Article

Conversion of cortisone to cortisol and prednisone to prednisolone.

British medical journal 05/1967; 2(5546):205-7. DOI: 10.1136/bmj.2.5546.205
Source: PubMed
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    ABSTRACT: This report describes a simple and sensitive reverse phase HPLC method with UV detection for the simultaneous determination of prednisolone and prednisone in human plasma. The analysis utilized a C18 analytical column and a mobile phase consisting of acetonitrile:0.08% trifluoroacetic acid in deionized water (28:72, v/v). Prednisolone, prednisone and corticosterone (internal standard) were extracted from plasma by one-step extraction with t-butyl methyl ether. Prednisolone, prednisone and the internal standard were eluted at 19.8, 21.4 and 34.3 min, respectively. The standard curves were linear (r ≥ 0.998) for prednisolone and prednisone over the concentration ranges of 2–1000 ng/mL and 5–100 ng/mL, respectively. The intra- and inter-day assay variabilities ranged from 1.8–10.5% and 0.7–9.5%, respectively, for prednisolone, and from 6.3–18.5% and 1.8–4.5%, respectively, for prednisone. The LOD and LOQ were 0.5 and 2 ng/mL, respectively, for prednisolone, and 1 and 5 ng/mL, respectively, for prednisone using a plasma sample volume of 0.5 mL. This highly sensitive and selective assay method was successfully applied to a pharmacokinetic study after oral administration of 10 mg prednisolone to human volunteers.
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    ABSTRACT: Glucocorticoids (GC), administered topically or systemically, form the cornerstone of asthma therapy. Delivered systemically, GCs serve as a major component of rescue therapy for acute asthma exacerbations. They also serve as chronic supplemental therapy in patients with severe persistent asthma who remain symptomatic despite high-dose inhaled GC therapy. Inhaled GCs are now the preferred controller medication for all asthmatics except for those with the mildest disease. Glucocorticoids have been used in the treatment of asthma for nearly 50 years, beginning soon after cortisone was first synthesized and following reports that cortisone and corticotropin were effective in the treatment of rheumatoid arthritis.34 The early studies with cortisone showed improvements in asthma symptoms and pulmonary function and reductions in the numbers of circulating lymphocytes and eosinophils.11, 27 and 57 Since then, great strides have been made in the understanding of how GCs act at the molecular and cellular level and also in the awareness of the multitude of adverse effects associated with prolonged use of GCs. Inhaled GC preparations have been developed that, because of their high topical-to-systemic effects, have proven to be safe and very effective in the treatment of asthma. This article provides a broad overview of the structure, pharmacokinetics, and pharmacodynamics of both systemically administered and inhaled GCs.
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    ABSTRACT: A rational, physiological schedule for parenteral glucocorticoid substitution therapy during surgical procedures is proposed based on the principle of imitating the normal hypothalamic-pituitary-adrenocortical response to surgery.The schedule includes the injection of 25 mg cortisol intravenously in all patients together with induction of anaesthesia. Following major surgery, 100 mg cortisol dissolved in saline or glucose is continuously infused intravenously every 24 hours until gastrointestinal function permits oral intake of usual glucocorticoid substitution therapy. In case continuous cortisol infusion is undesirable, 25 mg cortisol is injected intravenously every four hours. Following minor surgery, usual oral glucocorticoid therapy is started immediately after the operation.It is recommended to use water-soluble cortisol preparations and not cortisone acetate, which results in limited plasma cortisol levels.ZUSAMMENFASSUNGEs wird ein rationelles, physiologisches Schema für die parenterale Glukokortikoid-Substitutionstherapie vorgeschlagen, das auf dem Prinzip beruht, die normale hypothalamisch-hypophysär-adrenocorticale Reaktion auf die Operation nachzuahmen.Zusammen mit der Anaesthesie-Einleitung erhalten alle Patienten 25 mg Cortisol i.v. Nach großen Eingriffen werden über 24 Stunden 100 mg Cortisol, in Glukose- oder Kochsalzlösung aufgelöst, als i.v. Tropfinfusion verabreicht, bis die Magen-Darm-Tätigkeit eine orale Gluko-Kortikoid-Substitutions-therapie gestattet. Fur den Fall, daß die kontinuierliche Zufuhr von Cortisol unerwünscht sein sollte, werden 25 mg Cortisol alle 6 Stnnden i.v. injiziert. Nach kleinen operativen Eingriffen kann üblicherweise schon unmittelbar anschließend die Cortisoltherapie oral begonnen werden.Es wird empfohlen, wasserlosliche Cortisol-Präparate und nicht Cortison-Acetate zu verwenden, mit denen nur beschränkte Plasma-Cortisol-Spiegel erzielt werden können.
    Acta Anaesthesiologica Scandinavica 08/1975; 19(4):260-264. · 2.36 Impact Factor

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