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

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

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

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

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

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

IV
Rapidly given PO or PR
PO BA: 50%

IV

IV
PO BA 80-90%

CBG 70%, Alb 20%

80%

70%

0.5 L/kg

Low

Low

Liver – Tetrahydrocortisone

Liver

Liver – CYP3A4

Urine

Urine

Urine

167-283 ml/min

0.5-1.5h

2-4h

3.5-5h

▪ 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

Inhaled: oral candidiasis (poor technique), dysphonia, minor adrenal suppresion

▪ 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

▪ 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

Glucocorticoid

Glucocorticoid

Glucocorticoid

1. as replacement therapy in adrenocortical deficiency states and in the
treatment of
2. allergy and anaphylaxis
3. asthma
4. panoply of autoimmune disorders
5. eczema and contact sensitivity syndromes and
6. in leukaemia chemotherapy regimes and
7. for immunosuppression after organ transplantation

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.

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.

Natural
Dose Equivalence 25

Synthetic
Dose Equivalence 4

Synthetic
Dose Equivalence 0.75

Level 2

Level 2

Level 2

Anti-inflammatory

Anti-inflammatory

Anti-inflammatory

Dur: 8-36h

Dur: 12-36h

Dur: 36-54h

10/20mg tablets
White lyophilized power to be mixed in water
Other topical preparations

White powder – mixed with water

0.5/2mg tablets
Oral solution
Vials – white powder

PO,TOP, IV, IM, IA

PO,TOP, IV, IM, IA, epi

PO,TOP, IV, IM, IA

100

1

Short

20

Min

Intermediate

4

Min

Long