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At least 73 records · Page 4Linked to original sources
PubMed1986

Effects of valerate and isobutyrate on fatty acid secretion by the isolated perfused mammary gland of the lactating goat.

The isolated mammary glands of six lactating goats were perfused with heparinized and oxygenated blood for 8 to 11 h. Adequate quantities of glucose, acetate and amino acids (including valine) were added to the perfusate. Either unlabelled valerate or unlabelled isobutyrate was added in excess to the perfusate of one gland, while the respective symmetrical gland was used as a control. After the administration of valerate, the proportions of the odd-numbered fatty acids (C11:0, C13:0, C15:0) in the milk fat, collected every hour during perfusion, rose progressively after 5 h until the end. The synthesis of milk fatty acids from valerate is discussed. After isobutyrate was added to the perfusate, isoC12:O, isoC14:0 and isoC16:0 in the milk fat increased as compared to the control. The effect of isobutyrate indicated that valine acted as a precursor of milk iso-branched fatty acids after its metabolisation to isobutyryl-CoA. During perfusion in the presence of the complete substrate mixture, the proportion of certain major milk fatty acids (C10:0, C12:0, C14:0 and C16:0) increased, whereas the proportion of C18:0 and C18:1 decreased. These effects have been ascribed to the presence of acetate and beta-hydroxybutyrate in the substrate mixture.

Animals↗
PubMed1978

Topical betamethasone 17-valerate is an anticorticosteroid in the rat. 1. Dermal atrophy.

In the albino rat, topical betamethasone 17-valerate acts as an anticorticosteroid. This steroid is inactive in a dermal atrophy assay over a dose range where betamethasone and hydrocortisone display atrophogenic activity. At appropriate concentrations betamethasone 17-valerate competitively inhibits the atrophogenic effects of both betamethasone and triamcinolone acetonide. Since betamethasone and betamethasone 17-valerate penetrate rat skin in vivo at essentially the same rate, it is concluded that the latter compound is relatively resistant to hydrolysis during penetration, and that it binds to rat corticosteroid receptor proteins in such a manner as to prevent expression of corticosteroid activity. Therefore, the rat cannot be used as a model species to predict activity in man for this compound.

Administration, Topical↗
PubMed1975

Intranasal betamethasone valerate in the treatment of seasonal rhinitis.

Betamethasone valerate aerosol given in doses of 100 mug into each nostril twice daily was compared with a placebo in a double-blind, cross-over trial involving thirty patients with seasonal rhinitis. Patients recorded symptoms of eye irritation and watering, sneezing, rhinorrhoea, and nasal blockage, on a diary card. Analysis of the symptom scores showed that nasal symptoms were significantly better on betamethasone valerate than on placebo (P less than 0.01) and that nasal blockage in particular was improved (P less than 0.001). The patients' preference was significantly in favour of the active compound (p less than 0.02) and no side-effects were noted. It is concluded that betamethasone valerate offers a safe and effective form of treatment for seasonal rhinitis.

Administration, Intranasal↗
PubMed1975

A comparison of intranasal betamethasone valerate and sodium cromoglycate in seasonal allergic rhinitis.

A double-blind comparison of betamethasone valerate and sodium cromoglycate both given by the nasal route was carried out in forty patients with seasonal rhinitis caused by grass pollen. All patients kept daily symptom score cards, and half of them measured both oral and nasal peak expiratory flow rates twice daily. Adrenal function was monitored in thirty-one patients and found to be normal throughout. Sixteen of those patients receiving the steroid aerosol recorded success and two failure of treatment. By contrast, of those receiving sodium cromoglycate there were only two treatment successes and twelve failures. The total symptom score recorded in the group receiving betamethasone valerate was about half that recorded by the sodium cromoglycate group (P less than 0.01). No difference was observed between the two treatments in respect of nasal peak flow rate; specific IgE blood levels and weal sizes following prick tests were not significantly altered throughout the period of the trial, although total IgE was significantly increased. These results suggest that nasal betamethasone valerate offers patients with allergic rhinitis marked symptomatic benefit without the disadvantages previously associated with steroids.

Administration, Intranasal↗
PubMed1979

The stability of betamethasone-17-valerate in semi-solid bases.

The stability of betamethasone-17-valerate in semi-solid bases has been investigated. Emphasis has been placed on the stability problems which could arise upon dilution of proprietary preparations by the use of model systems. Betamethasone-17-valerate has been shown to decompose to betamethasone-21-valerate and betamethasone alcohol. Quantitation of the decomposition was by direct densitometry on thin layer chromatographic plates. The decomposition was found to be an apparent first order process and to depend on the diluent used and its concentration. Attempts were also made to relate the rate of decomposition to the pH of the base used, and to stabilize the products.

Betamethasone↗
PubMed1963

Incorporation of isobutyrate and valerate into cellular plasmalogen by Bacteroides succinogenes.

Wegner, G. H. (University of Wisconsin, Madison) and E. M. Foster. Incorporation of isobutyrate and valerate into cellular plasmalogen by Bacteroides succinogenes. J. Bacteriol. 85:53-61. 1963.-Bacteroides succinogenes was found to require both a branched-chain volatile fatty acid (e.g., isobutyric) and a straight-chain acid (e.g., valeric) for growth. The organism used the acids as precursors for the synthesis of long-chain fatty acids and fatty aldehydes, which in turn were employed in the synthesis of phospholipid, mainly ethanolamine plasmalogen. Isobutyric acid was incorporated primarily into branched-chain C(14) and C(16) acids (tentatively identified as 12-methyl tridecanoic and 14-methyl pentadecanoic acids, respectively), and into fatty aldehydes. Valeric acid was used mainly for the synthesis of n-C(13) and n-C(15) fatty acids and fatty aldehydes. Apparently the two short-chain fatty acids were built up by the addition of two-carbon units to form the long-chain acids and aldehydes of the plasmalogen.

Aldehydes↗
PubMed1981

Release of betamethasone 17-valerate from extemporaneous dilutions of a proprietary topical cream.

Six different vehicles for topical use were used to prepare 50% dilutions of Betnovate (betamethasone 17-valerate, 0.1%) cream. Blanching assessment as undertaken immediately after preparing the various dilutions and at 1 and 3 months thereafter. Few statistically significant differences were noted between any of the preparations tested indicating hat the rate of release of betamethasone 17-valerate is relatively unaffected by dilution. All preparations were assayed by a stability indicating high pressure liquid chromatographic technique for corticosteroid content. A diminution in the content of betamethasone 17-valerate in the E45 dilution was found 14 months after preparation. All other formulations tested were found to comply with label claim specifications.

Administration, Topical↗
PubMed2000

Net portal appearance of volatile fatty acids in sheep intraruminally infused with mixtures of acetate, propionate, isobutyrate, butyrate, and valerate.

The net portal appearance of volatile fatty acids (VFA) was investigated in four ruminally fistulated and multicatheterized sheep. During the experiments, the sheep were fed once every hour for 14 h and intraruminally infused with mixtures of VFA for the 12 h commencing 2 h after the initiation of the hourly feeding protocol. Paired arterial and portal blood samples were obtained hourly during the last 6 h of the experiments. In the control treatment (1), only water was infused intraruminally. In Treatments 2 through 4, the intraruminal infusion rates of propionate (40 mmol/h), isobutyrate (5 mmol/h), and valerate (5 mmol/h) were unchanged. In Treatments 2, 3, and 4, the acetate infusion rate was 100, 60, and 20 mmol/h, respectively, and the butyrate infusion rate was 10, 30, and 50 mmol/h, respectively. Thus, the infusion rate of VFA carbon was constant across Treatments 2 through 4. Portal recovery estimated from the increased net portal appearance in Treatments 2 through 4 compared to the control treatment was 85% for propionate and 60% for isobutyrate, and these recoveries were unaffected by treatment. The portal recovery of butyrate increased (from 21 to 32%) with increasing infusion rate of butyrate and decreasing infusion rate of acetate, as did the portal recovery of valerate (from 14 to 31%). The portal recovery of acetate was 55%, when measured as net portal appearance. Thus, it seems that the capacity for beta-oxidation in ruminal epithelium is limited, which would explain the increasing portal recovery of butyrate and valerate with increasing infusion rate of butyrate, when infusion rate of VFA carbon is unchanged.

Acetates↗
PubMed2000

Scalp psoriasis: topical calcipotriol 50 micrograms/g/ml solution vs. betamethasone valerate 1% lotion.

Forty-two patients aged between 6 and 61 years (mean: 33.5 years) with psoriasis of the scalp were enrolled in this study. Twenty-seven patients (69%) were males and 15 (31%) were females. The aim of our study was to evaluate the efficacy, safety and tolerability of topical calcipotriol 50 micrograms/g/ml solution vs. betamethasone valerate 1% lotion in the treatment of psoriasis of the scalp. The study was randomized with the twice-daily application of either calcipotriol solution or betamethasone valerate lotion for 6 weeks. Treatment evaluation was clinically based on signs of psoriasis (thickness, redness, scaliness) which were scored from 0 = absent to 4 = severest possible involvement and was performed at the start of treatment and at weeks 2 and 6 of treatment. The results showed a marked improvement and clearance at the end of treatment in 15 (72.8%) of the 24 patients in the calcipotriol group and in 13 of the 18 patients (72%) in the betamethasone group. The mean total sign score at baseline was 5.1 in the calcipotriol group and 5.4 in the betamethasone valerate group. At the end of treatment, this score was decreased to 2.1 and 1.49, respectively. No significant adverse effects were reported in either group except in two patients (8.3%) in the calcipotriol group who developed signs of irritation including itching and erythema. In conclusion, both drugs were effective and well tolerated in the treatment of scalp psoriasis but in some patients calcipotriol had to be given for more prolonged courses.

Administration, Topical↗
PubMed1992

In vitro diffusion cell design and validation. II. Temperature, agitation and membrane effects on betamethasone 17-valerate permeation.

An in vitro permeation cell has been designed and validated for use in monitoring the transmembrane permeation of betamethasone 17-valerate. The design utilizes common laboratory equipment and incorporates as many beneficial features as possible from other designs. The importance of fully validating the hydrodynamic performance of the cell prior to experimentation is stressed. The cell was validated by monitoring the diffusion of betamethasone 17-valerate in isopropyl myristate solution into purified isopropyl myristate receptor phase at different temperatures, different agitation rates and through different synthetic and biological membranes. The results of the hydrodynamic validation agree with data from other researchers and show that the permeation cell is adequately sensitive to these experimental parameters. The results of the membrane evaluation allow appropriate selection of the barrier material for representative transdermal experiments to be conducted. While human and porcine stratum corneum/epidermis are similar in diffusive properties, hairless mouse skin appears to be the most convenient animal membrane for these studies. Although silicone and cellulose membranes appear to be useful in this application, porous filter membranes and egg-shell membranes are insufficiently discriminatory to betamethasone 17-valerate diffusion to provide useful in vitro permeation data.

Animals↗
PubMedDate not supplied

A randomized controlled clinical trial assessing the effect of betamethasone valerate 0.12% foam on the short-term treatment of stasis dermatitis.

BACKGROUND: There are no published studies examining either the effectiveness of topical steroids in the treatment of stasis dermatitis or indicating what steroid strength or duration of treatment is optimal to treat this common condition. OBJECTIVE: To investigate the efficacy of twice-daily application of the topical steroid betamethasone valerate 0.12% foam for the treatment of stasis dermatitis. DESIGN: 42-day randomized, double-blinded, vehicle-controlled, pilot study. SETTINGS: Outpatient dermatology clinic at a university-affiliated clinic. SUBJECTS: 19 subjects, mean age of 73, with mild to moderate bilateral stasis dermatitis. INTERVENTION: Twice-daily application of betamethasone valerate 0.12% foam versus vehicle foam to bilateral randomly assigned lower legs for 28 days with follow-up to day 42. MAIN OUTCOME MEASURES: The primary clinical endpoints were the mean change in erythema, scale, swelling, petechiae, post-inflammatory hyperpigmentation, and self-reported pruritus, assessed on a 5-point Likert scale (0 = clear, 1 = almost clear, 2 = mild, 3 = moderate, 4 = severe). Secondary endpoints were changes in health related quality of life (HRQL) using the EuroQol-5D (EQ-5D) utility score and visual analog scale (VAS) and the Dermatology Life Quality Index (DLQI). RESULTS: Although there was no overall difference between the foam and vehicle-treated leg at days 14 and 28, the steroid-treated leg, but not the vehicle-treated leg, showed statistical improvement over baseline. Improvement in the steroid-treated leg was statistically better than vehicle at days 14 and 28 in terms of erythema (P < .05) and petechiae (P < .05). Improvement in VAS was notable at days 14 (7.1%), 28 (9.7%), and 42 (9.6%) (P < .001). Similarly, there was a statistically significant improvement in the DLQI compared to baseline on visit days 14 (188.9%) and 28 (126.1%) (P < .001). CONCLUSIONS: This study suggests that betamethasone valerate 0.12% foam is an effective and well-tolerated short-term treatment of stasis dermatitis, but that higher potency steroids may be needed to achieve better efficacy. Furthermore, these results are the first to suggest that the application of effective topical anti-inflammatory therapy can lead to improvement in HRQL.

Administration, Topical↗
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↗
PubMed1976

[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↗
PubMed1980

Pharmacological evaluation of a new topical preparation containing dextran sulphate and betamethasone 17-valerate.

The antiinflammatory activity of a topical preparation containing dextran sulphate and betamethasone 17-valerate was studied in comparison with that of the single active principles. In the rat carrageenan paw edema test, where compounds were applied topically as cream formulations, dextran sulphate alone was inactive but it greatly improved the antiinflammatory activity of betamethasone 17-valerate. The reported data indicate that dextran sulphate and betamethasone 17-valerate act synergistically in reducing the paw volume. Moreover, the drug combination administered s.c. demonstrated a statistically significant interaction, when compared with the single active principles, in reducing increased vascular permeability in the rat. The results are briefly discussed in relation to published clinical data.

Administration, Topical↗
PubMed1976

[Topical treatment of dermatoses with difluocortolone valerate fatty ointment].

The aim of the study was to compare the therapeutic effect of the new corticoid, diflucortolone valerate, with the effect of fluocinolone acetonide. The study was conducted as a randomised double-blind trial in 60 patients with various dermatoses. The results were good in 89% of the cases treated with diflucortolone valerate fatty ointment, while the same result was achieved in only 63.5% of the cases treated with fluocinolone acetonide ointment. No side effects were observed during the use of diflucortolone valerate fatty ointment, while local side effects occurred in 2 cases during the use of fluocinolone acetonide ointment.

Administration, Topical↗
PubMed1997

Comparative efficacy of calcipotriol (MC903) cream and betamethasone 17-valerate cream in the treatment of chronic plaque psoriasis. A randomized, double-blind, parallel group multicentre study. Calcipotriol Study Group.

The efficacy, safety and tolerability of calcipotriol cream was compared with betamethasone 17-valerate cream in the treatment of plaque-type psoriasis in a multicentre double-blind, parallel group study. Patients with stable mild-to-moderate chronic disease were randomized to treatment with either calcipotriol, 50 micrograms/g, in a cream formulation (210 patients) or betamethasone 17-valerate cream, 1 mg/g (211 patients). After a wash-out period of 2 weeks, the treatment was applied twice daily, without occlusion, for 8 weeks or to complete clearing. The severity of psoriasis was assessed using the PASI at baseline and after 4 and 8 weeks treatment. The mean percentage reduction of PASI from baseline to end of treatment was 47.8% in the calcipotriol group and 45.4% in the betamethasone group. The reduction from baseline was highly significant in both groups, but the difference between the groups was not significant. There was a difference in the reduction in thickness of the lesions in favour of calcipotriol. The investigator's as well as the patient's overall assessment of treatment response at end of treatment showed no difference between the two treatment groups. Treatment-related adverse events were more frequent with calcipotriol than betamethasone. Lesional/perilesional irritation was reported in 16% and 9% (P = 0.03), and facial irritation in 10% and 0.5% (P < 0.001), respectively. No change was found in serum levels of calcium. Calcipotriol in a cream formulation was effective, safe, well-tolerated, and equal in effect to betamethasone valerate cream.

Administration, Topical↗
PubMedDate not supplied

Betamethasone valerate in foam vehicle is effective with both daily and twice a day dosing: a single-blind, open-label study in the treatment of scalp psoriasis.

BACKGROUND: Psoriasis is a chronic relapsing skin disorder that affects about 2% of the U.S. population and involves the scalp approximately 50% of the time. Topical corticosteroids, including betamethasone valerate, have been used effectively in the treatment of corticosteroid-responsive dermatoses of the skin and scalp. Betamethasone valerate (BMV) in foam vehicle (Luxiq) is designed to improve patient compliance with topical therapy. Superior efficacy over a BMV lotion preparation has been demonstrated with twice-daily use. Even greater compliance would be expected if the drug is effective with once-daily application. PURPOSE: To compare the efficacy of the betamethasone valerate foam (Luxiq) in the treatment of scalp psoriasis following once-daily versus twice-daily dosing. METHODS: Seventy-nine patients with moderate to severe scalp psoriasis from seven centers were enrolled and treated with BMV foam either once a day or twice a day for four weeks. The physician-grader was blinded to the treatment regimen, and the subjects were randomly assigned to either once-daily or twice-daily dosing in a 1:1 ratio. RESULTS: The signs of psoriasis (plaque thickness, scaling, and erythema) were assessed before and after treatment. The investigator's and the patients' global assessments were also evaluated. The composite score improved from 7.7 +/- 2.1 to 3.0 +/- 2.2 with twice-a-day use and from 8.1 +/- 2.2 to 3.9 +/- 2.8 with once-daily use (p > 0.05 for the difference between groups). DISCUSSION: BMV foam is effective for scalp psoriasis with both once-a-day and twice-a-day use. This feature of the BMV foam is encouraging for expected improvement in clinical use.

Administration, Topical↗
PubMed1987

Kinetics of heat inactivation of phenyl valerate hydrolases from hen and rat brain.

Heat inactivation was studied at 45, 50, 55, and 60 degrees for all of the phenyl valerate hydrolases (PVase), including neurotoxic esterase (NTE) and inhibitor-resistant esterase (IRE), in homogenates of hen or rat brain or in preparations of hen brain microsomal membranes. Hen and rat brain homogenates were prepared in buffer (50 mM Tris/0.20 mM EDTA, pH 8.00, at 25 degrees). Hen brain microsomes were suspended either in buffer or in aqueous dimethyl sulfoxide (DMSO, 40%, w/v), or solubilized either in aqueous Triton X-100 (0.10%, w/v) or in 40% (w/v) DMSO. Enzyme activities were measured at 37 degrees using phenyl valerate as substrate. Each enzyme activity in all of the preparations exhibited biphasic heat inactivation kinetics. Apparent rate constants were calculated for the fast (kf) and slow (ks) reactions, along with the relative amounts of activity in each component (Af, As) expressed as percentages of the total activity. For a given preparation and temperature, respective values of kf or ks were similar for PVase, NTE, and IRE, with a mean kf/ks ratio of 52 across all preparations. Af and As were a function of temperature. Mean values of the apparent activation energies (Ea) for all activities and preparations were 44 and 25 kcal/mol for the fast and slow inactivation reactions respectively. These results indicate that all phenyl valerate hydrolases in hen and rat brain undergo a common heat-induced structural change leading to loss of enzymic activity.

Animals↗