Estrogens and Progesterones and Androgens Flashcards

1
Q

What are the indications for exogenous estrogens?

A

HRT- postmenopausal women
Oral contraceptives
Primary hypogonadism
Primary ovarian insufficiency

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2
Q

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

A

Women with a uterus- to prevent endometrial hyperplasia/cancer

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3
Q

Estrogens: contraindications?

A
High risk/Prior history Breast Cancer
History endometrial cancer
History thromboembolic disease
History of genital bleeding
Liver disease
Heavy smoking
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4
Q

Effect of tamoxifen in endometrium?

A

Partial agonist

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5
Q

Effect of tamoxifen in the bone?

A

partial agonist

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6
Q

Tamoxifen: indication?

A

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

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7
Q

Tamoxifen: adverse effects?

A

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

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8
Q

Effect of ralxoifene in the bone?

A

Partial agonist

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9
Q

Effect of raloxifene in the endometrium?

A

antagonist

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10
Q

Raloxifene: indications

A

Treatment of osteoporosis in postmenopausal women

Alternative to tamoxifen in prevention of breast cancer primary prevention

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11
Q

Effect of clomiphene in the hypothalamus/pituitary?

A

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

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12
Q

Effect of clomiphene in the ovary?

A

Partial agonist

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13
Q

Clomiphene: indication?

A

Treatment of anovulation in PCOS

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14
Q

Fulvestrant: indications?

A

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

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15
Q

Name three aromatase inhibitors?

A

Anastrazole
Letrozole
Exemestane

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16
Q

Aromatase inhibitors: indications?

A

Adjuvant therapy of ER+ breast cancers in postmenopausal women

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17
Q

Name 6 progestins

A
Norgestrel
Levongestrel
Norethindrone
Desogestrel
Gestodene
Norgestimate
18
Q

Progestins: indications?

A

Hormone replacement

Hormonal contraception

19
Q

How do progestins work as contraceptives?

A

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

20
Q

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

A
Menstrual cycle disorders
Hyperandrogenism (acne)
Bleeding due to fibroids
Endometriosis
Decrease risk of endometrial and ovarian cancer
21
Q

Combined oral contraception: contraindications

A
Age > 35 y & smoking
Coronary artery disease
History venous thrombosis
History of stroke
Systemic lupus
History breast cancer
History liver disease
22
Q

What the MOA of high dose levonorgestrel?

A

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

23
Q

When is high dose levonorgestrel effective?

A

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

24
Q

Ulipristal: MOA?

A

Partial agonist of PR: antagonist in the presence of progesterone

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

25
Q

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

A

Tx of uterine fibroids

26
Q

When is ulipristal effective at preventing unwanted pregnancy?

A

Effective if given up to 5 days after sex

27
Q

Mifepristone + misprostal: indication

A

abortifactant (<70 days gestation)

28
Q

What are the MOAs of Mifepristone and misprostal?

A

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

Misprostal: promotes uterine contraction to expel the fetus

29
Q

What are contraindications of mifepristone/misprostal?

A

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

Bleeding disorders or people on anticoagulants

30
Q

What is the only indication for giving exogenous testosterone?

A

Male hypogonadism

31
Q

What are contraindications for testosterone use?

A

Prostate cancer or high levels of PSA

Untreated sleep apnea (can worsen sleep apnea)

32
Q

Name 4 AR antagonists

A

Flutamide
Bicalutamide
Nilutamide
Enzalutamide

33
Q

What are the indications for the AR antagonists?

A

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
Q

Abiraterone: MOA?

A

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

35
Q

Abiraterone: indications?

A

Hormone-resistant prostate cancer not responding to

androgen deprivation therapy

36
Q

Spironolactone: MOA?

A

Antagonist/weak partial agonist of AR

-Also binds MR as a K+ sparing diuretic

37
Q

Spironolactone: indication?

A

Tx of women with hirsutism, acne, or androgenic alopecia

38
Q

Name 2 5-alpha reductase inhibitors

A

Finasteride

Dutasteride

39
Q

Finasteride/Dutasteride: MOA?

A

Inhibits testosterone–> DHT conversion

40
Q

Finasteride/Dutasteride: indications?

A

BPH, male pattern baldness, female hirsutism