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At least 199 records · Page 11Linked to original sources
PubMed1998

Comparative study of reductive amination reaction on 5-(4-formyl-3,5-dimethoxyphenoxy)valeric acid and its monomethoxy analog using the Multipin approach.

The 5-(4-formyl-3,5-dimethoxyphenoxy)valeric acid (Barany) linker and its monomethoxy analog were applied to the Multipin method of solid phase synthesis. A comparative assessment of reductive amination and cleavage of these linkers under conditions of multiple synthesis indicated that both were applicable to a broad range of primary amines including aniline and 4-nitroaniline. Apart from the greater lability of the dimethoxy version under TFA cleavage, there was no observable advantage of one linker over the other within the described experiment.

Amination↗
PubMed2003

Efficacy of betamethasone valerate mousse in comparison with standard therapies on scalp psoriasis: an open, multicentre, randomized, controlled, cross-over study on 241 patients.

BACKGROUND: The scalp is a common area for plaque psoriasis. Corticosteroid-based lotions are the most widely used therapy in this clinical setting. A new formulation of betamethasone valerate 0.12% in a thermophobic, low-residue foam vehicle (Bettamousse trade mark, Mipharm, Italy; BVM) is available for the treatment of scalp dermatoses. OBJECTIVES: In an open, investigator-blinded, multicentre (28 dermatology clinics), randomized, cross-over study, the efficacy, safety and patient acceptability of BVM in scalp psoriasis were evaluated in comparison with standard therapies (ST, i.e. corticosteroids or vitamin D analogues). ST were chosen by each centre according to its usual therapeutic protocols. METHODS: In total, 241 patients with moderate to severe scalp psoriasis participated in the trial. After a 2-week run-in period, each active treatment (BVM or ST) was applied for 4 weeks, with a wash-out period between the two active treatment phases of at least 4 weeks. Efficacy was evaluated by investigators unaware of treatment sequence analysing a 'target' lesion for erythema, scaling, itching and burning using a five-point grading score. Patient treatment acceptability and assessment of the influence on Psoriasis Disability Index were evaluated using an eight-item modified Finlay-Khan questionnaire at baseline and at the end of each treatment period. Safety was evaluated by recording any adverse event occurring during the study duration. BVM was applied twice daily, and ST were applied once or twice daily, according to the approved scheduled regimens. RESULTS: Analyses were by intention-to-treat. Two hundred and ten patients concluded the study. Fifteen patients withdrew from the study during BVM treatment, and 16 during ST (not significantly different). Both treatments were well tolerated. At baseline, the mean +/- SD clinical global score (the 'Sum' score = erythema + scaling + itching + burning) was 7.6 +/- 2.6. The ST chosen were topical corticosteroids (55% of cases; mainly mometasone and betamethasone dipropionate) or calcipotriol lotion (45% of cases). At the end of active treatments, BVM was significantly superior to ST (P < 0.001) in reducing, as compared with baseline, the mean +/- SD Sum score (1.5 +/- 1.9 with BVM and 3.1 +/- 2.7 with ST). During BVM treatment, 88% (95% confidence interval, CI 82-94%) of patients had a complete or nearly complete resolution of scaling in comparison with 66% (95% CI 58-74%) during ST therapy (P < 0.001). BVM was also considered an easier and more convenient formulation to use in comparison with ST (P < 0.01). CONCLUSIONS: BVM is more effective than lotion-based ST commonly used in the treatment of scalp psoriasis, and has higher patient acceptability.

Administration, Topical↗
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↗
PubMed1977

Betamethasone valerate aerosol in the treatment of oral lichen planus.

Betamethasone valerate aerosol, given in doses of up to 800 microgram per day, was compared with placebo in a double-blind trial involving 23 patients with oral lichen planus. The majority of patients receiving the active aerosol noted improvement within the first 2 weeks of treatment and at 8 weeks the lesions had almost cleared; in contrast, only 2 patients on placebo showed slight improvement over the same time period. The results suggest that this form of treatment is an effective and acceptable method of controlling the discomfort due to oral lichen planus, especially where minor erosions are present.

Adult↗
PubMed1983

The effect of serial dilution of betamethasone-17-valerate on blanching potential and chemical stability.

The effect of serial dilution of betamethasone-17-valerate (Betnovate ointment) in Unguentum Merck was investigated using a single application blanching assay in 10 subjects and high performance liquid chromatography. There was no statistically significant difference between any of the diluted formulations with regard to blanching potential. Chemical stability was maintained following a 1:32 dilution for 2 months and 1:4 dilution for 5 months at least, after storage at room temperature.

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↗
PubMed1993

Investigations into the mechanism of vasoconstrictor action of the topical steroid betamethasone-17-valerate in the rat.

1. The effect of topical betamethasone upon skin blood flow was investigated in the rat. Two types of vasodilator stimuli were used; local heating to the surface of the skin and intradermal application of inflammatory agents. Blood flow was measured by laser doppler velocimetry. 2. Topical betamethasone-17-valerate (1 g with an 18 h pretreatment) significantly inhibited the heat-induced vasodilatation in the rat skin, as also did systemically administered betamethasone (1 mg kg-1, 3 h pretreatment). 3. Angiotensin converting enzyme (ACE) inhibitors (captopril, 5 mg kg-1 and enalapril, 1 mg kg-1, 30 min pretreatments) were the only drugs out of several different types of systemically administered inhibitors and antagonists that were tested which also inhibited the heat-induced vasodilatation. Aprotinin (100,000 KIU kg-1, 5 min pretreatment) a serine protease inhibitor, significantly potentiated the heat-induced response. 4. Bradykinin (50 nmol per site), des-Arg9-bradykinin (5 nmol per site), substance P (0.1 nmol per site) and capsaicin (1 mumol per site) induced an increase in skin blood flow. 5. Topical betamethasone treatment resulted in a significant inhibition of the vasodilator response to des-Arg9-bradykinin, whereas captopril treatment inhibited the responses to substance P, capsaicin, bradykinin and des-Arg9-bradykinin. 6. Intradermal application of captopril (10-100 micrograms) also caused a dose-dependent inhibition of the heat-induced vasodilatation. 7. These results suggest that topical betamethasone may be acting in a manner similar to that of the ACE inhibitors to produce an inhibition of the flow responses in the skin and that this effect may be brought about by interfering with the action of vasodilator peptide(s) or protein(s).

Administration, Cutaneous↗
PubMed1967

Function of the glyoxylate-condensing enzymes. I. Growth of Escherichia coli on n-valeric acid.

Growth of Escherichia coli E-26 on valeric acid results in the formation of a mutant population characterized by the ability to form constitutively several glyoxylate-condensing enzymes. This mutant also differs from the parent organism in the ability to effect rapid growth on a series of short-chain fatty acids. These mutants were utilized in postulating genetic relationships among the various glyoxylate-condensing activities and also in correlating the presence of these enzymes with the ability of the mutants to initiate growth quickly on short-chain fatty acids.

Acetates↗
PubMed1981

Clinical, biochemical and morphological responses of patients with villous atrophy to oral betamethasone valerate and clobetasone butyrate.

10 patients with sub-total villous atrophy were given the topical corticosteroids betamethasone valerate or clobetasone butyrate for a period of 4 months whilst continuing on a normal diet. 5 patients improved symptomatically while red cell folate, urinary xylose and faecal fat excretion also improved. Brush border enzymes increased in patients treated with higher dosages of each drug. Enterocyte height increased and intra-epithelial lymphocytes were significantly decreased although overall morphological appearances remained indistinguishable from untreated coeliac disease. Suppression of the pituitary adrenal axis occurred in 8 patients and there did not appear to be useful separation of topical from systemic activity. These compounds offer no advantage over prednisolone in non-responsive coeliac disease.

Administration, Oral↗
PubMed1975

Topical treatment with urea-hydrocortisone in atopic dermatitis. A controlled study against betamethasone 17-valerate.

When comparing 1% hydrocortisone in a stabilized 10% urea cream with 0.1% betamethasone 17-valerate cream in a double-blind study on 49 patients with atopic dermatitis or atopic winter feet, betamethasone cream was found to be the most potent. The study also showed that in approximately 60% of the patients the clinical response was equal. It is suggested that the urea-hydrocortisone combination may have its place in the long-term topical treatment of atopic dermatitis on account of its water-binding effect.

Administration, Topical↗
PubMed1976

Clinical trial comparing hydrocortisone 17-butyrate to betamethasone 17-valerate in a series of patients with eczematous skin diseases.

A randomized, double-blind, left-right comparative study was carried out to compare the value of hydrocortisone 17-butyrate with that of betamethasone 17-valerate in the treatment of eczematous skin disorders. In a series of 23 patients with such disorders, no differences between the two preparations was demonstrated with regard to effectiveness.

Administration, Topical↗
PubMed1977

Tibicorten and betamethasone valerate: a double-blind comparative study.

Tibicorten, a new fluorine-substituted corticosteroid for topical application, was compared with betamethasone valerate in a double-blind investigation with left-right examinations. There appeared to be no significant difference between the results obtained with each substance in the treatment of patients with acute or chronic eczema or with psoriasis.

Acute Disease↗
PubMed1981

A double-blind trial of budesonide ointment and betamethasone-17-valerate ointment in psoriasis.

In a double-blind within-patient clinical trial in psoriasis, budesonide 0.025% ointment has been shown to be at least as efficient as betamethasone-17-valerate 0.1% ointment. A lower concentration of budesonide ointment, 0.01%, was used for 4 weeks of maintenance treatment. This concentration controlled residual symptoms well in a majority of the patients, thirty-two in number.

Adolescent↗
PubMed1982

Once daily application of diflorasone diacetate ointment compared with betamethasone valerate ointment twice daily in patients with eczematous dermatoses.

The clinical efficacy of 0.05% diflorasone diacetate applied once daily, for eczematous dermatoses, was compared with the twice daily application of betamethasone valerate. Both agents were supplied as ointments. Sixty patients were randomized to one of the two treatment regimens. The investigators were unaware of the regimen used. Evaluations were made at 1 and at 3 weeks. There were no statistically significant differences in eight parameters studied at any time during the study. No side-effects were reported.

Administration, Topical↗
PubMed1984

Comparison of topical treatment with desoxymethasone solution 0.25% with salicylic acid 1% and betamethasone valerate solution 0.1% in patients with psoriasis of the scalp.

A new preparation for treatment of psoriasis of the scalp, containing desoxymethasone 0.25%, salicylic acid 1% and polyol-fatty esters in ethanolic solution (Ibaril) was tested in patients with psoriasis of the scalp. In a double-blind study comprising forty patients there was a significant difference in favour of this solution in comparison with betamethasone valerate solution, 0.1% (Betnovat) after 2 weeks of treatment.

Administration, Topical↗
PubMedDate not supplied

Comparison of a modified hydrocortisone/urea cream and betamethasone valerate cream in the treatment of dry eczema.

A half-sided, single-blind, comparative study of a new modified formulation of 1% hydrocortisone/10% urea and 0.1% betamethasone valerate cream in the treatment of dry eczema showed that the two products were equally effective at the end of 1, 2 and 3 weeks of treatment in terms of efficacy and speed of action. No statistically significant differences could be detected between either preparation in any of the trial's measures (i.e. overall severity score, dryness/scaling, erythema, papules, itching, excoriation or lichenification) at any of the weekly assessments. The incidence of side-effects was the same with both treatments and patients' preference was equally divided between the two creams.

Administration, Topical↗
PubMedDate not supplied

A double-blind comparison of 0.25% and 0.05% desoxymethasone, 0.1% betamethasone valerate and 1% hydrocortisone creams in the treatment of eczema.

The efficacy and acceptability of 0.25% and 0.05% desoxymethasone, 0.1% betamethasone valerate and 1% hydrocortisone creams were compared in patients with eczema. A double-blind parallel group multi-centre design was employed in which 96 patients were recruited by four centres. Patients used one cream for a 3-week period and follow-up assessment visits were made at weekly intervals. Efficacy variables were: erythema/redness, scaling, itching and extent of area affected. These variables were assessed by both the investigator and the patient. The 0.25% desoxymethasone was the most effective treatment, producing the greatest degree of improvement in all clinical parameters, hydrocortisone was the least effective and 0.05% desoxymethasone was of intermediate effectiveness. The 0.1% betamethasone produced similar results to 0.25% desoxymethasone for half the assessments; for the other half the results were similar to 0.05% desoxymethasone. No adverse effects were reported during the study. The results are discussed in terms of physical properties of the vehicles and corticosteroid potency.

Administration, Topical↗