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Medical Pharmacology Chapter 28: Physiology and Pharmacology: Adrenocorticosteroids / Adrenocortical Antagonists
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Source:
Synthesized from cholic acid (from cattle sources) or
Synthesized from steroid sapogenins (diosgenin) (plant sources)
Disposition:
Oral administration; complete absorption
Metabolized similar to endogenous steroids
Molecular alterations given rise to differences in:
Affinity for mineralocorticoid or glucocorticoid receptors
Extent of protein binding
Stability
Spectrum of metabolic products
Prodrugs may be used (prednisone is converted to prednisolone)
Similar to those of cortisol (endogenous agents)
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Drug |
Anti-inflammatory |
Salt-retaining |
Dosage Forms |
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Short/medium-acting glucocorticoid |
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Hydrocortisone (cortisol) |
1 |
1 |
oral, injectable, topical |
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Cortisone (Cortone) |
0.8 |
0.8 |
oral, injectable, topical |
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Prednisone (Deltasone) |
4 |
0.3 |
oral |
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Prednisolone (Prelone) |
5 |
0.3 |
oral, injectable, topical |
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Methylprednisolone (Solu-Medrol) |
5 |
0 |
oral, injectable, topical |
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Intermediate-acting glucocorticoid |
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Triamcinolone (Aristocort) |
5 |
0 |
oral, injectable, topical |
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Fluprednisolone |
15 |
0 |
oral |
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Long-acting glucocorticoid |
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Betamethasone (Celestone) |
25-40 |
0 |
oral, injectable, topical |
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Dexamethasone (Decadron) |
30 |
0 |
oral, injectable, topical |
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Drug |
Anti-inflammatory |
Salt-retaining |
Dosage Forms |
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Mineralocorticoids |
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Fludrocortisone (Florinef) |
10 |
250 |
oral, injectable, topical |
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Desoxycorticosterone acetate |
0 |
20 |
injectable, pellets |
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Adapted from Table 39-1: Goldfien, A.,Adrenocorticosteroids and Adrenocortical Antagonists, in Basic and Clinical Pharmacology, (Katzung, B. G., ed) Appleton-Lange, 1998, p. 640. |
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Goldfien, A.,Adrenocorticosteroids and Adrenocortical Antagonists, in Basic and Clinical Pharmacology, (Katzung, B. G., ed) Appleton-Lange, 1998, pp 635-650.
Williams, G. H and Dluhy, R. G. , Diseases of the Adrenal Cortex, In Harrison's Principles of Internal Medicine 14th edition, (Isselbacher, K.J., Braunwald, E., Wilson, J.D., Martin, J.B., Fauci, A.S. and Kasper, D.L., eds) McGraw-Hill, Inc (Health Professions Division), 1998, pp 2035-2056
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