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Prednisolone has a relatively short half-life, ranging 2–4 hours. It also has a large therapeutic window, considering the dosage required to produce a therapeutic effect is a few times higher than what the body naturally produces. [14] Prednisolone is 70–90% plasma protein bound, it binds to proteins such as albumin. [14]
Corticosteroids act as agonists of the glucocorticoid receptor and/or the mineralocorticoid receptor. [ citation needed ] In addition to their corticosteroid activity, some corticosteroids may have some progestogenic activity and may produce sex-related side effects.
Chemically, methylprednisolone is a synthetic pregnane steroid hormone derived from hydrocortisone and prednisolone. It belongs to a class of synthetic glucocorticoids and more generally, corticosteroids. It acts as a mineralocorticoid and glucocorticoid receptor agonist.
Prednisolone: 4 0.8 16–36 Methylprednisolone: 5–7.5 0.5 18–40 Dexamethasone: 25–80 0 36–54 Betamethasone: 25–30 0 36–54 Triamcinolone: 5 0 12–36 Deflazacort: 6.5 – 1.3 Fludrocortisone acetate: 15 200 24 Deoxycorticosterone acetate: 0 20 – Aldosterone: 0.3 200–1000 – Beclometasone
Selective glucocorticoid receptor modulators (SEGRMs) and selective glucocorticoid receptor agonists (SEGRAs) formerly known as dissociated glucocorticoid receptor agonists (DIGRAs) are a class of experimental drugs designed to share many of the desirable anti-inflammatory, immunosuppressive, or anticancer properties of classical glucocorticoid drugs but with fewer side effects such as skin ...
Dexamethasone and other corticosteroids are agonists, while mifepristone and ketoconazole are antagonists of the GR. Anabolic steroids also prevent cortisol from binding to the glucocorticoid receptor.
Prednisone is a prodrug and must be converted to prednisolone by the liver before it becomes active. [6] [7] Prednisolone then binds to glucocorticoid receptors, activating them and triggering changes in gene expression. [4] Prednisone was patented in 1954 and approved for medical use in the United States in 1955.
Steroid ring system.. This is a list of corticosteroids (glucocorticoids and mineralocorticoids) or derivatives of cortisol (hydrocortisone).Most esters of these corticosteroids are not included in this list; for esters, see here instead.
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