Corticosteroids mineralocorticoid activity

Decrease dose or change corticosteroid to one with less mineralocorticoid activity (e.g., dexamethasone)... 

Hydrocortisone given parenterally is the corticosteroid of choice because of its combined glucocorticoid and mineralocorticoid activity. The starting dose is 100 mg IV by rapid infusion, followed by a continuous infusion or intermittent bolus of 100 to 200 mg every 24 hours. IV administration is continued for 24 to 48 hours. If the patient is stable at that time, oral hydrocortisone can be started at a dose of 50 mg every 8 hours for another 48 hours. A hydrocortisone taper is then initiated until the dosage is 30 to 50 mg/day in divided doses. 

Triamcinolone is a corticosteroid that is more potent than hydrocortisone and has a longer duration of action. Triamcinolone has only slight mineralocorticoid activity, whereas hydrocortisone has high mineralocorticoid activity and therefore triamcinolone is unsuitable for disease suppression on a long-term basis. Triamcinolone is available as injection, dental paste, nasal spray and as cream or ointment preparations. Hydrocortisone is available as cream, tablets and injections. 

Betamethasone Synthetic corticosteroid, displays glucocorticoid activity, lacks mineralocorticoid activity Use mainly as anti-inflammatory and immunosuppressive effect... 

Fludrocortisone acetate Synthetic corticosteroid with some glucocorticoid and potent mineralocorticoid activity Administered orally to treat primary adrenal insufficiency... 

Fluorination of corticosteroids at C-9 or/and C-6 increases glucocorticoid activity, while mineralocorticoid activity, responsible for sodium retention (the main adverse effect of corticoids), is decreased (cf. Chapter 4). Fluorocorticoster-oids were the first fluorinated compounds to be used clinically. They are still major drugs against many inflammatory disorders rheumatoid polyarthritis, ORL (asthma, rhinitis), brain edema, dermatological, allergies, anaphylactic shock, Quincke s edema). 

Prednisone [PRED ni sone] is a potent synthetic anti-inflammatory corticosteroid with less mineralocorticoid activity than cortisol (see p. 272). The use of this compound in the treatment of lymphomas arose when it was observed that patients with Cushing s syndrome (a syndrome associated with hypersecretion of cortisol) have lymphocytopenia and decreased lymphoid mass. These result from corticosteroid action on lymphocyte formation and distribution, that is, movement of these cells from the circulation to lymphoid tissue. 

Cortisone is a corticosteroid secreted by the adrenal cortex. It has glucocorticoid activity, as well as appreciable mineralocorticoid activity 25 mg cortisone acetate is equivalent in anti-inflammatory activity to about 5 mg prednisolone. 

Hydrocortisone is a corticosteroid with both glucocorticoid and, to a lesser extent, mineralocorticoid activity. 

Corticosteroids should only be used during acute exacerbations of ulcerative colitis. The total duration of therapy should not exceed 4 to 8 weeks. Many different corticosteroids are available and differ in anti-inflammatory potency and mineralocorticoid activity (Table 38-2). Choosing a corticosteroid and route of administration depends on the clinical presentation. 

B Methylprednisolone. Given the patient s electrolyte abnormalities, all of the other corticosteroid options would be ruled out since they have mineralocorticoid effects that may make this patient s electrolyte abnormalities worse. Methylprednisolone has anti-inflammatory properties and no mineralocorticoid activity. 

For patients who are hospitalized and present with electrolyte abnormalities, corticosteroids with high anti-inflammatory properties and minimal mineralocorticoid activity are preferred. 

A -cortisol prednisolone, cortisone (ban. inn] (cortisone acetate [usan] Kendall s compound E Reichstein s Substance Fa Wintersteiner s compound F NSC 9703 Cortisyl ) is a natural adrenal cortical hormone, a CORTICOSTEROID, which is converted to hydrocortisone in the liver. It has both GLUCOCORTICOID and MINERALOCORTICOID activity. It can therefore be used orally to make up for hormonal deficiency (especially mineral balance), for instance, following surgical removal of the adrenal glands. It can also be used for its ANTIINFLAMMATORY and ANTIALLERGIC properties in treating rheumatoid arthritis and in rheumatic fever therapy, cortisone acetate cortisone. 

Management of these disorders usually consists of treatment of the underlying cause of the mineralocorticoid excess. Patients who are taking corticosteroids may require a dosage reduction or may need to be switched to a corticosteroid with less mineralocorticoid activity. Patients with an endogenous source of excess mineralocorticoid activity may require surgery or the administration of spironolactone, amiloride, or triamterene. " " ... 

Dnig-htduceil. Thia/ide diuretics and corticosteroids are the most important. Carbenoxolone has mineralocorticoid activity. 

Budesonide is a potent corticosteroid agent used in the therapy of asthma. It is a glucocorticoid, but has potent mineralocorticoid activity. 

Corticosteroids traditionally are divided into mineralocorticoids and glucocorticoids according to their relative potencies in Na retention and effects on carbohydrate metabolism i.e., hepatic deposition of glycogen and gluconeogenesis) In general, potencies of steroids to sustain life in adrenalectomized animals closely parallel their mineralocorticoid activity, while potencies as antiinflammatory agents closely parallel their effects on glucose metabolism. The effects on Na" retention and the carbohydrate/anti-inflammatory actions are not closely related and reflect selective actions at distinct receptors. 

The immediate management of patients with acute adrenal insufficiency includes intravenous therapy with isotonic sodium chloride solution supplemented with 5% glucose and corticosteroids and appropriate therapy for precipitating causes such as infection, trauma, or hemorrhage. Because cardiovascular function often is reduced in the setting of adrenocortical insufficiency, the patient should be monitored for evidence of volume overload such as pulmonary edema. After an initial intravenous bolus of 100 mg, hydrocortisone (cortisol) should be given by continuous infusion at a rate of 50-100 mg every 8 hours. At this dose, which approximates the maximum daily rate of cortisol secretion in response to stress, hydrocortisone overwhelms the 11/1HSD2 barrier in mineralo-corticoid-responsive tissues and has sufficient mineralocorticoid activity to meet all requirements. As the patient stabilizes, the hydrocortisone dose may be decreased to 25 mg every 6-8 hours. Thereafter, patients are treated in the same fashion as those with chronic adrenal insufficiency see below). 

In general, the adrenocortical steroids (or adrenal corticosteroids) distinctly differ in their respective glucocorticoid activities i.e., carbohydrate-regulating), and mineralocorticoid activities (i.e., electrolyte-regulating). It has been observed that in human beings the following two compounds occur commonly ... 

Systemic corticosteroids can increase the loss of potassium, particularly those that are naturally occurring (cortisone, deoxycortone, hydrocortisone) whereas the synthetic derivatives (betamethasone, dexametha-sone, methylprednisolone, prednisolone, prednisone, triamcinolone) have much less mineralocorticoid activity. There is therefore the possibility of potassium depletion, particularly when corticosteroids are used long-term, which may increase the risk of digitalis toxicity. These corticosteroids also cause sodium and water retention, resulting in oedema and hypertension, which can lead to cardiac failure in some individuals. 

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