Steroids and Adrenal Hormones MC

Question 1

Endocrine secretion

Answer 1

Hormones into blood

Question 2

Paracrine excretion

Answer 2

Hormones into neighboring cells

Question 3

Autocrine excretion

Answer 3

Hormones into same cell

Question 4

Androgen Origin and Function

Answer 4

Testis

2nd male sex characteristics, sperm production, anabolic effects

Question 5

Estrogen and progestins Origin and Function

Answer 5

Ovary

Control menstrual cycle and 2nd sex characteristics

Question 6

Steroid MOA

Answer 6

Steroid diffuse into cell Binds to receptor in cytosol Enters nucleus Transcription

Question 7

2 classes of corticosteroids

Answer 7

mineralcorticoids

• aldosterone: maintains constant electrolyte balace, blood volume, BP, causes salt rention

glucocorticoids:

• cortisol: regulate carbs/lipids/protein metabolism

Question 8

Fludrocortisone acetate M vs. G compared to cortisol

Answer 8

M > G activity

increase salt retention (M) 200-800x

incrased anti-inflam (G) 11x

Question 9

3 pharmacophores of mineralcorticoids

Answer 9

3-keto-4-ene system

20-keto group

21-OH group

Question 10

18-formyl effect of M

Answer 10

dramatically increase activity

Question 11

11B-OH effect on M

Answer 11

no necessary for M but incrases G

Question 12

9a-F effect on M and G

Answer 12

increase salt retention (M)

incrase anti-inflammatory effect (G)

Question 13

3 spirinolactone indications

Answer 13

primary hyperaldosteronism, HTN, hypokalemia

Question 14

2 eplerenone indications

Answer 14

CHF after acute MI

HTN

Question 15

cortisol and aldosterone in liver and kidney

Answer 15

cortisol and aldosterone both bind to same receptors in liver and kidney

11B-HSD 1 is in liver and is reversible

11B-HSD2 is in kidney and not reversible

both change cortisol to cortisone (not active) so since not reversible in kidney aldosterone will only work in kidey not cortisol

Question 16

3-one vs 3a-OH

which one is active

Answer 16

3-one

Question 17

4-ene vs 5B-H

which one is active

Answer 17

4-ene

Question 18

11B-OH vs 11-one

which one is active

Answer 18

11B-Oh

Question 19

17B-ketol vs 17a-OH

which one is active

Answer 19

17B-ketol

Question 20

3 pharmacophores of glucocorticoids

Answer 20

3-keto-4-ene system

20-keto group

11-B-OH

21-Oh group common but not essential

Question 21

11B-OH activity on M and G

Answer 21

M no effect

G incrases activity

Question 22

17a-OH on M and G

Answer 22

G enhances activity not essential

M decreases activity sometimes

Question 23

3 drugs with no mineralcorticoid activity

Answer 23

triamcinolone

detamethasone

dexamethasone

Question 24

1-ene on G and M

Answer 24

increase G decrease M

Question 25

6-a-CH3 on G and M

Answer 25

increase G decrease M

Question 26

4 substituents that REALLY decrease M

Answer 26

16a-OH

16a-CH3

16B-CH3

16a/17a-ketal

Question 27

2 substituents that greatly increase G and M

Answer 27

9a-F

9a-CL

Question 28

C21 esters make what?

Answer 28

PRODRUGS

Question 29

Esters used topically ______________systemic absorbtion

Answer 29

slows

Question 30

Are 17a-esters, 16a-ester, 16a/17a-ketals Prodrugs?

Answer 30

NO