Steroids Flashcards
Corticosteroids
Used in treatment of inflammatory + autoimmune diseases
Lowest plasma circadian cortisol levels
1-5 ug/100ml
Highest plasma circadian cortisol levels
6-20 ug/100ml
Stress- induced cortisol plasma levels
30-100 ug/100ml
As Cortisol increases
Receptor conc increases
Mediator conc decreases
Side effects
Peptic ulcers Oedema Hypertension Osteoporosis (increases osteoclast activity, decreases osteoblast) Avascular necrosis Glaucoma Juvenile growth retardation
Cushing’s syndrome
High cortisol levels due to administration of corticosteroids
Lipid metabolism
Increased lipolysis by adipocytes
CNS
Regulation neuronal excitability
Skeletal system
Maintenance muscular tone
Carbohydrate metabolism
Inhibit insulin
Stimulate glucagon secretion
Immune system
Immunosuppressive
Human Glucocorticoid receptor
Found in cytoplasm + nucleus of most cells in body- can enter through cell membrane as are lipid
2 main forms
Alpha- binds steroid
Beta- does not bind steroid
Genomic (slow) activity
Transactivation of gene transcription by direct interaction with DNA
Transrepression by interaction with other proteins in cytoplasm or nucleus
Alpha receptor
Transactivation
Ligand binds to alpha to activate receptor
Translocated to nucleus
Regulated gene expression