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At least 667 records · Page 37Linked to original sources
PubMed1999

Betamethasone valerate foam 0.12%: a novel vehicle with enhanced delivery and efficacy.

BACKGROUND: A new topical formulation of betamethasone valerate (BMV) with enhanced dermal penetration has been developed. OBJECTIVE: These studies were designed to evaluate: (1) the relative bioavailability of BMV foam, and (2) the safety and efficacy of BMV foam in the treatment of scalp psoriasis as compared to a lotion formulation of BMV and placebo. METHODS: Safety and efficacy were evaluated in a randomized, multicenter, double-blind, active-and placebo-controlled trial in adult patients with moderate to severe scalp psoriasis. A separate study in 18 patients was conducted to evaluate the potential for suppression of the hypothalamic-pituitary-adrenal (HPA) axis. Relative bioavailability was measured using the human cadaver skin model. RESULTS: 72% of patients using BMV foam were clear or almost clear of disease at the end of 28-days of treatment as judged by the investigator's global assessment of response. Only 47% of BMV lotion patients and 21% of placebo showed a similar level of response. There was no evidence of increased toxicity or HPA-axis suppression for BMV foam, but assessment of relative bioavailability showed BMV penetration into the skin to be more than two-fold greater than from BMV lotion. CONCLUSIONS: A novel foam formulation with enhanced BMV bioavailability has been shown to be of increased efficacy in the treatment of scalp psoriasis without an associated increase in toxicity.

Administration, Cutaneous↗
PubMed2002

Clinical effects of betamethasone and hyaluronan, and of defocalized carbon dioxide laser treatment on traumatic arthritis in the fetlock joints of horses.

The clinical effects of intra-articular betamethasone together with hyaluronan (betaM/HA) and treatment with a defocalized carbon dioxide laser on acute traumatic arthritis of the fetlock joint were assessed. The horses in these studies were selected using a thorough lameness examination, including intra-articular anaesthesia abolishing the lameness. This investigation comprised an observer-blind study, including 10 sport horses (10 joints), and a prospective study, including 180 sport horses (333 joints). In both studies, the material was divided into two groups treated with either betaM/HA or a carbon dioxide laser. The treatment doses were 12 mg of betaM, 20 mg of HA or 60 J/cm2 of treated area. Convalescence before training was 21 days for both groups in the observer-blind study. In the prospective study, convalescence in the betaM/HA group was 21 days but was only 7 days for the laser-treated group. In the observer-blind study, three of five treated joints recovered in both cohorts. In the prospective study, the groups had significantly different recovery rates--68% of the betaM/HA-treated joints and 80% of the carbon dioxide laser-treated joints. These results indicate that the defocalized carbon dioxide laser should be an applicable mode of treatment of acute traumatic synovitis in horses. However, the biochemical functions related to carbon dioxide laser treatment require further elucidation.

Adjuvants, Immunologic↗
PubMed1989

Comparison of effects of verapamil, low calcium diet and betamethasone on duodenal calcium absorption efficiency in the chick.

The results indicate that oral administration of verapamil for 2 weeks to the chick is followed by an increase in the efficiency of the duodenal absorption of calcium. In these chicks both a decrease in serum calcium level and an increase in the activity of renal 1 alpha-hydroxylase were observed. The increased calcium absorption following prolonged treatment with verapamil resembles that induced by a low calcium diet. The mechanism of both responses presumably involves an increased production of 1,25-dihydroxyvitamin D3. Both verapamil- and low calcium diet-induced adaptations are capable of overcoming the inhibitory action of betamethasone on intestinal calcium absorption. No effects on calcium absorption were noted if verapamil was administered intraperitoneally which suggests that verapamil exerts its action directly on the intestinal mucosa.

25-Hydroxyvitamin D3 1-alpha-Hydroxylase↗
PubMed2002

Fluticasone propionate spray and betamethasone sodium phosphate mouthrinse: a randomized crossover study for the treatment of symptomatic oral lichen planus.

BACKGROUND: Symptomatic oral lichen planus (OLP) has been palliated with a wide spectrum of topical and systemic therapies. Although the majority of management strategies include corticosteroids, few have been evaluated in randomized controlled trials. OBJECTIVE: We investigated the acceptability and efficacy of topical fluticasone propionate spray (FP) and betamethasone sodium phosphate mouthrinse (BSP) upon the signs and symptoms of OLP, assessing patient quality of life changes as a consequence of these therapies. METHODS: We implemented a randomized, crossover study in which each drug was administered for a period of 6 weeks with an intervening washout period of 2 weeks at an outpatient oral medicine unit in London, United Kingdom. We treated 48 patients with biopsy-proven symptomatic OLP, and 44 patients (92%) completed the study. The dosage was 50 microg two dose unit sprays and BSP 500 microg, each 4 times daily. Symptomatic improvement was evaluated by means of a visual analogue scale (VAS), the McGill pain score, the Oral Health Impact Profile (OHIP), and Oral Health Quality of Life (OHQoL) questionnaires. The total surface area of the lesions, including all white, erythematous, and ulcerative lesions was measured at each visit. The efficacy, ease of application, and adverse effects associated with each medication were recorded. RESULTS: Both FP and BSP mouthwash caused both a statistically significant reduction in painful symptoms as measured by the VAS and improvement in quality of life as measured by the OHIP and OHoQL indices. There was no significant difference between the two corticosteroids in their efficacy in reducing painful symptoms (measured by the VAS) or in their effect on patient quality of life. Both FP and BSP significantly reduced the surface area of oral lesions. However, FP was statistically significantly better than BSP in reducing lesion surface area. There was no statistically significant difference between the patient-assessed effects of the 2 therapies. CONCLUSIONS: FP and BSP are both effective in the short-term clinical management of symptomatic OLP. FP is more acceptable to patients than BSP because of the convenience of the spray form.

Administration, Topical↗
PubMedDate not supplied

The characteristics of betamethasone-loaded chitosan microparticles by spray-drying method.

Betamethasone (BTM)-loaded microparticles prepared by a spray drying method using chitosan (CTS) as raw material, type-A gelatin and ethylene oxide-propylene oxide block copolymer (Pluronic F68) as modifiers. The BTM-loaded in varied chitosan/Pluronic F68/gelatin microparticle formulations was investigated. By properly choosing excipient type and concentration a high degree of control was achieved over the physical properties of the BTM-loaded microparticles. Microparticle characteristics (zeta potential, tap density, particle size and yield), loading efficiencies, microparticle morphology and in-vitro release properties were examined. Surface morphological characteristics and surface charges of prepared microparticles were observed by using scanning electron microscopy (SEM) and microelectrophoresis. A SEM micrograph shows that the particle sizes of the varied chitosan composed microparticles ranged from 1.1-4.7 microm and the external surfaces appear smooth. The BTM-loaded microparticles entrapped in the chitosan/Pluronic F68/gelatin microparticles with trapping efficiencies up to 93%, collected yield rate 44%, and mean particle size varied between 1-3 microm, positive surface charge (20-40 mv), and tap densities (0.04-0.40 g/cm3) were obtained. The collected BTM yield and size of particle was increased with increasing BTM-loaded amount but both zeta potential and tap density of the particles decreased with increasing BTM-loaded amount. The in vitro release of BTM showed a dose-dependent burst followed by a slower release phase that was proportional to the drug concentration in the concentration range between 5-30%w/w. The in vitro drug release from the chitosan/Pluronic F68/gelatin 1/0.1/0.4 microspheres had a prolong release pattern. These formulation factors were correlated to particulate characteristics for optimizing BTM microspheres in pulmonary delivery.

Anti-Inflammatory Agents↗
PubMed2005

Interconversion studies of betamethasone acetate polymorphs.

The polymorph interconversions of Betamethasone Acetate (BA) were studied under various pharmaceutical conditions, such as grinding, heating and suspending in water, based on differential scanning calorimetry, thermogravimetric analysis, and X-ray powder diffraction. There existed enantiotropic relationships between the three polymorphs of BA, which were named form II, Ialpha, and Ibeta work, respectively. It was concluded that form II was the most stable form when suspended in water.

Betamethasone↗
PubMed2006

Interconversion kinetic studies of betamethasone acetate polymorphs in water.

This study assessed the effect of polymers on the transformation of polymorphs of betamethasone acetate (BA) when suspended in water. The results showed that the polymers, in particular HPMC E5, retarded the transition of the forms Ialpha and Ibeta. However, the form Ialpha, as the metastable form, with the aid of HPMC E5, was preferred for BA suspension preparation through kinetic studies, while the form Ibeta was not suitable due to its instability in water.

Betamethasone↗
PubMed1997

The pathologic effects of intrathecal betamethasone.

STUDY DESIGN: The histopathologic effects of the intrathecal injection of betamethasone (Celestone Chronodose; Schering Corporation, Kenilworth, New Jersey) were assessed after the injection of various volumes of the preparation in 20 sheep. OBJECTIVE: To assess the safety of Celestone Chronodose injected into the intrathecal space. SUMMARY OF BACKGROUND DATA: The safety and efficacy of epidural steroid have received considerable attention in the medical literature in recent years. In Australia, reports of possible adverse effects of Depo-Medrol (methylprednisolone), including the complication of arachnoiditis, have been followed by statements from the manufacturers of commonly used steroid preparations recommending they should not be administered epidurally. Previous evidence suggests that arachnoiditis does not result from epidural administration of steroids, but may develop from the intrathecal administration of Depo-Medrol. There are no reports concerning the safety of Celestone Chronodose (beta-methasone). METHODS: Twenty-three adult merino sheep had lumbar punctures performed at the L6-S1 level, and different volumes of Celestone Chronodose or normal saline were injected into the subarachnoid space. The animals were killed after 6 weeks, and the spinal cord, meninges, and nerve roots of the lumbar spine were examined for evidence of pathologic changes. RESULTS: There were no abnormalities demonstrated in three sheep injected with up to 18 ml of normal saline solution. Eleven sheep injected with 1 ml (5.7 mg) of Celestone Chronodose even when repeated at weekly intervals (five sheep, three injections) did not demonstrate pathologic changes. One of six sheep injected with 2 ml of Celestone Chronodose and all of three sheep injected with greater volumes showed histopathologic changes of arachnoiditis. CONCLUSIONS: Given that the volume of cerebrospinal fluid in the sheep is approximately one third of that in humans, this study suggests that small volumes (up to 2 ml) of Celestone Chronodose injected intrathecally in humans are unlikely to cause arachnoiditis, but that the risk of this complication increases substantially with higher doses.

Animals↗
PubMed1994

Circadian activity of topical 0.05% betamethasone dipropionate in human skin in vivo.

The influence of treatment duration, vehicle, and time of day of application on topical 0.05% betamethasone dipropionate uptake into human stratum corneum and the resulting skin-blanching response was investigated in human subjects. Drug uptake into stratum corneum and the resulting skin color changes measured with a chromameter demonstrate an equilibrium delay. Maximal drug uptake occurred at 2 h, whereas maximal skin color changes occurred 6 h after a single application. Extent of decreased skin color was dependent on vehicle, treatment duration, and time of day of application. Time of maximal decreased skin color occurred at midnight independent of vehicle, treatment duration, or time of day of application. This time of maximal drug activity coincides with the well-known time period of lowest circulating cortisol concentrations (2000-0400 h). Application of a single 2- or 6-h dose of the 0.05% cream at 1600 h produced more extensive and prolonged changes in skin color over 24 h than a 0900-h application in the same subject. These data demonstrate that the extent and duration of topical corticosteroid activity in human skin is influenced by vehicle, treatment duration, and time of day of application. The prolonged changes in skin color measured with a single dose applied at 1600 h suggest that a once-a-day dosing regimen in the late afternoon may be sufficient for dermatologic therapy. Elucidation of these circadian responses with topical corticosteroids may provide a rational basis for the future re-evaluation of the appropriate therapeutic regimen with this class of drugs in dermatologic medicine.

Administration, Topical↗
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↗
PubMed1993

Oral mini-pulse therapy with betamethasone in vitiligo patients having extensive or fast-spreading disease.

BACKGROUND: Systemic corticosteroids can arrest the progression of vitiligo and lead to repigmentation in a significant proportion of patients, but may also produce unacceptable side effects. To minimize the side effects, we tried a new approach using mini-pulse therapy with betamethasone. METHODS: Forty patients having extensive and/or fast-spreading vitiligo were given 5 mg betamethasone/dexamethasone as a single oral dose after breakfast on 2 consecutive days per week. The response to treatment was evaluated by photographs taken every 2-4 months and recording the side effects. RESULTS: Within 1-3 months, progression of the disease was arrested in 89% of the 36 patients having active disease, while 2 patients needed an increase in the dose to 7.5 mg per day to achieve complete arrest of lesions. Within 2-4 months, 80% of the patients started having spontaneous repigmentation of the existing lesions which progressed with continued treatment. The extent of repigmentation varied in different patients and even in different lesions in the same patient. It was less than 10% in 14 (35%) patients and almost complete (> 90%) in three patients. The side effects included weight gain of 5 and 7 kg in two patients, mild headache in two patients, transitory general weakness for 2 days after the pulse in two patients, and bad taste in the mouth in three patients; 23 patients, including six children, had no side effects. CONCLUSIONS: Oral mini-pulse therapy with betamethasone/dexamethasone seems to be an effective treatment modality to arrest the progression of vitiligo. It also induces spontaneous repigmentation. It deserves to be tried on a large scale to evaluate its advantages over the currently available methods of treatment.

Administration, Oral↗
PubMed2004

Bioavailability of betamethasone dipropionate when combined with calcipotriol.

BACKGROUND: Calcipotriol and corticosteroids are commonly used treatments for psoriasis vulgaris, each with different mechanisms of action. The two agents have shown combined action, but current formulations do not permit simultaneous application. Daivobet (LEO Pharma, Denmark) ointment contains calcipotriol and the corticosteroid, betamethasone dipropionate. Such a formulation may provide convenience and enhanced activity compared with separate applications, but it is essential that the biological activity and bioavailability of either active agent is not adversely affected by the other component. OBJECTIVE: His study was designed to determine whether the bioavailability of the corticosteroid component of Daivobet was equivalent to that in a corticosteroid-only formulation (Diprosone, Schering-Plough Laboratories, France). METHOD: A vasoconstrictor assay measuring skin blanching was used to determine bioequivalence. RESULT: Skin blanching measured either by objective chromametric measurement or visual assessment showed Daivobet to be equivalent to Diprosone. CONCLUSION: The data indicate that the steroid component of Daivobet is not unfavorably affected by the calcipotriol.

Adolescent↗
PubMedDate not supplied

Outcome and recurrence in treatment of phimosis using topical betamethasone in children in Hong Kong.

AIM: To study the efficacy of treating phimosis with topical steroid, and its long-term outcome and side effects. We also looked into the effect of daily retraction and cleansing of prepuce on preventing recurrence of phimsosis. METHODS: This prospective study comprised 138 boys who were prescribed 0.05% betamethasone ointment (Diprocel) during 1 August 2001-31 July 2004. Five boys were excluded because of non-compliance. Of the remaining 133 boys, 108 were followed-up and assessed. Age ranged from 0.03 to 12.9 years (mean=3.38, SD=2.79). The number of treatment course received, short-term and long-term outcome, side effects and the effect of daily foreskin retraction were studied. RESULTS: The success rate of first treatment course was 81.5%, and 60.2% of boys remained free from phimosis upon latest assessment. The follow-up period ranged from 0.4 to 4.4 years (mean=2.45, SD=0.90). There were no side effects noted. We found a significant and linear relationship between daily foreskin retraction and sustained resolution of phimosis. CONCLUSION: Topical steroid is an effective and safe treatment for phimosis, especially when combined with a good hygiene practice of the foreskin with daily cleansing and retraction. A trial of topical steroid treatment should be offered upon considering circumcision.

Betamethasone↗
PubMed2006

A new formulation of an occlusive dressing containing betamethasone valerate 0.1% in the treatment of mild to moderate psoriasis.

BACKGROUND: Betamethasone valerate (BMV) is a medium-potency corticosteroid commonly used for the treatment of chronic psoriasis. Although occlusion has been shown to enhance the efficacy of BMV treatment, no ready-to-use occlusive BMV formulation is currently approved for the market. METHODS: Forty-two patients with mild to moderate psoriasis and with symmetrical lesions were treated with BMV 0.1% tape and BMV 0.12% cream for 30 days in a half-side distribution. Both treatments resulted in a significant clinical improvement. Efficacy and tolerability were evaluated by comparison of pre-treatment and post-treatment psoriasis area and severity index and self-administered psoriasis area and severity index scores, and by comparison of the changes from baseline in clinical appearance and hydration. RESULTS: Lesions treated with BMV 0.1% tape showed higher reductions from baseline in the psoriasis area and severity index and the self-administered psoriasis area and severity index scores (61.7% and 59.3%, respectively), compared with lesions treated with BMV 0.12% cream (39.5% and 34.0%, respectively). No serious local or systemic treatment-related adverse effects were reported. CONCLUSIONS: Our results indicate a higher efficacy of BMV 0.1% tape compared with BMV 0.12% cream in the treatment of mild to moderate chronic plaque psoriasis.

Administration, Cutaneous↗
PubMed1994

Comparative pharmacokinetics of two diastereoisomers dexamethasone and betamethasone in plasma and cerebrospinal fluid in rabbits.

The two diastereoisomers dexamethasone (DXM) and betamethasone (BTM) were infused at two different doses (2, 10 mg.kg-1) in anesthetized rabbits. Samples of plasma and cerebrospinal fluid were collected over a 180-min period. Steroid concentrations were measured by high performance liquid chromatography. The terminal half life (85.7 +/- 20.8 min and 102.2 +/- 29.6 min for DXM; 117.6 +/- 19.8 min and 118.5 +/- 15.8 min for BTM) and the mean residence time (121.4 +/- 27.7 min and 146.1 +/- 41.3 min for DXM; 168.6 +/- 28.1 min and 172.2 +/- 20.6 min for BTM) were unchanged between the doses. Dose-dependent changes in the area under the curve normalized by the dose, then volume distribution and clearance were observed. The average percentage of DXM and BTM bound to plasma proteins were 78.1 +/- 11.5% and 88.3 +/- 5.1% respectively at the lower dose, and decreased significantly with 10 mg.kg-1. DXM appeared more rapidly in the CSF, the highest concentrations of DXM were obtained within 15 min after the end of the injection. The CSF levels were lower than that of plasma unbound and the passage through the blood-brain barrier was saturable. These results will complicate pharmacokinetic and pharmacodynamic analysis.

Animals↗
PubMed1970

Recovery of hypothalamo-pituitary-adrenal function in the rat after prolonged treatment with betamethasone.

1. Betamethasone caused growth retardation, adrenal atrophy and impaired hypothalamo-pituitary-adrenal (HPA) activity in the rat.2. In spite of the profound impairment, recovery of normal HPA function was rapid, but the growth retardation persisted.3. The ability of the pituitary gland to secrete basal corticotrophin (ACTH), recovered more rapidly and the adrenocorticotrophic response to stress less rapidly than the ability of the adrenal cortex to respond to ACTH.4. The degree of HPA suppression was not determined by the total dose of steroid.5. The possible significance of the results is discussed.

Adrenal Glands↗
PubMed1971

Effects of stress and betamethasone on the production of corticosterone by the rat adrenal gland in vitro.

1. Production of corticosterone in vitro was studied using adrenal glands from rats which had been subjected to stress or treated with betamethasone.2. An increase in corticosterone production occurred in the first but not the second hour of incubation in adrenals removed immediately after stress. When the interval between stress and adrenalectomy was longer, the increased corticosterone production persisted.3. Betamethasone had no effect on corticosteroidogenesis in vitro when added directly to the incubation medium or when administered to rats shortly before removal of their adrenal glands.4. Corticosteroidogenesis in vitro was considerably reduced in the adrenals of rats given prolonged treatment with betamethasone.5. The significance of the results and the reliability of in vitro corticosteroid production as an index of hypothalamo-pituitary-adrenal activity is discussed.

Adrenal Glands↗
PubMed1984

Modification by betamethasone of the effects of bronchodilator drugs on cholinergic bronchoconstriction in rats.

Effects of betamethasone (BM), a long-acting glucocorticoid, given alone and in combination with bronchodilator drugs, terbutaline (Ter), theophylline (Theo), or ipratropium bromide (Ipra), were studied on dose-related methacholine (MeCh 2, 3, and 4.5 micrograms i.v.)-induced bronchoconstriction in anaesthetized rats. BM (0.4 or 2 mg kg-1) was given intraperitoneally 24 h before the experiment followed by a similar dose intravenously, 12 min before MeCh challenge. The bronchodilator drugs were given i.v. as acute single doses. BM 0.4 mg kg-1 counteracted significantly MeCh-induced bronchoconstriction without modifying MeCh-induced transient bradycardia and hypotension. BM 2 mg kg-1 failed to improve that response. A time interval of 24 h after pretreatment proved mandatory to produce these effects. Combined treatment with BM 0.4 mg kg-1 + Ter 20 micrograms kg-1 antagonized the MeCh-induced bronchoconstriction in an additive manner at 2 and 3 micrograms of MeCh, but a synergistic interaction was found at the largest MeCh dose. The effects of the other combinations (BM 0.4 mg kg-1 + Theo 20 mg kg-1 and BM 0.4 mg kg-1 + Ipra 0.5 microgram kg-1) on airways failed to exceed the expected sum of the individual drugs. The combination of BM + Ter was selective to the airways only, whereas BM + Theo also counteracted MeCh-induced bradycardia and BM + Ipra counteracted both hypotension and bradycardia. It is concluded that combined treatment with glucocorticoid and beta 2-adrenoceptor agonist may result in a synergistic interaction on severe airway obstruction without significant influence on cardiovascular system.

Animals↗