Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1    Pharmacodynamic properties

Pharmacotherapeutic group: glucocorticoid
ATC code:                  H02AB08

Triamcinolone is a synthetic glucocorticoid with marked anti-allergic, anti-inflammatory and membrane-stabilising properties, as well as effects on carbohydrate, protein and lipid metabolism.
Triamcinolone has less mineralocorticoid activity than prednisolone.

Glucocorticoids exert their biological effect by activating transcription of corticosteroid- sensitive genes. The anti-inflammatory, immunosuppressive and antiproliferative effects are induced by various factors, including reduced formation, release and activity of inflammatory mediators and inhibition of specific functions and migration of inflammatory cells. In addition, the effect of sensitised T-lymphocytes and macrophages on target cells may be prevented by corticosteroids.

If long-term corticosteroid medication is necessary, possible induction of transient adrenocortical insufficiency must be taken into consideration. Suppressibility of the hypothalamic-pituitary-adrenocortical axis depends, amongst other things, on individual factors.

Pharmacokinetic Properties

5.2   Pharmacokinetic properties

Triamcinolone is rapidly absorbed after oral administration. In humans, it is bound exclusively to albumin. No binding to transcortin takes place. The plasma half-life in humans is approximately 300 minutes. The biological action of glucocorticoids goes far beyond the plasma half-life, due to enzyme induction and the subsequent specific corticosteroid effect.
Metabolism in the liver as with all corticosteroids is about 70% conjugation with glucuronic acid and 30% sulphation. The excretion of inactive metabolites (including 6β hydroxy triamcinolone) is mostly renal (15% unchanged) and only to a lesser extent faecal.