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At least 19 recordsLinked to original sources
PubMed1977

Allergic contact dermatitis from fluocortolone, flucocortolone pivalate and fluocortolone caproate.

Two patients with contact allergy to Ultralan preparations are reported. Each Ultralan preparation contains two of three related fluocortolone derivatives. The first patient reacted to all three derivatives. The second patient reacted to flucortolone and when retested 4 months later also to fluocortolone pivalate but ot to flucortolone caproate. The negative reaction to fluocortolone pivalate at the first examination was probably false negative due to a low test concentration. In order to avoid false negative patch test reactions the fluorinated steroids should possibly be applied in concentrations higher than 1%. No cross sensitivity to the other steroids for topical use was found.

Aged↗
PubMed1976

[Multicentre-clinical trial of the novel corticosteroid diflucortolone valerate in the forms of cream, ointment and fatty ointment. Part I: Comparative study of diflucortolone valerate with fluocortolone, -capronate, -pivalate in a double-blind contralateral design with topical application (author's transl)].

6alpha,9-Difluor-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadiene-3,20-dione (diflucortolone valerate, Nerisona) 0.1% as a cream, ointment and fatty ointment was investigated in a double-blind contralateral design in 925 patients in comparison to fluocortolone (Ultralan), fluocortolone caproate and fluocortolone pivalate in three concurrently performed studies. The results of the contralateral study show Nerisona cream and ointment to be more effective (P less than 0.01) than Ultralan. The fatty ointment was also superior, but the difference was statistically significant (P less than 0.05) only in the indication psoriasis. No differences could be established in the less sensitive absolute assessment. The therapeutic success rate of 76-92% according to strict criteria-only complete healing and distinct improvement were counted as a success-clearly demonstrates the efficacy of the preparations. The local side effects recorded-mainly irritation and burning- were of a mild nature.

Administration, Topical↗
PubMed1977

The influence of fluocortolone treatment on the collagen content in guinea pig skin.

Specific pathogen free guinea pigs were treated with varying dosis of fluocortolone for 15 days. The treated animals showed the same per cent weight gain as the controls. The total hydroxyproline content of the skin and the hydroxyproline content in different collagen fractions was the same in treated and untreated animals. Thus fluocortolone seems to have no specific effect on the synthesis or the breakdown of collagen in the guinea pig skin. Also the physical development of the animals, kept under defined conditions, failed to show a catabolic effect of of fluorcortolone.

Animals↗
PubMed1977

[Clinical trial of fluocortin butylester in a double-blind contralateral comparison versus fluocortolone and hydrocortisone acetate (author's transl)].

Butyl 6alpha-fluoro-11beta-hydroxy-3,20-dioxo-16alpha-methyl-1,4-pregnadien-21-oate (fluocortin butylester, Vaspit) is a recently developed corticosteroid, its distinguishing properties being that it is non-embryotoxic and has practially no systemic effects. In the course of 6 multicentre studies fluocortin butylester was tested in the forms of cream, ointment and fatty ointment in a comparison with corresponding formulations containing fluocortolone (Ultralan) caproate or pivalate, or hydrocortisone acetate. The total study population comprised 1705 patients with various dermal disorders. The results of these double-blind contralateral studies permit the conclusion that the efficacy of the Vaspit preparations ranges between those of fluocortolone and hydrocortisone acetate. Considering the risks involved with local corticosteroid therapy in children the development of a local corticosteroid with the properties of fluocortin butylester must be acknowledged as an advance.

Administration, Topical↗
PubMed1976

In vitro studies on enzymatic cleavage of steroid esters in the female organism.

The decreasing water-solubility of steroid esters concomitant with increasing chain lenth of monocarboxylic acids provides a prolonged therapeutic effect of the steroid. Whether a slow release of the steroid from an oily depot in the muscle or a secondary storage of the enter in the body fat ("deep compartment") are responsible for this prolonged action, is open to discussion. The aim of this study was to investigate the steriod ester cleaving enzyme activity of human subcutaneous fatty tissue. The followeing steroid esters were investigated: Testosterone acetate and oenanthate, metenolone acetate and oenanthate, norethisterone acetate and oenanthate, dehydroepiandrosterone acetate and oenanthate, fluocortolone acetate and caproate. In the 10000 X g supernatant phase of the female subcutaneous fatty tissue the rate of enzymatic cleavage of the long-chain oenanthates was considerably greater than that of the corresponding short-chain steroid esters. The nature and position of the ester group in the steroid molecule exhibited a marked effect on the rate of enzymatic cleavage of steroid esters. The cleavage rate of long- and short-chain steroid esters in human myometrium and endometrium resembled that in the fatty tissue. On the other hand, the gastric mucosa, recuts musculature, placenta and vaginal mucosa split the short-chain steroid esters more rapidly than the long-chain esters. The marked differences in the relation of the cleavage rate of long- and short-chain steoid esters in the various tissues allow the assumption that long- and short-chain steroid esters are cleaved by different enzymes.

Adipose Tissue↗
PubMed1976

[Studies on the Pharmacology of 6alpha,9-difluoro-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadiene-3,20-dione (diflucortolon valerate) (author's transl)].

The topical and systemic anti-inflammatory action of 6alpha,9-difluoro-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadiene-3,20-dione (diflucortolone valerate, Nerisona) was studied in the rat in comparison with fluocortolone, diflucortolone and some other corticoids. In addition the effect of the compounds studied on the following parameters of corticoid activity was examined in the rat: body weight and weights of thymus, spleen and adrenals; blood sugar concentration and liver glycogen content; diuresis and Na+ and K+ elimination with the urine; the binding of diflucortolone and some diflucortolone-21-esters to the cytoplasmic corticoid receptor of the rat's thymus was also determined. In all tests diflucortolone was shown to be a corticoid with very potent topical and systemic action. Diflucortolone valerate showed the same potent anti-inflammatory action on topical application as the unesterified compound. After subcutaneous administration, however, the systemic corticoid action of the valerate was considerably inferior to that of diflucortolone on account of the kinetics of the more lipid soluble ester.

Adrenal Glands↗
PubMed1977

[Experimental studies in animals on the influence of fluocortin butylester on the course of generalized infections (author's transl)].

The influence of butyl 6alpha-fluoro-11beta-hydroxy-16alpha-methyl-3,20-dioxo-1,4-pregnadien-21-oate (fluocortin butylester, Vaspit), a new corticosteroidal compound with a marked dissociation between local antiinflammatory and systemic action, upon resistance against infections was studied in experimental bacterial and fungal infections in mice. The results of the experiments showed, that fluocortin butylester, even after repeated s.c. or oral administration of dosages up to 100 mg/kg did not depress the resistance of the animals against microbial infections. The relevance of the animal models was checked by parallel experiments with fluocortolone, hydrocortisone, prednisolone and cyclophosphamide.

Animals↗
PubMed1979

Effect of intratracheal and oral application of corticosteroids on the adrenal function test in beagle dogs after ACTH-stimulation.

The effect of synthetic corticosteroids given intratracheally or orally on the adrenal glands of beagle dogs was investigated. The adrenal function was evaluated using a standardized ACTH stimulation test. In addition, histological and morphometrical examinations of the adrenal cortex were performed at the end of the study. Beclomethasone dipropionate given intratracheally at daily dose levels of 0.05, 0.1 and 0.5 mg/kg body weight led to a dose dependent adrenal suppression on the basis of plasma cortisol concentration and eosinophil counts after ACTH stimulation and size of zona fasciculata and reticularis. A complete adrenal suppression was observed at the highest dose level of 0.5 mg/kg body weight. Also the oral administration of 0.1 mg/kg body weight/day of beclomethasone dipropionate had a definite adrenal suppressive effect comparaable to that of 0.1 mg/kg body weight given intratracheally. However, intratracheal administration of fluocortin butylester, a local antiinflammatory drug but systemically a nearly ineffective corticosteroid (2 X 8 mg/kg body weight/day) had no suppressive effect on the adrenal gland of the beagle dog, even after a 320 times higher dose.

Administration, Oral↗
PubMed1978

The effect of short-and long-term corticosteroid treatment on sleep-associated growth hormone secretion.

Eight healthy medical studients and four renal transplant patients had blood sampled two or three times hourly throughout EEG monitored nocturnal sleep. This was carried out on the healthy subjects for a total of 12 nights without medication (control nights asleep), a total of 12 nights following 40 mg of flucortolone the previous morning, and a total of 6 nights with similar blood sampling when sleep was prevented (control nights awake). Four renal transplant patients who were receiving long-term therapy with prednisolone were similarly studied (total of 7 nights asleep). Circulating corticosteroid and growth hormone (GH) levels were determined. A peak of GH was seen during the first 2 h of sleep on the control nights when slow-wave sleep predominated. The GH peak was absent on the control nights awake. The pattern of plasma corticosteroid levels was identical during control nights asleep and awake. Both single-dose and chronic corticosteroid administration inhibited the GH peak associated with slow-wave sleep. Chronic corticosteroid therapy, but no single-dose administration in the morning, suppressed the circadian rise of plasma corticosteroids which normally occurs late in sleep.

Adult↗
PubMed1978

Comparative blanching activities of proprietary diflucortolone valerate topical preparations.

The blanching activities and hence bioavailabilities of the cream, ointment and fatty ointment preparations of Nerisone and Temetex (diflucortolone valerate 0.1%) were evaluated using an occluded and unoccluded blanching assay. These products were compared to Synalar ointment and cream (fluocinolone acetonide 0.025%), established topical corticosteroid preparations. Statistical analysis showed no significant differences between similar formulations of diflucortolone valerate. Significant differences were noted between diflucortolone valerate and fluocinolone acetonide preparations.

Administration, Topical↗
PubMed1977

Temetex in the treatment of steroid-responsive dermatoses.

Five hundred and seventy-five patients with various steroid-responsive dermatoses were studied for up to six weeks in eighty-eight separate general practices using a new topical corticosteroid. Temetex (diflucortolone valerate 0-1%). It was concluded that Temetex is both effective and well tolerated in a wide variety of conditions, especially eczema and psoriasis. It was also shown that a large-scale general practice trial can be carried out efficiently with a very high compliance rate.

Administration, Topical↗
PubMed1977

[Clinico-pharmacological studies on the acne-inducing action of fluocortin butylester (author's transl)].

The acne-inducing effect of butyl 6alpha-fluoro-11beta-hydroxy-16alpha-methyl-3,20-dioxo-1,4-pregnadien-21-oate (fluocortin butylester, Vaspit) 0.75% was compared with that of hydrocortisone acetate 1.0% and diflucortolone valerate 0.1% in a model established by Plewig and Kligman. The steroid and the cream base uniformly used in all preparations were applied to the backs of 20 volunteers over 4 weeks. Dome-shaped red papules developed in the third week of occlusive treatment, and were counted in an area of 16 cm2 at the maximum of their development and graded according to a scale. The degree of papulation under diflucortolone valerate 0.1% was 2.15+/-0.75. No differences were observed between fluocortin butylester 0.75% (0.2+/-0.42), hydrocortisone acetate and the cream base (0.15+/-0.37).

Acne Vulgaris↗
PubMed1978

[Comparative studies on Bi-Nerisona cream (diflucortolone valerinate + chlorquinaldol) and on a combination preparation (betamethasone valerinate + gentamicin + tolnaftate + clioquinol) in a double-blind trial].

Bi-Nerisone cream and a control preparation, also in the form of a cream, have been clinically tested on 343 patients by means of a double blind study. Equilvalent results were obtained without registering any significant statistical differences, a finding, however, proving to be of great importance as Bi-Nerisone only contains two active substances (Diflucortolone valerat + Chlorquinaldol), whereas the control preparation contains a total of four (Betamethasone valerate + Gentamycin + Tolnaftate + Clioquinol).

Betamethasone Valerate↗