Core pharmacology

Class Group

Glucocorticoid

Legacy Cicm Level

Level 2

Introduction

Synthetic
Dose Equivalence 4

Indications Uses

1. as replacement therapy in adrenocortical deficiency states and in the
treatment of
2. allergy and anaphylaxis
3. hypercalcaemia
4. asthma
5. panoply of autoimmune disorders
6. some forms of red eye and
7. in leukaemia chemotherapy regimes and
8. for immunosuppression after organ transplantation.

Presentation

White powder – mixed with water

Main Action

Anti-inflammatory

Mechanism of action

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: 12-36h

Physiological effects

1. Metabolic effects
▪ ↑’s gluconeogensis
▪ ↑ protein catabolism and lipolysis → muscle wasting and thin skin and fat redistribution
(cushingoid)
▪ ↑ bone catabolism → osteoporosis
▪ ↑ glucose release but ↓ absorption from the GIT

2. Anti inflammatory effects
▪ ↓’d phospholipase A2 → ↓ arachidonic acid → ↓ prostaglandins

3. Immunosupression
▪ ↓’d inflammatory mediators
▪ ↓ IL 1-2 → ↓’d lymphocyte prod
▪ altered neutrophil and macrophage function

Adverse Effects Toxicity

▪ Adrenal supression via negative feedback on the HPA
▪ Fluid retention - via weak mineralcorticoid activity
▪ Vascular reactivity - plays a permissive role in the actions of catecholamines on vessels

Absorption

IV

Protein binding

80%

Volume of distribution

Low

Metabolism

Liver

Excretion

Urine

Half-life

2-4h

Special Points

20

Min

Intermediate

Route And Dose

PO,TOP, IV, IM, IA, epi