Estrogens and Progesterones and Androgens Flashcards Preview

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Flashcards in Estrogens and Progesterones and Androgens Deck (40)
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1

What are the indications for exogenous estrogens?

HRT- postmenopausal women
Oral contraceptives
Primary hypogonadism
Primary ovarian insufficiency

2

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

Women with a uterus- to prevent endometrial hyperplasia/cancer

3

Estrogens: contraindications?

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

4

Effect of tamoxifen in endometrium?

Partial agonist

5

Effect of tamoxifen in the bone?

partial agonist

6

Tamoxifen: indication?

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

7

Tamoxifen: adverse effects?

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

8

Effect of ralxoifene in the bone?

Partial agonist

9

Effect of raloxifene in the endometrium?

antagonist

10

Raloxifene: indications

Treatment of osteoporosis in postmenopausal women
Alternative to tamoxifen in prevention of breast cancer primary prevention

11

Effect of clomiphene in the hypothalamus/pituitary?

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

12

Effect of clomiphene in the ovary?

Partial agonist

13

Clomiphene: indication?

Treatment of anovulation in PCOS

14

Fulvestrant: indications?

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

15

Name three aromatase inhibitors?

Anastrazole
Letrozole
Exemestane

16

Aromatase inhibitors: indications?

Adjuvant therapy of ER+ breast cancers in postmenopausal women

17

Name 6 progestins

Norgestrel
Levongestrel
Norethindrone
Desogestrel
Gestodene
Norgestimate

18

Progestins: indications?

Hormone replacement
Hormonal contraception

19

How do progestins work as contraceptives?

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

20

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

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

21

Combined oral contraception: contraindications

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

22

What the MOA of high dose levonorgestrel?

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

23

When is high dose levonorgestrel effective?

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

24

Ulipristal: MOA?

Partial agonist of PR: antagonist in the presence of progesterone

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

25

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

Tx of uterine fibroids

26

When is ulipristal effective at preventing unwanted pregnancy?

Effective if given up to 5 days after sex

27

Mifepristone + misprostal: indication

abortifactant (<70 days gestation)

28

What are the MOAs of Mifepristone and misprostal?

Mifepristone: PR antagonist- promotes menses (also GR and AR antagonist)

Misprostal: promotes uterine contraction to expel the fetus

29

What are contraindications of mifepristone/misprostal?

Chronic adrenal insufficiency can precipitate and adrenal crisis (through GR receptor antagonism)

Bleeding disorders or people on anticoagulants

30

What is the only indication for giving exogenous testosterone?

Male hypogonadism

31

What are contraindications for testosterone use?

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

32

Name 4 AR antagonists

Flutamide
Bicalutamide
Nilutamide
Enzalutamide

33

What are the indications for the AR antagonists?

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

34

Abiraterone: MOA?

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

35

Abiraterone: indications?

Hormone-resistant prostate cancer not responding to
androgen deprivation therapy

36

Spironolactone: MOA?

Antagonist/weak partial agonist of AR

-Also binds MR as a K+ sparing diuretic

37

Spironolactone: indication?

Tx of women with hirsutism, acne, or androgenic alopecia

38

Name 2 5-alpha reductase inhibitors

Finasteride
Dutasteride

39

Finasteride/Dutasteride: MOA?

Inhibits testosterone--> DHT conversion

40

Finasteride/Dutasteride: indications?

BPH, male pattern baldness, female hirsutism