Glucocorticoid
Name Glucocorticoid potency Mineralocorticoid potency Terminal half-life ( hours )
Cortisol ( hydrocortisone ) 1 1 8
Cortisone 0.8 0.8 8
Prednisone 3.5-5 0.8 16-36
Prednisolone 4 0.8 16-36
Methylprednisolone 5-7.5 0.5 18-40
Dexamethasone 25-80 0 36-54
Betamethasone 25-30 0 36-54
Triamcinolone 5 0 12-36
Fludrocortisone acetate 15 200 24
Deoxycorticosterone acetate 0 20 -
Aldosterone 0.3 200-1000 -
Beclometasone 8 sprays 4 times every day equivalent to orally 14 mg prednisone once a day - -
Pharmacology
Dexamethasone - a synthetic glucocorticoid binds more powerfully to the glucocorticoid receptor than cortisol does . Dexamethasone is based on the cortisol structure but differs at three positions ( extra double bond in the A-ring between carbons 1 and 2 and addition of a 9-α-fluoro group and a 16-α-methyl substituent ) . A variety of synthetic glucocorticoids , some far more potent than cortisol , have been created for therapeutic use . They differ in both pharmacokinetics ( absorption factor , half-life , volume of distribution , clearance ) and pharmacodynamics ( for example the capacity of mineralocorticoid activity : retention of sodium ( Na+ ) and water ; renal physiology ) . Because they permeate the intestines easily , they are administered primarily per os ( by mouth ) , but also by other methods , such as topically on skin . More than 90% of them bind different plasma proteins , though with a different binding specificity . Endogenous glucocorticoids and some synthetic corticoids have high affinity to the protein transcortin ( also called corticosteroid-binding globulin ) , whereas all of them bind albumin . In the liver , they quickly metabolize by conjugation with a sulfate or glucuronic acid , and are secreted in the urine . Glucocorticoid potency , duration of effect , and the overlapping mineralocorticoid potency vary . Cortisol is the standard of comparison for glucocorticoid potency . Hydrocortisone is the name used for pharmaceutical preparations of cortisol . The data below refer to oral administration . Oral potency may be less than parenteral potency because significant amounts ( up to 50% in some cases ) may not reach the circulation . Fludrocortisone acetate and deoxycorticosterone acetate are , by definition , mineralocorticoids rather than glucocorticoids , but they do have minor glucocorticoid potency and are included in this table to provide perspective on mineralocorticoid potency .
Glucocorticoids are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebrate animal cell. The name glucocorticoid is a portmanteau (glucose + cortex + steroid) and is composed from its role in regulation of glucose metabolism, synthesis in the adrenal cortex, and its steroidal structure (see structure to the right). A less common synonym is glucocorticosteroid. Glucocorticoids are part of the feedback mechanism in the immune system which reduces certain aspects of immune function, such as inflammation. They are therefore used in medicine to treat diseases caused by an overactive immune system, such as allergies, asthma, autoimmune diseases, and sepsis. Glucocorticoids have many diverse (pleiotropic) effects, including potentially harmful side effects, and as a result are rarely sold over the counter. They also interfere with some of the abnormal mechanisms in cancer cells, so they are used in high doses to treat cancer. This includes inhibitory effects on lymphocyte proliferation, as in the treatment of lymphomas and leukemias, and the mitigation of side effects of anticancer drugs. Glucocorticoids affect cells by binding to the glucocorticoid receptor. The activated glucocorticoid receptor-glucocorticoid complex up-regulates the expression of anti-inflammatory proteins in the nucleus (a process known as transactivation) and represses the expression of proinflammatory proteins in the cytosol by preventing the translocation of other transcription factors from the cytosol into the nucleus (transrepression). Glucocorticoids are distinguished from mineralocorticoids and sex steroids by their specific receptors, target cells, and effects.