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At least 37 records · Page 2Linked to original sources
PubMed1995

Topical mometasone furoate and betamethasone-17-valerate decrease collagen synthesis to a similar extent in human skin in vivo.

Topical corticosteroids are used extensively to treat inflammatory skin diseases. Long-term use, however, may be associated with adverse effects such as skin atrophy. New steroids have been developed with the objective of increasing efficacy and reducing the incidence of adverse effects. Mometasone furoate (MMF) is one of these new derivatives. The aim of our study was to compare the effects of MMF and betamethasone-17-valerate (BM-17-valerate) on collagen synthesis in human skin in vivo. Fifteen healthy male volunteers applied MMF, BM-17-valerate and vehicle for 1 week to different areas of abdominal skin. Suction blisters were raised on these areas, and a control site, and procollagen propeptide (PICP, PINP, PIIINP) levels in the suction blister fluid were measured by radioimmunoassay. Skin thickness was measured ultrasonically by Dermascan A at the end of the treatment period. The levels of the three propeptides in suction blister fluid were reduced to similar extent by MMF and BM-17-valerate. The 1-week treatment period had no detectable influence on skin thickness. We conclude that MMF and BM-17-valerate decrease collagen synthesis to the same extent in human skin in vivo.

Administration, Topical↗
PubMed1985

Pharmacokinetics and biotransformation of estradiol valerate in ovariectomized women.

Estradiol valerate is well suited for treatment of the characteristic symptoms accompanying menopause in women. The pharmacokinetics and biotransformation of estradiol valerate were studied in women following intravenous, intramuscular and oral administration. Intravenously given, estradiol valerate is split by enzymatic hydrolysis into 17 beta-estradiol and the fatty acid. The estrogen arising in vivo from the steroid ester is subject to intermediate metabolism. The metabolites are eliminated at a nearly constant rate mainly in urine. The biotransformation of estradiol valerate was not different following intravenous or intramuscular injection. Orally given estradiol valerate is subject to an extensive first pass metabolism. Daily repeated oral administration does not result in accumulation of 17 beta-estradiol and its metabolites.

Administration, Oral↗
PubMed1986

Estrogen induction of liver proteins and high-density lipoprotein cholesterol: comparison between estradiol valerate and ethinyl estradiol.

The effects of ethinyl estradiol and estradiol valerate were compared in 135 postmenopausal women during estrogen replacement therapy. Subfractions of high-density lipoprotein (HDL) cholesterol and its apolipoproteins and the serum levels of 2 estrogen-sensitive liver proteins were followed during 3 cycles of unopposed treatment with either ethinyl estradiol 10 or 30 micrograms or estradiol valerate 2 mg daily. Estrogen therapy induced significant and dose-dependent changes in all serum factors except HDL3 cholesterol. The effects of 10 micrograms of ethinyl estradiol upon the lipoproteins were 1.5-2.5 times greater than those of 2 mg of estradiol valerate. Sex-hormone-binding globulin and the pregnancy zone protein were the most sensitive markers for the estrogenic effect and these 2 liver-derived plasma proteins were also much more sensitive to ethinyl estradiol than to estradiol valerate. Although satisfactory therapeutic effects were achieved with both estrogens, the marked influence of ethinyl estradiol on liver protein synthesis should make estradiol valerate the first choice in clinical replacement therapy.

Adult↗
PubMed1997

Differential effects of hormone-replacement therapy on endogenous nitric oxide (nitrite/nitrate) levels in postmenopausal women substituted with 17 beta-estradiol valerate and cyproterone acetate or medroxyprogesterone acetate.

Increased incidence of cardiovascular disease in postmenopausal women (PMW) is accompanied by ovarian dysfunction; hormone replacement therapy (HRT) can have cardioprotective effects. Because hypertension and atherosclerosis are associated with impaired release of endothelium-derived nitric oxide (NO) and increased levels of low-density lipoproteins (LDL), we investigated whether HRT augments NO release, and whether these increases are accompanied by a decrease in LDL levels in PMW. We determined serum nitrite/ nitrate (NO2-/NO3-) and LDL levels at baseline (before initiation of HRT) and during the 6th and 12th months of the study. The PMW (n = 26) received continuous oral administration of estradiol valerate (Progynova, 2 mg daily) for 21 days supplemented with either oral cyproterone acetate (CPA; 1 mg; n = 11) or medroxyprogesterone acetate (MPA; 5 mg; n = 15) on days 12-21 of each treatment cycle. Blood samples in the PMW receiving HRT were collected at times while the subjects were taking estradiol valerate alone and estradiol valerate plus CPA or MPA. Compared with the samples collected at baseline, serum NO2-/NO3- levels increased significantly from 20.1 +/- 1.58 mumol/L at baseline to 30 +/- 3.7 mumol/L (P < 0.01) in samples collected after 12 months of HRT while the PMW were not taking progestins (CPA or MPA), and to 25.4 +/- 2 mumol/L (P < 0.05) when all the samples, regardless of the treatment with CPA or MPA, were included in the analysis. Moreover, > 30% increase in serum NO2-/NO3- levels were observed only in 13 (responders) out of 26 PMW substituted with estradiol valerate, suggesting that estradiol may improve endogenous NO synthesis in a differential fashion. Compared with baseline, no significant increases in serum NO2-/NO3- were observed in samples collected while the estradiol-treated responders were taking either CPA or MPA. In contrast to NO2-/NO3- serum LDL levels were significantly reduced in samples collected after 12 months of HRT (P < 0.05 vs. baseline). Furthermore, levels of NO2-/NO3 showed a significant negative correlation with the levels of LDL (r2 = 0.17; P < 0.05) in the responders but not in nonresponders. These results indicate that oral administration of estradiol valerate in PMW for HRT increases circulating NO levels, an effect that may contribute to the cardioprotective effects of HRT in PMW. In addition, our data suggests but does not prove that concomitant administration of a progestin may attenuate the beneficial effects of estrogen replacement therapy with regard to NO release. Finally, our data provides evidence for the existence of responders and nonresponders to postmenopausal estrogen treatment with respect to improvement of endogenous NO levels, suggesting that a significant number, but not all, of the hormonally substituted PMW profit fully from the beneficial properties of a HRT.

Estradiol↗
PubMed1988

Diflucortolone valerate. Asian experience.

More than 10 years ago, diflucortolone valerate (Nerisone, Nerisona) was introduced in Germany and soon after in Asian countries in a concentration of 0.1% in cream, ointment and fatty ointment bases. 897 patients were included in the first Southeast Asian multicentre trial with these 3 formulations, and good efficacy and tolerability combined with a rapid onset of effect were shown. These results were confirmed later in Indonesia in an extended follow-up trial which included 1295 patients. A combination of 0.1% diflucortolone valerate with 1.0% chlorquinaldol was introduced after a multicentre Southeast Asian trial involving 8668 patients with inflammatory or allergic skin conditions for which a supplementary anti-infective treatment, for prophylaxis or therapy, was considered to be indicated. Excellent results were obtained in terms of efficacy, tolerability and cosmetic properties. A randomised double-blind trial comparing this preparation with a so-called 'shotgun' combination containing 0.05% betamethasone 17-valerate, 0.1% gentamicin, 1.0% tolnaftate and 1.0% clioquinol in 288 patients in the Philippines resulted in a better efficacy for the diflucortolone preparation in the 80 patients with bacterially or mycotically infected skin diseases. A 0.3% concentration of diflucortolone valerate was developed and introduced as a high potency topical corticosteroid. A trial in the Philippines which involved 143 patients with mostly severe chronic recurrent and resistant corticosteroid-responsive skin disease confirmed a pronounced clinical efficacy with a low incidence of side effects. For the treatment of inflammatory or eczematised dermatomycosis. 0.1% diflucortolone was combined with 1.0% isoconazole nitrate (Travocort). In a randomised double-blind study of 294 patients in Thailand, this preparation was compared with a plain 1.0% clotrimazole formulation. The results were significantly better for the diflucortolone plus isoconazole nitrate combination in terms of remission of symptoms, and after 1 week the mycological cure rates were also better, as shown in potassium hydroxide and culture investigations. It is concluded, therefore, that diflucortolone valerate in the available galenic bases and in effective combinations with other agents has been proven in extensive clinical trials to be a valuable therapeutic tool in dermatological practice.

Asia↗
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↗
PubMed1984

Clinical evaluation of hydrocortisone valerate 0.2% ointment.

Evaluations of the comparative efficacy and safety of hydrocortisone valerate 0.2% ointment were made in six double-blind, multicenter trials involving a total of 485 patients, 209 with atopic dermatitis and 276 with plaque psoriasis. The vasoconstrictor activity of hydrocortisone valerate 0.2% ointment was also assessed in normal subjects. Hydrocortisone valerate 0.2% ointment displayed therapeutic effects within three days. In terms of global evaluations of efficacy, hydrocortisone valerate was more effective than vehicle and was comparable to other intermediate or moderate potency corticosteroid ointments. The vasoconstrictor activity of hydrocortisone valerate 0.2% ointment was greater than that of other moderate potency ointments.

Adrenal Cortex Hormones↗
PubMed1990

Effects of intravenous injection of butyrate, valerate and their isomers on endocrine pancreatic responses in conscious sheep (Ovis aries).

1. The effects of intravenous injection of n-butyrate, iso-butyrate, n-valerate and iso-valerate on insulin and glucagon secretion was examined in conscious sheep. 2. Each sodium salt of the short chain fatty acids increased plasma insulin and glucagon concentrations in a dose-dependent manner (312-1250 mumol/kg body wt). 3. Both butyrate and valerate isomers with branched carbon chains had larger insulin releasing activity than isomers with straight carbon chains. 4. The glucagon responses to butyrate or valerate did not differ between the isomers with straight carbon chains and those with branched carbon chains. 5. Our results suggest that the receptive mechanism to short chain fatty acids, which may involve the nervous system, differs between the A cell and the B cell in sheep in vivo.

Animals↗
PubMed1994

Plasma concentrations of betamethasone after topical application of betamethasone 17-valerate: comparison with oral administration.

Plasma concentrations of betamethasone were measured by r.i.a. after oral administration of 0.6 mg betamethasone and topical application of betamethasone 17-valerate in the same five healthy subjects. Betamethasone 17-valerate was prepared as a suspension in medical grade pressure sensitive adhesive and applied to a 100 cm2 area on the back for 28 h. Mean maximum plasma concentrations were 5.0 and 0.24 ng ml-1 and mean AUC values were 75.4 and 7.74 ng ml-1 h after oral and topical administrations, respectively. The mean plasma elimination half-life of betamethasone after the removal of topical betamethasone 17-valerate was 16.6 h which was twice that after oral administration, 8.1 h. Betamethasone 17-valerate may require application to the skin more than twice daily.

Administration, Oral↗
PubMed1982

The stability and blanching efficacy of betamethasone-17-valerate in emulsifying ointment.

The bio-availability of betamethasone-17-valerate (Betnovate ointment) in emulsifying ointment (1 in 4 dilution) was investigated in ten subjects using a single-application vasoconstrictor assay; the blanching induced was measured using a skin reflectance spectrophotometer. The vasoconstrictor activity of the diluted preparations decreased with age. There was no significant difference between the vasoconstrictor activity of freshly made Betnovate 1 in 4 in emulsifying ointment and undiluted Betnovate ointment, and between 3-4 week old diluted Betnovate and emulsifying ointment base. Blanching induced by freshly prepared 4, 8 and 16-fold dilutions was not significantly different but a large reduction in blanching occurred on diluting 32-fold with emulsifying ointment. The degradation of betamethasone -17-valerate in emulsifying ointment was quantified by high performance liquid chromatography. More than 60% of the betamethasone -17-valerate underwent degradation within 6 h. There was a simultaneous increase in the concentration of betamethasone-21-valerate which peaked within 2 days and was followed by a slow degradation (half-life 8 days) to betamethasone free alcohol.

Betamethasone↗
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↗
PubMed1984

Comparative efficacy of once a day diflorasone diacetate and twice a day betamethasone valerate ointment applications in eczematous dermatitis.

The efficacy of once a day applications of 0.05% diflorasone diacetate ointment and twice a day applications of 0.1% betamethasone valerate ointment was compared in 70 patients with eczematous dermatitis. Altogether 32 patients completed the 3-week study. Fourteen patients in the diflorasone group and 6 on betamethasone left the study earlier because of total (100%) improvement of lesions. Eight patients left because of unsatisfactory progress and 6 because of personal reasons. There were only two noticeable differences observed between treatment groups. At Week 2, the diflorasone diacetate group improved significantly more than the betamethasone valerate group with respect to pruritus. At Week 3, this difference in the improvement of pruritus was marginally significant in favour of diflorasone diacetate. Excluding the complications due to a secondary infection, no adverse reactions were recorded in the diflorasone diacetate-treated patients; 1 betamethasone valerate-treated patient developed telangiectasia. The once a day applications of diflorasone diacetate not only proved to be slightly more efficacious than the twice a day applications of betamethasone valerate, but also provided the advantages of patient convenience and compliance.

Adolescent↗
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↗
PubMed1995

[Betamethasone valerate reference standard (Control 941) of the National Institute of Health Sciences].

The raw material for betamethasone valerate was tested for preparation of the "Betamethasone Valerate Reference Standard (Control 941)". Analytical data obtained were as follows: melting point, 194.3 degrees C (decomposition); UV and infrared spectra, the same as those for JP Betamethasone Valerate Reference Standard (Control 844); optical rotation, [alpha]20D = +79.4 degrees; thin-layer chromatography and high-performance liquid chromatography (HPLC), no impurities were detected; assay, 100.0% by HPLC. Based on the above results, the candidate material was authorized as the JP Betamethasone Valerate Reference Standard (Control 941).

Betamethasone Valerate↗
PubMed1996

Pharmacology of N,N-di(n-butyl)adriamycin-14-valerate in the rat.

Lipophilic N-alkylanthracyclines such as AD 198 (N-benzyladriamycin-14-valerate) or AD 201 [N,N-di(n-propyl)adriamycin-14-valerate], which exert their cytotoxicity through mechanisms which are not yet fully defined, possess inherent abilities to circumvent multidrug resistance in vitro and in vivo, possibly though alterations in normal intracellular drug trafficking. As part of structure-activity studies with this class of agent, we have now examined the pharmacology of AD 202 [N,N-di(n-butyl)adriamycin-14-valerate], another analog possessing superior antitumor activity to doxorubicin in vivo and an ability to circumvent multidrug resistance in vitro. Following the administration of AD 202 (20 mg/kg, i.v.) to anesthetized rats, rapid drug distribution (T1/2 5 min) was followed by more gradual elimination (T1/2 3.6h). Plasma clearance of AD 202 (224 +/- 63.6 ml/min per kg) and steady state volume of distribution (25.7 +/- 11.1 l/kg) were indicative of extensive tissue sequestration and/or a large degree of extra-hepatic metabolism. The parent drug predominated in plasma until 20 min, thereafter N,N-di(n-butyl)adriamycin became the principal circulating anthracycline. The systemic exposure to this biotransformation product (area under the plasma concentration-time curve from time zero to 480 min AUC(0-480) 28 1672 ng.min/ml) was > tenfold higher than for the other detected plasma products (N-butyladriamycin-14-valerate, N-butyladriamycin, and three unidentified fluorescent signals; P1-3). Total urinary elimination over 8h was limited (1.9% of dose), occurring predominantly as N,N-di(n-butyl)adriamycin (1.2% of dose), N-butyladriamycin (0.4% of dose), and their corresponding 13-carbinol metabolites (<0.1% of dose each). Low levels of adriamycin (ADR), aglycones and two unidentified products were also seen. Parental AD 202 was found in urine only up to 1h. By contrast, hepatic elimination of parent drug was seen, albeit at low levels, through 8h. Excretion by this route (22% of dose) occurred principally as N-butyl-adriamycin (8% of dose), N-butyladraimycinol (2.1% of dose) with lower levels of N,N-di(n-butyl)adriamycin (1.6% of dose), N,N-di(n-butyl)adriamycin (0.8% of dose), and aglycones (4.3% of dose, combined). Other products included ADR (1.1% of dose) and two unidentified signals (3.4% of dose, combined). The relatively poor mass balance in these studies is attributed to prolonged intracellular retention (elimination T1/2 24.2h) of N,N-di(n-butyl)adriamycin. Thus, in common with other N-alkylanthracyclines, the pharmacology of AD 202 is complex but its therapeutic properties clearly are not derived from an ADR prodrug effect. Significant differences continue to be noted as to the metabolic fate of congeners of this class of anthracycline analogs.

Animals↗
PubMed1991

A double-blind, multicenter, parallel-group trial with 0.05% halobetasol propionate ointment versus 0.1% diflucortolone valerate ointment in patients with severe, chronic atopic dermatitis or lichen simplex chronicus.

In a double-blind, parallel-group, multicenter, comparative trial in 120 evaluable patients with chronic, localized atopic dermatitis or lichen simplex chronicus, the success rate (described as "healed" and "marked improvement") was 91.5% in patients treated with halobetasol propionate ointment and 83.6% in those in the diflucortolone valerate treatment group. Of patients treated with halobetasol propionate ointment, 40.7% reported healing within 17 days, whereas of those in the diflucortolone valerate treatment group, 32.8% reported healing within that time. Early onset of therapeutic effect, that is, within 3 days of the start of treatment, was reported in a higher percentage of patients treated with halobetasol propionate ointment than in those treated with diflucortolone valerate ointment (70% versus 59%). Adverse effects at the site of application were less frequently reported in patients belonging to the halobetasol propionate treatment group than in those treated with diflucortolone valerate ointment (3% versus 8%).

Adolescent↗
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↗
PubMed2001

Molecular models of N-benzyladriamycin-14-valerate (AD 198) in complex with the phorbol ester-binding C1b domain of protein kinase C-delta.

N-Benzyladriamycin-14-valerate (AD 198) is a semisynthetic anthracycline with experimental antitumor activity superior to that of doxorubicin (DOX). AD 198, unlike DOX, only weakly binds DNA, is a poor inhibitor of topoisomerase II, and circumvents anthracycline-resistance mechanisms, suggesting a unique mechanism of action for this novel analogue. The phorbol ester receptors, protein kinase C (PKC) and beta2-chimaerin, were recently identified as selective targets for AD 198 in vitro. In vitro, AD 198 competes with [3H]PDBu for binding to a peptide containing the isolated C1b domain of PKC-delta (deltaC1b domain). In the present study molecular modeling is used to investigate the interaction of AD 198 with the deltaC1b domain. Three models are identified wherein AD 198 binds into the groove formed between amino acid residues 6-13 and 21-27 of the deltaC1b domain in a manner similar to that reported for phorbol-13-acetate and other ligands of the C1 domain. Two of the identified models are consistent with previous experimental data demonstrating the importance of the 14-valerate side chain of AD 198 in binding to the C1 domain as well as current data demonstrating that translocation of PKC-alpha to the membrane requires the 14-valerate substituent. In this regard, the carbonyl of the 14-valerate participates in hydrogen bonding to the deltaC1b while the acyl chain is positioned for stabilization of the membrane-bound protein-ligand complex in a manner analogous to the acyl chains of the phorbol esters. These studies provide a structural basis for the interaction of AD 198 with the deltaC1b domain and a starting point for the rational design of potential new drugs targeting PKC and other proteins with C1 domains.

Antibiotics, Antineoplastic↗