Adrenal Corticosteroid drugs DSA

Question 1

mineralcorticoids

Answer 1

fludrocortisone

Question 2

short to medium acting glucocorticoids

Answer 2

hydrocortisone
cortisone
prednisone
prednisolone
methyprednisolone

Question 3

intermediate acting glucocorticoids

Answer 3

triamcinolone

Question 4

long acting glucocorticoids

Answer 4

DBs go long

betametasone
dexametasone

Question 5

steroid syntheis inhibitors

Answer 5

aminoglutethimide
ketoconazole
metyrapone
mitotane

Question 6

glucocorticoid antagonist

Answer 6

mifepristone

my pristine body doesn’t need sugar

Question 7

steroid hormones are transported by what

cortisol bound to ___ considered ___

Answer 7

protein carriers bc they are hydrophobic

• transcortin or CBG
• rest loosely bound to albumin
• albumin bound cortisol should be considered free

Question 8

when is transcortin and CBG high

low?

Answer 8

pregnancy

low in liver failure

Question 9

half life of cortisol is increased in what pts

Answer 9

pts with liver disease

hypothyroid pts

Question 10

direct effects of mineralocorticoids on CV system:

1) effects on gene expression
2) aldosterone excess causes

Answer 10

gene expression:
NAPDH reductase-->oxidative stress
collagen, TGFB--> fibrosis
IL-6, CAM-->inflammation
PAI-1-->inhibition of fibrinolysis, blood clotting

Cat NIP

2) aldosterone excess:
- cardiac fibrosis and hypertophry
- vascular remodeling and inflammation

Question 11

glucocorticoid effects

Answer 11

transactivation: effect on carb, lipid, protein metab

transrepression mech: GR-ligand complex binds other txn factor complexes and suppresses gene txn
-NF-Kb, AP-1 = anti-inflamm, immunosupp, anti growhth

Question 12

what receptor may be responsible for glucocorticoid resistance

Answer 12

GR beta

-no ligand binding, inactive

Question 13

11B-HSD type 2 role

Answer 13

converts cortisol into inactive cortisone so cannot bind MR
-this is how aldosterone gets effect bc aldost and cortisol bind MR with same affinity but more cortisol is produced daily

Question 14

what tissues does 11B-HSD type 2 convert cortisol to cortisone

Answer 14

renal tubular epithelium
salivary glands
sweat glands
colon epithelium

Question 15

inhibtion of 11B-HSD type 2 results in

Answer 15

hypertension and edema with excess MR stim by cortisol

Question 16

what may inhibit 11B-HSD2

Answer 16

glycyrrhizin (licorice root extract)

carbenoxolone

Question 17

glucocorticoid effect on carb metabolism

3 enzymes
transporter
development of what

Answer 17

increase PEPC–>increased gluconeogenesis

increased glucose 6 phosphatase = more glucose in circulation

increased glycogen synthase

decreased GLUT4

development of hyperglycemia

Question 18

glucocorticoid effect on lipid metabolism

Answer 18

promote stimulation of HSL

increasedd FFA and glycerol into gluconeogenic pathway

increased insulin secretion

increase fat deposition and chane in fat distribution

Question 19

glucocorticoids in skeletal muscle

Answer 19

suppressed protein synthesis will lead to myopathy and muscle wasting

Question 20

gluocorticoids and phospholipase A2 and COX

Answer 20

decrease production

= less prostaglandins and leukotriens

Question 21

glucocorticoids on CVS

Answer 21

increased Epi and ?Ne
increased HR and CO
increased BP
residual mineralocorticoid activity (Na+/H20+ retention)

Question 22

glucocorticoids on GI

Answer 22

decreased gastroprotective prostaglandins
decrease immune response H pylori
increase gastric acid and pepsin secretion

Question 23

glucocort on CNS

Answer 23

insomnia
irritanility
euprhoia then depression
decreased libido in males

Question 24

glucocort in bones/growth

Answer 24

decreased intest absorption calcium
increase osteoclast activity (osteoporis)
growth retardation in children

Question 25

glucocort in skin

Answer 25

dfragile and thin skin with stretch marks

Question 26

treatment addisons

Answer 26

hydrocortisone and fludrocortisone

Question 27

cataracts, peptic ulcers, glaucoma in what steroid

Answer 27

glucocortioids

Question 28

a prodrug activated by esterases present in bronchial epithelial cells; systemically absoerbed active drug bound to serum proteins

Answer 28

ciclesonide

Question 29

pt populations in which systemic glucocorticoids administration is problematic

Answer 29

``` immunocompromidsed diabetics pts with infections pts with peptic ulcer pts with CV conditions pts with psychiatric condistions pts with osteoporosis children ```

Question 30

aminoglutethimide MOA - indication - side effects

Answer 30

blocks conversion of cholesterol to pregnenolone reduces all steroid hormones adrenocortical cancer drowsiness GI upset

Question 31

ketocanzole MOA indication AE

Answer 31

p450 inhibition, reduces adrenal and sex hormones prostate cancer antifungal cushing syndrome stops androgenic hair loss PACH of keys hepatotox and gynecomastia in males

Question 32

metyrapone MOA indication AE

Answer 32

inhibtion of steroid 11 hydroxylation stops cortisol and corticosterone cushing syndrome (only drug for this in pregnancy) (tyra banks pregnant) accumulation 11 deoxycortisol = increased aldosterone = more sodium and water retention -also increased androgens = hirsutism in women GI upset dizziness

Question 33

mitotane MOA indication AE

Answer 33

sodium and calcium ionophore PKC and AC inhibitor cytotoxic action on adrenal cortex adrenal carcinoma depression, somnolence GI upset rashes too tan gets rashes, GI problems bc he eats, and depression from eating too much/being fat

Question 34

mifepristone MOA indications AE

Answer 34

glucocorticoid receptor antagonist stabilizes hsp90-GR complex in cytosol, no nuclear translocation -progest receptor antagonist endogenous cushings anti progest action for termination intrauterine preg dizziness GI upset fatigue

Question 35

spirnonolactone MOA indications side effects

Answer 35

aldosterone receptor antagonist also antagonist at androgen receptors primary hyperaldost hirsutism in women diuretic for HF and HTN hyperkalemia gynecomastia and impotence in men menstrual abnormalty in women

Question 36

eplerenone MOA indications side effects

Answer 36

antag of aldosterone at mineralocorticoid receptors lower affinity for androgen recept than spironolact HTN HF hyperkalemia