Long-acting glucocorticoid

Mechanism of Action A long-acting glucocorticoid that inhibits accumulation of inflammatory cells at inflammation sites, phagocytosis, lysosomal enzyme release and synthesis, and releaseof mediators of inflammation. Therapeutic Effect Prevents and suppresses cell and tissue immune reactions and inflammatory process. Pharmacohinetics Rapidly, completely absorbed from the G1 tract after oral administration. Widely distributed. Protein binding High. Metabolized in the liver. Primarily excreted in urine. Minimally removed by hemodialysis. Half-life 3-4.5 hr. 

It is a selective and very potent long acting glucocorticoid. It causes suppression of pituitary adrenal axis. Used in shock due to trauma, allergic emergencies, rheumatoid arthritis, asthma, nephrotic syndrome and suppression of inflammation in eye and skin disorders. 

Long-acting agents, such as salmeterol and formoterol, have superseded short-duration bronchodilators such as albuterol and fenoterol. In addition, more potent, site-specific, rapid-onset, and long-acting glucocorticoids, such as fluticasone and budesonide, have superseded the delayed onset of action of less specific molecules such as beclomethasone. 

Betamethasone is an extremely potent long-acting glucocorticoid having a 20-30 folds enhanced activity in comparison to cortisol. It has been duly observed that it veiy rarely causes induction of sodium and water retention, and potassium depletion viz., co-treatment with cortisone and several other adrenal corticoids. 

Tolrestat (28) is a long-acting aldose reductase inhibitor useful in the prophylaxis of diabetic neuropathy, retinopathy, and cataracts [24 25] Lastly, the introduction of fluorine into steroids probably ushered in the modem era of fluonnated drugs Many commercial products were introduced [2] Typical of the products are the anti inflammatory glucocorticoids dexamethasone (29 X = F, Y = H), para-methasone (29, X = H, Y = F), and flumethasone (29, X = H, Y = F)... 

Yates DH, Kharitonov SA, Barnes PJ. An mhaled glucocorticoid does not prevent tolerance to the bronchoprotec-tive effect of a long-acting inhaled beta 2-agonist. Am J Respir Crit Care Med 1996 154(6 Pt l) 1603-7. Erratum in Am J Respir Crit Care Med 1997 155(4) 1491. 

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