Steroids fluocinolone acetonide

In this group we find deficiency diseases (vitamin deficiencies, diabetes, Addison s disease, etc ). The logical treatment is to compensate these deficiencies by an outside supply of the missing molecule (vitamin or hormone). In hormonology often modified versions of the original endogenous hormone were developed. Examples are modified vitamins (menadione, benfotiamine), steroids (fluocinolone acetonide, flumethasone) and modified peptides (modified TRH, angiotensine, somatostatine, etc.). 

Research teams at Glaxo then undertook the synthesis of derivatives of betamethasone that might afford superior local anti-inflammatory and anti-allergic effectiveness. Using McKenzie and Stoughton s [21] new human-based pharmacologic test that could identify with ease the relative topical potency of steroid inflammatory compounds, a series of 17-esters of betamethasone prepared by Elks [22] was evaluated. This resulted in compounds with new standards of topical potency such as triamcinolone acetonide and fluocinolone acetonide. It was then discovered, that potency peaked with betamethasone-17-valerate and betamethasone-17,21-dipropionate, which were between four- and ten-fold more potent than the standard. 

Fluocinolone acetonide is a steroid acetal used to treat skin conditions such as eczema and psoriasis. The acetal group decreases the water solubility of the parent steroid, enhancing its potency and allowing for a longer duration of action. 

Some of the most important physiological steroids are the adrenocortical hormones, synthesized by the adrenal cortex. Most of these hormones have either a carbonyl group or a hydroxyl group at Cl 1 of the steroid skeleton. The principal adrenocortical hormone is cortisol, used for the treatment of inflammatory diseases of the skin (psoriasis), the joints (rheumatoid arthritis), and the lungs (asthma). Figure 25-10 compares the structure of natural cortisol with two synthetic corticoids fluocinolone acetonide, a fluori-nated synthetic hormone that is more potent than cortisol for treating skin inflammation and beclomethasone, a chlorinated synthetic hormone that is more potent than cortisol for treating asthma. 

Currently, there are three main pharmacologic approaches to the treatment of DME in practice or under study steroids (the intravitreal injection of triamcinolone acetonide, fluocinolone acetonide sustained drug delivery implant, dexamethasone biodegradable implant), PKC inhibitors, and VEGF inhibitors. 

For dermatitis, a topical steroid preparation (eg, triamcinolone acetonide, fluocinolone acetonide, flurandrenolone, or betamethasone-17-valerate) is the principal therapeutic agent. Oozing lesions should be treated with wet dressings (moistened with fluids such as 1 40 Burow s solution). Appropriate antibiotics should be given for secondary infection, and oral antihistamines for itching.13 Vesicating lesions have been successfully treated with compresses of a cold silver nitrate solution (1 1,000)... 

More recently, the search for better antedrugs for the treatment of asthma at Glaxo Wellcome has focused on the incorporation of remote lactones onto the glucocorticoid nucleus (5). It was discovered that lactone hydrolysis is an ideal antedrug mechanism for inhaled steroids. For example, in the 21-thio derivatives of fluocinolone acetonide, the ethyl ester 5 showed some lability in... 

Examples of group I, i.e. weak or low efficacy topical steroids, are hydrocortisone acetate in various concentrations, methylprednisolone 1.0% and prednisolone 0.5%. Group II, the moderately potent steroids, includes alclometasone dipropionate 0.05%, hydrocortisone butyrate 0.1%, triamcinolone acetonide 0.025% and fluocinolone ace-tonide 0.01%. Group III, the potent steroids, contains among others betamethasone valerate 0.1%, betamethasone dipropionate 0.05%, budesonide 0.025%, desoximetasone 0.05%, fluticasone propionate 0.05%, amcinonide 0.1%, fluocinonide 0.05% and mometasone furoate 0.1%. Group IV comprises the very potent agents such as clobetasol propionate 0.05% and halobetasol propionate 0.05%. 

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