16-Methylated STEROIDS. II. 16α-Methyl ANALOGS OF CORTISONE, a NEW GROUP OF ANTI-INFLAMMATORY STEROIDS. 9α-Halo DERIVATIVES

Arth, Glen E.; Fried, J. H.; Johnston, David B.; Hoff, Dale R.; Sarett, L. H.; Silber, Robert; Stoerk, Herbert C.; Winter, Charles A.

doi:10.1021/ja01545a063

Cited by 75 publications

(14 citation statements)

References 8 publications

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“…Dexamethasone is a synthetic version of naturally occurring corticosteroid hormone and was first made in 1958 and heralded as a potent anti-inflammatory drug [86]. In 1976, Glover and Labadie reported that dexamethasone appeared to cause the formation of significantly smaller and lighter blood clots in CSDH, without the presence of a capsule [87].…”

Section: Pharmacotherapymentioning

confidence: 99%

Pathophysiology of chronic subdural haematoma: inflammation, angiogenesis and implications for pharmacotherapy

Edlmann

Giorgi-Coll

Whitfield

et al. 2017

J Neuroinflammation

424

360

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Chronic subdural haematoma (CSDH) is an encapsulated collection of blood and fluid on the surface of the brain. Historically considered a result of head trauma, recent evidence suggests there are more complex processes involved. Trauma may be absent or very minor and does not explain the progressive, chronic course of the condition. This review focuses on several key processes involved in CSDH development: angiogenesis, fibrinolysis and inflammation. The characteristic membrane surrounding the CSDH has been identified as a source of fluid exudation and haemorrhage. Angiogenic stimuli lead to the creation of fragile blood vessels within membrane walls, whilst fibrinolytic processes prevent clot formation resulting in continued haemorrhage. An abundance of inflammatory cells and markers have been identified within the membranes and subdural fluid and are likely to contribute to propagating an inflammatory response which stimulates ongoing membrane growth and fluid accumulation. Currently, the mainstay of treatment for CSDH is surgical drainage, which has associated risks of recurrence requiring repeat surgery. Understanding of the underlying pathophysiological processes has been applied to developing potential drug treatments. Ongoing research is needed to identify if these therapies are successful in controlling the inflammatory and angiogenic disease processes leading to control and resolution of CSDH.

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Section: Pharmacotherapymentioning

confidence: 99%

Pathophysiology of chronic subdural haematoma: inflammation, angiogenesis and implications for pharmacotherapy

Edlmann

Giorgi-Coll

Whitfield

et al. 2017

J Neuroinflammation

424

360

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“…The depressant effects on wool growth of a potent analogue of cortisol, dexamethasone [9-fluoro-ll,17,21-trihydroxy-16 a-methyl-pregna-l,4-diene-3,20-dione (Arth et al 1958;Sarett 1959)], was reported by Ferguson et al (1965) and of some dexamethasone derivatives by Panaretto et al (1975) but in neither investigation were plasma concentrations of the hormone or analogues reported. Panaretto et al (1975) also reported much variability in wool growth depression between sheep given identical single intravenous doses of dexamethasone derivatives.…”

Section: Introductionmentioning

confidence: 94%

Dexamethasone Concentrations in Ovine Plasma During its Intravenous Infusion, its Relation to the Production of Some Endogenous Hormones, and Some of the Effects on Wool Growth

Ba¹,

Wallace²

1978

Aust. Jnl. Of Bio. Sci.

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Plasma concentrations of dexamethasone have been measured in sheep during an 8-day infusion of dexamethasone-21-phosphate. The dexamethasone concentration profiles generally revealed a reproducible pattern with three phases-a peak during the first 48 h infusion which was followed by falling concentrations during the next 5 days, and a small increase in dexamethasone concentration during the final 24 h infusion was not uncommon. The pattern of dexamethasone concentrations was retained when dosage was arranged in such a way as to infuse increasing quantities of hormonal analogue as infusion progressed. Aspects of the metabolism of the analogue are discussed.Endogenous thyroxine and cortisol were significantly depressed during infusion. In these experiments wool was completely shed in three out of four animals dosed at a rate of 8·5 mg dexamethasone/kg o · 75 • The recovery of wool growth to its pretreatment values occurred by about one month after infusion. The consumption of food and body weight increases were satisfactory during the post-infusion period.

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“…This increased anti-inflammatory activity four to five times. During 1957, Arth et al synthesized dexamethasone (9-alpha-fluoro, 16-alpha-methylprednisolone) which is a synthetic analogue of methylprednisolone in which a methyl group has been added at the carbon 16 position and a fluorine atom at the carbon 9 position [ 8 , 9 ]. The addition of fluorine at the carbon 9 position greatly enhances the anti-inflammatory activity of the new compound.…”

Section: Introductionmentioning

confidence: 99%

Do Corticosteroids Still Have a Role in the Management of Third Molar Surgery?

Ngeow

Lim

2016

Adv Ther

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IntroductionThe use of corticosteroids to reduce the post-operative sequelae of lower third molar surgery, namely pain, swelling and trismus, has been well studied by many researchers over the past 6 decades. This study reviewed the reported outcome of corticosteroids used in controlling the above sequalae after third molar surgery.Materials and MethodsA PubMed, Medline, EMBASE and Google search was undertaken of all controlled clinical trials on the effects of corticosteroids on pain, swelling and trismus after lower third molar surgery. The review was limited to studies published over the last 10 years (2006–2015).ResultsOf the 46 initially retrieved articles, 34 were finally included. Eleven studies compared the effect of 2 similar (but different dose) or different group of corticosteroids. Thirty-one studies reported the effects of corticosteroids on all sequale, 2 reported the outcome on swelling and trismus and another 1 on swelling and pain only. In 16 of the studies, corticosteroid use resulted in significant reductions in pain after third molar removal. Twenty-two out of 29 studies reported reduced swelling against negative control while 18 out of 25 studies reported improved mouth opening. Fourteen studies reported the benefit of corticosteroids on all 3 sequelae, with 71.4% resulted from the use of methylprednisolone.ConclusionAlthough there are some conflicting effects, the results of this analysis shows in general the benefits derived from short-term use of corticosteroids in relation to pain, swelling and trismus following third molar surgical extraction, with no side effects observed.FundingThis work was supported by the University of Malaya’s High Impact Research grant UM.C/625/1/HIR/MOHE/05.

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16-Methylated STEROIDS. II. 16α-Methyl ANALOGS OF CORTISONE, a NEW GROUP OF ANTI-INFLAMMATORY STEROIDS. 9α-Halo DERIVATIVES

Cited by 75 publications

References 8 publications

Pathophysiology of chronic subdural haematoma: inflammation, angiogenesis and implications for pharmacotherapy

Pathophysiology of chronic subdural haematoma: inflammation, angiogenesis and implications for pharmacotherapy

Dexamethasone Concentrations in Ovine Plasma During its Intravenous Infusion, its Relation to the Production of Some Endogenous Hormones, and Some of the Effects on Wool Growth

Do Corticosteroids Still Have a Role in the Management of Third Molar Surgery?

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