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Flashcards in Corticosteroids Deck (40):
1

Treatment regimen for Cushings Disease (3 pharm)

Surgery is main option
A Aminoglutethimide
K Ketoconazole
M Metyrapone

2

Aminoglutethimide inhibits what CYP?

CYP11A1

3

Mechanism of Aminoglutethimide

inhibits CYP11A1 resulting in inhibition of corticosteroid synthesis

4

Aminoglutethimide side effects

adrenal insufficiency

5

Aminoglutethimide drug interaction

increased metabolism of other drugs such as
warfarin, theopyylline and digitoxin

6

Ketoconazole Mechanism (3)

high doses - inhibits CYP17, inhibiting glucocorticoid and androgen synthesis
even higher doses - inhibits CYP11A1, inhibiting all steroidogenesis
also reduces ACTH secretion at therapeutic doses

7

Another name for CYP11A1 and action

Cholesterol Desmolase

converts Cholesterol to Pregnenolone

8

Use for Ketoconazole?

Treat Cushing's Disease and fungal infections

9

Drug Interaction of Ketoconazole (2)

inhibits multiple CYPs, many potential interactions

inhibits P-glycoprotein so may increase levels of P-gp substrates

10

Metyrapone mechanism

selective inhibitor of CYP11B1 reducing the biosynthesis of cortisol

11

What CYP does Metyrapone inhibit?

CYP11B1

12

Metyrapone clinical use?

hypercorticism
diagnostic test for Cushings

13

Metyrapone main side effect and why it occurs?

Hirsutism - due to increased synthesis of adrenal androgens upstream from the enzymatic block

14

Mifepristone (RU-486) mechanism (2)

Inhibits the release of the glucocorticoid receptor from the chaperone proteins
Also competitive inhibitor of progestins at progesterone receptors

15

Mifepristone (RU-486) clinical use (2)

controlling hypercortisolism in patients with Cushing's syndrome due to inoperable ectopic ACTH secreting tumors

abortion pill

16

Mifepristone (RU-486) main side effect

Heavy vaginal bleeding

17

Mifepristone (RU-486) drug interaction

increased metabolism of other drugs such as warfarin, theopyylline and digitoxin

18

Cosyntropin test is used for what?

Determining primary vs secondary adrenal insufficiency

19

Primary Adrenal Insufficiency treatment

hydrocortisone or cortisone
supplementation with fludrocortisone for mineralocorticoid effect

20

Secondary Adrenal Insufficiency treatment

hydrocortisone, cortisone or prednisone
mineralocorticoids are not necessary.

21

Why are Mineralocorticoids only given once a day

because their release does not show circadian
effects normally.

22

Most common cause of Congenital Adrenal Hypoplasia

Deficiency in CYP21

23

Presentation of Congenital Adrenal Hypoplasia males vs females

Males normal at birth precocious puberty
females psedudohermaphroditism

24

Spironolactone Mechanism

Blocks renal aldosterone receptors
Also progesterone agonist and androgen antagonist

25

Spironolactone clinical use

treatment of aldosteronism for non-surgical candidates

26

Spironolactone side effects

breast tenderness and menstrual irregularities in women
impotence, decreased libido, and gynecomastia in men

27

Glucocorticoids have excellent ___ activity and are they curative?

Excellent anti-inflammatory activity
Underlying cause is still present

28

What occurs if you rapidly withdraw glucocorticoids?

adrenal insufficiency, must wean off

29

What demographic must you be careful about with glucocorticoids?

post-menopausal women and osteoporosis patients

30

Corticosteroids inhibit what transcription factor?

NF-kB

31

What does cortisol bind to in blood and what raises the protein's levels?

90% of cortisol binds to corticosteroid binding globulin (CBG) & albumin in the plasma

Pregnancy and estrogen therapy

32

Metabolism of corticosteroids?

first pass hepatic conjugation and then renally excreted

33

Why should people with infections or AIDS avoid corticosteroids?

they are highly immunosuppressive

34

What must you supplement post-menopausal woman with when giving corticosteroids?

Vitamin D and Calcium with high protein diet

35

Why use caution giving glucocorticoids to psychotic patients?

may exacerbate condition - side effect of drugs

36

Which corticosteroid can induce cleft palate and still birth

Dexamethasone

37

Why recommend no breast feeding in systemic steroid treatment.

can redistribute in breast milk

38

Why be cautious in treating diabetics with steroids?

induces hyperglycemia

39

Why be cautious in treating heart patients with steroids?

due to potential weight gain and hypertension and hyperlipidemia induced by steroids

40

Hepatic microsomal enzyme inducers (barbiturates, carbamazepine, phenytoin) do what to corticosteroid metabolism?

promote corticosteroid metabolism.