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PubMedDate not supplied

Betamethasone increases the beta-adrenergic receptor density of human polymorphonuclear leukocytes.

Prolonged incubation (18h) of human polymorphonuclear leukocytes (PMNs) with betamethasone (BT) (10(-7) M) increased (3H)-DHA binding to human PMN membranes, apparently causing an increase in the number of beta-adrenergic receptors. Inhibition of this effect by cycloheximide (2 micrograms/ml) suggests that it is dependent on protein synthesis. BT had no effect on basal levels of cAMP in PMNs, but synergistically potentiated the increase in cyclic AMP (cAMP) induced by isoproterenol. Propranolol completely abolished the synergistic effect of BT plus isoproterenol, suggesting that the potentiating effect of BT on cAMP metabolism required the activation of beta-adrenergic receptors. Thus, BT increased the number of beta-adrenergic receptors in human PMN membranes and potentiated the cAMP changes induced by beta-agonists.

Betamethasone↗

PubMed2003

Differential-pulse polarography (DPP) determination of betamethasone valerate in dosage form.

The electrochemical reduction of betamethasone valerate (BV) in a pharmaceutical formulation containing neomycin has been carried out in Britton-Robinson buffer (BRB) (0.04 mol L(-1)) by differential-pulse polarography (DPP). BV exhibits a well-defined irreversible reduction peak at -1.03 V/ref. The influence of pH on the reduction of BV was studied in Britton-Robinson buffer (pH range 1.7-10). A method for the analysis of BV in BRB (0.04 mol L(-1)), which allows quantification over the range 3.9x10(-6)-1.1x10(-4) mol L(-1), was proposed and successfully applied to the determination of BV in tablets with mean recovery and relative standard deviation of 100.81% and 0.45%, respectively.

Betamethasone Valerate↗

PubMed2002

Antenatal betamethasone and favourable outcomes in fetuses with 'poor prognosis' diaphragmatic hernia.

Congenital diaphragmatic hernia (CDH) is a common abnormality affecting 1 in 2,000 gestations. The mortality exceeds 50% despite recent advances in postnatal treatment. The widespread antenatal use of glucocorticoids to induce lung maturation in fetuses at risk of premature delivery suggests a potential for a therapeutic effect in other fetuses with impaired lung development. The parents of three fetuses referred with CDH and features suggesting a poor postnatal prognosis (early diagnosis, liver herniation, and lung area-to-head circumference ratio <1.0, or associated abnormalities) elected to receive maternal betamethasone starting at 24 to 26 weeks' gestation rather than undergo a fetal tracheal plug. All three infants survived and were extubated within 10 days. The long-term use of antenatal steroids in the treatment of CDH may thus be of benefit and warrants further study.

Anti-Inflammatory Agents↗

PubMed2001

Betamethasone valerate foam for treatment of nonscalp psoriasis.

BACKGROUND: Although betamethasone valerate (BMV) foam, 0.12% (Luxiq, Connectics Corporation, Palo Alto, CA) is approved by the Food and Drug Administration for the treatment of corticosteroid-responsive scalp dermatoses, no data are available for its use on nonscalp psoriasis. OBJECTIVE: We evaluated the safety and efficacy of BMV foam in treating psoriatic lesions at nonscalp sites. METHODS: We conducted a randomized, double-blind, placebo-controlled, paired-comparison, split-body study of 40 patients with mild to moderate plaque-type psoriasis. Patients applied BMV foam and placebo foam twice daily for 12 weeks. RESULTS: At the end of the treatment period, 70% of patients had greater than 50% improvement of lesions on their active foam-treated side compared with 24% of patients with similar improvement on their placebo foam-treated side. Adverse effects were limited to temporary stinging, burning, or itching in several patients. Three patients (7.5%) withdrew because of stinging or itching. CONCLUSIONS: The results indicate that BMV foam is effective against nonscalp psoriasis. Twice-daily applications are well tolerated, compliance exceeds 90%, cosmetic characteristics are acceptable, and the medication may reduce the need for multiple prescriptions.

Administration, Topical↗

PubMed1977

Effect of betamethasone on analysis of amniotic fluid in the rhesus-sensitized pregnancy.

Betamethasone was administered to six rhesus-sensitized pregnant women carrying seven fetuses in an attempt to accelerate fetal pulmonary maturation. A reduction in optical density of amniotic fluid at 450 mmu was observed in all cases following steroid therapy; however, only minimal changes were noted in the lecithin-sphingomyelin ratio. The implications of these findings for the management of rhesus-sensitized pregnancies are discussed.

Amniocentesis↗

PubMed1977

In vitro metabolism of prednisolone, dexamethasone, betamethasone, and cortisol by the human placenta.

Many of the factors influencing the pharmacologic action of corticosteroids on the maternal-placental-fetal unit remains obscure. To clarify the effect of the placenta on corticoid transfer, tritiated steroids were incubated in saline for 2 hours with minces of midgestational or term placental tissue. The media were extracted and chromatographed on Sephadex-LH-20. Large peaks corresponding to the inactive 11-keto metabolites were observed for cortisol (67 per cent) and prednisolone (51 per cent) while conversion of dexamethasone (1.8 per cent) and betamethasone (7.1 per cent) was low or negligible.

Betamethasone↗

PubMed1979

Betamethasone and the rhesus fetus: multisystemic effects.

In this controlled study of betamethasone administration to pregnant rhesus monkeys, using dosages per gram of fetal body weight similar to those reported in several human clinical studies, the most significant fetal pulmonary changes observed were increases in maximum lung volumes. The fact that comparable increases in peak volumes were demonstrated on saline filling supports our contention that these changes are related primarily to lung structural alterations rather than surfactant effects. Additional findings in the treated animals included reduced fetal head circumference, thymus weight, adrenal weight, placental weight, and maternal postoperative weight and increased fetal hepatic weight. Any of these glucocorticoid-induced changes could portend serious side effects. Further studies are needed to delineate the risk:benefit ratio of such treatment.

Adrenal Glands↗

PubMed1979

Changes in human amniotic fluid lecithin/sphingomyelin ratio and dipalmitoyl lecithin associated with maternal betamethasone therapy.

In an effort to understand the biochemical changes responsible for the decreased incidence of neonatal RDS observed in premature infants delivered after maternal glucocorticoid therapy we have compared quantitative changes in L/S ratio and qualitative changes in dipalmitoyl lecithin in serial amniotic fluid samples from 20 pregnant women treated with betamethasone and 11 patients who had repeated amniocentesis at similar gestational age but did not receive glucocorticoids. Initial L/S ratio values were not significantly different between treated (1.24 +/- 0.24 [S.D.]) and control (1.09 +/- 0.29 [S.D.]) groups but the values obtained within 1 week after therapy (1.49 +/- 0.21 [S.D.]) were significantly higher (t=3.8; p less than 0.01) than those obtained after a similar period in the untreated group (1.24+/- 0.29 [S.D.]). However, only one of the treated patients reached a mature L/S ratio (2.0 or more). Simultaneously, 10 of 17 treated patients exhibited increases in the amount of dipalmitoyl lecithin within the first week after treatment, wheras no change was detected in serial samples from six control patients (p = 0.016). These results indicate that qualitative changes in amniotic fluid lecithin composition are a part of the fetal response to glucocorticoids which may be responsible for the decreased incidence of RDS observed after treatment.

Amniocentesis↗

PubMed1980

Results of a double-blind controlled study on the use of betamethasone in the prevention of respiratory distress syndrome.

A double-blind controlled study on the prenatal use of betamethasone in the prevention of respiratory distress syndrome (RDS) was carried out on 137 patients from 24 to 34 weeks' gestation. The incidence of RDS was less in the treated group (5%) than in control group (17%). The neonatal mortality rate was lower in the treated group (5%) than in the control group (18%) due to an excess of neonatal deaths in the placebo group.

Betamethasone↗

PubMed1979

Glucocorticoid induction of pulmonary maturation in the rabbit fetus. The effect of maternal injection of betamethasone on the activity of enzymes in fetal lung.

1. Maternal administration of betamethasone (0.2 mg/kg) on day 25 or 26 of gestation produced a significant decrease in the lung/body weight ratio of the rabbit fetuses within 24 h. 2. The incorporation of [14C]choline but not [14C]ethanolamine into the lipids of fetal lung slices was significantly increased, indicating that there was a specific effect on phosphatidylcholine synthesis. 3. The activities of a number of marker enzymes for subcellular organelles were elevated, especially in the lungs of fetuses delivered on day 26. The increases in monoamine oxidase (mitochondrial outer membrane), beta-glycerophosphatase and aqueously dispersed phosphatidic acid-dependent phosphatidic acid phosphohydrolase (lysosomal) activities were significant. 4. Although the activity of cholinephosphotransferase was not affected by glucocorticoid treatment, the activities of glycerol-3-phosphate phosphatidyltransferase and the activities of two enzymes in the auxiliary pathways for the production of disaturated phosphatidylcholine (lysophosphatidylcholine:lysophosphatidylcholine transacylase and lysophosphatidylcholine:acyl-CoA acyl-transferase) were significantly increased. 5. Membrane-bound phosphatidic acid-dependent phosphatidic acid phosphohydrolase activity was elevated to a lesser extent than the aqueously dispersed phosphatidate-dependent activity and this increase was not significant. 6. The incorporation of E135S]methionine into protein by slices of fetal lung was significantly reduced after maternal treatment with betamethosone. 7. These results are consistent with the general view that glucocorticoids can induce pulmonary maturation and surfactant production in the rabbit fetus but indicate that some of the former hypotheses regarding the mechanism by which lipid synthesis is accelerated must be reevaluated.

Animals↗

PubMed1980

A case report of maternal death associated with betamimetics and betamethasone administration in premature labor.

A fatal case of pulmonary edema is reported after prolonged treatment with beta-mimetics during pregnancy for threatened premature labor. The mother had received betamethasone in order to enhance fetal lung maturity. Myocardial failure occurred 5 days after discontinuation of betamimetics. The potential toxic effects of beta-adrenergic agents and their association with corticosteroids are discussed. Caution is recommended when high doses of betamimetics are to be delivered to prevent premature labor. No patient should be treated unless her cardiac condition is normal. Cardiovascular evaluation should be regularly performed during the course of treatment. No patient should be discharged after treatment without a normal cardiovascular check-up.

Adrenergic beta-Agonists↗

PubMed1979

Qualitative study of prostaglandins in pregnant uterine tissues: effects of estradiol- 17 beta and betamethasone.

The presence of prostaglandins (PGs) E1 and F2 alpha in extracts of endometrial, myometrial and placental samples from 19 pregnant women at term, was investigated. The tissue samples were obtained from the following group of patients: untreated, A) with onset of labor, B) without onset of labor; pre-treated (without onset of labor); C) with betamethasone, D) with estradiol-17 beta. Thin-layer chromatography determinations demonstrated PGE1 presence in all tissue samples from the four groups. On the other hand, PGF2 alpha was consistently found in placenta and endometrial samples from groups A, C, and D, but it was absent in those from group B. The results suggest a physiological role of PGF2 alpha in human parturition, and a possible influence of estrogens and corticosteroids on the appearance of this prostaglandin.

Betamethasone↗

PubMed1982

Drug immunotoxicological approaches with some selected medical products: cyclophosphamide, methylprednisolone, betamethasone, cefoxitine, minor tranquillizers.

Alterations of the normal immune response were estimated in C57B1/6 mice pretreated with cyclophosphamide, methylprednisolone sodium succinate, betamethasone sodium phosphate or cefoxitine as positive controls and three minor tranquillizers: dipotassium chlorazepate, diazepam and meprobamate. The specific immune response against sheep red blood cells (SRBC) was evaluated by numeration of the direct plaque-forming cells (PFC; humoral immunity) and by measurement of the footpad swelling (delayed-type hypersensitivity, DTH). In our experiments, the results with the positive controls were in the same order as those described by others, and at the dose levels used, these three minor tranquillizers did not really alter the specific humoral and cellular immune response against SRBC in the C57B1/6 mice.

Animals↗

PubMedDate not supplied

Cholinomimetic drugs modify betamethasone suppression in the rat.

This study was performed to investigate the effect of different cholinomimetic drugs (CD) on ACTH levels in betamethasone (BET) pretreated rats (40 mg/kg in the drinking water for 24 h). Animals were injected with atropine methylbromide (1 mg/kg, i.p.) and, after 10 min, with physostigmine (25, 50, 100, 200 micrograms/kg), arecoline (AR) or oxotremorine (OX) (150, 300 micrograms/kg) intravenously. They were killed 10 and 20 min after CD injection, to measure ACTH plasma levels. The lowest dose of AR and both doses of OX were able to induce an escape from BET suppression. The hypothesis that a stimulation of central muscarinic (and, probably, not nicotinic) receptors is involved in the CD-induced escape from glucocorticoid suppression is discussed.

Adrenocorticotropic Hormone↗

PubMed2006

Betamethasone effects on ovine uterine and umbilical placental perfusion at the dose used to enhance fetal lung maturation.

OBJECTIVE: The purpose of this study was to examine glucocorticoid effects on umbilical placental perfusion. STUDY DESIGN: Pregnant sheep instrumented with uterine and umbilical ultrasound transit-time flow probes received 2 doses of 12 mg betamethasone (n = 6) or saline (n = 5) intramuscularly 24 hours apart. RESULTS: Maternal blood pressure and uterine flow did not change during glucocorticoid exposure. Fetal blood pressure increased, and umbilical resistance showed a transient increase after each injection (P < .05), followed by an increase of umbilical flow (P < .05) that was closely correlated to an increase in fetal heart rate (r = 0.85, P < .001), which determines cardiac output of the developing heart. Umbilical waveform indices were decreased over the entire treatment period, indicating a decrease of resistance in the fetoplacental microcirculation (P < .05). CONCLUSION: Fetoplacental perfusion during glucocorticoid exposure is not limiting for nutrition exchange. Clinical interpretation of Doppler waveform indices needs to be interpreted with caution because they do not reflect dynamics of umbilical placental perfusion.

Animals↗

PubMed2005

Treatment of experimental autoimmune uveoretinitis with poly(lactic acid) nanoparticles encapsulating betamethasone phosphate.

We have developed nanoparticles (NPs), which are capable of targeting a specific lesion and gradually releasing the agent at the site over a prolonged time period after a single intravenous administration. In this study, we evaluated the effects of intravenously administered poly(lactic acid) nanoparticles encapsulating betamethasone phosphate (BP-PLA NPs) on experimental autoimmune uveoretinitis (EAU) in Lewis rats. To determine the localization of NPs within the retina and choroid of rats with EAU, rhodamine (Rh)-encapsulated PLA NPs were injected intravenously and visualized by confocal microscopy. After the disease onset of EAU induced by S-antigen peptide in Lewis rats, either BP-PLA NPs, BP, or saline was injected intravenously, and the eyes were obtained 7 days following treatment and the histological score was determined. The clinical course of EAU was examined using pathological findings and the expression of the glial fibrillary acidic protein, rod opsin, and the surface markers of inflammatory cells (ED1 and pan T-cell) were immunohistochemically determined. Furthermore, T-cell proliferation and delayed-type hypersensitivity (DTH) to S-antigen were assessed. Intravenously injected Rh-PLA NPs accumulated in the retina and choroid of rats with EAU within 3 hr and remained over the succeeding 7-day-period. Furthermore, systemically administered BP-PLA NPs reduced the clinical scores of rats with EAU in 1 day, which were maintained for 2 weeks and decreased the histological scores. In addition, the ocular infiltration of activated T-cells and macrophages in addition to the hypertrophy of Müller cells were markedly reduced with this treatment. Meanwhile, T-cell proliferation and DTH of BP-PLA NPs-treated rats against S-antigen peptide were not significantly different from those of saline-treated rats. Systemically administered BP-PLA NPs inhibit the development of EAU due to the targeting and the sustained release of steroids in situ. The results of these studies suggest that the systemic administration of BP-PLA NPs may lead to a new therapeutic strategy in controlling intraocular inflammation.

Animals↗

PubMed2004

Method development for betamethasone and dexamethasone by micellar liquid chromatography using cetyl trimethyl ammonium bromide and validation in tablets. Application to cocktails.

An isocratic liquid chromatographic method for the determination of betamethasone (BM) and dexamethasone (DM) using methylprednisolone (MPL) as internal standard and micellar mobile phases consisting of cetyl trimethyl ammonium bromide (CTAB) and organic modifiers such as propanol, butanol and pentanol has been developed. The effect of organic modifiers, surfactant concentration, temperature and flow-rate on the separation has been studied. Method validation for dexametasone or bethametasone in tablets was carried out using a mobile phase 0.24% pentanol and 32.5 mM CTAB, a flow-rate of 0.5 ml min(-1), an Hypersil C18 column (60 degrees C), and UV detection at 243 nm. The recoveries for BM and DM found in the accuracy test were 99 +/- 3 and 101 +/- 2, respectively. Repeatability and intermediate precision expressed as R.S.D. were lower than 5% for both compounds. The proposed method was applied to cocktails containing both compounds.

Betamethasone↗

PubMed2000

Characterization of inclusion complexes of betamethasone-related steroids with cyclodextrins using high-performance liquid chromatography.

HPLC was used to study the inclusion complexes formed between various beta- and gamma-cyclodextrins and a series of corticosteroids related to betamethasone. Apparent association constants were measured in acetonitrile-water for a set of 13 steroids. An increase in the stability of the steroid-cyclodextrin complex is observed at lower concentrations of acetonitrile. The effects of the nature of the halide at the 9-position, the location of a double bond within the C-ring, substitution at the 9- and 11-positions, and modification of the D-ring of the steroid backbone were studied. The 11- and 17-positions were found to be critically involved in the inclusion process. Larger apparent association constants were obtained with gamma-cyclodextrin (gamma-CD) than with beta-cyclodextrin (beta-CD) due to the increased diameter of the gamma-CD cavity. Van't Hoff plots were constructed to examine the thermodynamic properties of the inclusion process. Plots constructed using retention factors were found to be nonlinear when gamma-CD was present in the mobile phase. This is due to an increase in the strength of the inclusion complex as temperature decreases. Plots constructed using apparent association constants were linear, indicating that the mechanism of inclusion does not change over the range of temperatures studied (10 to 80 degrees C). Enthalpy-entropy compensation was observed for 11 of the 13 steroids studied. The usefulness of cyclodextrins to achieve the separation of steroids in HPLC is discussed and a practical application for the analysis of a steroid and three potential impurities is described.

Betamethasone↗