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At least 1,189 records · Page 66Linked to original sources
PubMed1986

Glucocorticoid-induced vasoconstriction in human skin. An inhibitory role on phospholipase A2 activity.

The ability of topically applied betamethasone valerate to reduce erythema produced by a variety of vasodilators was assessed. The steroid significantly reduced the erythema induced by topical arachidonic acid, intradermal histamine, and compound 48/80. We postulated that the steroid reduced endogenous phospholipase activity either before or after application of the vasodilators, or both. This action may explain the mechanism of glucocorticoid-induced vasoconstriction in the skin and part of the steroids' action in acute inflammatory skin disease.

Administration, Topical↗
PubMed1978

[Chemical modification of epsilon-amino lysine groups in horseradish peroxidase. Its effect on catalytic properties and spatial structure of the enzyme].

Effect of chemical modification of horseradish peroxidase lysine epsilon-amino groups by propionic, butyric, valeric, succinic anhydrides and trinitrobenzolsulfonic acid (TNBS) on catalytic properties of the enzyme is investigated. All the preparations of modified peroxidase have 100% peroxidase activity for o-dianizidine at pH 7.0, which indicates the absence of lysine epsilon-amino group in the enzyme active site. pH-dependencies of modified peroxidase relative activity are studied; modification by anhydrides of monobasic acids is not found to result in changes of the relative activity pH-profile, while modification by succinic anhydride widens it. Absorption and circular dichoism spectra of native and modified peroxidase within 260--270 nm are obtained, some changes in the enzyme tertiary structure after its epsilon-amino groups modification are observed. Modification of four epsilon-amino groups by buturic and succinic anhydrides and of three epsilon-amino groups by TNBS is found to increase the regidity of protein surrounding of heme, and modification of six epsilon-amino groups by TNBS results in more unwrapped enzyme structure as compared with its native molecule.

Butyrates↗
PubMed1988

Potency ranking of two new topical corticosteroid creams containing 0.1% desonide or 0.05% halometasone utilising the human skin blanching assay.

The human blanching assay was used to assess the potency of two new proprietary corticosteroid creams. The blanching abilities of 0.1% desonide cream and 0.05% halometasone cream were evaluated relative to the blanching elicited by 0.05% clobetasol 17-propionate cream, 0.1% betamethasone 17-valerate cream and 0.05% clobetasone 17-butyrate cream. The results of the trial indicated that the 0.1% desonide cream falls into the potent group of topical corticosteroid preparations and the 0.05% halometasone cream falls into the moderately potent group.

Administration, Topical↗
PubMed1978

Topical use of caffeine with hydrocortisone in the treatment of atopic dermatitis.

In a double-blind study, topically applied caffeine 30%-hydrocortisone 0.5% in hydrophilic ointment was compared to betamethasone valerate 0.1% cream and to hydrocortisone 0.5% in hydrophilic ointment. Eighty-three patients were evaluated over a three-week period for pruritus, erythema, scaling, lichenification, excoriation, oozing, and global impression. The betamethasone and caffeine-hydrocortisone groups performed significantly better than the hydrocortisone group on three of the seven scales: lichenification, excoriation, and global impression. Also, the betamethasone group differed significantly from the hydrocortisone group on six of the seven scales, but did not differ significantly from the caffeine-hydrocortisone group on any scale. It is suggested that caffeine is effective because it elevates local levels of cyclic adenosine-3',5'-monophosphate by inhibiting phosphodiesterase.

Administration, Topical↗
PubMed1978

Desoximetasone--a new topical corticosteroid: short- and long-term experiences.

A new potent topical corticosteroid, desoximetasone, was clinically evaluated in several hundred patients with steroid-responsive dermatoses. Both short-term and long-term comparative studies showed desoximetasone emollient cream (0.25 percent) to be highly effective. Studies comparing betamethasone valerate cream C0. p1 percent) with desoximetasone emollient cream (0.25 percent) showed the new topical steroid to be clinically superior in the relief of moderate and severe inflammatory manifestations of psoriasis and atopic dermatitis. In addition, desoximetasone was found to be safe, well tolerated, and accepted by the patients.

Administration, Topical↗
PubMed1987

Are generic formulations equivalent to trade name topical glucocorticoids?

Trade name glucocorticoid formulations triamcinolone acetonide, fluocinolone acetonide, and betamethasone valerate were compared with their generic equivalents because of increasing substitution of generic formulations for trade name formulations. The vasoconstrictor assay was the method used for these comparisons. Large differences were found between generic and trade name formulations containing the same steroid in the same concentration in both cream and ointment vehicles. If generic substitutions are to be used for trade name formulations, the physician must be aware that significant differences in therapeutic effectiveness may be expected.

Administration, Topical↗
PubMed1985

[Testing the loss of efficacy (tachyphylaxis) during external steroid application].

The steroids fluprednylidene-21-acetate (FA) and betamethasone-17-valerate (BV) were tested in comparison to their inactive bases for loss of activity (tachyphylaxis) after 2 weeks of application. In the croton oil test, both steroids produced equal inhibition of the pustular inflammatory reaction. The vasoconstriction test after 14 days of use revealed a clear decrease in the blanching reaction - which was, however, not statistically significant in the case of BV.

Administration, Topical↗
PubMed1975

Cellular changes in the psoriatic epidermis. X. Microplanimetric studies on epidermal cell size during treatment.

Results of microplanimetric measurements of cells in the pronounced macrocytic psoriatic epidermis during treatment with flubenisolon 17 alpha-valerate are reported. The size of cytoplasm, nucleus and nucleolus has been estimated weekly in biopsies until complete regression. No significant differences in the ratios nucleus/cytoplasm and nucleolus/nucleus could be demonstrated. When the lesions are clinically healed, the epidermal cells are still slightly enlarged.

Adult↗
PubMed1981

[Biochemistry of the evolutive cycle of Triatoma infestans (vinchuca). V. Volatile fatty acids emission].

The composition of the volatile fatty acids emitted by Triatoma infestans of both sexes was studied. They were constituted by a mixture of the acids acetic, propionic, butyric, isobutyric, isovaleric, valeric and traces of isohexanoic and octanoic. Acetic acid was predominant followed by isobutyric and then by propionic acid. The other fatty acids are minor constituents. When acetic acid was discounted, the remaining composition was similar to the volatile fatty acid distribution pattern of Brindley gland. Both sexes showed a similar composition and therefore discard the possibility that they may function as sexual pheromones.

Acetates↗
PubMed1982

Response of the small intestinal mucosa to oral glucocorticoids.

These studies explored the effects of oral pharmacological doses of glucocorticoids on the normal small intestine of the adult rat. Short-term (7 days) prednisolone had little effect on mucosal structure or cell kinetics but enhanced the maximum absorptive capacities of the jejunum and ileum for galactose. This was due to an increase in carrier-mediated transport in the individual enterocytes and not to a change in the cell population. Activities of brush border enzymes were elevated and turnover studies indicated an increased rate of synthesis of brush border proteins associated with an enhanced glycoprotein content of the microvillus membrane. Subcellular fractionation studies demonstrated a large increase in the membrane-bound ribosomal RNA content of the enterocytes consistent with an enhanced synthesis of membrane proteins. These findings implicate a direct action of prednisolone on the enterocytes to increase their absorptive and digestive capacities by the induction of specific functional proteins. These effects on the absorptive and digestive functions of the small intestine were sustained with long-term (28 days) prednisolone feeding. An equivalent long-term oral dose of betamethasone-17-valerate, a locally rather than a systemically active glucocorticoid, had a similar effect on the enterocytes. However, an inhibition of crypt cell turnover resulted in a marked hypoplasia and hence no net change in the functional capacity of the mucosa. These findings emphasise the separate and opposing actions of glucocorticoids on the adult mucosa, on the one hand to stimulate enterocyte function, but on the other to reduce the enterocyte population. The predominant activity appears to be a function of each individual steroid. The predominant stimulatory action of prednisolone was further emphasised by investigating the effects of this glucocorticoid on the adapted ileum following jejunal resection. Indeed, short-term prednisolone enhanced the adaptive hyperplasia in the ideal remnant by increasing the functional capacity of the expanded population of enterocytes.

Adaptation, Physiological↗
PubMed1981

Carcinogen bioassay and mutagenicity studies with the hypolipidemic agent gemfibrozil.

Gemfibrozil, a novel hypolipidemic agent identified chemically as 2,2-dimethyl-5-(2,5-xylyoxy) valeric acid, was evaluated for mutagenic potential in in vitro assays with Salmonella typhimurium. For evaluation of tumorigenic potential, gemfibrozil was administered in the diet (0.30, and 300 mg gemfibrozil/kg) to groups of noninbred CD-1 mice (72/sex) and noninbred CD rats (50/sex) for 78 and 104 weeks, respectively. In the bacterial mutagenesis assays, between 100 and 2,500 microgram gemfibrozil/plate failed to induce a significant increase in revertant bacterial colonies. Neither was a mutagenic response in bacterial assays induced at concentrations up to 300 microgram of five in vivo metabolites of gemifibrozil isolated from rat urine/plate. In mice, gemfibrozil did not significantly increase the frequency or the mean latency period of tumors. In rats, the statistically significant increases in hepatocellular tumors and interstitial cell tumors of the testes were dose related. Adrenal medullary and pancreatic acinar tumors were increased in male rats but were inversely dose related. Under the conditions of this assay, gemfibrozil did not elicit a tumorigenic potential in mice and female rats. In male rats and related to the hepatocellular tumor response, the peroxisome proliferation seen did not occur in humans chronically administered hypolipidemics.

Animals↗
PubMed1981

Short chain fatty acids and potassium uptake in a simple lipid-water partition.

Chemical evidence is presented to demonstrate that short chain fatty acids selectively bind potassium instead of sodium in a simple lipid-water partition. The preference for potassium ions as measured by the K+/Na+ relationship increases from valeric acid (C5) to the higher members of the series, reaching a maximum at pelargonic acid (C9) under physiological conditions (37 C and potassium and sodium concentrations as in normal serum). Anions play a very important role in the selection of K+ ions. When NaHCO3, at the concentration present in normal serum, is added to the aqueous phase, a great increase in the absorption of K+ ions is observed, if compared with the same solution without NaHCO3 and at the same pH. A model is described as a working hypothesis which would explain the behavior of the fatty acids.

Blood↗
PubMed1975

[Comparison between 2 steroid dosage forms in psoriasis and eczema].

This trial was designed to evaluate the clinical effect of a new Topical steroid, the desoximetasone (test name A 41 304 from Hoechst Aktiengesellschaft). A randomized, double-blind, right-left comparative trial has been carried out in 22 patients with atopic dermatitis and on 24 patients with psoriasis. As a comparative drug, a betamethasone 17-valerate preparation, being the strongest on the market, has been used. The new compound showed a better effect on both indications, the difference being significant (p less than 0,005) on psoriasis.

Adolescent↗
PubMedDate not supplied

[Topical treatment of various dermatosis with difluocortolone valerianate. (ointment) Double blind comparative study].

The trial preparation, diflucortolone valerate, was tested clinically in the form of fatty ointment on 27 patients: 4 with psoriasis, 4 with neurodermatitis, 4 with contact dermatitis, 2 with actinodermatitis, 10 with eczema, 2 with cutaneous reticulosis and 1 with radiodermitis. In 89% of the cases the results were good; in 11% were they regular.

Adolescent↗
PubMedDate not supplied

[Investigation of a new product (HK 183 MB) in various dermatoses].

The new trial preparation, diflucortolone valerate, was tested clinically in the form of a cream on 41 patients with weeping dermatitis. 34 cases were treated without a dressing, 5 with a dressing and 2 with an occlusive dressing. A complete cure or a distinct improvement was obtained in 100% of the cases. No undesired side effects developed.

Adrenal Cortex Hormones↗
PubMed1976

[Clinical tests of a new corticoid for topical use: Nerisona].

Diflucortolone valerate 0.1% (Nerisona), a new topical corticoid, was clinically investigated in ointment form in 51 patients suffering from neither weeping nor very dry allergic and inflammatory skin diseases. The results obtained were good, improvement being observed in 92.1% of the treated cases. The cosmetic properties of the preparation were excellent. No local or systemic side effects were observed.

Adolescent↗
PubMed1976

[Evaluation of a new corticoid for various dermatoses].

Diflucortolone valerate 0.1% (investigational number SH K 183 MB) in the form of a cream was clinically investigated in 41 patients with dermatological disorders. All the patients had been treated previously with other topical preparations, but without success. Complete healing or distinct improvement of the objective and subjective symptoms of the disorders was achieved in 100% of the cases treated with the investigational preparation. No side effects were observed at all.

Adolescent↗
PubMed1993

[Determination of drug availability from commercial topical formulations with a multilayer membrane model].

Using the multilayer membrane system (MMS) the drug availability of four drugs from commercial topical formulations are determined. It was found that the availability differs when commercial formulations of beta-methasone-17-valerate, hydrocortisone, diclofenac-Na and clotrimazole were studied. It is shown that the drug availability for characterizing topical formulations has to be taken into account. The MMS applied in this study can be used for the determination of this parameter.

Administration, Topical↗