Pharmacology of Reproduction Flashcards

1
Q

What are the 3 major categories of sex hormones?

A

Estrogens (estradiol, E), Progestins (progesterone, P) and Androgens (testosterone, T)

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2
Q

What is the primary female sex steroid?

A

Estrogen

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3
Q

What is the primary male sex steroid?

A

Androgens

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4
Q

True or false: Progestins both facilitate and oppose estrogen actions

A

True

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5
Q

Most potent endogenous estrogen is

A

17 beta-estradiol

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6
Q

Most potent endogenous progestin is

A

Progesterone

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7
Q

True or false: Estrogens are only present in females and androgens are only present in males

A

False. All three classes of endogenous steroids are present in both males and females

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8
Q

Steroid hormones are synthesized from ___________

A

Cholesterol

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9
Q

Estrogens are derived from ___________ of precursor androgens

A

Aromatization

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10
Q

Which is the most potent circulating estrogen?

A

estradiol (E2)

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11
Q

What enzyme converts testosterone to DHT (5-alpha-dihydrotestosterone)?

A

5-alpha-reductase

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12
Q

Finasteride and dutasteride MOA

A

Inhibits 5-alpha-reductase enzyme

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13
Q

True or false: The quantity of sex hormones present in male and female is different

A

True

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14
Q

True or false: Continuous GnRH secretion induces gonadotropin release

A

False

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15
Q

What are the two gonadotropins?

A

Luteinizing hormone (LH) and follicle stimulating hormone (FSH)

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16
Q

Rise in levels of what hormone indicates blastocyst implantation in uterine lining

A

human chorionic gonadotropin (hCG)

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17
Q

Pathophysiology of polycystic ovarian syndrome (PCOS)

A

Disruption of hypothalamic-pituitary-reproduction-axis

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18
Q

Pathophysiology of hypogonadism and menopause

A

Decreased estrogen or androgen secretion

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19
Q

GnRH agonist MOA and example

A

Continuous administration. Leuprolide, goserelin, nafaralin, etc.

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20
Q

GnRH receptor antagonist examples

A

Cetrorelix, ganirelix or degarelix

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21
Q

Aromatase inhibitors can (inc/dec) estrogen levels

A

Decrease

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22
Q

Aromatase inhibitors can be used to inhibit the growth of ________ dependent tumors

A

Estrogen

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23
Q

Tamoxifen drug class

A

Estrogen receptor antagonists

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24
Q

True or false: Steroidal aromatase inhibitors are competitive inhibitors of aromatase

A

False. Steroidal aromatase inhibitors bind covalently to aromatase. Ex. exemestane, formestane

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25
Q

True or false: Nonsteroidal aromatase inhibitors are competitive inhibitors of aromatase

A

True. Ex. anastrazole, letrozole

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26
Q

Adverse effect of aromatase inhibitors

A

Increased risk of osteoporosis (estrogen helps regulate bone density)

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27
Q

True or false: Estrogenic activities are tissue specific

A

True

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28
Q

Two types of estrogen receptors

A

ER-alpha and ER-beta

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29
Q

Agonist/antagonist action of estrogen in the breast? Endometrium? Bone?

A

Full agonist. Full agonist. Full agonist

30
Q

Agonist/antagonist action of tamoxifen in the breast? Endometrium? Bone?

A

Antagonist. Partial agonist. Partial agonist.

31
Q

Agonist/antagonist action of raloxifene in the breast? Endometrium? Bone?

A

Antagonist. Antagonist. Moderate agonist.

32
Q

Agonist/antagonist action of bazedoxifene in the breast? Endometrium? Bone?

A

Antagonist. Antagonist. Partial agonist.

33
Q

What is tamoxifen used for?

A

Prophylaxis and treatment of breast cancer

34
Q

Tamoxifen should not be used longer than how many years and why?

A

5 years due to increased risk of endometrial cancer

35
Q

Adverse effects of tamoxifen

A

Increased risk of endometrial cancer, deep vein thrombosis and stroke

36
Q

Raloxifene agonist/antagonist action in bone and liver

A

Agonist in bone. Agonist in liver

37
Q

Is clomiphene an estrogen receptor agonist or antagonist?

A

Antagonist

38
Q

Clomiphene is used for treatment of _______. And it induces ________ and ________

A

Infertility; LH surge and ovulation

39
Q

In what instance is letrozole more effective than clomiphene in inducing ovulation and pregnancy?

A

Obese women with PCOS

40
Q

Toremifene is a SERM used for treatment of what?

A

Metastatic breast cancer in postmenopausal women

41
Q

Bazedoxifene blocks estrogen induced proliferation of the ________

A

endometrium

42
Q

Ospemifine helps improve _______ atrophy in postmenopausal women

A

Vulvovaginal

43
Q

Androgen receptor antagonists MOA

A

Competitively inhibits the binding of endogenous androgens to androgen receptor

44
Q

Androgen receptor antagonists are used in the treatment of _______

A

Hirsutism (growth of coarse, dark hair in areas where women typically grow fine hair or no hair at all)

45
Q

Androgen receptor antagonist examples

A

Flutamide, bicalutamide, nilutamide, enzalutamide and spirinolactone

46
Q

Progesterone receptor antagonist examples

A

Mifepristone (RU-486), misoprostol (prostaglandin analogue), asoprisnil

47
Q

Two common classes of oral contraceptives

A

Progestin only and estrogen-progestin combo

48
Q

What are the cons of orally administered natural estrogens?

A

Poor solubility
Extensive first pass metabolism
Very short half life

49
Q

How is bioavailability administered estrogens increased?

A

Small particles/micronized
Transdermal administration
Synthetic estrogens
Conjugated estrogens

50
Q

Common example of synthetic estrogen

A

Ethinyl estradiol

51
Q

Estrogen action in pituitary gland

A

Regulate LH and FSH release

52
Q

Estrogen action in ovary

A

Stimulate follicular growth

53
Q

Estrogen action in uterus

A

Stimulate growth and proliferation of non-secretory endometrium

54
Q

Estrogen action in vagina

A

Change in skin tone

55
Q

Estrogen action in cervix

A

Increase thin mucosa (favoring sperm)
Develop and maintain genitalia
Develop and maintain secondary sex characteristics

56
Q

Estrogen action in bones

A

Maintain calcium content/ decreased resorption

57
Q

Estrogen action in liver

A

Improved cholesterol profile

58
Q

Estrogen action in blood

A

Increase in coagulation

59
Q

Progestin only contraception is ___ - ___ % effective

A

96-98%

60
Q

Progestin only contraception MOA

A

Primary: Alter frequency of GnRH pulsing and decrease anterior pituitary gland responsiveness to GnRH
Secondary: Alter cervical mucus, endometrial receptivity and tubal peristalsis

61
Q

True or false: Patients taking progestin only contraceptives experience typical menstruation

A

False. They do not normally experience menstruate, but sometimes experience spotting

62
Q

True or false: In estrogen-progestin contraceptives are mostly combos of synthetic estrogen and synthetic or conjugated progestin

A

True. The synthetic estrogen used is either ethinyl estradiol or mestranol

63
Q

True or false: Patients taking estrogen-progestin contraceptives experience typical menstruation

A

True. These are typically used for 21 days with off period of 7 days

64
Q

How effective are estrogen-progestin combo contraceptives?

A

99% effective

65
Q

What are the four forms of contraception?

A

Natural
Barrier; condoms, spermicides
Hormonal; the pill, plan B
Sterilization; vasectomy, hysterectomy

66
Q

What are the two types of emergency contraception?

A

Mifepristone (RU-486) and levonorgestrel

67
Q

Emergency contraceptive MOAs

A

Prevention or delay of ovulation
Changed rate of tubal transport of ovum
Changes in endometrium unfavorable to implantation

68
Q

Why is inhibition of spermatogenesis difficult?

A

Even a 99% reduction will still result in sufficient number of viable sperm for fertilization

69
Q

What is the goal of male contraception?

A

Reversibly suppress endogenous sperm production

70
Q

Menopause results in a large reduction of what two hormones?

A

Estrogen and progesterone

71
Q

Menopause results in a large increase of what two hormones?

A

LH and FSH

72
Q

Androgen replacement therapy is effective in treatment of _______

A

Hypogonadism