Corticosteroids Flashcards
Cortisol Metabolic Functions
Provide Energy for stress state
- Gluconeogenesis
- Glycogenolysis (indirectly by Glucagon)
- Lipolysis
Blood glucose increase, Insulin
- Lipogenesis, Net fat deposition increases
Cortisol Regulation
Axis - Negative feedback: Cortisol to Hypothalamus
Inflammation - Pro-inflammatory cytokines TNFa, IL1, IL6
Cortisol Catabolic Functions
Proteolysis (for gluconeogenesis)
Lipolysis (but Insulin then encourages lipogenesis)
Reduce Calcium Absorption;
Reduce Bone formation
Cortisol Inflammatory Functions
Decrease expression of pro-inflammatory cytokines, chemokines:
- Limit adhesion molecules
- Decrease IL2Receptors, TCR
- Decrease enzymes - COX, 5-LOX, PLA2
Increase other targets
- B2 receptors, for bronchodilation
Overall decrease T cell, B cell, M, E , B; just increase neutrophils, promote resolution of inflammation; decrease type IV hypersensitivity rxn, hence Immunosuppressant for transplants;
Miscellaneous Cortisol Functions
- Increase surfactant production in lungs
Hydrocortisone (Cortisol)
Cortisone
Which is prodrug
Cortisone is prodrug
Prednisolone
Prednisone
Which is prodrug
Prednisone is prodrug
Whats the deal with Methylprednisolone, Triamcinolone, Dexamethasone and Betamethasone
Increasing glucocorticoid effect
NO water retention effect (aldosterone)
Beta and Dexa 1-3 days MOA, increase potency;
Side effects
Cushing’s Syndrome:
Hyperglycaemia
Obesity
Muscle Wasting
Growth Retardation
Delayed Wound Healing, Skin thinning (limited ECM and collagen production)
Water retention, Edema, Hypertension, CHF
Oesteoporosis
GI bleeding
Must taper dose off or else insufficiency;