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
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    • "This difference is consistent with clinical observations that cortisone acetate has about two thirds the potency of cortisol (Boland, 1952; Ward et al., 1952). The cause of the reduced bioavailability of cortisone relative to that of cortisol is not clear although Jenkins and Samson (1967) have produced evidence that enhanced A ring reduction of cortisone may be important. "
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    ABSTRACT: Plasma cortisol levels were measured before and for 6 h after the intravenous injection of 50 mg cortisol as sodium succinate and oral administration of 50 mg cortisol and 50 mg cortisone acetate in 10 subjects with primary or secondary adrenal failure and in two normal volunteers. Peak cortisol levels of 1518 +/- 190 nmol 1(-1) (mean +/- s.e. mean) and 739 +/- 74 nmol 1(-1) were found 1.46 +/- 0.25 and 1.79 +/- 0.16 h after oral cortisol and cortisone acetate respectively. The relative bioavailability of oral cortisol and cortisone acetate varied widely (cortisol 26-91%, mean 54 +/- 6.9%, cortisone acetate 21-95%, mean 44 +/- 6.5%) but despite this wide variation there was, in individual subjects, a highly significant correlation between the bioavailability of the two steroids (r = 0.870, P less than 0.001). This suggests that the wide interindividual variations in plasma cortisol levels seen after oral cortisone acetate are not related to variations in bioconversion of cortisone.
    British Journal of Clinical Pharmacology 02/1984; 17(1):55-9. DOI:10.1111/j.1365-2125.1984.tb04999.x · 3.88 Impact Factor
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    • "p<0.03). Discussion In 1967 Jenkins and Sampson (1967) reported an almost unchanged conversion of prednisone to prednisolone in two patients with not clearly defined liver function. Powell and Axelsen (1972) studied six patients with acute hepatitis and 16 patients with chronic liver disease of whom nine had 'active' liver disease. "
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    ABSTRACT: Fourteen patients with liver cirrhosis received oral prednisone or prednisolone (0.3 mg per kg) randomised on two consecutive days. Serum prednisone and prednisolone were measured over the following four hours. Mean serum prednisolone concentration after oral prednisone decreased with impaired liver function estimated by galactose elimination capacity (r = 0.64, P less than 0.03). Mean serum prednisolone concentration after oral prednisone in the seven patients with severely impaired liver function was only 53% (P less than 0.05) of that observed in the seven patients with slightly impaired liver function. Conversely, mean serum prednisone concentration after oral prednisone in the patients with severely impaired liver function was 74% higher (P = 0.05) than in patients with slightly impaired liver function. Mean serum prednisolone after oral prednisolone was independent of liver function. As only prednisolone exerts glucocorticoid activity, our results indicate that prednisolone should be preferred to prednisone in the treatment of patients with impaired liver function.
    Gut 02/1980; 21(1):52-6. DOI:10.1136/gut.21.1.52 · 14.66 Impact Factor
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    • "Prednisone is frequently prescribed for the treatment of chronic active liver disease (CALD) (Soloway etal., 1972; Murray-Lyon et al., 1973) and must be reduced at the 1 I, keto group for conversion to its active therapeutic derivative, prednisolone (Jenkins and Sampson, 1967). This conversion depend on an 1If dehydrogenase, mainly located in the liver (Bush and Mahesh, 1964). "
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    ABSTRACT: Serum concentrations of prednisolone were measured by radioimmunoassay after the administration of prednisone (10, 20, or 30 mg) by mouth to five healthy volunteers, five patients with severe chronic active liver disease (CALD), and five patients with CALD in remission induced by prednisone. Only minor differences were found between the groups and bioavailability was linearly related to the dose of prednisone (r = 0.993). After prednisone (10 mg) was given by mouth and by vein to similar groups of volunteers and 11 additional patients with CALD, bioavailability of oral prednisone approximated 100% of the intravenous dose and no differences were found in the pharmacokinetics of prednisolone. We conclude that prednisone is effectively absorbed and converted to prednisolone in health and CALD and find no pharmacological evidence that either drug would be superior to the other for treating CALD.
    Gut 01/1979; 19(12):1131-5. DOI:10.1136/gut.19.12.1131 · 14.66 Impact Factor
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