Antirheumatic potency of chemically modified adrenocortical steroids

Boland, Edward W.

doi:10.1016/0002-9343(61)90142-5

Cited by 21 publications

(7 citation statements)

References 25 publications

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“…The ratio of the concentrations of' cortisol required to inhibit hair follicles in cultured skin, 7·5 J1g/ml medium (Singh and Hardy 1975), and of flumethasone required to cause wool fibre shedding here, about 7 ng/ml plasma, is approximately 1000: 1, a proportion not markedly dissimilar to 700: 1 reported for the same two chemicals in the liver glycogen deposition assay (Fried 1960) or from 730: 1 in the granuloma inhibition assay in rats (Boland 1961).…”

Section: Discussionmentioning

confidence: 53%

The Administration of Flumethasone, by Three Different Routes, its Measurement in the Plasma and Some Effects on Wool Growth in Merino Wethers

Panaretto¹,

Wallace²

1978

Aust. Jnl. Of Bio. Sci.

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Flumethasone was given to Merino wethers weighing 30-50 kg at rates of 0·62-1· 35 mg/kgO' 7 5 by intravenous (experiments 1 and 2), intraruminal (experiment 4) and subcutaneous (experiment 5) routes over 8 days. In experiment 3, 1· 2 mgflumethasone/kg'"?" was given intravenously over 4, 5 or 6 days. The plasma concentration profiles showed concentrations in the order: intravenous > subcutaneous > intraruminal. Plasma concentration patterns usually were highest during the first 48 h of infusion followed by relatively stable values. This last feature was not evident in experiments when the rate of hormone infusion was increased. Estimates of the metabolic clearance rates for flumethasone in experiments 1, 2 and 5 were 200-700 ml/min during the' equilibrium concentration periods.The effects of flumethasone on some, aspects of wool growth revealed interactions between the routes of administration, the period of dosage and the rate of wool growth in the recipients.In experiments 1 and 2 intravenous infusion of 1·20-1· 33 mg flumethasone/kg'"?" caused the shedding of all wool fibres about 30 days after treatment. Some effects of dosing sheep with flumethasone at a time when wool growth was decreasing were also observed in experiment 2. Flumethasone given at a rate of 1· 2 mg/kg'"?" over 4, 5 or 6 days caused the shedding of only some wool fibres which were firmly retained on the sheep by the continuous fibres. Intraruminal and subcutaneous infusions of O·62-1· 35 mg flumethasone/kg'"?" had similar results to the last in the majority of animals although in a few cases no discontinuity of wool fibres was observed.Recovery in wool growth was observed after treatment. Animals regained their pretreatment wool growth in experiments 1, 4 and 5 by 60 days after treatment and probably equalled at that, time wool growth in controls. Recovery was retarded in some individuals in experiment 2 and in some groups in experiment 3. In experiment 1, 21 days wool growth was estimated to have been lost. Some aspects of complete versus partial shedding of wool fibres are discussed particularly with reference to wool harvesting. Some similarities in the appearance of fleeces of steroid-treated sheep and naturally shedding animals are also discussed.In some experiments, particularly when the infusion rate of flumethasone was increased (experiment 3), the sheep showed temporary but significant feed refusals during, but more commonly after, treatment. Speculative discussion as to the metabolic causes of this response is included.

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Section: Discussionmentioning

confidence: 53%

The Administration of Flumethasone, by Three Different Routes, its Measurement in the Plasma and Some Effects on Wool Growth in Merino Wethers

Panaretto¹,

Wallace²

1978

Aust. Jnl. Of Bio. Sci.

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“…They are often simply exchanged for each other in the dose ratio of 10:1, because a single tablet contains either 5 mg of prendnisolone or 0.5 mg of betamethasone as an equivalent dose. This equivalency, however, has been decided on the basis of very early reports (Silber, 1959;Tolksdorf, 1959;Boland, 1961;Roberts, 1962).…”

mentioning

confidence: 99%

Relative potency in acute and chronic suppressive effects of prednisolone and betamethasone on the hypothalamic-pituitary-adrenal axis in man.

et al. 1980

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The relative potency in the hypothalamic-pituitary-adrenal (HPA) suppression of both prednisolone and betamethasone was examined in an acute study with normal volunteers and in a chronic study with glucocorticoid-treated patients. Circadian rhythm of plasma cortisol was studied after a single dose administration of 5 to 30 mg prednisolone or 0.5 to 3.0 mg betamethasone at 08 : 00 hr. Morning-rise of plasma cortisol occurred on the morning after the administration of 30 mg or less prednisolone but no morning rise was noted after the administration of 1.0 mg or more betamethasone. Plasma ACTH was slightly elevated on the morning after 30 mg prednisolone administration but showed low levels throughout the night after 3.0 mg betamethasone administration.Plasma cortisol responsiveness to ACTH was examined in patients before and during therapy with either prednisolone or betamethasone.The basal cortisol level was not suppressed and the responsivenessto ACTH remained nearly normal during long-term 5 mg prednisolone therapy, but these were completely suppressed during long-term 0.5 mg betamethasone therapy.The responsiveness to ACTH was nearly normal in patients receiving alternate-day therapy with prednisolone in such large doses as 50 or 60 mg every other day, but was completely suppressed in patients receiving 1.0 mg betamethasone every other day. The relative potency of betamethasone in acute and chronic suppressive effects on the HPA system seems to be much stronger than that of prednisolone inequivalent doses with comparable anti-inflammatory effects. It is also suggested that the alternate-day therapy with such long-acting steroids as betamethasone are useless in preventing HPA suppression.

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“…This order of decreasing activity is closely related to that described by others (16, 17). Similarly, one may also correlate steroidal modifications such as the addition of A1, 6-methyl,6-fluoro, 9-fluoro, 6,9-difluoro, 16-methy1, and 16,17-acetonide to the increasing order of biological activity ( 5 , 16,18,19).…”

Section: Discussionmentioning

confidence: 99%

Modified Granuloma Pouch Procedure for the Evaluation of Topically Applied Anti-inflammatory Steroids

DiPasquale¹,

Rassaert²,

McDougall³

1970

Journal of Pharmaceutical Sciences

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Antirheumatic potency of chemically modified adrenocortical steroids

Cited by 21 publications

References 25 publications

The Administration of Flumethasone, by Three Different Routes, its Measurement in the Plasma and Some Effects on Wool Growth in Merino Wethers

The Administration of Flumethasone, by Three Different Routes, its Measurement in the Plasma and Some Effects on Wool Growth in Merino Wethers

Relative potency in acute and chronic suppressive effects of prednisolone and betamethasone on the hypothalamic-pituitary-adrenal axis in man.

Modified Granuloma Pouch Procedure for the Evaluation of Topically Applied Anti-inflammatory Steroids

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