Endrocrine drugs 2: Corticosteroids

Question 1

corticosteroid synthesis inhibitors

Answer 1

ketoconazole

Question 2

corticosteroid receptor antagonists

Answer 2

glucocorticoids
-mifepristone

mineralocorticoid
-spironolactone
»for heart failure, hypokalemia, hyperaldosteronism
»also with weak antagonist effect at the androgen receptor

Question 3

ACTH stimualtes the activity of this enzyme

Answer 3

desmolase

(cholesterol —> pregnenolone

Question 4

formation of cortisol

Answer 4

CHOLESTEROL

1 via desmolase
PREGNENOLONE

2 via 3 β hydroxysteroid dehydrogenase
PROGESTERONE

3 via 17-α hydroxylase
17-HYDROXYPROGESTERONE

4 via 21 β hydroxylase
†11-DEOXYCORTISOL

5 via 11 β hydroxylase
CORITSOL

†11-deoxycorticosterone (DOC)if aldosterone pathway (no 17 α hydroxylase step)

Question 5

what converts 17-hydroxypregnenolone to DHEAS?

Answer 5

17,20-lyase
DeHydroEpiAndroSterone

will be acted upon by 3 β hydroxysteroid dehydrogenase to become
ANDROSTENEDIONE

Question 6

What has same equivalence with cortisol

Answer 6

hydrocortisone (1)

cortisone (0.8)
prednisone (4)
prednisolone (5)
Triamcinolone (5)
betamethasoen (25-40)
dexamethasone (30)

Question 7

medium potency short acting glucocorticoids

Answer 7

fluticasone

mometasone

Question 8

short actin, high-potency glucocorticoids

Answer 8

clobetasol

desoximetasone

Question 9

unfamiliar s/e of systemic glucocorticosteroids

Answer 9

growth inhibition
muscle wasting (remember proximal myopathy?)
psychosis “steroid rage”
poor wound healing (easy bruises, right?)
benign intracranial hypertension

Question 10

prednisone and prednisolone

Answer 10

prednisolone is the active metabolite of prednisone

Question 11

desmolase inhibitor

Answer 11

amino-glutethimide

USES

• breast cancer
• cushing syndrome

Abused by body builders to lower circultaing levels of cortisol in the body and prevent muscle loss

Question 12

unfamiliar uses of glucocorticoids

Answer 12

chemothrepy-induced vomoiting
hypercalcemia
mountain sickness

Question 13

other glucocorticoid synthesis inhibitors

Answer 13

KETOCONAZOLE

• cyp450 inhibitor
• inhibits cholesterol side-chain cleavage
• alt: ITRACONAZOLE

Question 14

DOC for pregnant patients with Cushing’s syndrome

Answer 14

METYRAPONE
-11 β hydroxylase inhibitor

USES

• diagnostic testing for adrenal function
• cushing syndrome (esp pregnant)

Question 15

glucocorticoid antagonist

Answer 15

Mifepristone
-competitive inhibitor at the GC receptor as well as progesterone receptor

USES
-Cushing syndrome

Question 16

drugs for cushing syndrome

Answer 16

“MMAKI”

Metyrapone
Mifepristone
aminoglutethimide (desmolase inh)
Ketokonazole
Itraconazole