Corticosteroids—glucocorticoids topical

Flumetasone pivalate is a corticosteroid used topically for its glucocorticoid activity in the treatment of various skin disorders. It is usually employed as a cream, ointment, or lotion. Flumetasone pivalate is also used in ear drops. 

Editor s notes In this chapter adverse effects and reactions that arise from the oral or parenteral administration of corticosteroids (glucocorticoids and mineralocorti-coids) are covered in the section on systemic administration. Other routes of administration are dealt with in the sections after that inhalation and nasal administration are dealt with in Chapter 16, topical administration to the skin in Chapter 14, and ocular administration in Chapter 47. 

Topical corticosteroids are used in the treatment of inflammatory dermatoses. The general pharmacology are discussed in chapter Glucocorticoids. ... 

The study design is dependent on the nature of the active drug. The bioequivalence study can be a comparative skin blanching study as in glucocorticoids (FDA, Topical Dermatological Corticosteroids In Vivo Bioequivalence, June 2,1995.) or a comparative clinical trial or any other appropriate vahdated bioequivalence study (e.g., dermatopharmacokinetic study) for the topical dermatological drug product. 

N. Bodor, Design of novel soft corticosteroids, Topical Glucocorticoids with Increased Benefit-Risk Ratio, Vol. 21 (H. Korting, ed.) Karger AG, Basel, 1993,... 

Beclomethasone dipropionate is a corticosteroid with mainly glucocorticoid activity that is started to exert a topical effect on the lungs, without significant systemic activity. It is used by inhalation, generally from a metered-dose aerosol, for the prophylaxis of asthma. Inhalation of nebulized beclomethasone dipropionate has also been used in the management of asthma in children. 

Figure 12-1 Aqueous humor steroid activity using the glucocorticoid receptor assay after administration of topical unlabeled fluorometholone 0.1% and fluorometholone acetate 0.1% in rabbits. (Adapted from Polansky JR. Basic pharmacology of corticosteroids. Curr Top Ocul Inflam 1993 1 19.)...

The therapeutic effectiveness of topically applied corticosteroids is attributed primarily to their antiinflammatory activity. The relative efficacy of topical corticosteroids appears to be in the following order hydrocortisone, prednisolone, betamethasone < hydrocortisone valerate or butyrate, betamethasone valerate, triamcinolone acetonide, flucinolone acetonide < betamethasone dipropionate, fluocino-nide. In addition to the nature of the corticosteroid, its solubility, and, to a lesser extent, the concentration used, clinical efficacy is influenced by the formulation of the preparation. Glucocorticoids appear to have greater efficacy when formulated in ointment bases than in cream or lotion vehicles. This could be attributed to the occlusive effect provided by ointments. The application of an occlusive dressing further enhances penetration and persistence of the steroid (reservoir effect) in the stratum corneum. " ... 

The main adverse effect of pimecrolimus is local skin irritation, with a stinging or burning sensation, which occurs in 30% of patients. Typically, children have less skin irritation than adults. Adverse effects such as local immunosuppression and an increased risk of local bacterial and viral infections (notably eczema herpeticum) are less common than with topical glucocorticoids (5). In addition, there is a lack of skin atrophy (6,7). However, topical corticosteroids have the advantage of better skin penetration than pimecrolimus and will therefore continue to be used for more heavily keratinized skin such as in psoriasis (8). 

Glucocorticoid contact allergy is well known (SEDA-21, 158) and has to be particularly suspected in chronic conditions affecting the perianal area (17), after long-term topical medication, and in cases of failure to ameliorate dermatitis with corticosteroids. Patch tests should then be performed both with the recommended markers, budeso-nide (0.1% petrolatum) and tixocortol pivalate (1% petrolatum), and with the patient s own formulations. 

Dexacort dexamethasone. dexamethasone [ban, inn] (dexamethasone acetate, [usan] dexamethasone acefurate [inn] dexamethasone sodium phosphate [usan] dexamethasone pivalate dexamethasone phosphate dexamethasone metasulphobenzoate [ban] Dexacort Decadron Hexadrol Stiedex and many other names) is a potent CORTICOSTEROID, a GLUCOCORTICOID with ANTIINFLAMMATORY and ANTIALLERGIC properties. It is used topically to treat severe, non-infective inflammation of the skin caused by conditions such as eczema and psoriasis. It can be used systemically or orally for adrenocortical insufficiency, dexamethasone acefurate dexamethasone. dexamethasone acetate dexamethasone. dexamethasone phosphate dexamethasone. dexamethasone pivalate dexamethasone. dexamethasone metasulphobenzoate dexamethasone. 

Glucocorticoids have a very wide application as antiinflammatory agents in therapeutics. The route by which they are administered depends largely on their relative freedom from dangerous side-effects. Many are used by topical application, but some are intrinsically more powerful than others and may only be used when weaker corticosteroids have failed. Different salts may be used for certain purposes. 

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