Cortisol potency

The natural compounds cortisol [50-23-7], cortisone [53-06-5], and corticosterone [50-22-6] vary only slightly in stmctures and pharmacologic properties (see Steroids). The synthetic analogues inmore modem practice, prednisolone [52438-85-4], dexamethasone [50-02-2], triamcinolone [124-94-7], and betamethasone have greater antiinflammatory potency, and their effects on sodium retention tend to be less severe. 

Synthetic steroid with strong glucocorticoid-agonistic activity. Dexamethasone is over 10 times more potent than cortisol due to a higher binding affinity for glucocorticoid receptor and a decreased clearance rate of the compound. Due to its potency, dexamethasone is widely used in the clinics for the treatment of inflammatory diseases. 

A 27-year-old female is diagnosed with hypercortisolism. To determine whether cortisol production Is Independent of the pituitary gland, you decide to suppress ACTH production by giving a high-potency glucocorticoid. Which glucocorticoid is the best for this indication ... 

The actions of the synthetic steroids are similar to those of cortisol (see above). They bind to the specific intracellular receptor proteins and produce the same effects but have different ratios of glucocorticoid to mineralocorticoid potency (Table 39-1). 

It is generally considered dial aldosterone, and to some extent the other honnnnes. have a regulatory effect upon the metabolism of electrolytes and water, particularly upon the concentration of the ions of the alkali metals in intracellular lluids. Administration of steroids also increases the concentration of calcium ions in those fluids. However, all three of these hormones have a number of other effects, roughly in the order of potency—cortisol, corticosterone, aldosterone. They produce changes in the metabolism of carbohydrates, proteins, and fats. 

Steroid Anti-Inflammatory Potency (% Compared to Cortisol) Sodium Retention (% Compared to Cortisol)... 

Dexamethasone has approximately 10 times the potency of cortisol. It is extremely long acting. 

All absorbable corticoids possess the ability to produce adrenal suppression [11, 76]. The degree of suppression is related to potency. Comparative quantitative studies employ the Food and Drug Association s (FDA) diseased-skin protocol. As little as 14 g per week of clobetasol has induced suppression. Optimized betamethasone diproprionate is somewhat less suppressive, requiring over 49 g per week to significantly reduce plasma cortisol. Incomplete data with difluorosone suggests that it may be less suppressive. Fortunately, plasma cortisol usually returns to normal within 3 days when the superpotents are discontinued, at least in short-time application studies. 

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