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[Systemic effect of diflucortolone valerate after dermal application (author's transl)].

The systemic effect of 6alpha,9-difluor-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadiene-3,20-dione (diflucortolone valerate, Nerisona) 0.1% as an ointment and fatty ointment was investigated in two studies. The parameters used were the plasma 11-OHCS values and the urinary 17-OHCS and 17-KS values, respectively. Suppression of the plasma cortisol values was observed after topical application of both diflucortolone valerate and betamethasone-17-valerate to healthy subjects under extreme conditions of whole-body occlusion. However, it was still possible to stimulate the adrenal cortex with ACTH. No reduction of the 17-OHCS of 17-KS values in the 24-h urine was observed during open, large-surface treatment of patients with skin diseases.

17-Hydroxycorticosteroids

Effect of fluocortin butylester and beclomethasone dipropionate on the adrenal gland in beagle dogs.

The effect of butyl-6 alpha-fluoro-11 beta-hydroxy-16 alpha-methyl-3,20-dioxo-1,4-pregnadien-21-oate (fluocortin butylester, Vaspit) administered intratracheally and of beclomethasone dipropionate given intratracheally or orally on the adrenal glands of beagle dogs was investigated. The adrenal function was evaluated using a standardized ACTH stimulation test including eosinophil counts 5 h after a single i.v. injection of 0.02mg (approximately 2 IU) ACTH/kg body weight were found as well as the histological and morphometrical examination of the adrenal cortex. The cortisol determination (with Clark's method) 1.5 h and eosinophil counts to be the optimum indices for the evaluation of adrenal function. Beclomethasone dipropionate given intratracheally at daily dose levels of 0.05; 0.1 and 0.5 mg/kg body weight lead to a dose dependent adrenal suppression on the basis of plasma cortisol concentration, 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 bw. Also the oral administration of 0.1 mg/kg bw./day of beclomethasone dipropionate had a definite adrenal suppressive effect comparable to that of 0.1 mg/kg bw. given intratracheally. However, intratracheal administration of fluocortin butylester even after a 320 times higher dose (2 X 8 mg/kg bw./day) had no suppressive effect on the adrenal gland of the beagle dog.

Adrenal Glands

[Transient myopia with angle closure glaucoma. Case report and biometric findings (author's transl)].

A 36-year-old man suffered from diarrhoea for some weeks and was treated with Salazosulphapyridie and Fluocortulon when he developed a transient myopia combined with an angle closure glaucoma. The refraction of his mild hyperopic eyes (+0,5 dpt) changed to -5,5 dpt and the intraocular pressure increased to 40 mm Hg in the right and 42 mm Hg in the left eye. Accommodation and pupillary reflexes were normal. Ultrasonic examination showed an increased axial diameter and a forward shifting of the lens. The resulting flattening of the anterior chamber induced the angle closure glaucoma. All symptoms disappeared within a week after the administration of Fluocortulon had been discontinued.

Adult

The effect of norgestrel and clogestone on the spontaneous motility of the human fallopian tube.

Spontaneous isometric contractions in vitro of both isthmic and ampullary parts of the human fallopian tube were studied. The tubes were obtained during the early luteal phase of the menstrual cycle from patients undergoing abdominal hysterectomy and who had ingested clogestone acetate or norgestrel, either 1 or 12 hours prior to the experiment. A dose of 150 microgram dl-norgestrel given orally 12 hours preoperatively caused a significant increase in the frequency of spontaneous isometric contractions together with a significant reduction in the area under the curve for each contraction. The possible effect of this altered pattern of motility is discussed.

Fallopian Tubes

[Diflucortolone valerianate (Nerisona) in the treatment of corticoid-sensitive dermatoses in childhood].

The efficacy and tolerance of 0.1% diflucortolone valerate (Nerisona) in cream, ointment and fatty ointment formulations were investigated in a study in which no control preparations were used. The study was conducted in 657 children over a period of three weeks. The results were compared with those of a trial with the same design conducted with 4,878 adults. Our observations were mainly concentrated on the two groups eczema/dermatitis and neurodermatitis (atopic dermatitis). Nearly 90% of the children taking part in the study exhibited these clinical pictures. By far the best therapeutic results were obtained in neurodermatitis. There was only one therapy failure among 198 patients (99.5%). Overall the results obtained in children were markedly better than those recorded for adults.

Administration, Topical

[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

[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

[Clinical comparative study of between difluocortolone and flumethasone].

We report the results of a controlled double blind assay of treatment in 51 dermatologic cases, with a new steroid cream (diflucortolone) and an already known one (flumetasone). The diflucortolone valerate was significantly better than the flumetasone pivalate in the treatment of 16 cases of psoriasis, 33 eczemas and two cases of lichên planus.

Clinical Trials as Topic