetivos repor glico e mineralocorticóides, evitar a virilização dos genitais externos, prevenir a desidratação por perda de sal, controlar o hiperandrogenismo sem afetar a velocidade de crescimento, preservar a função gonadal, fertilidade e estatura final. Relatamos a nossa experiência no acompanhamento de 96 pacientes com HSRC-21OH. Nas crianças utilizamos como glicocorticóide o acetato de cortisona (18-20 mg/m 2 /dia) e nos adultos a dexametasona (0,25-0,75 mg/dia). Quando necessário, a reposição do mineralocorticóide foi feita com 9α-fluor-hidrocortisona 50-250 µg/dia dependendo da faixa etária. Apesar da substituição adequada com glico e/ou mineralocorticóides o resultado final do tratamento da HSRC-21OH ainda deixa a desejar, principalmente em relação ao crescimento, já que a estatura final na maior parte das casuísticas está entre -1 e -2 DP em relação a estatura alvo. Novas terapêuticas da HSRC-21OH, como a associação de hidrocortisona, fludrocortisona, flutamida e testolactona ou a suprarrenalectomia cirúrgi-ca ainda estão em fase experimental e a evolução a longo prazo é necessária para avaliar seu real efeito. ABSTRACTThe purpose of the treatment for congenital adrenal hyperplasia due to 21-hydroxylase deficiency (CAH-21OH) is to replace gluco and mineralocorticoids, prevent virilization of the external genitalia, salt loss and hyperandrogenism and preserve gonadal function, fertility and final height. Our experience in the treatment of 96 patients with CAH-21OH is presented. Children have been treated with cortisone acetate (18-20 mg/m2/day) and adults with dexamethasone (0.25-0.75 mg/day). If necessary, mineralocorticoid replacement was accomplished with 9α-fludrocortisone, 50-250 µg/day, according to chronological age. Despite therapy with gluco and mineralocorticoids the end results for CAH-21OH is still inadequate, especially when growth is concerned; in most reports final height reaches between 1 to 2 SD bellow target height. New therapeutic approaches for CAH-21OH, such as the association of flutamide and testolactone to hydrocortisone and fludrocortisone, and even surgical or chemical adrenalectomy, are still experimental and long-term follow-up is necessary to evaluate their validity.

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Plasma cortisol delivery from oral cortisol and cortisone acetate: relative bioavailability.

Cited by 39 publications

References 13 publications

Long-Acting Hydrocortisone for Glucocorticoid Replacement Therapy

Long-Acting Hydrocortisone for Glucocorticoid Replacement Therapy

Substitution therapy in adult patients with congenital adrenal hyperplasia

Tratamento da hiperplasia supra-renal congênita por deficiência da 21-hidroxilase

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