Estrogens and Progesterones and Androgens

Question 1

What are the indications for exogenous estrogens?

Answer 1

HRT- postmenopausal women
Oral contraceptives
Primary hypogonadism
Primary ovarian insufficiency

Question 2

Estrogens must be given with progestins in which women? Why?

Answer 2

Women with a uterus- to prevent endometrial hyperplasia/cancer

Question 3

Estrogens: contraindications?

Answer 3

High risk/Prior history Breast Cancer
History endometrial cancer
History thromboembolic disease
History of genital bleeding
Liver disease
Heavy smoking

Question 4

Effect of tamoxifen in endometrium?

Answer 4

Partial agonist

Question 5

Effect of tamoxifen in the bone?

Answer 5

partial agonist

Question 6

Tamoxifen: indication?

Answer 6

Primary prevention of high risk breast cancer
Treatment of advanced breast cancer
Treatment of male gynecomastia

Question 7

Tamoxifen: adverse effects?

Answer 7

Hot flashes
Increased risk of thromboemoblic events
INCREASED RISK OF ENDOMETRIAL CANCER

Question 8

Effect of ralxoifene in the bone?

Answer 8

Partial agonist

Question 9

Effect of raloxifene in the endometrium?

Answer 9

antagonist

Question 10

Raloxifene: indications

Answer 10

Treatment of osteoporosis in postmenopausal women

Alternative to tamoxifen in prevention of breast cancer primary prevention

Question 11

Effect of clomiphene in the hypothalamus/pituitary?

Answer 11

Antagonist- inhibits negative feedback from E2 and promotes release of LH/FSH

Question 12

Effect of clomiphene in the ovary?

Answer 12

Partial agonist

Question 13

Clomiphene: indication?

Answer 13

Treatment of anovulation in PCOS

Question 14

Fulvestrant: indications?

Answer 14

Treatment of advanced ER+ metastatic breast cancer- typically following failure of tamoxifen therapy

Question 15

Name three aromatase inhibitors?

Answer 15

Anastrazole
Letrozole
Exemestane

Question 16

Aromatase inhibitors: indications?

Answer 16

Adjuvant therapy of ER+ breast cancers in postmenopausal women

Question 17

Name 6 progestins

Answer 17

Norgestrel
Levongestrel
Norethindrone
Desogestrel
Gestodene
Norgestimate

Question 18

Progestins: indications?

Answer 18

Hormone replacement

Hormonal contraception

Question 19

How do progestins work as contraceptives?

Answer 19

Decrease GnRH frequency –> decrease gonadotropin release and ovulation
Thickens cervical mucus

Question 20

Other than contraception, what are combined oral contraceptives used for?

Answer 20

Menstrual cycle disorders
Hyperandrogenism (acne)
Bleeding due to fibroids
Endometriosis
Decrease risk of endometrial and ovarian cancer

Question 21

Combined oral contraception: contraindications

Answer 21

Age > 35 y & smoking
Coronary artery disease
History venous thrombosis
History of stroke
Systemic lupus
History breast cancer
History liver disease

Question 22

What the MOA of high dose levonorgestrel?

Answer 22

Activates PR –> inhibits/delays ovulation by inhibiting the LH surge

Question 23

When is high dose levonorgestrel effective?

Answer 23

Only effective if given 1-2d prior to LH surge. Must be given within 72h of intercourse
- Taken once daily for 5 d

Question 24

Ulipristal: MOA?

Answer 24

Partial agonist of PR: antagonist in the presence of progesterone

Effective at delaying/inhibiting ovulation even if given during LH surge

Question 25

Other than use as "plan B" - what is another indication for ulipristal?

Answer 25

Tx of uterine fibroids

Question 26

When is ulipristal effective at preventing unwanted pregnancy?

Answer 26

Effective if given up to 5 days after sex

Question 27

Mifepristone + misprostal: indication

Answer 27

abortifactant (<70 days gestation)

Question 28

What are the MOAs of Mifepristone and misprostal?

Answer 28

Mifepristone: PR antagonist- promotes menses (also GR and AR antagonist) Misprostal: promotes uterine contraction to expel the fetus

Question 29

What are contraindications of mifepristone/misprostal?

Answer 29

Chronic adrenal insufficiency can precipitate and adrenal crisis (through GR receptor antagonism) Bleeding disorders or people on anticoagulants

Question 30

What is the only indication for giving exogenous testosterone?

Answer 30

Male hypogonadism

Question 31

What are contraindications for testosterone use?

Answer 31

Prostate cancer or high levels of PSA | Untreated sleep apnea (can worsen sleep apnea)

Question 32

Name 4 AR antagonists

Answer 32

Flutamide Bicalutamide Nilutamide Enzalutamide

Question 33

What are the indications for the AR antagonists?

Answer 33

Treatment of advanced prostate cancer - used in combo with androgen deprivation therapy (GnRH agonists/antagonists) Flutamide is also used in treatment of hyperandrogenism in women

Question 34

Abiraterone: MOA?

Answer 34

Inhibition of CYP17A1: Inhibits synthesis of testosterone (also affects cortisol ,but not aldosterone)

Question 35

Abiraterone: indications?

Answer 35

Hormone-resistant prostate cancer not responding to | androgen deprivation therapy

Question 36

Spironolactone: MOA?

Answer 36

Antagonist/weak partial agonist of AR -Also binds MR as a K+ sparing diuretic

Question 37

Spironolactone: indication?

Answer 37

Tx of women with hirsutism, acne, or androgenic alopecia

Question 38

Name 2 5-alpha reductase inhibitors

Answer 38

Finasteride | Dutasteride

Question 39

Finasteride/Dutasteride: MOA?

Answer 39

Inhibits testosterone--> DHT conversion

Question 40

Finasteride/Dutasteride: indications?

Answer 40

BPH, male pattern baldness, female hirsutism