Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1   Pharmacodynamic properties
Pharmacotherapeutic group: glucocorticoids, ATC code: H02AB06 
Sintredius oral solution contains the equivalent of 1.0 mg/ml of prednisolone in the form of the 21-disodium phosphate ester. Prednisolone sodium phosphate is a synthetic glucocorticoid with the same general properties as prednisolone itself and other compounds classified as corticosteroids. Prednisolone is four times as active as hydrocortisone on a weight for weight basis.
Prednisolone sodium phosphate is very soluble in water, and is therefore less likely to cause local gastric irritation than prednisolone alcohol, which is only slightly soluble.
This is important when high dosages are required, as in immunosuppressive therapy.

Pharmacokinetic Properties

5.2    Pharmacokinetic properties
Absorption
Prednisolone is readily absorbed from the gastrointestinal tract with peak plasma concentrations achieved by 1-2 hours after an oral dose. Plasma prednisolone is mainly protein bound (70-90%), with binding to albumin and corticosteroid-binding globulin. The plasma half-life of prednisolone, after a single dose, is between 2.5-3.5 hours.
Distribution
The volume of distribution and clearance of total and unbound prednisolone are concentration dependent, and this has been attributed to saturable protein binding over the therapeutic plasma concentration range.
Metabolism
Prednisolone is extensively metabolised, mainly in the liver, but the metabolic pathways are not clearly defined.
Excretion
Over 90% of the prednisolone dose is excreted in the urine, with 7-30% as free prednisolone, and the remainder being recovered as a variety of metabolites.