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Prednisone is a synthetic glucocorticoid used for its anti-inflammatory and immunosuppressive properties. [36] [37] Prednisone is a prodrug; it is metabolised in the liver by 11-β-HSD to prednisolone, the active drug. Prednisone has no substantial biological effects until converted via hepatic metabolism to prednisolone. [38]
A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. [1] [2] Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted . [3] [4]
Prednisolone is a synthetic pregnane corticosteroid closely related to its cognate prednisone, having identical structure save for two fewer hydrogens near C 11. It is also known as δ 1 -cortisol , δ 1 -hydrocortisone , 1,2-dehydrocortisol , or 1,2-dehydrohydrocortisone , as well as 11β,17α,21-trihydroxypregna-1,4-diene-3,20-dione .
Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex of vertebrates, as well as the synthetic analogues of these hormones.Two main classes of corticosteroids, glucocorticoids and mineralocorticoids, are involved in a wide range of physiological processes, including stress response, immune response, and regulation of inflammation, carbohydrate metabolism ...
Like many other steroid esters, they are prodrugs. Unlike other steroid esters however, they bypass first-pass metabolism with oral administration and have high oral bioavailability and potency, abolished first-pass hepatic impact, and long elimination half-lives and durations of action. They are under development for potential clinical use.
Cortisone is a pregnene (21-carbon) steroid hormone.It is a naturally-occurring corticosteroid metabolite that is also used as a pharmaceutical prodrug. Cortisol is converted by the action of the enzyme corticosteroid 11-beta-dehydrogenase isozyme 2 into the inactive metabolite cortisone, particularly in the kidneys.
Chloroprednisone is a topical glucocorticoid first reported in 1960. [1] It is a chlorinated derivative of prednisone.The acetate ester prodrug, chloroprednisone 21-acetate, was sold under the brand name Topilan as an anti-inflammatory agent.
The history of prodrugs, like Prednisone, is not always a happy one. See Phenacetin the prodrug of Paracetamol (Tylenol in the USA). Phenacetin was banned in 1984 (I think it was'84). Because if you lacked the gene/s that produced the specific enzyme required to convert Phenacetin to Paracetamol death could and did result.
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109 S High St #100, Columbus, OH · Directions · (614) 224-4261
Ranked at No. 20 on the 2020 Disruptor 50 list. - CNBC