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Single (0 . 25 mg/100 g body wt) or multiple (5 x 20 microgram/100 g) injections of testosterone propionate were given to castrated male rats fed normally or restricted to a 50% intake. Serum FSH and LH levels were higher in the underfed rats and the effectiveness of testosterone propionate in suppressing serum levels of gonadotrophins was increased by underfeeding.
Sexual behaviour was not induced in ovariectomized cows by single doses of 100 or 250 micrograms oestradiol benzoate or by 3 injections of 50 micrograms oestradiol benzoate given at 12-h intervals. Treatment with 3 doses of 250 or 500 micrograms oestradiol benzoate at 12-h intervals produced plasma levels that were similar to those during pro-oestrus and oestrus in intact cows, and 11 of 12 treated animals showed oestrous behaviour. The higher dose resulted in a more pronounced response in 'mounting' and 'mounted' behaviour and a shorter interval to the onset of behavioural signs of oestrus. Oestrous behaviour was not observed in any ovariectomized cows treated with 1,2 or 20 mg testosterone propionate, doses that resulted in plasma levels comparable to those in intact pro-oestrous animals. Treatment with pharmacological doses of testosterone propionate resulted in transient mounting and interest in similarly treated females, but the results were inconsistent.
To elucidate the process underlying polycystic ovary (PCO) syndrome, we tried to produce experimental PCO by sterilizing rats with androgen and investigated the formation of PCO endocrinologically and histologically. Wistar-Imamichi strain female rats were given an injection of testosterone propionate 1.25 mg on 5 days of age. On 5, 10, 20, 40, 60, 80, 100, 130, 160, 200 days after the injection the ovaries were obtained. Ovarian wedge resection was also performed at 100 and 200 day-rats. Serum gonadotropins, prolactin and steroids were measured with RIA and compared with ovarian pathology. Serum prolactin was increased drastically 40 days after the injection and maintained at a constant level higher than control. Through wedge resection, the serum LH level returned to normal, but FSH slightly increased. Serum estradiol decreased more markedly than estrone did. The 40 day-ovaries showed polycystic features, lack of corpus luteum, hyperthecosis, luteinization of stroma, while no thickening of tunica albuginea. In conclusion, the rats treated with testosterone propionate had many endocrinological and histological aspects similar to those of human PCO syndrome.
The rise in concentrations of FSH and LH in serum seen 24 h after castration was suppressed by the administration of an extract of bull seminal plasma or testosterone propionate at the time of castration. Whereas testosterone propionate preferentially suppressed LH, the seminal plasma extract suppressed FSH and LH equally. Small doses of bull seminal plasma extract and testosterone, that had little effect separately, acted synergistically to supress levels of FSH and LH to those found in intact animals, while combinations of larger doses had little further effect. This selective interaction suggests how inhibin and testosterone might together regulate concentrations of FSH and LH in the blood of the male rat.
Tarentaise heifers fitted with a rumen cannula (539 +/- 7.5 and 487 +/- 15.7 kg avg initial BW in Exp. 1 and 2, respectively) were used in two Latin square metabolism experiments having 2 x 2 factorial treatment arrangements to determine the effects of supplementation with Aspergillus oryzae fermentation extract (AO) or laidlomycin propionate (LP) on intake, digestion, and digestive characteristics of Neotyphodium coenophialum-infected (IF) or uninfected (FF) tall fescue (Festuca arundinacea) hay diets consumed ad libitum. Heifers were housed in individual stanchions in a metabolism facility with ambient temperatures controlled to range between 26.7 and 32.2 degrees C daily. Total feces and urine were collected for 5 d following a 21-d dietary adaptation period. In situ DM and NDF disappearance and ruminal fermentation characteristics were also determined. In Exp. 1, DMI was 24% greater (P < 0.01) by heifers offered FF than by those offered IF (6.7 vs 5.4 kg/d). Heifers fed 2 g/d AO tended (P = 0.09) to consume 4% more DM than those fed a diet without AO. Degradable DM and NDF fractions of IF were greater (P < 0.01) than those of FF, but AO supplementation did not affect situ disappearance (P > or = 0.42). In Exp. 2, DMI was 18.9% greater (P < 0.01) by heifers offered FF than by those offered IF (6.6 vs 5.5 kg/d). Heifers fed LP (50 mg/d) consumed 10.6% less (P < 0.05) DM than those not fed LP (5.7 vs 6/5 kg/d). Digestibility of NDF tended to be greater (P = 0.08) and digestibility of ADF was greater (P < 0.05) from FF than from IF. Conversely, apparent N absorption (%) was greater (P < 0.05) from IF than from FF. Heifers fed LP had lower (P < 0.05) ADF digestibility than those not fed LP. In situ degradable DM and NDF fractions were greater (P < 0.01) from IF than from FF. Diets supplemented with LP had higher (P < 0.01) indigestible DM and NDF fractions than those without LP. Propionic acid and total VFA concentrations were greater (P < 0.05) from heifers offered FF than from those offered IF and from heifers fed LP than from those not fed LP. Therefore, it appears the major effect of N. coenophialum was a reduction in forage intake and total-tract fiber digestibility in certain situations. Response to the feed additives was similar whether heifers were offered IF or FF and no evidence was apparent that either additive would improve performance substantially by animals consuming low-quality fescue hay diets.
Because biological indicators alone do not adequately represent the comprehensive health status of a patient with asthma, we also assessed patients' health-related quality of life (HRQOL) in a randomized, double-blind, placebo-controlled study of the effects of the inhaled corticosteroid fluticasone propionate (FP). A total of 342 patients with moderate asthma were treated twice daily for 12 weeks with FP powder (50, 100, or 250 micrograms) or placebo. At regular intervals, patients completed the Medical Outcomes Study Short Form-36, acute version (SF-36A), a general health status questionnaire measuring eight dimensions of HRQOL; the 20-item Living with Asthma (LWA-20) questionnaire, a disease-specific instrument measuring HRQOL; and three additional questions related to sleep loss and number of nighttime awakenings. Each of the three FP groups compared with placebo had significantly higher scores at study endpoint on the Physical Functioning (p < 0.001) and Role-Physical (p < or = 0.0001) dimensions of the SF-36A; the FP 100- or 250-micrograms groups compared with placebo also had significantly higher scores on General Health Perceptions (p < 0.03), Vitality (p < 0.007), and Mental Health (p < 0.02). At endpoint, all three FP groups compared with placebo had significantly better scores on the LWA questionnaire (p < 0.05) and on the sleep-related items (p < 0.0001). These data, collected using both a general health status questionnaire and an asthma-specific questionnaire, demonstrate that fluticasone propionate powder can improve HRQOL in patients with mild-to-moderate asthma.
1-Acetoxyethyl 2-(2-fluoro-4-biphenylyl) [14C-methyl]propionate (14C-Me-FP 83), a novel nonsteroidal antiinflammatory agent for injection, was synthesized in order to investigate the metabolic fate. 14C-Me-FP 83 was obtained by the condensation of 2-(2-fluoro-4-biphenylyl) [14C-methyl]propionic acid with 1-chloroethyl acetate. The chemical yield of 1 was 62% after purification. The specific activity was 258 kBq/mg (6.99 microCi/mg) and its radiochemical purity was 99% in thin layer chromatographic method.
BACKGROUND: The skin of patients with atopic dermatitis is colonized with Staphylococcus aureus. Reduction of bacterial colonization has been reported to be effective in the treatment of atopic dermatitis. AIM: To assess the efficacy and safety of a combination of fluticasone propionate 0.005% and mupirocin 2.0% ointment twice daily for 2 weeks in patients with atopic dermatitis clinically suspected of secondary bacterial infection. METHODS: An open-label, non-randomized study of 122 patients (64 males and 58 females) from 20 centers was conducted. Atopic dermatitis was diagnosed by clinical assessment and scoring was done on the visual analogue scale (VAS). Clinical evaluation of the lesions was done on day 1 (baseline), day 8 and on day 15 of study visits. RESULTS: At baseline, many patients had moderate itching (41.8%), moderate dryness (41.8%) and mild weeping lesions (49.2%). The baseline proportions of the clinicians' global impressions (CGI) scale for mild, moderate and severe atopic dermatitis lesions were 19.7%, 55.7% and 12.2% respectively. At the end of the treatment period, 67.2% patients had mild disease, whereas only 9% and 0.8% patients had moderate and severe disease respectively. At baseline, only 33.65% patients were comfortable with the existing lesions when assessed on visual analog scale (VAS). However, after the treatment, this proportion increased to 51.77% and 78.60% patients on day 8 and on day 15 respectively. CONCLUSION: Twice daily topical application of a fluticasone propionate 0.005% and mupirocin 2.0% ointment is an effective and safe therapeutic regimen in atopic dermatitis.
This open, randomized trial was conducted at the Medical Out patient Department of University College Hospital, Nigeria to compare the clinical efficacy of Beclomethasome dipropionate (Becotide) with Fluticasone propionate (Fluvent) in patients with mild to moderate bronchial asthma. The study was performed as a week screening, 8-weeks open comparative clinical trial involving Fluticasone propionate (Fluvent) at a daily dose of 22 microg and Beclomethasone Dipropionate (Becotide) at a dose of 400 microg daily delivered through pressurized metered-dose inhaler (pMDI). The main objective of this study is to assess the efficacy of Fluvent in patients with mild to moderate asthma compared to Becotide. At the second visit (end of 1 week), 10 patients were given either Becotide of Fluvent but all were maintained on as needed beta2agonist (Salbutamol inhaler) therapy throughout the study. Efficacy was assessed by changes in symptoms, number of times beta2-agonist was used and results of pulmonary function tests (PEFR and FEV1) while safety was assessed by adverse event experiences. The baseline characteristics of the patients randomized into the two drug groups were comparable and of no statistical significance. The changes in the pulmonary function tests as well as the reduction in the asthma symptoms suggest a statistically significant improvement in the asthma status of the patients. However, these changes were more rapid among the patients using Fluvent. Also, there was higher percentage decline in the episodes of asthma symptoms either in the morning, day or night in the Fluvent group than Becotide group. The drugs were well tolerated and no adverse event was noticed on any of the patients. We therefore concluded that Fluvent would be more efficacious than Becotide in the treatment of Asthma.
During recent years, 48 patients with therapy-resistant chronic skin lesions of atopic dermatitis have been treated once a week with clobetasol propionate lotion left under Duoderm occlusive patches. They had previously failed to respond, or responded only sparsely, to topical corticosteroids. The lesions resolved completely in 44 patients, while partial remission was observed in the remaining 4. The mean time needed to obtain complete remission was, for lichenifications, 2 weeks; pruriginous lichenoid papules, 12 days; chronic hand eczema, 2.5 weeks; nummular eczema, 8 days; perioral eczema, 11 days, and breast eczema, 10 days. Adverse experiences were mild and infrequent. The amount of topical corticosteroid required was reduced to at most one-twentieth and to as little as one-hundredth of the amount of common topical steroid treatment needed. We conclude that clobetasol propionate and Duoderm once a week is the best treatment for resistant lesions of atopic dermatitis.
This report reviews the evidence for the role of fluticasone propionate in the management of asthma, based on efficacy and safety trial data in over 4000 adults and more than 1600 children suffering from asthma of varying severity. Overall, fluticasone propionate at half the daily dose is at least as effective as budesonide and as effective as beclomethasone dipropionate across a range of doses.
BACKGROUND: Mometasone furoate [9a, 21-dichloro-llb, 17dihydroxy-16a-methyl-pregna-14-dione-3, 20-dione-17-(2furoate)] is a synthetic, 17-heterocyclic corticosteroid which has been shown to be highly effective as an anti-inflammatory agent which is approximately half as potent is suppressing hypothalamic-pituitary-adrenal (HPA) axis function as betamethasone valerate. METHOD: The present open, randomised, third party blinded, left-right sided study was designed to compare the therapeutic efficacy of mometasone furoate cream 0.1% with clobetasol propionate cream 0.05% applied twice daily in chronic eczema following a 3-week course of therapy. PATIENTS/RESULTS: Sixty consecutive patients with moderate to severe bilateral chronic eczema on the limbs were recruited into the study. The mean scores of various signs/symptoms including erythema, induration, crusting, scaling, excoriation and pruritus before and after 3 weeks treatment with mometasone furoate (MF) and clobetasol propionate (CP) cream, were compared. The baseline scores for MF and CP treated sites were almost identical. There was significant decrease in the mean scores of all signs/symptoms after 3 weeks treatment with MF and CP. There was also a significant difference in the mean scores between MF and CP treated sites after 3 weeks of treatment. The mean scores were significantly lower for CP treated sites than MF treated sites. More CP treated sites achieved "cleared" or "marked improvement" response than MF treated sites. There were more "excellent" or "good" grades on CP treated sites than MF treated sites at the end of 3 weeks of treatment. None of the patients showed any side-effects after 4 weeks of treatment. CONCLUSION: Overall, 53% of patients considered the MF treated sites to be good or excellent vs 88% for CP treated sites.
A randomized, double-blind, cross-over study was conducted to assess the efficacy and safety of fluticasone propionate 1 mg twice daily administered via a pressurized metered dose inhaler (pMDI) containing the new non-chlorofluorocarbon (CFC) propellant (HFA 134a), or the established CFC propellants 11 and 12 in patients with severe asthma. The study comprised a 2-week run-in period followed by two 6-week treatment periods, with no washout period in between. One hundred and nineteen symptomatic adult patients with severe asthma, who were receiving inhaled beclomethasone 2-4 mg day(-1) or equivalent, were randomized to treatment. Patients were randomized to one of two sequence groups (sequence 1: HFA 134a pMDI then CFC pMDI or sequence 2: CFC pMDI then HFA 134a pMDI). The sequence groups differed with respect to mean peak expiratory flow (PEF) at baseline; however, the magnitude of the increase in PEF from baseline during treatment was similar in the two sequence groups. Mean PEF at baseline was 334 l min(-1) in sequence group 1 (HFA 134a-->CFC pMDI) and this increased to 357 l min(-1) and 366 l min(-1) during treatment with the HFA 134a and CFC pMDI, respectively. In sequence group 2 (CFC-->HFA 134a pMDI) mean PEF at baseline was 297 l min(-1) and this increased to 336 l min(-1) and 328 l min(-1) during treatment with the HFA 134a and CFC pMDI, respectively. Based on an overall analysis of the two treatment groups at week 6, equivalence was demonstrated; the mean treatment difference (HFA 134a-CFC pMDI) in morning PEF was 0 l min(-1) (90% confidence interval (CI), for difference between groups: -7, 6 l min(-1)). There was a comparable improvement in secondary efficacy variables, including clinic lung function measurements, in the two treatment groups. The incidence and type of most adverse events were similar in the two treatment groups. There was no difference in the adjusted geometric mean morning serum cortisol levels after treatment with the HFA 134a and CFC pMDI. Therefore, the fluticasone propionate HFA 134a pMDI constitutes a suitable replacement for the established CFC pMDI at a microgram equivalent dose.
Fluticasone propionate is the first of a new generation of fluorinated corticosteroids that have been synthesized with a view to separating local activity from undesirable side effects. In recent years, contact allergy to the newer topical corticosteroids has received increasing attention. The results of patch testing with fluticasone propionate, even in patients with a known contact allergy to corticosteroids, argue for a low sensitization and cross-sensitization potential.
Small quantities of diethylstilbestrol and testosterone proprionate were implanted into the hypothalamic arcuate nucleus of male rats of the Wistar-Imamichi strain at 43 days of age. The animals were sacrificed at 64 or 76 days of age. Diethylstilbestrol suppressed the development of all genital organs and disturbed spermatogenesis. The damage was found to have recovered slightly in rats sacrificed at 76 days of age. Testosterone propionate was also effective for the atrophy of some genital organs. Its influence was not so severe as that of diethylstilbestrol. It extinguished almost completely 33 days after implantation. On the contrary, the numbers of spermatogonia and spermatocytes per cross section of the seminiferous tubule were smaller at 76 days than at 64 days of age. The diameter of the seminiferous tubule in the rat implanted with testosterone propionate was longer at 76 days than at 64 days of age. Therefore, the tubular diameter did not always represent the quantity or quality of spermatogenesis. The results also suggested that spermatogenesis might have been disturbed in some of the rats in which androgen was considered to be secreted almost normally.
A culture of propionic acid bacteria grown in a glucose-containing minimal medium, as well as the culture liquid and logarithmic-phase cells obtained from this culture, were found to inhibit the base pair substitution mutations induced by 4-nitroquinoline N-oxide, N-methyl-N'-nitro-N-nitrosoguanidine, and sodium azide and the frameshift mutations induced by 9-aminoacridine. The antimutagenic activity of the culture liquid (CL) was presumably due to the presence of an extracellular thermolabile protein with a molecular mass of no more than 12 kDa based on the facts that this activity considerably decreased after the treatment of the CL with pronase, its heating at 92 degrees C, and its dialysis in a cellulose sack, which retains substances with molecular masses greater than 12 kDa. The residual antimutagenic activity of the dialyzed culture liquid was probably related to the interaction of the mutagen with thiols, rather than to the presence of organic acids (acetic or propionic). Thiols may also contribute to the antimutagenic activity of the P. shermanii cells.
BACKGROUND: Chronic controller therapy, particularly with inhaled corticosteroids, is required in patients with persistent bronchial asthma. Long-acting beta agonists provide prolonged bronchodilatation, improve symptoms and reduce exacerbations. A powder inhaler containing both fluticasone propionate and salmeterol xinafoate combines anti-inflammatory treatment and bronchodilatation in a single user-friendly device (Diskus). OBJECTIVE: The goal of the present study was to evaluate the efficacy and safety of salmeterol/ fluticasone (50/250 microg twice daily) as initial treatment for symptomatic patients with mild to moderate bronchial asthma who had not previously received appropriate anti-asthma medication. METHODS: This prospective study was conducted in 17 study centres located predominantly in private practices. 127 patients with mild to moderate asthma (FEV(1) >60% of predicted) aged 12 years and older were recruited into a one-week screening phase. If they used rescue medication on > or =3 of 7 days or had a total asthma symptom score of > or =5 points, they were admitted to the treatment phase and received salmeterol xinafoate (50 microg) and fluticasone propionate (250 microg) in a single dry powder inhaler (Diskus) for four weeks. RESULTS: Combined salmeterol/fluticasone therapy improved morning and evening peak expiratory flow rates (PEFR) as measured by patients and reported in asthma diaries within the first week of treatment (by 35 and 28 L/min, respectively). At week 4, morning PEFR had increased by 57 L/min or 13.0 % predicted compared to baseline, and forced expiratory volume in one second (FEV1) had improved by 12.5% of predicted (p<0.001). Use of rescue medication declined by 1.9 puffs per day. Both patients and physicians regarded treatment as a major benefit: two thirds assessed treatment as "excellent". The combination was well tolerated. CONCLUSIONS: The combined inhalation of salmeterol and fluticasone from a single dry powder inhaler (DiskuS) was an effective initial treatment for patients with mild to moderate asthma. Improvements of symptoms and lung function were documented by the first week of treatment. This combination provides rapid and effective asthma control that is highly acceptable to both the patient and physician.
alpha-(6-Methoxyl-2-naphthyl) ethanol can be carbonylated to form methyl-alpha-(6-methoxyl-2-naphthyl)propionate catalyzed by a catalyst in the pressnce of methanol. High efficiency capillary gas chromatography and GC/MS technique were used for determining products which were obtained from the carbonylation. An OV-101 fused silica capillary column (25 m x 0.2 mm i.d.) and a flame ionization detector (FID) were employed in the GC analysis. The column temperature was kept at 250 degrees C. Mass spectra were obtained by electron impact at 70 eV. The structures of four compounds were identified. The major product is methyl-alpha-(6-methoxy-2-naphthyl) propionate, and the two by-products are 2-vinyl-6-methoxynaphthalene and 1-methoxy-(6'-methoxy-2'-naphthyl)ethanol.