Anti-inflammatory glucocorticoids

Tolrestat (28) is a long-acang aldose reductase inhibitor useful in the prophylaxis of diabetic neuropathy, retinopathy, and cataracts [24 25] Lastly, the intro-ducuon 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)... 

Therapeutic Function Topical anti-inflammatory glucocorticoid... 

Pharmacology The naturally occurring adrenal cortical steroids have both anti-inflammatory (glucocorticoid) and salt-retaining (mineralocorticoid) properties. These compounds are used as replacement therapy in adrenocortical deficiency states and may be used for their anti-inflammatory effects. 

Knowles, R.G., Salter, M., Brooks, S.L. and Moncada, S. (1990). Anti-inflammatory glucocorticoids inhibit the induction by endotoxin of nitric oxide synthase in the lung, liver and aorta of the rat. Biochem. Biophys. Res. Comm. 172, 1042-1048. 

C2 H36 F2O6 Anti-inflammatory Glucocorticoid Antipruritic Topical cream 2002-29-1 Prior to 1982/ Novartis... 

C22H28FNa08P Anti- inflammatory Glucocorticoid Injectable (Dog, Horse) 1869-92-7 April 2004/ Cross Vetpharm Group Ltd. Watson Laboratories, Inc. IVX Animal Health... 

C22H28F205 Anti- inflammatory Glucocorticoid Injectable Oral tablet Liquid 2135-17-3 (Ophthalmic) (Dog, Cat, Horse) Prior to 1982/ Fort Dodge Animal Health, Division of Wyeth Elanco Animal Health, A Division of Eli Lilly Co.A... 

Anabolic steroids such as nandrolone and testosterone, anti-inflammatory glucocorticoids such as methylprednisolone, and contraceptives such as estradiol and levonorgestrel all have slow-release formulations of their ester prodrugs in the market. 

Winder, Wax, Burr, Been and Rosiere showed that, at reasonable dose-levels, there is a good correlation between the erythema-delaying action and antirheumatic action of non-steroidal compounds. Of over 100 pharmacologically active agents examined, only 10 pyrazole, salicylate and cinchophen derivatives delay ultra-violet erythema anti-inflammatory glucocorticoids are inactive. 

Reid and his colleagues put forward the theory that the anti-inflammatory action of salicylate is due to its power to form metal chelate complexes. On this basis, it would be predicted that 2,6-dihydroxybenzoic acid (y-resorcylic acid) would be an even more potent anti-inflammatory agent. As already seen (page 77), early hopes of increased potency of this compound were not fulfilled. Nevertheless, the fact remains that many anti-inflammatory substances form coloured complexes with ferric ions in circumstances in which chemically related but inactive compounds do not . Salicylate, phenylbutazone and cinchophen behave in this way. Wiesel described metal chelate compounds of the anti-inflammatory glucocorticoids and showed that... 

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