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PubMed1978

A differential interaction of daunomycin, adriamycin, and N-trifluoroacetyladriamycin 14-valerate with mouse peritoneal macrophages.

The interaction of three anthracycline drugs, daunomycin, Adriamycin, and N-trifluoroacetyladriamycin 14-valerate, with mouse peritoneal macrophages was explored. As assessed by drug-specific cytofluorescence, Adriamycin and daunomycin accumulated slowly within macrophages, first staining the nucleus and then the cytoplasmic inclusions that were induced by the drug treatment. N-Trifluoroacetyladriamycin 14-valerate distributed rapidly into the cells, was excluded from the nucleus, and induced numerous cytoplasmic inclusions. Electron microscopy revealed that the cytoplasmic inclusions were vacuoles containing some amorphous material and not the classical autophagic vacuoles containing organelles and membrane lamellae. All the drugs induced cell shrinkage with time and brought about cell death within 24 hr. Loss of cell function and viability was dose and time dependent; i.e., a 6-hr incubation with daunomycin or Adriamycin, 2.5 microgram/ml, brought about a 50% reduction in the phagocytic capacity of the treated macrophages. The damaging potency towards macrophages (daunomycin greater than Adriamycin greater than N-trifluoroacetyladriamycin 14-valerate) is in the reverse order to the in vivo therapeutic efficiency.

Animals↗
PubMed1981

Comparative effects of adriamycin and N-trifluoroacetyladriamycin-14-valerate on cell kinetics, chromosomal damage, and macromolecular synthesis in vitro.

N-Trifluoroacetyladriamycin-14-valerate differs from Adriamycin in its rapid intracellular transport and lack of fluorescent binding to nuclei or chromosomes. Both of these anthracyclines cause inhibition in the incorporation of labeled precursors into nucleic acids, extensive chromosomal damage, and arrest of cell cycle traverse in G2. In human lymphoid cells, N-trifluoroacetyladriamycin-14-valerate, unlike Adriamycin, does not show cell cycle phase-specific or proliferation-related cytotoxic effects. In an L1210 soft-agar assay, both Adriamycin and N-trifluoroacetyladriamycin-14-valerate show no enhanced sensitivity of mid-S-phase cells to their cytotoxic action.

Animals↗
PubMed1980

Diflucortolone valerate (Nerisona): a comparative vasoconstriction test in artificially induced hyperemia of the skin.

In 20 healthy volunteers of both sexes the vasoconstrictive activity of diflucortolone valerate in two of its commercially available formulations (water-in-oil emulsion and pure fat base) was compared with that of four other substances: fluocinonide; betamethasone-17,21-dipropionate; hydrocortisone-17-butyrate; and clobetasol-17-propionate in corresponding galenical formulations. The visual assessment of vasoconstrictive activity after 10 hours revealed a statistically significant superiority of diflucortolone valerate in its fat base over the corresponding galenical formulations of fluocinonide, clobetasol-17-propionate, and hydrocortisone-17-butyrate. Diflucortolone valerate in a water-in-oil emulsion was statistically better after eight hours than the cream formulations of fluocinonide; clobetasol-17-propionate, and betamethasone-17,21-dipropionate.

Administration, Topical↗
PubMed1993

N-benzyladriamycin-14-valerate (AD 198)-resistant cells exhibit highly selective cross-resistance to other anthracyclines that circumvent multidrug resistance.

N-Benzyladriamycin-14-valerate (AD 198)-resistant murine J774.2 macrophage-like cells (A300) exhibited a novel mechanism of resistance in which P-glycoprotein was overexpressed without decreased AD 198 accumulation. Cross-resistance to Adriamycin (ADR), N-benzyladriamycin, and Adriamycin-14-valerate was due, at least in part, to reduced accumulation, suggesting that circumvention of P-glycoprotein-mediated transport was associated with extreme lipophilicity conferred by both substitutions. Thus, unlike multidrug resistance mediated by either P-glycoprotein, the multidrug resistance-associated protein (MRP), or decreased topoisomerase II activity, cross-resistance in A300 cells was highly structure-specific. In order to further characterize the specificity of AD 198 resistance, the cytotoxicity, accumulation, and intracellular localization of a series of 3'-morpholinyl, 3'-deamino and halogenated ADR congeners that have been reported to circumvent MDR was determined in AD 198-resistant J774.2 and P388 AD 198-resistant cells. Cross-resistance correlating with increased AD 198 resistance was observed for 2'-bromo-4'-epi-hydroxy-daunomycin (13-fold), morpholinyl doxorubicin (24-fold), and 4'-iodo-4'-deoxydoxorubicin (2.8-fold), but was attributable to decreased accumulation. Cross-resistance to 3'-hydroxy-14-O-palmitoyl-doxorubicin (6-fold) was not due to reduced accumulation. No cross-resistance was observed for the highly cytotoxic metabolite of WP474, 3'-hydroxyldoxorubicin (hydroxyrubicin; WP159), nor for the much less cytotoxic 3'-O-benzylated congeners, including 3'-O-benzyl-doxorubicin-14-valerate. These findings indicate that AD 198 resistance confers cross-resistance to compounds that, like AD 198, localize in the cytoplasm but are metabolized to highly cytotoxic, nuclear-localizing compounds.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1996

[Effect of estradiol valerate and chlormadinone acetate in hormone replacement therapy in postmenopause on Kupperman index, body weight, blood pressure, lipids, enzymes and electrolytes].

Kupperman-index, weight, blood pressure, serum lipids, blood count, thrombocytes, fibrinogen, thrombine time, electrolytes, enzymes, serum proteins, bilirubine and other parameters were studied in 16 healthy post-menopausal women treated for 18 months with 2 mgs estradiol valerate continuously sequentially combined with the antiandrogenic progestogen chlormadinone acetate (CMA) 2 mgs from 1st to 12th every month of treatment. The women were examined after the 1st, 3rd, 6th, 12th, and 18th month during the last 3 days of the progestogen phase, where the CMA had been added to the estradiol valerate for at least 12 days. The combined estradiol-CMA therapy resulted in a significantly reduced Kupperman-index. The total serum cholesterol- and LDLC-levels were also reduced and the HDL-cholesterol and HDLC-cholesterol-quotient increased. Triglycerides, weight, blood pressure, enzymes, and other parameters were unchanged. The positively metabolic effects of estradiol valerate were not altered after the chlormadinone acetate in a sequential regime.

Adult↗
PubMed1998

Pharmacokinetics of orally administered estradiol valerate. Results of a single-dose cross-over bioequivalence study in postmenopausal women.

A randomized, single-dose cross-over study in 32 postmenopausal women was performed to demonstrate bioequivalence of two estradiol valerate containing formulations (first sequence of Klimonorm as test preparation). The serum levels of estradiol, free and conjugated estrone were measured until 48 h after an oral dosage of 4 mg estradiol valerate (CAS 979-32-8). The mean AUC(0-48) of estradiol was calculated as 1006.6 +/- 479.4 h x pg x ml-1 (Test) and 1015.2 +/- 555.2 h x pg x ml-1 (Reference). The corresponding (AUC(0-48) of the active metabolite, free estrone, exceeded that of estradiol at 3578.3 h x pg x ml-1 (Test) and 3485.1 h x pg x ml-1 (Reference). Much higher was the AUC(0-48) for conjugated estrone at 132.4 h x ng x ml-1 (Test) and 133.6 h x ng x ml-1 (Reference). Mean estradiol Cmax values of 39.8 +/- 17.7 pg/ml (Test) and 42.9 +/- 21.0 pg/ml (Reference) were attained 8.2 +/- 4.5 h (Test) and 10.0 +/- 5.9 h (Reference) after the administration of 4 mg estradiol valerate. Maximal free estrone concentrations of 163 pg/ml (Test) and 174.3 pg/ml (Reference) were reached after 7.2 h (Test) and 7.5 h (Reference). Maximal conjugated estrone concentrations of 15.5 ng/ml (Test) and 16.2 ng/ml (Reference) were reached after 2.4 h (Test) and 2.0 h (Reference). The terminal elimination half-life of estradiol was calculated at 16.9 +/- 6.0 h (Test) and 15.0 +/- 4.8 h (Reference), that of free estrone at 16.3 h (Test) and 13.5 h (Reference), that of conjugated estrone at 11.8 h (Test) and 10.6 h (Reference). After logarithmic transformation, the 90% confidence intervals of the AUC(0-48) and Cmax ratios for estradiol and also for the metabolites (free and conjugated estrone) were within the acceptance ranges for bioequivalence. Therefore the test preparation and the reference preparation are bioequivalent.

Administration, Oral↗
PubMed1999

Long-term sequential treatment with combined estradiol valerate and cyproterone acetate in early postmenopause.

BACKGROUND: We sought to evaluate the long-term safety and efficacy of cyclic combined estradiol valerate and cyproterone acetate. METHODS: A six-year, single center, open study was performed of forty-eight recently postmenopausal women. We evaluated biochemical markers of bone turnover, bone mineral content, bone mineral density, serum lipids, climacteric symptoms, and bleeding throughout the six-year period. Ultrasound evaluation of the endometrium was performed yearly for the first two years. RESULTS: Markers of bone turnover were decreased over the study period, while bone mineral content and density remained unchanged. High density lipoprotein cholesterol levels were increased with unchanged blood pressure over the six years. Menopausal symptoms showed significant improvements within 6 months. Endometrial scan results never required hysteroscopic evaluation. CONCLUSION: Sequentially combined estradiol valerate and cyproterone acetate can be used for an indefinite number of years in women with recent natural menopause. Cyproterone acetate provides adequate endometrial protection and cycle control while allowing estradiol valerate to exert its positive effects on lipid profile, bone metabolism, and climacteric symptoms.

Cyproterone Acetate↗
PubMed1991

Double-blind, right/left comparison of calcipotriol and betamethasone valerate in treatment of psoriasis vulgaris.

The therapeutic efficacy and tolerability of calcipotriol ointment and betamethasone valerate ointment in psoriasis were compared in a multicentre, prospective, randomised, double-blind, right/left trial. 345 inpatients and outpatients with psoriasis vulgaris of symmetrical distribution were treated twice daily for 6 weeks with calcipotriol ointment 50 micrograms/g and betamethasone ointment 0.1% randomly assigned to opposite sides of the body. The main outcome measures--the psoriasis area and severity index (PASI), the investigators' assessments of erythema, thickness, and scaling, and the patients' own assessments of the overall response to treatment--were sought at weeks 2, 4, and 6. Both treatments significantly reduced the PASI scores and the investigator's assessment scores, but at each visit the PASI score was significantly (p less than 0.001) lower with calcipotriol than with betamethasone. At 6 weeks the mean PASI reduction was 68.8% with calcipotriol and 61.4% with betamethasone (95% confidence interval for difference 5.1-9.8, p less than 0.001). The scores for erythema, thickness, and scaling were significantly (p less than 0.001) lower with calcipotriol than with betamethasone at the end of treatment. The patients considered that 82.1% of calcipotriol-treated sides and 69.3% of betamethasone-treated sides had improved greatly or cleared up by the end of treatment (p less than 0.001). 57 adverse events were reported by 52 patients (15.1%). The most common adverse event, lesional/perilesional skin irritation, was slightly but not significantly (p = 0.12) more common with calcipotriol treatment. 15 (4.3%) patients were withdrawn from the study, 3 because of local adverse events. There were no changes in serum calcium during the study. Thus, calcipotriol ointment was superior to betamethasone valerate ointment in psoriasis vulgaris. Though long-term results are not yet available, calcipotriol holds great promise as an antipsoriatic agent.

Administration, Topical↗
PubMed1991

A comparative, multicenter, double blind trial of 0.05% halobetasol propionate ointment and 0.1% betamethasone valerate ointment in the treatment of patients with chronic, localized plaque psoriasis.

In a double-blind, parallel-group, multicenter comparative trial in 84 evaluable patients with severe, localized plaque psoriasis, 0.05% halobetasol propionate ointment proved significantly superior (p = 0.02) to 0.1% betamethasone valerate ointment with respect to the success rate, as indicated by ratings of "healed" or "marked improvement" (88.1% versus 64.3%). The therapeutic effect was observed within 5 days of the start of treatment in 76% and 67% of the patients treated with halobetasol propionate and betamethasone valerate ointments, respectively. Both preparations were well tolerated. Minor adverse effects at the site of application were reported in only 2% of the patients in each treatment group. Neither skin atrophy nor systemic adverse effects were observed.

Adult↗
PubMed1992

Comparative study of calcipotriol (MC 903) ointment and betamethasone 17-valerate ointment in patients with psoriasis vulgaris.

BACKGROUND: Topical vitamin D analogues have been reported to be an effective treatment in patients with psoriasis. Comparative studies with existing treatments are required. OBJECTIVE: Our purpose was to compare the effectiveness of calcipotriol (50 micrograms/gm) and betamethasone 17-valerate (1 mg/gm) ointments twice daily in the treatment of stable plaque psoriasis. METHODS: This study was a randomized, double-blind comparison over 6 weeks in 409 patients. Efficacy, as measured by the Psoriasis Area and Severity Index (PASI), and safety were assessed at 2, 4, and 6 weeks. RESULTS: Reduction of PASI was statistically significant at all time points for both treatments but there were no significant between-treatment differences. At the completion of 6 weeks of treatment, the mean PASI reduction was 5.50 for calcipotriol and 5.32 for betamethasone (95% confidence interval [CI] -0.40 to 0.78). Analysis of patient assessment at 6 weeks showed clearance or marked improvement in 61.2% of the calcipotriol patients and 50.5% with betamethasone (95% CI 1.4 to 20.8). Calcipotriol produced significantly more local side effects (19.5% compared with 3.9%, p less than 0.001); however, these were minimal leading to withdrawal in only 3 of 205 patients. CONCLUSION: Calcipotriol ointment was as effective as betamethasone 17-valerate ointment as measured by the PASI and superior as measured by self-assessment in patients with stable plaque psoriasis. Both treatments were well tolerated.

Betamethasone Valerate↗
PubMed1980

Estradiol valerate therapy and the renin--aldosterone system in castrated women.

The effect of estradiol valerate (Progynova, 2 mg daily) on the renin--aldosterone system was studied in nine women after bilateral oophorectomy. Plasma renin activity (PRA) and the daily urinary excretion of aldosterone (dU-Ald) were determined 4 mth after the operation -- during which no estrogen was given -- and after 3 mth on estrogen therapy. Plasma estradiol concentration rose in 7 subjects to the normal postovulatory level. No changes were found in PRA or dU-Ald. The results suggest that an effective estradiol valerate therapy is not accompanied with activation of renin--aldosterone system, while synthetic and non-human natural estrogens (Premarin) were shown earlier to increase PRA.

Aldosterone↗
PubMed1979

High-performance liquid chromatographic assay of betamethasone 17-valerate and its degradation products.

A high-performance liquid chromatographic assay of betamethasone 17-valerate is described. The procedure may be use for quantitative assay of the degradation products, betamethasone 21-valerate and betamethasone, and the application to the analysis of ointments is described. The method is also suitable for the determination of the kinetics of decomposition from one experimental run, and the determination of rate constants from a four-compartment sequential reaction is described. The procedure is also applicable to other corticosteroids, and hydrocortisone 17-butyrate, hydrocortisone 21-butyrate, and hydrocortisone may similarly be determined without modification to the method.

Betamethasone↗
PubMed1976

A clinical study of the prophylactic use of betamethasone valerate and sodium cromoglycate in the treatment of seasonal allergic rhinitis.

The prophylactic use of betamethasone valerate and sodium cromoglycate in seasonal allergic rhinitis has been investigated in 20 patients in an open study. The subjective assessment of the symptoms recorded on a daily record card was significantly lower in the betamethasone valerate group compared with the sodium cromoglycate group. Patients' and physician's overall assessment of the treatment favoured the steroid aerosol. No clinically significant side effects were noted.

Aerosols↗
PubMed1998

Comparison of calcipotriol monotherapy and a combination of calcipotriol and betamethasone valerate after 2 weeks' treatment with calcipotriol in the topical therapy of psoriasis vulgaris: a multicentre, double-blind, randomized study.

A clinical study was conducted to determine whether, in the topical treatment of psoriasis, a combination of calcipotriol and betamethasone valerate after previous treatment with calcipotriol alone was more effective than the continuation of the monotherapy with calcipotriol, especially in 'low responders'. Patients (n = 169) with the clinical diagnosis 'chronic plaque-type psoriasis' were treated twice daily for 2 weeks with calcipotriol, followed by a 4-week treatment with calcipotriol monotherapy in 87 patients or combined calcipotriol/betamethasone valerate in 82 patients; all patients were followed for 8 weeks. The psoriasis area and severity index (PASI) was used to compare the two treatment groups. The overall therapeutic result was also assessed by the investigators and patients. The combination therapy was more effective, as assessed by all evaluated variables; moreover, patients showing insufficient response to calcipotriol alone after 2 weeks showed a regression of psoriatic lesions using the combination regimen. Thus, the combination of calcipotriol and topical steroids is recommended as the therapy of first choice for patients who do not respond well to treatment with 2 weeks of calcipotriol alone. Furthermore, this combination reduces the hazards associated with the long-term use of topical corticosteroids (atrophy and rebound) as well as the irritation associated with calcipotriol.

Adolescent↗
PubMed2003

Efficacy of betamethasone valerate foam formulation in comparison with betamethasone dipropionate lotion in the treatment of mild-to-moderate alopecia areata: a multicenter, prospective, randomized, controlled, investigator-blinded trial.

BACKGROUND: Betamethasone valerate foam (BVF) is a new topical corticosteroid formulation. In scalp psoriasis patients BVF has induced a significantly greater clinical improvement in comparison with corticosteroid lotions. No data are available to date regarding the efficacy and safety of BVF in mild-to-moderate alopecia areata (AA). STUDY AIM: To evaluate the efficacy, tolerability and safety of BVF treatment in patients with mild-to-moderate AA. SUBJECTS AND METHODS: Sixty-one patients (26 men and 35 women; mean age 41 +/- 13 years) with mild-to-moderate AA (hair loss < 26%) were enrolled in a parallel-group, investigator-blinded trial. Subjects were assigned randomly to BVF (31 patients) or to betamethasone dipropionate lotion (BDL) (30 subjects). Both treatments were applied to the affected areas twice a day for 12 consecutive weeks. OUTCOMES: The primary study outcome was to compare the hair regrowth rate. Efficacy was evaluated at weeks 8 and 12 and at follow up (week 20), using a hair regrowth score (RGS) with a scale ranging from 0 (regrowth < 10%) to 4 (regrowth > 75%). RESULTS: Fifty-seven subjects (93%) completed the trial. At week 20, the RGS was 3.1 +/- 1.5 and 1.8 +/- 1.6 in the BVF and BDL groups, respectively (P < 0.01). A RGS > 3 was observed in 61% of patients in the BVF group (19/31) in comparison with 27% (8/30) in the BDL group (P < 0.03). No serious adverse events were observed in both groups during the study. CONCLUSION: Betamethasone valerate foam has shown to be an effective and well-tolerated treatment of mild-to-moderate AA. Further trials are warranted to evaluate the role of this new formulation in comparison or in combination with intralesional corticosterioids in AA treatment.

Administration, Topical↗
PubMed1976

The response of psoriasis to betamethasone valerate and clobetasol propionate. A 6-month controlled study.

Twelve patients with symmetrical psoriasis were studied for a period of 6 months. Clobetasol propionate 0-05% ointment was applied to the lesions on one side and betamethasone valerate 0-1% ointment to those on the other side as a double-blind controlled trial of these two treatments. All the patients showed a relative improvement on the side treated with clobetasol propionate. Clobetasol propionate-treated lesions tended to clear for longer than the corresponding betamethasone valerate treated lesions. The condition of five of the patients was better at the end of the study period than at the beginning.

Adult↗
PubMed1981

Six-month controlled study of effect of desoximetasone and betamethasone 17-valerate on the pituitary-adrenal axis.

Twenty-two patients were treated with desoximetasone emollient cream 0.25% twice daily without occlusion for 6 months. Patients applied the medication to approximately one-third of their body over psoriatic lesions. Corticosteroid plasma cortisol values decreased to below normal limits in nine patients before the 6-month study was terminated. In four of these the plasma cortisol spontaneously returned to normal despite therapy; in four other patients, however, the plasma cortisol was still suppressed at the end of 5 months of continual therapy but returned to normal within 7 days of discontinuation of the medication. In one patient, lost to further follow-up at 5 1/2 months of therapy, the trend at the fourth month was an increase in plasma cortisol to within one unit of normal range. Betamethasone 17-valerate 0.1% cream applied twice daily did not suppress plasma cortisol in twenty-three patients similarly tested. The clinical response to desoximetasone emollient cream was significantly better than to betamethasone valerate cream. This study closely approximates the way in which many patients with steroid-responsive dermatoses use potent topical steroids, namely over a long time period and without occlusion.

Adolescent↗
PubMed1993

Topical betamethasone-17-valerate inhibits heat-induced vasodilatation in man.

Topical betamethasone-17-valerate inhibits the vasodilatation response to local non-pathological heating of rat skin. We have shown that this effect can also be demonstrated in man. Topical betamethasone-17-valerate significantly inhibited the increase in human forearm cutaneous blood flow in response to heat of 44 degrees C, as measured by laser-Doppler velocimetry. This suggests that the effects of topical steroids upon skin blood flow in the rat and in man are similar, and supports the use of the animal model as a paradigm for studying human skin blood flow, and changes in response to anti-inflammatory steroids.

Administration, Topical↗