Summary Drug Metabolism Explained

Glucocorticoids (GC)

NATURAL: SYNTHETIC (fluorinated:

 Cortisone  Betamethasone
 Hydrocortisone  Dexamethasone
 Prednisone (from prednisolone)



Clinical use:

1. Asthma
2. Eczema
3. Allergic conjunctivitis
4. Allergic rhinitis
5. Autoimmune conditions
 RA
 IBD
6. Prevent graft vs. host disease following:
 Organ transplantation
 Bone marrow transplantation
7. Neoplastic disease
 Hodgkin’s disease
 ALL
8. ↓ Cerebral edema
 Metastatic brain tumors
 1 brain tumors (dexamethasone)
9. Addison’s disease

, CORTISOL:
 25-30mg/day

CUSHING’S syndrome: ADDISON’S
 OVERproduction  INSUFFICIENCY
 400 mg/day  0.8 mg/day
↑ Na+ and H2O ↓ Na+ and H2O
↓ K+ ↑ K+


 Destruction of proteins (skin, muscles, bone,
vessels)
 ↑ glycemia
 Redistribution of fat (trunk, neck, face)
 Hypertension
 Hirsutism


Biological activities:

Functions Effects
Metabolism Carbohydrate and protein
Regulates Water and electrolyte equilibrium
Blood circulation Release of catecholamines
 ↑ BP
 Also via Adrenaline
Muscles  ↓ muscular mass
 K+ depletion
 Catabolic effect
CNS Modify excitability of the brain via:
 Action on GABA
Bones  ↑ Bone catabolism
 Mobilization of proteins (on skin, muscles
tendons also)
Retrocontrol (feedback)  HPA-axis
 ACTH production
Anti-inflammatory  Inhibit PLA2
 ↓ Aa
 ↓ PGs