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At least 19 recordsLinked to original sources
PubMed1976

Onset of the vasoconstrictor effect of diflucortolone valerate, betamethasone valerate, and fluocinolone acetonide ointments applied for varying periods under occlusive dressings.

Evaluation of cutaneous vasoconstriction after applications of varying duration of topical corticoids on the flexor surfaces of the forearms of 20 patients with intact skin shows a significantly faster blanching effect with diflucortolone valerate ointment than with fluocinolone acetonide and betamethasone valerate ointments. Furthermore, the test shows that even for a highly active preparation, such as the diflucortolone valerate ointment, an application time of less than 3 h only exceptionally leads to vasoconstriction in the healthy skin.

Administration, Topical↗
PubMed1976

[Comparative studies in man on the percutaneous absorption of diflucortolone valerate, betamethasone-17-valerate, beclomethasone dipropionate and fluocinolone acetonide].

Percutaneous absorption of 6alpha,9-difluor-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadience-3,20-dione (diflucortolone valerate, DFV, Nerisona), betamethasone 17-valerate (BV), beclomethasone dipropionate (BDP) and fluocinolone acetonide (FA) by damaged skin was examined on the backs of 4 healthy males from whom the stratum corneum had been removed by "stripping". The determination of percutaneous absorption was performed on the one hand by a method employing radioactive labelled compounds (DFV, BV) and measuring the elimination with the urine and faeces and on the other hand by photometric determination (DFV, BV, BD, fa) of the corticoid remaining on the skin immediately following application and at the end of a 24-h period of exposure. Direct measurement of the radioactivity in the urine and faeces revealed that percutaneous absorption from a new W/O emulsion takes place up to 2.2+/-0.8% in the case of DFV (0.1%) and to at least 12.2+/-3.3% in the case of BV (0.12%) within 24 h. The determination of percutaneous absorption via recovery from the skin produced the following results for the 4 corticoid preparations examined: DFV (14.8+/-4.2%) and BDP (14.0+/-4.3%) approximately equal, BV (23.5+/-4.1%) a marked increase and FA (39.2+/-2.4%) the highest level of absorption. This order for percutaneous absorption appears to correlate to the frequency of systemic side effects.

Administration, Topical↗
PubMed1992

Resistance to N-benzyladriamycin-14-valerate in mouse J774.2 cells: P-glycoprotein expression without reduced N-benzyladriamycin-14-valerate accumulation.

N-Benzyladriamycin-14-valerate (AD 198) is a highly lipophilic analogue of Adriamycin with novel cytotoxic mechanisms, greater in vivo antitumor activity, and the ability to circumvent multidrug resistance due to P-glycoprotein-mediated drug efflux or decreased topoisomerase II activity. To identify the mechanism(s) which may confer AD 198 resistance, J774.2 mouse macrophage-like cells were selected for growth in cytotoxic levels of AD 198 (AD 198R). AD 198R cells exhibited over-expression of the mdr1b (P-glycoprotein) gene, cross-resistance to Adriamycin and vinblastine, and potentiation of drug cytotoxicity by verapamil. However, net intracellular accumulation of AD 198 in AD 198R cells was unchanged compared to parental cells, while Adriamycin and vinblastine accumulations were reduced 40% and 95%, respectively. AD 198 was localized in the perinuclear region of the cytoplasm in both parental and AD 198R cells, with additional vesicular compartmentalization in AD 198R cells. Verapamil-induced reversal of AD 198 resistance coincided with some drug redistribution from cytoplasmic vesicles, but without redistribution of AD 198 into the nucleus. These results suggest that AD 198 resistance was not conferred through a P-glycoprotein-mediated reduction in intracellular drug accumulation but through other cytoplasmic mechanisms, including, but not limited to, drug compartmentalization.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
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↗
PubMed2025

Versatile sugar and valerate metabolic pathways in Paraburkholderia xenovorans LB400 enable tailored poly(3-hydroxybutyrate-co-3-hydroxyvalerate) production.

Poly(3-hydroxybutyrate) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) polymers are accumulated by diverse prokaryotes. Their distinct monomer compositions enable their use as tailored bioplastics. The aims were to characterize the poly(3-hydroxybutyrate) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) synthesis by Paraburkholderia xenovorans LB400 using different sugars and valerate, and to gain genome-oriented insights into polyhydroxyalkanoate production. d-Glucose, d-mannitol, d-gluconate, and d-xylose were evaluated as sole carbon sources or supplemented with valerate. Polyhydroxyalkanoates synthesized by strain LB400 were characterized through GC-MS, GC-FID, FTIR, and 1H and 13C-NMR. P. xenovorans LB400 reached 1.00-1.39 g L-1 of dry cell weight (DCW) with a P(3HB) content of 21-43% w w-1 when grown on different sugars. The addition of valerate to the sugar-grown LB400 cultures yielded a DCW of 1.79 to 2.29 g L-1 and a P(3HB-co-3HV) content of 50.0‒51.2% w w-1, with varying 3HV compositions (28‒43 mol%). The highest 3HV incorporation was observed with d-xylose and valerate. Genomic analyses of strain LB400 revealed key elements of sugar metabolism influencing growth, polymer accumulation, and monomer composition. LB400 genome encodes the PhaJ-like R-specific hydratase and FadJ epimerase, which are potentially useful for modulating copolymer composition. PHA production under bioreactor conditions was evaluated. In a bioreactor fed with d-glucose, LB400 achieved a P(3HB) concentration of 2.2 g L-1. These findings highlight the metabolic versatility of P. xenovorans LB400 in utilizing diverse sugars to produce either P(3HB) or tailor-made P(3HB-co-3HV), supporting the development of bioplastics for specific applications. KEY POINTS: • Strain LB400 produced P(3HB-co-3HV) from various sugars and valerate. • Sugar type drives LB400 PHA copolymer synthesis and composition. • Strain LB400 PHA production was scaled up to a bioreactor.

Polyesters↗
PubMed1978

Topical betamethasone 17-valerate is an anticorticosteroid in the rat. 2. Anti-inflammatory and anti-lymphocyte activities.

In the oxazolone-induced delayed hypersensitivity inflammation in the rat ear, betamethasone 17-valerate, in contrast to other topical corticosteroids, is incapable of suppressing oedema. When given in combination with triamcinolone acetonide, betamethasone 17-valerate competitively antagonizes the anti-inflammatory action of the active steroid. When tested in the mouse, betamethasone 17-valerate behaved as an anti-inflammatory agent 15 and 80 times as potent as betamethasone and hydrocortisone respectively. In an in vivo lymphocyte culture system in which preincubation with corticosteroids prevents subsequent phytohaemagglutinin induced DNA synthesis, betamethasone 17-valerate was less active than even hydrocortisone when rat lymph node cells were used, but with human cell preparations it was more potent than either hydrocortisone or betamethasone. Betamethasone 17-valerate behaves uniquely in the rat as an anticorticosteroid; in mouse and in man the compound behaves as a normal corticosteroid.

Administration, Topical↗
PubMed1977

Changes in serum lipids during treatment with norgestrel, oestradiol-valerate and cycloprogynon.

The serum concentrations of triglycerides, cholesterol, and free glycerol were determined in 23 climacteric women, before and after the administration of three different steroid drugs. Each drug was given within a period of 12 weeks (3 cycles). Period I: Norgestrel, 0.5 mg daily from the 12th to 21st day of each cycle. Period II: Oestradiol-valerate (Progynon) 2 mg daily from the 2nd to 21st day of each cycle. Period III: Oestradiol-valerate 2 mg from the 1st to 11th day followed by oestradiol-valerate 2 mg+0.5 mg dl-norgestresl from day 12 to 21 of each cycle (Cycloprogynon). A significant decrease in triglycerides was observed following the administration of norgestrel and Cycloprogynon, whereas oestradiol-valerate had no effect on the triglyceride levels. On the other hand, oestradiol-valerate, following a period of norgestrel, produced an increase in serum cholesterol levels.

Adult↗
PubMed1975

Betamethasone valerate in the treatment of summer hay fever.

Betamethasone valerate nasal aerosol in a daily dose of 400 micrograms was compared with a placebo in a double-blind trial involving 103 patients with summer hay fever. The patients' and physicians' preference for the active compound was statistically significant (P less than 0.001), with 88% of the patients receiving betamethasone valerate obtaining substantial relief of symptoms. The analysis of patients' daily symptom scores showed that nasal symptoms were significantly reduced by the active aerosol (P less than 0.001). A day-by-day comparison of nasal symptom scores with pollen counts indicated a decreasing allergic response as the season progressed; possible reasons for this are discussed. No clinically significant side effects were observed. Short tetracosactrin tests from ten randomly chosen patients on betamethasone valerate showed no abnormality and nasal swabs for Candida culture from a further thirty-two patients were negative. It is concluded that intranasal betamethasone valerate is an effective and safe form of therapy for seasonal rhinitis.

Administration, Intranasal↗
PubMed1977

Topical halcinonide and betamethasone valerate effects on plasma cortisol: acute and subacute usage studies.

The effect of topical application of halcinonide cream and betamethasone valerate cream on plasma cortisol was studied in an acute usage study as well as a subacute study, which more closely approximated common clinical usage. In the acute study, halcinonide cream caused a marked decrease in plasma cortisol, both with and without occlusion, in patients with extensive psoriasis, but only with occlusion in normal subjects. Betamethasone valerate cream decreased plasma cortisol levels in patients with extensive psoriasis when applied with occlusion and, to a lesser extent, without occlusion. In a double-blind subacute usage study without occlusion, two of 23 patients treated with halcinonide cream showed decreased plasma cortisol levels during the treatment period, while none of the 21 patients treated with betamethasone valerate cream showed such decreases. Three patients in the halcinonide group developed striae. Clinical response to halcinonide was superior to that with betamethasone valerate cream, but a similar number of patients were resistant to treatment with each medication.

Administration, Topical↗
PubMed1978

Serum oestrone, oestradiol and oestriol concentrations during oral oestradiol valerate and oestriol succinate therapy in ovariectomized women.

Serum oestrone, oestradiol and oestriol concentrations were investigated during oral treatment with oestradiol valerate and oestriol succinate in ovariectomized women. The dosages used were 1 mg oestradiol valerate in the morning and 2 mg oestriol succinate in the evening of the first day and 2 mg oestradiol valerate in the morning of the second day of treatment. The other group of patients received the same therapy in reverse order. The variation in the serum oestrone and oestradiol concentrations with a daily dose of 1 or 2 mg of oestradiol valerate were considerable. 2 mg oestriol succinate caused a fairly small elevation of serum oestriol concentration. In both treatment groups the quotient E3/(E2 + E1) was similar to that found at the 6-7th day and in the middle of the normal menstrual cycle, the quotient E1/(E2 + E3) was somewhat higher than during normal cycle.

Castration↗
PubMed1992

Epidermal cytokeratin and immunocyte responses during treatment of psoriasis with calcipotriol and betamethasone valerate.

Changes in epidermal immunocytes and cytokeratins were investigated during treatment of psoriasis with calcipotriol and betamethasone valerate. Skin biopsies were obtained from 10 subjects on each treatment from lesional and non-lesional skin at baseline, and from treated lesions after 4 weeks. In each subject, changes in expression of cytokeratins K5, K10 and K16, and changes in epidermal immunocyte counts were assessed. Responses were compared with a separate histological parameter of improvement, epidermal thickness. Both treatments produced a marked normalization of cytokeratins. The reduction of K16 expression was similar on each treatment and correlated significantly with reduction in epidermal thickness. Expression of both K5 and K10 improved less than thickness with betamethasone valerate but more than thickness with calcipotriol, although these differences did not reach statistical significance. With calcipotriol there was an increase in K5 and K10 responses with increasing response of epidermal thickness, which was not seen with betamethasone valerate. T6+ cells, HLA-DR+ dendritic cells and T lymphocytes were all reduced by betamethasone valerate. There was a remarkable similarity in the level of normalization between cell types and also between cellular response and reduction in thickness. Calcipotriol produced a similar consistent reduction in cell numbers and in thickness, with the exception of T6+ cells which increased in some subjects during treatment. Only in subjects in whom thickness had virtually returned to normal was there a marked decrease in T6+ cells.

Adult↗
PubMed1975

Effect of placebo substitution during long-term betamethasone valerate aerosol treatment in asthmatic children.

Ten children with severe asthma, who had been well controlled on maintenance betamethasone valerate aerosol for an average of 11 months, were given placebo aerosols without their knowledge. The period of placebo substitution was campared with one 28-day period of betamethasone valerate therapy beforehand, and two 28-day periods afterwards. Symptoms were increased during the placebo period, and patients did not return to their previous well-controlled state until the second month after reinstitution of therapy. Changes in the means of twice-daily peak expiratory flow readings (PEFR) followed the same pattern as changes in symptoms. The exacerbation of asthma which occurred during placebo treatment was accompanied by a widening in the diurnal variation between morning and evening PEFR. In comparison with the previous period, morning PEFR fell by a greater amount than evening PEFR. Standardized running tests suggest an increase in exercise-induced bronchoconstriction and in the Exercise Lability Index when the child was receiving only placebo treatment as compared with betamethasone valerate treatment. The trial provided further evidence of the efficacy of betamethasone valerate aerosol in the prophylatic therapy of severe childhood asthma. As 2 of these children were able to discontinue long-term therapy it is unlikely that this drug causes dependency.

Aerosols↗
PubMed1992

Is 1 mg of estradiol valerate or 0.625 mg of conjugated estrogens sufficient for all women to prevent menopausal bone loss?

Bone mineral content was measured by dual photon absorptiometry in 35 women who needed estrogen replacement therapy but did not want the addition of progestogens because they did not want regular bleeding. A total of 23 women were treated with estradiol valerate 1 mg per day over a mean period of 3.7 years; 12 women received conjugated estrogens 0.625 mg per day over a mean period of 5.3 years. The mean values of bone mineral content in both groups did not change. In the women on estradiol valerate, 61% had a decrease, and in those on conjugated estrogens, 67% had a decrease in bone mineral content. However, the calculated decrease per year was within the limits of the intraindividual reproducibility of the measurements. A difference between two measurements with a decrease of > 1.0 g hydroxyapatite/year over a period of > 3 years is larger than the limits of the intraindividual reproducibility. A decrease in bone mineral content > 1.0 g hydroxyapatite/year over a mean period of 3.98 years, SD 0.35, was observed in six of 23 (26%) of the women on estradiol valerate with a mean decrease of 5.28 g hydroxyapatite, SD 0.97. Only one of 12 (8%) of the women on conjugated estrogens had a decrease of 6.1 g hydroxyapatite over a period of 5.2 years. Periodic measurement of bone mineral is recommended in women on estrogen replacement therapy with estradiol valerate 1 mg per day or conjugated estrogens 0.625 mg per day for prevention of postmenopausal bone loss.

Adult↗
PubMed1975

Induction of abortion in cattle with prostaglandin F2alpha and oestradiol valerate.

Twenty, 2 to 5 months pregnant heifers were injected with 25 mg. and 12.5 mg. Prostaglandin F2alpha on two consecutive days or with a single dose of 20 mg. of a long acting oestrogen (oestradiol valerate). Abortion occurred at an average interval of 3,6 days in the 10 PG F2alpha treated animals and after 10,8 days in 8 out of 10 oestradiol valerate treated heifers. The foetuses of the PG F2alpha treated heifers were in a fresh state while the oestradiol foetuses were already degenerating at the time of abortion. A rather severe vaginal discharge after abortion was more often observed in oestradiol valerate induced abortion. Development of the mammary glands and prolonged oestrus periods also was more pronounced in these animals. In both treatments the concentration of progestins in peripheral blood dropped to less than 1 ng/ml at the time of abortion. The decline was very rapid after administration of PG F2alpha and rather slow after oestradiol valerate. Based on its rapid luteolytic effect and rapid elimination after administration which prevents interferring with the endocrine system for a prolonged time, PG F2alpha is preferred as an abortifacient during the first 4 to 5 months of pregnancy in cattle.

Abortion, Induced↗
PubMed1977

Betamethasone valerate ointment compared with fluocinonide FAPG.

Betamethasone 0.1% as valerate in an ointment base and fluocinonide 0.05% in a fatty alcohol propylene glycol (FAPG) base have been compared in a double-blind trial of 76 patients with either eczema or psoriasis. The results show betamethasone valerate ointment to be significantly (P less than.05) superior to fluocinonide FAPG in the treatment of both these skin conditions. In the light of publications from other studies on betamethasone valerate cream this trial indicates that the ointment base considerably increases the efficacy of betamethasone valerate.

Betamethasone↗
PubMed1992

Relationship between in vivo skin blanching and in vitro release rate for betamethasone valerate creams.

Betamethasone valerate creams from two firms were evaluated using the skin blanching procedure. In both studies, the same cream formulation exhibited significantly higher blanching compared to the other product. An in vitro release rate was determined for these betamethasone valerate cream products using a diffusion cell system, with a cellulose acetate membrane and a 60% ethanol:water receptor medium. The release rate (flux) of betamethasone valerate was higher for the higher blanching formulation and was statistically different from the other product. The integrity of the cellulose acetate membrane in 60% ethanol:water mixture was ascertained using hydrocortisone cream product. The in vitro drug release method, using a diffusion cell system and a synthetic membrane, can serve as a good quality control test method for topical creams.

Betamethasone Valerate↗
PubMed1992

0.25% prednicarbate cream and the corresponding vehicle induce less skin atrophy than 0.1% betamethasone-17-valerate cream and 0.05% clobetasol-17-propionate cream.

The atrophogenic potential of medium-potent topical glucocorticoids is still controversial. In a double-blind controlled trial 24 healthy volunteers either applied 0.25% prednicarbate cream or the corresponding vehicle to one and 0.1% betamethasone-17-valerate cream or 0.05% clobetasol-17-propionate cream to the other forearm twice daily. Skin thickness was regularly assessed during the six week period of application and for further three weeks thereafter, using both the B- and A-mode of a 20 MHz ultrasound scanner. Both betamethasone-17-valerate and clobetasol-17-propionate cream significantly reduced skin thickness as compared to cream base while prednicarbate cream did not. Given that 0.1% betamethasone-17-valerate- and 0.25% prednicarbate cream are reported to be about equipotent in the treatment of atopic eczema the latter preparation shows an increased ratio between its desired anti-inflammatory and its unwanted atrophogenic effect.

Adult↗
PubMed1975

Betamethasone valerate in corticosteroid-dependent asthmatics. The integrity of the hypothalamic pituitary adrenal axis.

In a single-blind trial 29 patients with corticosteroid-dependent asthma reduced their daily dose of oral prednisolone by 1 mg/week while using a placebo inhaler until an unacceptable degree of asthma occurred. Betamethasone-17-vlaerate in a dose of 800 mug/day and if necessary 1600 mug/day was then substituted for the placebo inhaler and the reduction of oral prednisolone continued until the prednisolone was withdrawn completely or an unacceptable degree of asthma recurred. In 22 patients (76%) prednisolone was withdrawn completely, 11 on 800 mug and 11 on 1600 mug betamethasone-17-valerate. The mean reduction of prednisolone was 3-8 mg on placebo, 5-4 mg on 800 mug and a further 1-8 mg in patients requiring 1600 mug of betamethasone-17-valerate. The hypothalamic pituitary adrenal (HPA) axis was assessed by tetracosactrin and insulin stress tests at the start of the study and after withdrawal of oral prednisolone. The results indicate that an HPA axis which is completely suppressed by systemic corticosteroids can regain normal integrity when the systemic steroid is replaced by betamethasone-17-valerate in a dose of either 800 mug/day or 1600 mug/day. Candidiasis was observed, but will be reported later.

Adrenal Glands↗