Source: Υπουργείο Υγείας (CY) Revision Year: 2021 Publisher: MEDOCHEMIE LTD, 1-10 Constantinoupoleos street, 3011 Limassol, Cyprus
Pharmacotherapeutic group: glucocorticoids
ATC code: H02AB06
Prednisolone is a corticosteroid with predominant glucocorticosteroid activity. Glucocorticosteroids (short name glucocorticoids) have predominantly a catabolic effect in peripheral tissues. The uptake and conversion of glucose and amino acids in the cells are inhibited, resulting in increased protein breakdown and a rise in blood sugar levels, whereas glycogenesis and gluconeogenesis are stimulated in the liver.
However, glucocorticoids owe largely their effect to a couple of other properties:
Prednisolone sodium phosphate is a readily soluble prednisolone ester which possesses a four times greater anti-inflammatory activity than the natural adrenal cortex hormone, hydrocortisone. On the contrary, the influence on the water and electrolyte balance is only 0.8 times that of hydrocortisone. The biological activity of prednisolone occurs later than what could be expected because of the plasma levels, certainly because the activity occurs indirectly through stimulation of the intracellular enzyme synthesis. The biological half-live is 12-36 hours.
Prednisolone sodium phosphate is a readily soluble prednisolone ester. After administration of prednisolone, the prednisolone sodium phosphate is rapidly converted to prednisolone.
Prednisolone is 60-70% bound to plasma proteins transcortin and albumin. Prednisolone crosses the placenta and small amounts are excreted in breast milk.
Prednisolone is mainly excreted in the urine as free and conjugated metabolites, together with an appreciable proportion of unchanged prednisolone. Prednisolone has a plasma half-life of at least 200 minutes.
Cleft palate is observed in rats, mice, hamsters, rabbits and primates; it is not seen in horses and sheep. The abnormalities are sometimes accompanied by defects of the central nervous system and heart. In primates, brain damage was observed in antenatal exposure. Additionally, intrauterine growth was inhibited. These phenomena were observed after use of high doses.
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