Source: Health Products Regulatory Authority (IE) Revision Year: 2021 Publisher: Phoenix Labs, Suite 12, Bunkilla Plaza, Bracetown Business Park, Clonee, Co. Meath., Ireland
Naturally occurring glucocorticoids (hydrocortisone and cortisone), which also have salt-retaining properties, are used as replacement therapy in adrenocortical deficiency states. Their synthetic analogues such as prednisolone are primarily used for their potent anti-inflammatory effect in disorders of many organ systems.
Glucocorticoids cause profound and varied metabolic effects. In addition, theymodify the body’s immune responses to diverse stimuli.
Prednisolone is rapidly and apparently almost completely absorbed after oral administration; it reaches peak plasma concentrations after 1-3 hours. There is however wide inter-subject variation suggesting impaired absorption in some individuals.
Plasma half-life is about 3 hours in adults and somewhat less in children. Its nitial absorption, but not its overall bioavailability, is affected by food. Prednisolone has a biological half-life lasting several hours, making it suitable for alternate-day administration regimens.
Although peak plasma prednisolone levels are somewhat lower after administration of Deltacortril Enteric and absorption is delayed, total absorption and bioavailability are the same as after plain prednisolone. Prednisolone shows dose dependent pharmacokinetics, with an increase in dose leading to an increase in volume of distribution and plasma clearance. The degree of plasma protein binding determines the distribution and clearance of free, pharmacologically active drug. Reduced doses are necessary in patients with hypoalbuminaemia.
Prednisolone is metabolised primarily in the liver to a biologically inactive compound. Liver disease prolongs the half-life of prednisolone and, if the patient has hypoalbuminaemia, also increases the proportion of unbound drug and may thereby increase adverse effects.
Prednisolone is excreted in the urine as free and conjugated metabolites, together with small amounts of unchanged prednisolone.
None stated.
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