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Flashcards in Adrenocorticosteroids Deck (43)
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1

Hydrocortisone

naturally occuring glucocorticoids 

tightly regulated by CNS 

inhibited by exogenous cortosil 

MOA: gene transcription 

2

effects of hydrocortisone

95% of hormonal activity is d/t cortisol

Gluconeogenesis

increase serum glucose levels leading to stimulation of insulin release and inhibiting uptake by muscle cells

lipolysis

protein catabolism 

Net: maintains adequate glucose supply to brain 

 

3

what is cortisols catabolic effect on bone?

osteoporosis

major limitation for long term use 

4

what is cortisols catabolic effect in children?

growth retardation

major limitation for long term use 

5

cortisol immunosuppressive effects 

increased neutrophils

decreased lymphocytes, monocytes, eosinophils, basophils 

vasoconstriction d/t suppresion of mast cell degranulation - decreased histamine release and cap permeability

6

cortisol immunosuppressive effects

vasoconstriction d/t suppresion of mast cell degranulation

decreased histamine release and cap permeability 

7

cortisol anti-inflammatory effects 

  • inhibition Phospholipase A2 blocking arachidonic acid release 
  • decreased prostaglandins, prostacyclin, thromboxane
  • inhibits NF-KB → inhibits COX-2
  • induction of MAPK phosphatase I (inhibits activated proinflammatory signaling pathways) 

8

other effects of cortisol

  • behavioural changes: insomnia, euphoria leading to depression
  • large doses: increased intracranial pressure 
  • suppression of ACTH, GH, TSH, LH
  • Peptic ulcers: stimulation of H. Pylori, suppression of immune response to H. Pylori 
  • increase platelets and RBCs
  • Impaired renal function
  • Development of fetal lungs 

9

cortisol (hydrocortisone) PK

- Relatively short duration of action
- Diffuses poorly across skin (unless inflamed)
- Diffuses well across mucous membranes
- Some salt-retaining effects

10

Glucocorticoids 

  • Prednisone
  • Hydrocortisone
  • Dexamethasone
  • Beclomethasone
  • Triamcinolone
  • Methylprednisolone

11

Mineralocorticoids

  • Aldosterone
  • Fludrocortisone

12

synthetic glucocorticoids 

  • Rapidly and completely absorbed orally
  • Long t1/2’s
  • Reduced salt-retaining effects

13

glucocorticoid administration

all can be taken orally

14

IM glucocorticoid

triamcinolone

15

IM, IV glucocorticoid

  • Dexamethasone
  • Hydrocortisone
  • Methylprednisolone
  • Prednisolone

16

Aerosol glucocorticoid

  • Beclomethasone
  • Triamcinolone

17

topical glucocorticoid 

  • Beclomethasone
  • Dexamethasone
  • Hydrocortisone
  • Triamcinolone

18

Mineralocorticoid MOA

Major effect of activation of the aldosterone receptor:

increased expression of Na+/K+ ATPase
increased expression of ENaC

19

aldosterone

natural mineralocorticoid 

major role: salt-retaining hormones 

Na+ reabsorption from renal tubule

K+ H+ excretion 

20

Fludrocortisone

synthetic mineralocorticoid, MCly prescribed 

21

mineralocorticoid AEs

  • hypokalemia
  • metabolic alkalosis 
  • increased plasma volume
  • HTN

22

anti-inflammatory vs. salt-retaining effects 

23

treating Chronic adrenocorticol insufficiency

(Addison's disease)

  • weakness, fatigue, weight loss, hypotension, hyperpigmentation, inability to maintain blood glucose levels during fasting 
  • daily oral Hydrocortisone + Fludrocortisone
  • NO dexamethasone (lacks salt-retaining effects) 

24

treating acute adrenocorticol insufficiency

  • associated with life-threatening shock, infection or trauma 
  • start corticosteroids immediately 
  • for patients with previous dx: 
    • Large amounts of parenteral corticosteroids + correction of fluid & electrolyte abnormalities
    • give salt-retaining hormone once hydrocortisone levels are reduced (~ 5 days)

25

treating undiagnosed acute attack adrenocorticol insufficiency

dexamethasone to avoid interference with testing of cortisol levels 

fluid and electrolyte replacement 

26

treating congenital adrenal hyperplasia 

  • Glucocorticoid to suppress ACTH
  • Treat initially as an acute adrenal crisis
  • Once stabilized: oral hydrocortisone or prednisone + fludrocortisone
  • fetus protected in high risk pregnancy w/ dexamethasone admin. to mother 

27

Cushing’s Syndrome

  • resection of 1 or both adrenals 
  • must receive high doses of cortisol before and after surgery
  • Dose has to be slowly decreased to prevent withdrawal
  • cushing disease: irradiation of pituitary tumor 

28

aldosteronism 

  • Primary aldosteronism: renal loss of K+ (hypokalemia, alkalosis & elevation of serum Na+)
  • Treat w/ spironolactone

29

stimulation of lung maturation of fetus 

  • Fetal lung maturation regulated by cortisol secretion
  • premature delivery is expected?
    • give mom large doses of glucocorticoids reduces incidence of respiratory distress syndrome
  • IM steroids - dexamethasone

30

other clinical uses for synthetic corticosteroids 

  • Numerous immunological inflammatory conditions: asthma, collagen vascular disorders (Rheumatoid arthritis), ocular diseases (uveitis, optic neuritis, exopthalmos),
  • Allergic reactions (contact dermatitis, urticaria etc)
  • Hodgkin’s lymphoma - prednisone
  • Cerebal Edema - dexamethasone
  • Chemotherapy-induced vomiting
  • Hematologic disorders (anemia, leukemia etc)
  • Organ transplants (prevention of rejection)
  • Renal disorders (nephrotic syndrome)
  • Hypercalcemia
  • Mountain Sickness
  • Inflammatory bowel disease etc.
  • Idiopathic orthostatic hypotension (fludrocortisone)