Pharmacopeia

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Field METHYLPREDNISOLONE
Endocrine · Endocrine · Level 3
DEXAMETHASONE
Endocrine · Endocrine · Level 3
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

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

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

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

Absorption

IV

IV
PO BA 80-90%

Protein binding

80%

70%

Volume of distribution

Low

Low

Metabolism

Liver

Liver – CYP3A4

Excretion

Urine

Urine

Half-life

2-4h

3.5-5h

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

▪ 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

Class Group

Glucocorticoid

Glucocorticoid

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.

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.

Introduction

Synthetic
Dose Equivalence 4

Synthetic
Dose Equivalence 0.75

Legacy Cicm Level

Level 2

Level 2

Main Action

Anti-inflammatory

Anti-inflammatory

Onset Peak Duration

Dur: 12-36h

Dur: 36-54h

Presentation

White powder – mixed with water

0.5/2mg tablets
Oral solution
Vials – white powder

Route And Dose

PO,TOP, IV, IM, IA, epi

PO,TOP, IV, IM, IA

Special Points

20

Min

Intermediate

4

Min

Long