Betamethasone
Pros:
Anti-inflammatory (1)Cons:
Take only under medical supervision (1)10 pts from Street82
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"Betamethasone studies" about Betamethasone Review Consensus 10 by Street82 (2968 pt) | 2022-Nov-17 15:05 |
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Compendium of the most significant studies with reference to properties, intake, effects.
Dołowy M, Pyka A. Evaluation of lipophilic properties of betamethasone and related compounds. Acta Pol Pharm. 2015 Jul-Aug;72(4):671-81.
Abstract. The lipophilicity (R(MW)) of betamethasone and its four related compounds: betamethasone-17,21-dipropionate, betamethasone-17-valerate, betamethasone-21-valerate and also betamethasone disodium phosphate was determined by reversed phase HPTLC and various mobile phase systems (methanol-water, dioxane-water and acetonitrile-water). The chromatographic lipophilicity parameters obtained for all examined compounds using abovementioned mobile phases onto three chromatographic plates (RP-2F254, RP-8F254, RP-18WF254) were compared with the theoretical partition coefficients which have been calculated by different computing programs: AlogPs, AClogP, AlogP, MlogP, KOWWIN, xlogP2, xlogP3, logP(ChemDraw) as well as with logP measured by shake-flask method. The results of this work demonstrate that regardless of applied method the greatest similarity in lipophilic properties show betamethasone-17-valerate, betamethasone-21-valerate and also betamethasone 17,21-dipropionate. The influence of solvent system as mobile phase on R(MW) values of examined compounds was observed. Among different mobile phases (organic modifier-water) proposed in this study, which allowed obtaining the reliable chromatographic lipophilicity parameters for all studied compounds is methanol-water mixture. The performance investigations showed that RP-HPTLC method has proved to be a rapid and cost effective analytical tool for describing the lipophilic properties of betamethasone and its related compounds.
Chaiswing L, Xu F, Zhao Y, Thorson J, Wang C, He D, Lu J, Ellingson SR, Zhong W, Meyer K, Luo W, St Clair W, Clair DS. The RelB-BLNK Axis Determines Cellular Response to a Novel Redox-Active Agent Betamethasone during Radiation Therapy in Prostate Cancer. Int J Mol Sci. 2022 Jun 8;23(12):6409. doi: 10.3390/ijms23126409.
Abstract. Aberrant levels of reactive oxygen species (ROS) are potential mechanisms that contribute to both cancer therapy efficacy and the side effects of cancer treatment. Upregulation of the non-canonical redox-sensitive NF-kB family member, RelB, confers radioresistance in prostate cancer (PCa). We screened FDA-approved compounds and identified betamethasone (BET) as a drug that increases hydrogen peroxide levels in vitro and protects non-PCa tissues/cells while also enhancing radiation killing of PCa tissues/cells, both in vitro and in vivo.
Perna-Barrull D, Murillo M, Real N, Gomez-Muñoz L, Rodriguez-Fernandez S, Bel J, Puig-Domingo M, Vives-Pi M. Prenatal Betamethasone Exposure and its Impact on Pediatric Type 1 Diabetes Mellitus: A Preliminary Study in a Spanish Cohort. J Diabetes Res. 2022 Mar 10;2022:6598600. doi: 10.1155/2022/6598600.
Abstract. The main aim of this study was to evaluate the possible association between betamethasone prenatal exposure and T1D in humans.
Kakoulidis I, Ilias I, Linardi A, Stergiotis S, Togias S, Michou A, Koukkou E. Glycemic profile assessment during betamethasone administration in women with twin pregnancies after IVF with or without gestational diabetes. Diabetes Metab Syndr. 2022 Jun;16(6):102534. doi: 10.1016/j.dsx.2022.102534.
Abstract. We assessed the glycemic profile of 30 women with twin pregnancies after in-vitro-fertilization who were given betamethasone.
Fachin EV, Scarparo RK, Pezzi AP, Luisi SB, Sant'ana Filho M. Effect of betamethasone on the pulp after topical application to the dentin of rat teeth: vascular aspects of the inflammation. J Appl Oral Sci. 2009 Jul-Aug;17(4):335-9. doi: 10.1590/s1678-77572009000400012.
Abstract. This study investigated the pulpal effect of topically applied betamethasone to the dentin of rat molars in the vascular phase of inflammation... Betamethasone applied on the dentin of rat teeth proved to reduce the vascular phase of pulp inflammation regarding vessel diameter and number of blood vessels.
Verdurmen KMJ, Warmerdam GJJ, Lempersz C, Hulsenboom ADJ, Renckens J, Dieleman JP, Vullings R, van Laar JOEH, Oei SG. The influence of betamethasone on fetal heart rate variability, obtained by non-invasive fetal electrocardiogram recordings. Early Hum Dev. 2018 Apr;119:8-14. doi: 10.1016/j.earlhumdev.2018.02.011.
Abstract. To describe the effect of betamethasone on fetal heart rate variability, by applying spectral analysis on non-invasive fetal electrocardiogram recordings.
Salem II, Najib NM. Pharmacokinetics of betamethasone after single-dose intramuscular administration of betamethasone phosphate and betamethasone acetate to healthy subjects. Clin Ther. 2012 Jan;34(1):214-20. doi: 10.1016/j.clinthera.2011.11.022.
Abstract. Betamethasone is used for its antiinflammatory and immunosuppressive effects in disorders of many organ systems. However, the pharmacokinetic properties of betamethasone in plasma after intramuscular injection of betamethasone sodium phosphate and betamethasone acetate dual-acting suspension need further investigation.
Salim R, Suleiman A, Colodner R, Nachum Z, Goldstein LH, Shalev E. Measurement of betamethasone concentration in maternal serum treated for fetal lung maturity; Is it feasible? Reprod Biol Endocrinol. 2016 Feb 10;14:7. doi: 10.1186/s12958-016-0142-4.
Abstract. The association between maternal serum concentration of betamethasone given for fetal lung maturity and perinatal outcome has not been investigated. This may be due to an absence of a reliable method for measuring serum betamethasone concentrations. We aimed in the current study to assess the feasibility of a specific ELISA kit to measure the concentrations of betamethasone in maternal serum and to examine the trend of sequential measurements after a course of betamethasone for fetal lung maturity.
Jobe AH, Nitsos I, Pillow JJ, Polglase GR, Kallapur SG, Newnham JP. Betamethasone dose and formulation for induced lung maturation in fetal sheep. Am J Obstet Gynecol. 2009 Dec;201(6):611.e1-7. doi: 10.1016/j.ajog.2009.07.014.
Abstract. We hypothesized that maternal treatments with betamethasone acetate induce fetal lung maturation comparably to the betamethasone phosphate+betamethasone acetate used clinically.... A single maternal dose of betamethasone acetate effectively induces fetal lung maturation in sheep with minimal fetal exposure.
Knych HK, Stanley SD, Harrison LM, Mckemie DS. Pharmacokinetics of betamethasone in plasma, urine, and synovial fluid following intra-articular administration to exercised thoroughbred horses. Drug Test Anal. 2017 Sep;9(9):1385-1391. doi: 10.1002/dta.2170.
Abstract. The use of corticosteroids, such as betamethasone, in performance horses is tightly regulated. The objective of the current study was to describe the plasma pharmacokinetics of betamethasone as well as time-related urine and synovial fluid concentrations following intra-articular administration to horses.
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"Descrizione" about Betamethasone Review Consensus 10 by Street82 (2968 pt) | 2023-Sep-11 10:11 |
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Betamethasone is a chemical compound, a synthetic corticosteroid. The class of steroid hormones, corticosteroids, produced by the adrenal cortex, consists of glucocorticoids and corticosteroids.
Glucocorticoids (cortisone, cortisol and corticosterone) represent one of the two types of corticosteroids or steroid hormones that are produced by the adrenal cortex and are generated from the zona fasciculata of the adrenal cortex, the second of the two types being corticosteroids that are generated from both the zona fasciculata and the zona glomerulosa of the adrenal cortex. But while glucocorticoids are a single type of corticosteroid, corticosteroids are both glucocorticoids and mineralocorticoids.
Appears in the form of a white or whitish powder, incompatible with strong oxidising agents.
What it is used for and where
Take only under medical supervision
Medical
Inflammation is a reaction induced by physical, chemical or biological agents, locally, of vascular tissues characterised, in the extravascular or interstitial environment, by the loss of blood and liquid cells.
Betamethasone has anti-inflammatory, metabolic, immunosuppressive and anti-asthmatic long-acting properties. Specific intracellular glucocorticoid receptors are intercepted by Betamethasone, which binds to DNA, inhibiting the synthesis of certain inflammatory mediators and reducing autoimmune reactions and chronic inflammation. It is administered orally, intravenously, intramuscularly and subcutaneously.
It is used locally as a contrast to inflammatory skin conditions such as eczema, to manage autoimmune disorders, ophthalmic irritations with negligible mineralocorticoid activity. In cases of anaphylactic and allergic reactions, soft tissue lesions, Alzheimer's disease and Addison's disease it is also able to modulate gene expression for anti-inflammatory activity, suppressing the immune system response, however corticosteroids have a tendency to mask some symptoms of infection and overlapping infections may occur during their use (1). The efficacy of betamethasone in nano-betamethasone form in treating experimental nickel-induced contact dermatitis has been shown to be superior to betamethasone (2)
Eye infections are often treated with corticosteroids and antibacterial eye drops containing betamethasone, which helps relieve redness of the eye by reducing inflammation (3).
The US Food and Drug Administration (FDA) has banned the injection of epidural steroids, a non-surgical option to relieve spinal pain, with particulate steroids. This study confirms the efficacy of betamethasone as an appropriate non-particulate steroid for this particular type of injection (4).
Recently, a hydrogel of silk fibroin, a natural fibre of a protein nature produced by certain insects, together with betamethasone encapsulated and injected into intra-articular cavities increased therapeutic efficacy in the inflamed joints of patients with rheumatoid arthritis, a rheumatic disease currently without curative treatment (5).
Some esters, salts and derivatives of this compound also have similar properties, namely: betamethasone-17,21-dipropionate, betamethasone-17-valerate, betamethasone-21-valerate e betamethasone disodium phosphate.
Safety
The long-term use of corticosteroids administered in high doses poses some concern due to side effects. Like all drugs it can cause side effects. Always ask the physician.
The most relevant studies and their abstracts have been selected to explore this in more depth:
Appearance | White powder |
Boiling Point | 568.2±50.0°C at 760 mmHg |
Melting Point | 235-237°C |
Flash Point | 297.5±30.1°C |
Density | 1.3±0.1 g/cm3 |
PSA | 94.83000 |
LogP | 1.87 |
Refraction Index | 1.592 |
Vapor Pressure | 0.0±3.5 mmHg at 25°C |
Safety |
Synonyms
References_________________________________________________________________
(1) Artini M, Papa R, Cellini A, Tilotta M, Barbato G, Koverech A, Selan L. Effect of betamethasone in combination with antibiotics on gram positive and gram negative bacteria. Int J Immunopathol Pharmacol. 2014 Oct-Dec;27(4):675-82. doi: 10.1177/039463201402700426.
(2) Hudan-Tsilo I, Tokarskyy O, Shevchuk O, Korda M. Chitosan self-assembled polymeric nanoparticles for percutaneous delivery of betamethasone in contact dermatitis. Drug Dev Ind Pharm. 2021 Aug;47(8):1310-1317. doi: 10.1080/03639045.2021.1989457.
(3) Sabry HS, Al-Shohani ADH, Mahmood SZ. Formulation and Evaluation of Levofloxacin and Betamethasone Ophthalmic Emulgel. J Pharm Bioallied Sci. 2021 Apr-Jun;13(2):205-211. doi: 10.4103/jpbs.JPBS_338_20.
(4) Lee GY, Lee JW, Lee E, Yeom JS, Kim KJ, Shin HI, Kang HS. Evaluation of the efficacy and safety of epidural steroid injection using a nonparticulate steroid, dexamethasone or betamethasone: a double-blind, randomized, crossover, clinical trial. Korean J Pain. 2022 Jul 1;35(3):336-344. doi: 10.3344/kjp.2022.35.3.336.
(5) Oliveira IM, Gonçalves C, Shin ME, Lee S, Reis RL, Khang G, Oliveira JM. Anti-Inflammatory Properties of Injectable Betamethasone-Loaded Tyramine-Modified Gellan Gum/Silk Fibroin Hydrogels. Biomolecules. 2020 Oct 17;10(10):1456. doi: 10.3390/biom10101456.
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Last update:   2022-07-29 16:38:46 | Chemical Risk:   |