Glucocorticoids synthetic

Also, a high proportion of depressed patients do not show the reduction in cortisol secretion which is seen when normal subjects are challenged with the synthetic glucocorticoid, dexamethasone, that normally decreases further release through feedback... 

Cortisol, the most important g/ucocorticoid, is synthesized by the adrenal cortex, it is involved in regulating protein and carbohydrate metabolism by promoting protein degradation and the conversion of amino acids into glucose. As a result, the blood glucose level rises (see p. 152). Synthetic glucocorticoids (e.g., dexamethasone) are used in drugs due to their anti-inflammatory and immunosuppressant effects. 

Many synthetic glucocorticoid derivatives are widely used as immunodepressants. Glucocorticoids (cortisone, prednisone, methylprednisolone, betamethasone, dexamethasone,... 

Pharmacokinetics Hydrocortisone and most of its congeners are readily absorbed from the Gl tract altered onsets and durations are usually achieved with injections of suspensions and esters. Hydrocortisone is metabolized by the liver, which is the rate-limiting step in its clearance. The metabolism and excretion of the synthetic glucocorticoids generally parallel hydrocortisone. Induction of hepatic enzymes will increase the metabolic clearance of hydrocortisone and the synthetic... 

Dexamethasone Synthetic glucocorticoid, lacks mineralocorticoid activity Used to treat range of inflammatory diseases. Used to treat some forms of asthma, also cerebral oedema and congenital adrenal hyperplasia... 

Methylprednisolone Synthetic glucocorticoid Used as an anti-inflammatory agent and as an immunosuppressant... 

Synthetic glucocorticoids are prednisolone, prednisone, methylprednisolone, dexamethasone, betamethasone and triamcinolone (Table 13.2). Hydrocortisone is available as either succinate or phosphate salts for oral and intravenous administration. It is the drug of choice when a rapid effect is required, e.g. acute adrenal insufficiency, or as peri-operative replacement therapy. Prednisolone can also be given intravenously. It has about 0.8 of the mineralocorticoid activity of hydrocortisone. Prednisone is a prodrug that is converted to prednisolone in the body. For chronic therapy, synthetic steroids without mineralocorticoid activity are preferred, such as dexamethasone, betamethasone or triamcinalone. Beclo-metasone passes membranes poorly and is more active topically than when given orally. It is used as an aerosol for chronic rhinitis and asthma, and topically in severe eczema. Fludrocortisone is a synthetic halogenated derivate of cortisol that is used for its mineralocorticoid effect. 

Glucocorticoids have potent anti-inflammatory and immunosuppressive properties. This is particularly evident when they are administered at pharmacological doses. A variety of synthetic glucocorticoids, some far more potent than cortisol, have been created for therapeutic use, such as hydrocortisone, prednisone, prednisolone, dexamethasone and betamethasone. 

Occupational exposure to glucocorticoids can cause adverse effects. Facial plethora has been found in workers manufacturing synthetic glucocorticoids, some of them having grossly abnormal responses to tetracosactide. 

Newton RW, Browning MC, Iqbal J, Piercy N, Adamson DG. Adrenocortical suppression in workers manufacturing synthetic glucocorticoids. BMJ 1978 l(6105) 73 l. 

Steroid structure and biosynthesis have been used from a pharmacologic standpoint. Pharmacologists have tried to develop more effective and less toxic synthetic steroids by manipulating the chemical side groups of these compounds. An example is the synthetic glucocorticoid dexamethasone, which is 25 times... 

The effectiveness and extensive clinical use of natural and synthetic glucocorticoids must be tempered by... 

Rifampicin and pregnenolone-16a-carbonitrile (PCN) induce members of the CYP3A family and represent a third type of inducer, in that the substrate specificity of the microsomes from treated animals differs from that of the microsomes from either phenobarbital-treated or TCDD-treated animals. Inducing substrates of this class include endogenous and synthetic glucocorticoids (e.g., dexamethasone), pregnane... 

B. M. Vayssiere, S. Dupont, A. Choquart, F. Petit, T. Garcia,C. Marchandeau, H. Gronemeyer, and M. Resche-Rigon, Synthetic glucocorticoids that dissociate transactivation and AP-1 transrepression exhibit antiinflammatory activity in vivo, Mol. Endocrinol. 11 1245 (1997). 

British Medical Journal 316 244-245 Newton R W et al 1978 Adrenocortical suppression in workers manufacturing synthetic glucocorticoids. British Medical Journal 1 73... 

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