Core pharmacology

Class Group

Mineralocorticoid

Legacy Cicm Level

Level 3

Introduction

Synthetic

Indications Uses

used to treat adrenocortical insufficiency and salt-losing adrenogenital syndrome.

Presentation

100mcg tablets

Main Action

To replace endogenous aldosterone

Mechanism of action

Bind to mineralocorticoid receptors →
Renal: ↑ Na resorption, K excretion

lipid solubile → crosses cell membranes → bind to steroid receptors via “zinc finger” binding site
→ signal trascribed via second messenger → alters gene transcription and the production of proteins

Onset Peak Duration

Dur: 3-5 days

Physiological effects

- sodium and water retention (aldosterone like)
- inc Na reabsorption on distal tubles, K+ and H+ excretion

Glucocorticoid action: Metabolic, Anti-inflammatory effects, Immunosuppresion

Adverse Effects Toxicity

GI disturbances
Weight gain
Allergy

Absorption

Rapid and complete

Protein binding

70-80% (Albumin, Corticosteroid binding Globulin)

Volume of distribution

80-85 L

Metabolism

Liver – CYP3A - 2 main metabolites

Excretion

80% urine
20% feces

Clearance

40 L/h

Half-life

18-36hrs

Special Points

15

150

Long

Route And Dose

PO