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PubMed1981

Effect of oestriol, oestradiol valerate and ethinyloestradiol on serum proteins in oestrogen-deficient women.

The effect of oestriol (3 mg for 3 mth), oestradiol valerate (2 mg for 3 mth) and ethinyloestradiol (0.025 mg for 21 days) on sex hormone binding globulin (SHBG), transcortin, ceruloplasmin and pregnancy-associated macro-globulin (PAG) was analysed in oestrogen-deficient women. The doses of oestrogens were therapeutically effective for the treatment of oestrogen-deficiency symptoms. Treatment with 0.025 mg ethinyloestradiol induced a 281% increase in PAG, a 119% increase in SHBG, a 74% increase in transcortin and a 74% increase in ceruloplasmin levels. Administration of 2 mg oestradiol valerate resulted in a 40% increase in SHBG, a small increase in transcortin and ceruloplasmin, whereas PAG levels remained unaffected. None of the parameters tested were affected by oestriol treatment. PAG was clearly the most sensitive parameter for ethinyloestradiol while SHBG was the most sensitive parameter for oestradiol valerate. These results show no relationship between clinical efficacy and effect of plasma protein synthesis, and demonstrate that one has to be very careful when comparing potency estimates for different oestrogens and different parameters.

Adult↗

PubMed1984

Neural microtubular and lysosomal phenyl valerate esterases and proteases in relation to organophosphate-induced delayed neurotoxicity.

At least three forms of phenyl valerate esterases are present in hen brain cytoplasmic microtubules (MT). Thermostability studies reveal two additional forms in brain homogenates of cow, mouse, pig, rabbit and rat. The distribution of these brain esterases is not related to the age of the hens or the susceptibility of the species to organophosphate (OP)-induced delayed neurotoxicity. MT phenyl valerate esterases are distinct enzymes from the MT-associated proteases degrading high-molecular weight MT-associated proteins (hmw MAPs). Hen brain and spinal cord lysosomes on in vitro incubation release phenyl valerate esterase(s) and hmw MAPs-protease(s). OP neurotoxicants act in vitro to stabilize rat but not hen brain lysosomes. In vivo studies with hen brain and spinal cord lysosomes indicate that OP-induced delayed neurotoxicity is not initiated by disruption of lysosomal stability.

Acid Phosphatase↗

PubMed2004

Adsorption of valeric acid from aqueous solution onto activated carbons: role of surface basic sites.

Adsorption of valeric acid was studied on two activated carbons of different origins, wood and bituminous coal. The effect of oxidation on the adsorption uptake was investigated. Both initial samples were oxidized with nitric acid, which caused the introduction of a significant number of oxygen-containing groups onto the carbon surface. Boehm titration, potentiometric titration, thermal analysis, and sorption of nitrogen were used for detailed surface characterization. Valeric acid adsorption from aqueous solution was measured at 333 K. The calculated isotherms showed a good fitting to the Freundlich equation. The capacity coefficients revealed a direct correlation with the number of basic groups present on the surface. The amount of valeric acid adsorbed at its low concentration is dependent on the number of basic groups, whereas at high concentration the amount adsorbed depends on the volume of micropores smaller than 10 A, where the adsorption potential is the strongest.

Journal Article↗

PubMed2000

Continuous-combined treatment of the menopause with combinations of oestradiol valerate and dienogest - a dose-ranging study.

OBJECTIVES: To determine the progestational efficacy of continuous treatment with various doses of dienogest, combined with oestradiol valerate, on the basis of endometrial histology, effect on climacteric symptoms and bleeding profile in postmenopausal women. METHODS: Patients were randomised to one of five fixed-combination treatments, oestradiol valerate 2.0 mg plus dienogest 0.5, 1.0, 2.0, 3.0 or 4.0 mg. Efficacy was assessed by endometrial biopsy, menstrual charts and change in climacteric symptoms. RESULTS: The endometrium was classified as atrophic in 20.0, 31.3, 25.0, 55.6 and 57.1% of patients in the 0.5, 1.0, 2.0, 3.0 and 4.0 mg dienogest groups, respectively. The frequency of uterine bleeding was dose-dependent. The most favourable bleeding profile was seen in the 3.0 mg dienogest group, whereas the lower doses of dienogest had advantages with respect to the efficacy of the combined preparation. CONCLUSIONS: Dienogest 2.0 and 3.0 mg are the optimal doses for combination with 2.0 mg oestradiol valerate for continuous-combined hormone replacement therapy.

Adult↗

PubMed2000

Double-blind, placebo-controlled, randomized, right-left study comparing calcipotriol monotherapy with a combined treatment of calcipotriol and diflucortolone valerate in chronic plaque psoriasis.

A double-blind, randomized clinical study was conducted to compare the efficacy and tolerability of twice-daily topical calcipotriol treatment with a combination treatment of calcipotriol once a day in the morning and diflucortolone valerate in the evening. Sixty-three patients with a clinical diagnosis of chronic plaque psoriasis and comparable psoriatic lesions on both sides of the body were included. After a washout phase of 1 week, psoriatic lesions were treated for 4 weeks with calcipotriol ointment twice daily on one side of the body and a combination of calcipotriol and diflucortolone valerate ointment on the other side. The treatment period was followed by a period of 4 weeks without any treatment. The psoriasis area and severity index (PASI) was used to compare the 2 groups. Furthermore, the overall therapeutic results were assessed independently by the investigators and by the patients. Both treatment regimens showed a significant, nearly identical, reduction in PASI. The mean PASI for calcipotriol alone was 5.7 at baseline, 1.9 after 4 weeks of treatment and 3.8 at the end of the follow-up period. For combination therapy, these values were 5.7, 1.8 and 3.8, respectively. There was a statistically significant advantage in favor of combined calcipotriol and diflucortolone valerate treatment at weeks 1 and 2 (p < 0.05); however, at the end of the treatment phase the difference between the 2 therapies was not significant. Subjective evaluation of efficacy by both the investigators and the patients revealed no difference between the 2 treatments. The frequency of side effects (e.g. irritation) was low in both groups. In conclusion, both therapies were effective for the treatment of chronic plaque-type psoriatic lesions. The combination of calcipotriol and a topical steroid appeared to produce a more rapid clinical response and was shown to be as effective as calcipotriol therapy alone.

Administration, Topical↗

PubMed1993

High fecundity rates in donor oocyte recipients and in-vitro fertilization surrogates using parenteral oestradiol valerate.

Ovum donation and in-vitro fertilization (IVF) surrogacy can help couples with difficult infertility problems achieve pregnancy. Most centres using oral oestrogens and oestradiol patches report pregnancy rates in the range of 30% per cycle. Parenteral oestradiol valerate has pharmacological properties that make it an attractive option for preparing the endometrium in the recipients undergoing these procedures. When the egg providers were under age 35 years, and using oestradiol valerate in the recipients, we achieved a 61% clinical pregnancy rate in 62 cycles. These improved results suggest that parenteral oestradiol valerate should be used to prepare the endometrium in recipients, and that the hormonal milieu of the endometrium plays an important role in the higher implantation rates obtainable in ovum donor and IVF surrogate cycles.

Adult↗

PubMed1998

Cytotoxicity and intracellular biotransformation of N-benzyladriamycin-14-valerate (AD 198) are modulated by changes in 14-O-acyl chain length.

N-benzyladriamycin-14-valerate (AD 198) is pharmacologically superior to Adriamycin (ADR) based upon comparable cytotoxicity, decreased cardiotoxicity and the ability of AD 198 to circumvent multidrug resistance conferred by either P-glycoprotein overexpression or reduced topoisomerase II activity. AD 198, however, suffers from systemic lability of the 14-O-valerate moiety to enzymatic and non-enzymatic cleavage to yield N-benzyladriamycin (AD 288), which is more similar to ADR in activity. The purpose of this study was to determine whether stability of the ester linkage could be achieved while preserving the favorable characteristics of AD 198 by using a series of N-benzylated ADR congeners containing 14-O-acyl substitutions of incrementally shorter carbon chain lengths. Results from this study indicate that the linear five-carbon valerate substitution is the minimum length necessary to circumvent P-glycoprotein and prevent inhibition of topoisomerase II activity. In addition, although AD 198 is not a pro-drug of AD 288, intracellular 14-O-acyl cleavage appears to contribute to the cytotoxicity of AD 198.

Animals↗

PubMedDate not supplied

Cyproterone acetate could counteract the benefits of estradiol valerate in oophorectomized cholesterol-fed rabbits.

OBJECTIVE: The administration of hormonal replacement treatment to women with an intact uterus needs to be supplemented with progestogenic compounds to avoid endometrial hyperplasia. However, progestins may cancel the beneficial effects of estrogens on the cardiovascular system. The goal of this study was to examine the effects of adding cyproterone acetate to estradiol (E(2))on aorta atherogenesis. DESIGN: Thirty-two cholesterol-fed New Zealand white rabbits were studied for 4 months. The animals underwent laparotomy and were randomly allocated to four groups. Twenty-four rabbits underwent bilateral ovariectomy, and the other eight were sham-operated (group S). The ovariectomized rabbits were allocated to three groups of eight animals each receiving E(2) valerate (group E), E(2) valerate plus cyproterone acetate (group EC), or placebo after sterilization (group C). RESULTS: After 4 months, the cholesterol-rich diet caused atherosclerotic aortic lesions in both treated groups that affected 17.91% +/- 10.19% and 28.16% +/- 7.97% of the aortic surface of groups E and EC, respectively, with a markedly lower aortic plaque size in group E than in groups C and S. Rabbits from group E (but not from group EC) had aortic cholesterol content significantly lower than rabbits from the sham-operated and control groups. CONCLUSION: E(2) valerate reduces aortic atheromatosis in cholesterol-fed, ovariectomized rabbits, and the addition of cyproterone acetate may neutralize this effect.

Analysis of Variance↗

PubMed1978

A study of the comparative efficacy of diflucortolone valerate 0.3% ointment and clobetasol propionate 0.05% ointment.

Three hundred and fifty-four patients with symmetrical dermatoses took part in a multicentre, doubleblind, half-side study in order to compare the efficacy of a new topical steroid, diflucortolone valerate 0.3% (Nerisone Forte) against that of an established, potent topical steroid, clobetasol propionate 0.05% (Dermovate). The assessment of overall response, as judged by the physicians' preference for one side or another, showed no difference between the two compounds. However, when the results were examined by separate diagnostic category, the number of preferences was greater for diflucortolone valerate 0.3% in eczema, and for clobetasol propionate 0.05% in psoriasis, although neither of these differences reached levels of statistical significance. The graded assessments of response indicated that both compounds were highly effective, potent, topical steroids. Eighty-one percent of all patients showed marked improvement or healing with diflucortolone valerate 0.3%, and 84% showed marked improvement or healing with clobetasol propionate 0.05%. This difference was not statistically significant. Analysis of response, either by diagnosis or grade of severity, showed no statistically significant differences between the two compounds. No significant differences in the incidence of severity of side-effects were observed. It was concluded that the two compounds were of equal clinical efficacy.

Adrenal Cortex Hormones↗

PubMed1978

Plasma cortisol values after topical application of diflucortolone valerate (0.3%) or clobetasol propionate (0.05%) in psoriatic patients.

A double-blind randomized study to compare the plasma cortisol values at both 9.00 a.m. and 12 midnight following topical application fo 10 g daily for 7 days of either diflucortolone valerate 0.3% (Nerisone Forte) ointment or clobetasol propionate 0.05% (Dermovate) ointment in 20 hospital inpatients suffering from severe psoriasis, showed that clinically both compounds behaved as potent, highly active topical preparations and caused rapid clinical improvement. Diflucortolone valerate 0.3% caused only slight and non-significant depression of mean plasma cortisols. On the other hand, clobetasol caused an immediate, persistent and statistically significant depression of the 9.00 a.m. coritsol values, which appeared to recover towards normality only on the third day after therapy had been withdrawn. the difference between these 2 compounds was found to be statistically significant (P less than 0.05). From these observations, it is concluded that diflucortolone valerate 0.3% ointment suppresses adreno-cortical function to a significantly lesser extent than clobetasol propionate 0.05% ointment.

Adrenal Cortex Hormones↗

PubMed1975

Betamethasone 17-valerate in childhood asthma. A double-blind crossover trial in children not taking other corticosteroid therapy.

A double-blind crossover trial of Betamethasone 17-Valerate steroid aerosol compared with placebo was carried out on 18 children with severe intermittent or chronic asthma. Seventeen of the 18 children showed a clinically obvious improvement on the active drug. The remaining child was unable to use the inhaler properly. In 14 children the response was dramatic. Improvement was shown at home by a reduction in the number of asthmatic symptoms, improvement in twice daily peak flow rates and by a lowered intake of sympathomimetic tablets. At monthly clinic visits, improvement was shown by chest examination, weight gain and by detailed respiratory function tests. By each of these criteria for improvement the benefit of Betamethasone 17-Valerate over the placebo was highly significant. There were no side effects attributable to the therapy and no evidence, as judged by short tetracosactrin tests, of adrenal suppression resulting from the drug. Betamethasone 17-Valerate appears to be a safe and effective therapy in children with severe asthma.

Adolescent↗

PubMed2003

The effect of herbal medicine on nerve growth factor in estradiol valerate-induced polycystic ovaries in rats.

A type of polycystic ovary resembling some aspects of human polycystic ovarian syndrome (PCOS) can be induced in the rat with a single injection of long-acting estradiol valerate. Among several theories behind the development of polycystic ovaries (PCO), the involvement of the sympathetic nervous system draws much attention, and herbal medicine is known to relieve the abnormal symptoms of PCO. Two herbal formulas, Changbudodam-Tang (cang fu dao tan tang) and Yongdamsagan-Tang (long dan xie gan tang), were used in the present study. The administration of herbal medicine was done every other day for 60 days. The morphological changes of ovaries from herbal medicine treatment were compared to those from an oil-treated control group and an estradiol valerate-injected group. This study also examined the possible hypothesis of neurogenic participation in terms of nerve growth factor (NGF) in the pathology of ovarian dysfunction. The nerve growth factor was analyzed in the central nervous system and ovaries by immunohistochemistry. The main findings of the present study were: (1) PCO were fully developed in rats with a single intramuscular injection of estradiol valerate, (2) PCO resulted in the expression of NGF in the ovaries and the brain tissues, and (3) herbal medicine administration significantly decreased the elevated NGF staining in the ovaries without affecting the brain tissues significantly.

Animals↗

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↗

PubMed1984

Relative fatty acid composition of lecithin during postmenopausal replacement therapy--a comparison between ethinyl estradiol and estradiol valerate.

The relative fatty acid composition of serum lecithin was followed in groups of women during postmenopausal replacement therapy. The effects of estradiol valerate and ethinyl estradiol in two different doses, and the modulating influence of various progestogens and antiestrogens were compared. Unopposed estrogen treatment enhanced liver lecithin synthesis along pathway I, i.e. reduced the amount of stearic acid and increased the amount of palmitic acid. The effect was clearly dose-dependent and even the low dose of 10 micrograms of ethinyl estradiol was more potent than 2 mg of estradiol valerate. No qualitative difference between the two estrogens was recorded. The sequential addition of the antiestrogen tamoxifen significantly reduced the influence of ethinyl estradiol. Liver lecithin synthesis along pathway I may be stimulated by all estrogens and not only by 17C-alkylated compounds. The prostaglandin precursors, dihomogammalinolenic and arachidonic acid, showed a seemingly dose-dependent increase during estrogen treatment. The comparatively weaker effects of estradiol valerate on lipid metabolism should make this non-alkylated estrogen the first choice in clinical practice.

Adult↗

PubMed1994

Phenyl valerate and choline ester hydrolases in the platelets of human, hen, rat and mouse.

1. The levels of phenyl valerate and choline ester hydrolases in the platelets of human and certain laboratory animals have been determined for comparison. 2. The activities of total phenyl valerate hydrolase (PVase), paraoxon insensitive phenyl valerate hydrolase (PI-PVase), paraoxon and mipafox resistant esterase (PMRE) and propionyl-cholinesterase (PChE) were maximal in hen followed by mouse, rat and human. 3. Neurotoxic esterase (NTE) and acetylcholinesterase (AChE) activities were concentrated in the platelets of hens followed by humans, rats and mice in order. 4. Maximum concentration of butyrylcholinesterase (BChE) was found in the platelets of hens followed by mice, humans and rats. 5. It is concluded that the normal levels of enzyme activities in the platelets of humans and various species of animals may help to evaluate the exposure risk to neurotoxic organophosphorous compounds.

Acetylcholinesterase↗

PubMed1976

[Efficacy of diflucortolone valerate in the vasoconstriction tests].

The efficacy of a new topical corticosteroid, 6alpha,9-difluor-11beta-hylerate, Nerisona), as a 0.1% cream, ointment and fatty ointment was investigated in the vasoconstriction test in two series of studies after application to human skin in which hyperaemia had been experimentally induced. The diflucortolone valerate W/O emulsion proved to be 100 times more effective than fluocortolone in an identical base. In a further study diflucortolone valerate as well as in the three preparations was compared with nine known corticosteroids or their commercial preparations. In the comparison of the preparations only the cream with 0.05% betamethasone-17,21-dipropionate was superior to the diflucortolone valerate cream. As regards all the other preparations of formulations the new substance proved to be more or at least equally effective.

Administration, Topical↗

PubMed1992

N-benzyladriamycin-14-valerate and drug resistance: correlation of anthracycline structural modification with intracellular accumulation and distribution in multidrug resistant cells.

N-Benzyladriamycin-14-valerate (AD 198) is a highly hydrophobic analogue of Adriamycin (ADR) which can circumvent multidrug resistance (MDR) in various cell lines. Unlike ADR, AD 198 avoids extrusion by P-glycoprotein (P-gp) in AD 198-resistant murine macrophage-like J774.2 cells and localizes in the cytoplasm. To determine the structural modification(s) responsible for these different characteristics, intracellular accumulation and distribution of ADR, AD 198, and the two half-substituted AD 198 congeners. N-benzyladriamycin (AD 288) and adriamycin-14-valerate (AD 48), were analyzed in AD 198-sensitive (J774.2) and -resistant (A300) cells. A300 cells exhibited cross-resistance to and reduced accumulation of ADR, AD 48, and AD 288. ADR and AD 288 rapidly localized in the nuclei of parental and A300 cells, while AD 48 and AD 198 localized in the cytoplasm. AD 48 redistributed into nuclei and cytoplasm of both cell lines, but AD 198 maintained a punctate cytoplasmic distribution in A300 cells. These results suggest that both the N-benzyl and C14-valerate substitutions of AD 198 are required for P-gp circumvention and stable cytoplasmic localization in A300 cells, probably as a result of differing intracellular drug trafficking.

ATP Binding Cassette Transporter, Subfamily B, Mem↗

PubMed2006

[Early effect of non-surgical treatment using betamethasone valerate ointment for phimosis in childhood].

We evaluated the early efficacy of non-surgical treatment using 0.07% betamethasone valerate ointment on, 34 boys with phimosis between January 2001 and June 2005. Patients were treated with 0.07% betamethasone valerate ointment applied to the distal aspect of the prepuce every other day for 2-6 weeks. During the treatment period, patients were instructed to retract the foreskin to penis root without overstraining. The overall success rate was 94.1% and therapeutic effects were observed in 58.8% of the patients in two weeks. There were no medical side effects. Treatment using betamethasone valerate ointment is very effective, easy and safe. We recommend this treatment for patients with phimosis and/or those with recurring balanoposthitis.

Anti-Inflammatory Agents↗