Core pharmacology

Class Group

Glucocorticoid

Legacy Cicm Level

Level 2

Introduction

Synthetic
Dose Equivalence 0.75

Indications Uses

1. as replacement therapy in congenital adrenocortical deficiency states
and in the treatment of
2. allergic disorders
3. asthma
4. many autoimmune and rheumatologic disorders
5. eczema and contact sensitivity syndromes and
6. leukaemia and lymphoma chemotherapy regimes and
7. immunosuppression after organ transplantation
8. palliative treatment of tumours
9. prevention of post-operative and chemotherapy-induced nausea and
vomiting
10. ophthalmic inflammatory diseases
11. acute exacerbations of inflammatory bowel disease
12. acute severe skin diseases
13. cerebral oedema
14. bacterial meningitis—prevents hearing loss
15. tests for Cushing’s syndrome
16. hypercalcaemia of malignancy, sarcoidosis, and vitamin D toxicity
17. antenatal use in preterm labour
18. myasthenia gravis
19. autoimmune renal disease and
20. has been used for epidural injection.

Presentation

0.5/2mg tablets
Oral solution
Vials – white powder

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: 36-54h

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
PO BA 80-90%

Protein binding

70%

Volume of distribution

Low

Metabolism

Liver – CYP3A4

Excretion

Urine

Half-life

3.5-5h

Special Points

4

Min

Long

Route And Dose

PO,TOP, IV, IM, IA