MEDOPRED Solution for injection / infusion Ref.[28364] Active ingredients: Prednisolone

Source: Υπουργείο Υγείας (CY)  Revision Year: 2021  Publisher: MEDOCHEMIE LTD, 1-10 Constantinoupoleos street, 3011 Limassol, Cyprus

5.1. Pharmacodynamic properties

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:

  • an anti-inflammatory activity (anti-inflammatory effect), suppression of inflammatory reactions of various origins (trauma, allergy, auto-immunity, micro-organisms). The underlying mechanisms are not completely known, the following can be named: reduction of capillary permeability, lysosomal membrane stabilisation, whereby the inflamed cells are destroyed less quickly, inhibition of phospholipase A2, whereby the production of arachidonic acid-derived inflammatory mediators is inhibited, and inhibition of granulation tissue formation.
  • an immunosuppressive effect (anti-allergic) activity, immunoreactions are suppressed. How this effect occurs is not exactly known, the cellular immune-reactivity is inhibited more strongly than the humeral immune-reactivity.

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.

5.2. Pharmacokinetic properties

Absorption

Prednisolone sodium phosphate is a readily soluble prednisolone ester. After administration of prednisolone, the prednisolone sodium phosphate is rapidly converted to prednisolone.

Distribution

Prednisolone is 60-70% bound to plasma proteins transcortin and albumin. Prednisolone crosses the placenta and small amounts are excreted in breast milk.

Metabolism and excretion

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.

5.3. Preclinical safety data

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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