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At least 19 recordsLinked to original sources
PubMed1993

In vitro percutaneous permeation of betamethasone and betamethasone 17-valerate.

The percutaneous permeation and sorption isotherm (equilibrium) profiles of betamethasone and betamethasone 17-valerate were estimated in an in vitro study with excised human skin. Corticosteroids were measured by HPLC. The stratum corneum (dry weight)/water partition coefficient of betamethasone 17-valerate was 20 times greater than that of betamethasone. Nevertheless, when aqueous saturation was maintained in the donor solution, the mean steady-state flux of betamethasone 17-valerate through split-thickness skin was 57.6 ng/cm2/h, whereas that of betamethasone was 15.2 ng/cm2/h. This was presumably because the aqueous saturation concentration of betamethasone (60 micrograms/mL) was 11 times greater than that of betamethasone 17-valerate (5.4 micrograms/mL), so that the calculated saturation concentrations of the two corticosteroids in stratum corneum were within a factor of 2. However, the drug amounts or concentrations of the more lipophilic corticosteroid (betamethasone 17-valerate) attained in viable layers (viable epidermis and dermis) at steady state were predicted to be greater than those of the less lipophilic corticosteroid (betamethasone) when the results in the permeation and equilibrium studies were interpreted by a mathematical model. The drug distribution pattern predicted (i.e., that a more lipophilic corticosteroid preferentially partitions into viable layers) was reasonable when compared with that observed in the permeation study. The mean drug amount of betamethasone 17-valerate in dermis was four times greater than that of betamethasone, whereas the drug amounts of both corticosteroids in epidermis were similar to each other.

Adolescent↗
PubMed1986

Studies on the effects of betamethasone, L-carnitine, and betamethasone-L-carnitine combinations on the dipalmitoyl phosphatidylcholine content and phosphatidylcholine species composition in foetal rat lungs.

Administration of L-carnitine or betamethasone to pregnant rats failed to increase either the total phospholipid or dipalmitoylphosphatidylcholine (DPPC) contents in foetal rat lungs on the 20th day of gestation, compared to controls. The combined administration of betamethasone (0.3 mg/kg) and L-carnitine (80 mg/kg) resulted in a pronounced increase of dipalmitoylphosphatidylcholine (7.8 +/- 2.5 mg/g dry weight) compared with the control group (5.4 +/- 1.8 mg/g dry weight), and compared with the groups receiving betamethasone (5.9 +/- 1.9 mg/g dry weight) or L-carnitine (5.6 +/- 1.5 mg/g dry weight) alone. The proportion of dipalmitoylphosphatidylcholine in the phosphatidylcholine species increased from 20.9 +/- 2.1% in the foetal lungs of the control group to 22.6 +/- 5.0% in the L-carnitine group, to 24.3 +/- 3.3% (p less than 0.01) in the betamethasone-L-carnitine (20 mg/kg) group, to 25.2 +/- 3.5% (p less than 0.01) in the betamethasone group, to 27.1 +/- 2.6% (p less than 0.01) in the betamethasone-L-carnitine (40 mg/kg) group, and to 28.4 +/- 3.7% (p less than 0.01) in the betamethasone-L-carnitine (80 mg/kg) group, while the palmitic acid portion in the phosphatidylcholine fatty acids was nearly unchanged. A pronounced increase of palmitoyl-myristoyl phosphatidylcholine (PC-30), the second disaturated phosphatidylcholine species present in lungs in significant amounts beside dipalmitoylphosphatidylcholine, was noted only in betamethasone treated animals. Furthermore, after betamethasone and betamethasone-L-carnitine treatment, a significant diminution (p less than 0.01) of the proportion of palmitoyl-palmitoleyl phosphatidylcholine (16 : 0/16 : 1-PC) in the phosphatidylcholine species was demonstrated.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1996

Effects of prenatal treatment with betamethasone, L-carnitine, or betamethasone-L-carnitine combinations on the phosphatidylcholine content and composition of the foetal and maternal rat lung.

Pregnant rats received 0.10 or 0.20 mg/kg body weight betamethasone, or 100 mg/kg body weight L-carnitine, or L-carnitine 100 mg/kg plus betamethasone 0.05 or 0.10 mg/kg body weight, or saline (controls) for three days before delivery of foetuses at day 19 of gestation. Dose-related effects on the dipalmitoyl phosphatidylcholine content and the phosphatidylcholine species composition of foetal and maternal lungs were determined. Betamethasone (0.10 and 0.20 mg/kg) or L-carnitine (100 mg/kg) significantly increased (p < 0.05) the dipalmitoyl phosphatidylcholine content in the foetal lungs, while only small changes were found in relative terms. Combinations of betamethasone (0.05 or 0.10 mg/kg) with L-carnitine (100 mg/kg) also significantly increased the dipalmitoyl phosphatidylcholine content of the foetal lungs above control values (p < 0.01) and above the values achieved with betamethasone alone (p < 0.05). In the maternal lungs a significant increase of the dipalmitoyl phosphatidylcholine content above the control values was only found after treatment with betamethasone-carnitine combinations, whereas compared with the foetal lung the relative increase of dipalmitoyl phosphatidylcholine as a fraction of total phosphatidylcholine was more pronounced after betamethasone treatment. The gas chromatographic method used separates two monoenoic phosphatidylcholine species with 32 carbon atoms in the acyl residues. These two phosphatidylcholine species showed striking differences between adult and foetal lungs. Palmitoleyl palmitoyl phosphatidylcholine predominates in the maternal lung, whereas palmitoyl palmitoleyl phosphatidylcholine is the major monoenoic phosphatidylcholine species with 32 carbon atoms in the foetal lung. These two species were not affected in maternal or foetal lung by betamethasone or L-carnitine treatment. In contrast, after treatment with betamethasone-carnitine combinations, a significant increase of the fraction of palmitoyl palmitoleyl phosphatidylcholine was found in foetal but not in the maternal lung. The results of the present study demonstrate that maternal glucocorticoid and carnitine treatment affects the maternal as well as the foetal lung but with different effects on the dipalmitoyl phosphatidylcholine content and phosphatidylcholine species composition.

1,2-Dipalmitoylphosphatidylcholine↗
PubMedDate not supplied

[L-carnitine-betamethasone combination therapy versus betamethasone therapy alone in prevention of respiratory distress syndrome].

In this prospective randomised study the effects of antenatal treatment with a low dose betamethasone (2 mg/1 day)-L-carnitine (4 g/5 days) combination were compared with those of a high dose betamethasone, given alone (8 mg/2 days) on the prevention of respiratory distress syndrome (RDS) and mortality in preterm infants. One-hundred women entering the trial gave birth to 109 liveborn infants, 55 in the betamethasone group (A), 54 in the betamethasone-L-carnitine combination group (B). Eight of the 55 (14.5%) infants in group A developed RDS, four of the 54 (7.3%) in group B, which was significantly more (p < 0.05), although in group B the betamethasone dose was dramatically reduced. The mortality also was significantly lower after treatment with a betamethasone-L-carnitine combination compared to betamethasone alone (4 of 55 infants or 7.3% in group A versus 1 of 54 infants or 1.8% in group B, p < 0.05). The present results demonstrate that in combination with L-carnitine, the betamethasone dose is markedly reducible with a concomitant significant reduction of the incidence of RDS and mortality of premature newborns.

Betamethasone↗
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↗
PubMed1989

[Antiemetic efficacy of betamethasone versus betamethasone combined with metoclopramide in cisplatin-treated cancer patients].

This study was designed to compare the antiemetic effect of betamethasone alone with that of betamethasone combined with metoclopramide. Forty-seven patients on chemotherapeutic regimens including cisplatin were entered into this study. Betamethasone was given in 4 doses of 20 mg/body at 30 minutes before and at 2.5 and 8 hours after cisplatin. Metoclopramide was given in 4 doses of 1mg/kg on the same schedule. Within 24 hours after the administration of cisplatin, no vomiting was observed in 42.9% of the patients treated with betamethasone alone and in 76.9% with betamethasone and metoclopramide. Betamethasone combined with metoclopramide was superior to betamethasone alone for the antiemetic effect in cisplatin-treated patients.

Adult↗
PubMed1999

[Prenatal induction of lung maturation in the fetus. Betamethasone versus betamethasone+thyrotropin-releasing hormone].

During the period from May 1, 1994 till December 31, 1997 at the First and Second Departments of Gynaecology and Obstetrics Masaryk University Brno 311 neonates with birthweights from 500 to 2000 g were born. A retrospective study was made comparing neonatal results of three methods of prenatal induction of maturing of surfactant in premature neonates. The first group was without treatment, in the second group only betamethasone was administered and in the third group betamethasone and thyrotropin releasing hormone (TRH). The neonates were divided into three body weight groups: 500-999 g, 1000-1499 g and 1500 g and more. The most favourable results with administration of betamethasone and TRH were obtained in the group weighing 500-999 g. This pertained to the smaller number of post-partum administration of surfactant, reduction of the oxygenation index and period of artificial pulmonary ventilation. IVth grade RDS and other complications in the child. In the group of neonates weighing 1000-1499 g administration of betamethasone and TRH had a positive effect only on the oxygenation index and grade of RDS. In the group of neonates with weights above 1500 there were no statistically significant differences between the described three groups. It may be concluded that the greatest effectiveness was achieved by a combination of betamethasone and TRH in neonates weighing 500-999 g, this combination was less effective in the group weighing 1000-1499 g and without effect in those weighing 1500 g or more.

Betamethasone↗
PubMed1980

Simultaneous determination of betamethasone, betamethasone acetate and hydrocortisone in biological fluids using high-performance liquid chromatography.

A sensitive, specific, reproducible and rapid high-performance liquid chromatographic method for the simultaneous quantitation of betamethasone, betamethasone 21-acetate and hydrocortisone in biological fluids is described. Hydrocortisone acetate is used as an internal standard and the samples are extracted with dichloromethane before chromatographing on a reversed-phase system. Detection at two ultraviolet wavelengths (254 nm and 240 nm) was used to assess the specificity of the system, and the sensitivity was found to be greater than 10 ng for all steroids. The speed with which this assay can be performed makes it particularly useful for pharmacokinetic studies, and plasma concentration--time profiles resulting from the administration of betamethasone phosphate and betamethasone acetate are presented.

Betamethasone↗
PubMed1976

A comparison of betamethasone benzoate gel and betamethasone valerate cream.

One hundred and twenty-one patients were treated in a double-blind fashion with .025% betamethasone benzoate gel and 0.1% betamethasone valerate cream. Results were not statistically significant, although 14 of 16 patients with psoriasis showed excellent results with betamethasone benzoate gel, as opposed to six of 14 patients given betamethasone valerate cream.

Betamethasone↗
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↗
PubMed1985

Effect of betamethasone and betamethasone with neomycin nasal drops on human nasal mucociliary clearance and ciliary beat frequency.

The effects of two topical nasal preparations on human nasal ciliary beat frequency in vitro and on nasal mucociliary clearance in vivo were investigated. Betamethasone and betamethasone with neomycin drops were found to be ciliotoxic when ciliated epithelium was exposed to them in vitro, mainly owing to the effects of the preservatives benzalkonium chloride and thiomersal. The nasal mucociliary clearance and in vitro ciliary beat frequency of nasal ciliated epithelium taken from healthy subjects were not adversely affected after topical application; neither did treatment with betamethasone, with or without neomycin, for four weeks affect these indices in two groups of patients with rhinitis. Thus, despite a ciliotoxic effect when ciliated epithelium is exposed to these preparations in vitro, they do not affect nasal clearance or ciliary beat frequency (as measured in vitro) adversely when administered topically to the nose.

Administration, Intranasal↗
PubMed1980

[Effects of betamethasone 17-propionate and betamethasone on hypothalamo-pituitary-adrenal cortex axis in rats (author's transl)].

Effects of betamethasone, 17, 21-dipropionate (BMDP) and betamethasone (BM) on hypothalamo-pituitary-adrenal cortex axis following the intravenous or subcutaneous administration were studied in rats. The active site of the main metabolite of BMDP -- betamethasone 17-propionate (BMP) -- and BM was investigated by the stereotaxical implantation of these glucocorticoids. The ether-induced increase of plasma corticosterone was not suppressed by intravenous administration of BMDP in a dose of 300 mu g/kg, but BM suppressed this increase at doses over 10 mu g/kg. Subcutaneous administration of a large amount of these steroids (BMDP, 20 mg/kg; BM, 16 mg/kg) induced a significant suppression of the ether-induced plasma corticosterone increase. The implantation of the main metabolite of BMDP--BMP--into the anterior or medial hypothalamic area and septum was effective in significantly reducing the ether-induced increase of plasma corticosterone. BMP implants into the posterior hypothalamus or pituitary gland proved to be ineffective. In contrast, BM, when placed into the hypothalamic area (anterior, medial or posterior), septum or pituitary, lowered the plasma corticosterone levels.

Animals↗
PubMed1993

Comparison of the bioactivity of mometasone furoate 0.1% fatty cream, betamethasone dipropionate 0.05% cream and betamethasone valerate 0.1% cream in humans. Inhibition of UV-B-induced inflammation monitored by laser Doppler blood flowmetry.

The bioactivity of a novel topical glucocorticosteroid, mometasone furoate 0.1% fatty cream was compared with betamethasone dipropionate 0.05% cream and betametasone valerate 0.1% cream. An ultraviolet light (UV-B)-induced inflammation assay in humans was used, and the combined effect of a single, open application of the corticosteroids was evaluated. Reduction of UV-B induced inflammation was monitored by laser Doppler blood flowmetry, clinical skin scoring and skin reflectance spectrophotometry. Skin scoring and reflectance spectrophotometry were found unsuitable because one of the cream vehicles contained titanium dioxide which shielded skin erythema. Laser Doppler blood flowmetry showed that mometasone furoate 0.1% fatty cream was more than twofold better in reducing UV-B-induced inflammation than betamethasone dipropionate 0.05% cream and betametasone valerate 0.1% cream, and that the effect was sustained for at least 24 h after a single application.

Administration, Topical↗
PubMed1978

[Irritative activity of antiinflammatory agents, betamethasone 17-valerate, beclomethasone 17, 21-dipropionate, betamethasone 17, 21-dipropionate, or indomethacin on the gastrointestinal tract in rats and dogs (author's transl)].

Irritative effects of three steroidal anti-inflammatory drugs on the gastrointestinal tract of rats and dogs were determined. With either single or repeated subcutaneous administration these drugs dose dependently irritated the gastric mucosa of both species. The intestinal mucosa was less affected. Concomitant oral administration of aspirin or subcutaneous administration of indomethacin revealed an aggravation of aspirin-induced gastric ulcers by betamethasone valerate and inhibition of indomethacin-induced intestinal ulcers by beta-methasone dipropionate. These two steroidal drugs had no noxious effect on healing of chronic gastric ulcers induced in rats and dogs. Betamethasone valerate, however, delayed the healing of gastric ulcer in rats. Indomethacin, a non-steroidal anti-inflammatory drug, also induced serious damage to the gastric and intestinal mucosa both of rats and dogs. Indomethacin ingestion delayed the healing of chronic gastric ulcer in rats but not in dogs. Since both steroidal and non-steroidal drugs induce damage to the gastrointestinal tract, a careful monitoring of the patients' complaints should be carried out when these compounds are used as a systemic treatment. Steroidal drugs used in this study, however, appear to be highly safe from the point of dose inasmuch as they are used as a topical treatment.

Animals↗
PubMed1986

Fusidic acid-betamethasone combination in infected eczema: an open, randomized comparison with gentamicin-betamethasone combination.

Ninety-nine patients with secondarily infected eczema were allocated at random to receive 10-days' treatment with either 2% fusidic acid plus 0.1% betamethasone cream or 0.1% gentamicin plus 0.1% betamethasone cream. Both preparations were applied to the lesions twice daily and assessment of the signs and symptoms was carried out before, after 2 to 4 days, and after 7 to 12 days of treatment, severity being rated on a 4-point scale. Bacteriological tests were carried out before and after treatment. The results showed that the combination with fusidic acid was marginally superior in clinical effect. Staphylococcus aureus was the most commonly isolated pathogen from eczematous lesions (86%) and fusidic acid showed the lowest resistance rate (9%), followed by gentamicin (21%). Chloramphenicol, neomycin and tetracycline showed resistance rates from 48% to 59%.

Adult↗
PubMed2003

Immediate and delayed effects of antenatal corticosteroids on fetal heart rate: a randomized trial that compares betamethasone acetate and phosphate, betamethasone phosphate, and dexamethasone.

OBJECTIVE: The purpose of this study was to evaluate the role of different formulations and different administration kinetics of antenatal corticosteroid therapy on fetal heart rate. STUDY DESIGN: One hundred five patients who were at high risk for preterm delivery were assigned randomly to receive two injections of betamethasone acetate + phosphate, four injections of betamethasone phosphate, or four injections of dexamethasone phosphate. Computerized fetal heart rate was recorded daily through day 4. RESULTS: The three formulations did not differ in their effect on fetal heart rate, which varied significantly as a function of the time of injection. During treatment (day 0-day 1), fetal heart rate variability increased (+9%, P <.05), as did the number of fetal movements felt by the mother (+60% at day 0, P <.001). After treatment (day 2-day 3), variability fell significantly (-14%, P <.01), as did accelerations (-35% at day 2, P <.01). No modifications were still detectable on day 4. CONCLUSION: Antenatal corticotherapy is responsible for two different phases of fetal heart rate modifications that do not vary according to the corticosteroid or the dosage regimen.

Betamethasone↗
PubMed1983

[Therapy of erythrosquamous dermatoses. Betamethasone dipropionate plus salicylic acid in comparison with betamethasone dipropionate solution].

Efficacy and tolerance of an alcoholic solution containing 0.64 mg betamethasone-dipropionate plus 20 mg salicylic acid (Diprosalic Solution) were compared with an alcoholic solution containing 0,64 mg betamethasone-dipropionate in a 3 week double blind study in 100 patients with psoriasis and other steroid-responsive dermatoses of dry nature, comprising scalp and other hairy and non-hairy areas of the body. This double blind study was followed by a 3 week open study in another 100 patients with similar diagnosis, using Diprosalic Solution only. Although the therapeutic results of the double blind study showed no significant differences between both treatment groups, distinct advantages of the drug containing salicylic acid could be clearly demonstrated, such as: 1. More rapid onset of action, 2. rapid clearing of scaling, pruritus and inflammation, 3. these advantages are in compliance with the fact that topically applied salicylic acid softens keratin, loosens cornified epithelium and desquamates the epidermis, making the underlying layers more accessible to the antiinflammatory steroid.

Administration, Topical↗
PubMed1991

Betamethasone-dixyrazine versus betamethasone-metoclopramide as antiemetic treatment of cisplatin-doxorubicin-induced nausea in ovarian carcinoma patients.

In a prospective and randomized pilot study two antiemetic regimens comprising dixyrazine (240 mg) and metoclopramide (10 mg/kg) in high doses and given by continuous i.v. infusion were compared as means of preventing cisplatin-doxorubicin-induced nausead and vomiting. Twenty chemotherapy-naive women with the diagnosis of ovarian carcinoma stages III-IV (FIGO) were included in the study. Medium doses (50 mg/m2) of cisplatin and doxorubicin were used. The antiemetic drugs (the above-mentioned ones plus betamethasone 20 mg, and biperiden 5 mg) were administered by small portable infusion pumps during 24 hours. The effects and adverse reactions were evaluated during the course of chemotherapy and the first week thereafter. Complete protection from nausea during the first 24 hours was achieved in 80% by the metoclopramide cocktail and in 50% by the dixyrazine combination. During days 2-7 there were no significant differences between the two regimens. Vomiting was not satisfactorily prevented by either treatment. Sedation was significantly more common after dixyrazine than after metoclopramide but other recorded side effects were similar for the two antiemetic regimens. Serum concentrations of dixyrazine and metoclopramide were determined.

Activities of Daily Living↗