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Comparison of the analysis of corticosteroids using different techniques.

In this work we have optimized the analysis of 18 human corticosteroids, some endogenous (tetrahydrocortisol, tetrahydrocortisone, cortisol, and cortisone) and others synthetic (betamethasone, budesonide, cortisone acetate, desonide, dexamethasone, dexamethasone acetate, flunisolide, fluocinolone acetonide, halcinonide, methylprednisolone, prednisolone, prednisone, triamcinolone, and triamcinolone acetonide). Three analytical techniques were developed: ELISA, gas chromatography coupled with mass spectrometry (GC-MS), and liquid chromatography coupled with mass spectrometry (LC-MS). Several sample-preparation methods were optimized for each technique and enabled compounds of interest to be extracted from small urine samples (several mL). The results enabled us to assess the possibilities and the sensitivity of each technique for application to doping tests.

Adrenal Cortex Hormones↗

Contact dermatitis due to multiple corticosteroid creams.

A patient was allergic to the corticosteroids halcinonide, fluocinonide, desonide, and triamcinolone acetonide. She also was allergic to ethylendiamine hydrochloride, neomycin, thimerosal, formaldehyde solution, and nystatin.

Adolescent↗

Androstene-17-thioketals. 1st communication: glucocorticoid receptor binding, antiproliferative and antiinflammatory activities of some novel 20-thiasteroids (androstene-17-thioketals).

The unique replacements of the alpha-hydroxyl and beta-ketol groups of corticoids at C17 with selected, simple alkylthio or (2-fluoroalkyl)thio groups resulted in the structurally novel steroids, C17-alkylthioketals of 9 alpha-fluoro-11 beta-hydroxy-androsta-1,4-diene-3,17-dione. The described androstene-17-thioketals (20-thiasteroids) had high affinities for the glucocorticoid receptor protein of rat liver cytosol. Most were more potent than triamcinolone acetonide, a clinically moderately potent corticoid, in antiproliferative and antiinflammatory activities in mice. Specifically, (11 beta, 17 alpha)-17-(ethylthio)-9 alpha-fluoro-11 beta-hydroxy-17-(methylthio) androsta-1,4-dien-3-one (tipredane, SQ 27,239) and (11 beta, 17 alpha)-17-(ethylthio)-9 alpha-fluoro-17-[2-(fluoroethyl)thio] - 11 beta - hydroxy-androsta-1,4-dien-3-one (SQ 28,300), topically applied, were as potent as halcinonide, a clinically highly potent corticoid, in inhibition of croton oil-induced edema in the mouse. It is suggested that both thiasteroids could be moderately to highly potent topical antiinflammatory agents in man.

Adrenalectomy↗

[Comparative study on the efficacy of diflucortolone valerate in the psoriasis plaque test (author's transl)].

Diflucortolone valerate was administered to 35 psoriatic patients of both sexes in 0.3% concentration as a W/O emulsion in comparison with various commercially available preparations to study its action in the psoriasis plaque test according to Scholtz and Dumas. The study showed the test substance to be equipotent with the halcinonide, clobetasol-17-propionate and desoximetasone preparations and significantly superior to those containing betamethasone-17,21-dipropionate, betamethasone-17-valerate and fluocinonide.

Adult↗

Characterization of the anti-inflammatory activity and reduced potential for dermal atrophy of (11 beta, 16 beta)-9-fluoro-1',2',3', 4'-tetrahydro-11,21-dihydroxypregna-1,4-dieno[16,17-b]naph thalene-3, 20-dione hydrate (1 : 1) (SQ 26,490), a topically active corticoid.

SQ 26,490, (11 beta, 16 beta)-9-fluoro-1',2',3',4'-tetrahydro-11, 21-dihydroxypregna-1,4-dieno[16,17-b]naphthalene 3,20-dione hydrate (1 : 1), was a moderately potent inhibitor of edema formation in the rat. After extended topical application, SQ 26,490 totally inhibited edema formation without appreciable production of skin atrophy, measured under identical conditions. This atrophy was maintained at a low plateau level of 15-20% at doses beyond those necessary to achieve optimal anti-inflammatory activity. In contrast, the potent corticoids, fluocinolone acetonide and halcinonide, and the moderately potent corticoid, clobetasone butyrate, produced inhibition of edema with a concomitant dose-related atrophy. Hydrocortisone, a weakly potent corticoid, totally inhibited edema and produced at high doses a low atrophy. SQ 26,490 possesses the property for a greater separation of anti-inflammatory and atrophogenic activities than comparative corticoids.

Administration, Topical↗

Delayed hypersensitivity to topical corticosteroids.

Topical hypersensitivity to corticosteroids was studied by epicutaneous testing using the Finn Chamber technic. The steroids were tested in both ethanol and white petrolatum and, in certain cases, in dimethyl sulfoxide. Additionally, commercial preparations were tested. Three groups of patients were studied: (1) patients with a history of hypersensitivity to at least two topical preparations (five of ten patients studied showed a positive patch test reaction for corticosteroids), (2) patients in whom topical corticosteroid hypersensitivity was suspected because of treatment-resistant eczema (seven of twenty-five patients showed a positive patch test reaction), and (3) dermatologic inpatients and outpatients undergoing epicutaneous testing for suspected topical hypersensitivity. Hydrocortisone-17-butyrate (H-17-B) was included in the standard patch test series; of 450 patients tested, two showed a positive patch test reaction. All the patients with corticosteroid hypersensitivity had a positive reaction to H-17-B. In six patients, additional hypersensitivities to one or several other steroid preparations were seen. Use testing was performed as an open test, with 0.1% or 1% H-17-B in ethanol on normal skin of the flexor side of the upper extremities. A positive test reaction was seen in only one of nine patients. Results of use testing with the commercial 0.1% H-17-B (Locoid) ointment were always negative. Our study suggests that the sensitivity of patch tests for corticosteroid hypersensitivity can be increased by using ethanol as vehicle.

Administration, Topical↗

Efficacy versus systemic effects of six topical steroids in the treatment of atopic dermatitis of childhood.

Six groups of children suffering from widespread atopic dermatitis were treated once daily with six topical steroids of different potency. Systemic effects were measured by the morning estimation of plasma cortisol. A clear relationship was demonstrated between clinical efficacy of the steroid treatment and degree of reduced adrenal function. This study demonstrated that a rapid and marked therapeutic effect can be obtained with potent topical steroids applied once daily without occlusion, but in children is accompanied by a fall in plasma cortisol.

Administration, Topical↗

Polymorphic light eruption in childhood.

The purpose of this article is to acquaint the pediatrician with polymorphic light eruption (PMLE) a light-induced, eczematous, cutaneous reaction that frequently begins in childhood. This sun-induced eruption is frequently misdiagnosed because of its similarity to atopic dermatitis.

Child↗

Palmar-plantar lichen sclerosus et atrophicus.

A 57-year-old woman has had lichen sclerosus et atrophicus confined to the palms and soles for the past six years. Diagnosis was confirmed by histologic study. Our patient's disease has been resistant to therapy.

Biopsy↗

Risks of unoccluded topical steroids in clinical trials.

Data were reviewed on the beneficial responses and adverse reactions among 2,849 patients in 14 paired-comparison studies with eight unoccluded topical corticosteroids in six steroid-responsive dermatoses. Adverse reactions were found to be mild, transient, and, for the most part, rare. Of 5,698 treatment exposures, 249 (4.39%) adverse reactions were reported, including irritation (1.3%), itching (0.95%), burning (0.81%), dryness (0.46%), scaling (0.30%), and vesicle formation (0.16%). Other reactions occurred in less than one in 1,000 treatment exposures. No severe reactions were observed. Five subjects (0.17%) terminated treatment early because of adverse reactions. The incidence of adverse reactions to vehicle alone was 6.7%. The benefit-risk ratio for mild reactions was 17:1. Therefore, long lists of adverse reactions are inappropriate in written consent forms for prospective volunteers for clinical trials. Al alternative warning statement is proposed.

Administration, Topical↗