Med Chem

Question 1

Glucocorticoids (Adrenocorticoids) - MOA - examples

Answer 1

• regulate carbohydrate, lipid, & protein metabolism - prednisolone, triamcinolone, dexamethasone

Question 2

Mineralocorticoids (Adrenocorticoids) - MOA - example

Answer 2

• influence salt balance and water retention - fludrocortisone

Question 3

Adrenocorticoid Antagonists - MOA - example

Answer 3

• compete for binding to steroid receptors - spironolactone (Aldactone), mifepristone (Mifeprex, RU486)

Question 4

Testosterone Derivatives - MOA - example

Answer 4

• stimulate androgen receptors - testosterone esters, 17-alpha methyltestosterone, fluoxymesterone (Androxy)

Question 5

5-alpha reductase inhibitors - MOA - example

Answer 5

• IRREVERSIBLE modification of 5-alpha reductase enzyme - finasteride (Proscar), dutasteride (Avodart)

Question 6

Androgen Antagonists - MOA - example

Answer 6

• block the effects of testosterone and DHT by binding to androgen receptors - bicalutamide (Casodex), flutamide (Apo-Flutamide), nilutamide (Nilandron)

Question 7

Steroidal Estrogens - MOA - example

Answer 7

• stimulate estrogen receptors - ethynyl estradiol, mestranol, estradiol 17-beta valerate, estradiol cypionate

Question 8

SERMs (Selective Estrogen Receptor Modulators) - MOA - example

Answer 8

• partial agonism and antagonism at estrogen receptors in various tissues - tamoxifen (Soltamox), toremifene (Fareston), raloxifene (Evista)

Question 9

Pure Estrogen Receptor Antagonists - MOA - example

Answer 9

• antagonism of estrogen receptors - fulvestrant (Faslodex)

Question 10

Aromatase Inhibitors - MOA - example

Answer 10

• block the conversion of androgens to aromatase - anastrozole (Arimidex), letrozole (Femara), exemestane (Aromasin)

Question 11

Synthetic Progestins - MOA - example

Answer 11

• mimic the activities of natural progestins - medroxyprogesterone acetate, megestrol acetate, norethindrone, norgestrel, levonogestrel

Question 12

Progesterone Receptor Modulators - MOA - example

Answer 12

• selectively modulates progesterone receptors - ulipristal acetate (Ella, EllaOne)

Question 13

fludrocortisone

Answer 13

9α-fluoro analog of hydrocortisone → potent corticosteroid, used widely as a mineralocorticoid