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Drug Action > Pharmacology of Reproduction > Flashcards

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
True or false: Nonsteroidal aromatase inhibitors are competitive inhibitors of aromatase
True. Ex. anastrazole, letrozole
26
Adverse effect of aromatase inhibitors
Increased risk of osteoporosis (estrogen helps regulate bone density)
27
True or false: Estrogenic activities are tissue specific
True
28
Two types of estrogen receptors
ER-alpha and ER-beta
29
Agonist/antagonist action of estrogen in the breast? Endometrium? Bone?
Full agonist. Full agonist. Full agonist
30
Agonist/antagonist action of tamoxifen in the breast? Endometrium? Bone?
Antagonist. Partial agonist. Partial agonist.
31
Agonist/antagonist action of raloxifene in the breast? Endometrium? Bone?
Antagonist. Antagonist. Moderate agonist.
32
Agonist/antagonist action of bazedoxifene in the breast? Endometrium? Bone?
Antagonist. Antagonist. Partial agonist.
33
What is tamoxifen used for?
Prophylaxis and treatment of breast cancer
34
Tamoxifen should not be used longer than how many years and why?
5 years due to increased risk of endometrial cancer
35
Adverse effects of tamoxifen
Increased risk of endometrial cancer, deep vein thrombosis and stroke
36
Raloxifene agonist/antagonist action in bone and liver
Agonist in bone. Agonist in liver
37
Is clomiphene an estrogen receptor agonist or antagonist?
Antagonist
38
Clomiphene is used for treatment of _______. And it induces ________ and ________
Infertility; LH surge and ovulation
39
In what instance is letrozole more effective than clomiphene in inducing ovulation and pregnancy?
Obese women with PCOS
40
Toremifene is a SERM used for treatment of what?
Metastatic breast cancer in postmenopausal women
41
Bazedoxifene blocks estrogen induced proliferation of the ________
endometrium
42
Ospemifine helps improve _______ atrophy in postmenopausal women
Vulvovaginal
43
Androgen receptor antagonists MOA
Competitively inhibits the binding of endogenous androgens to androgen receptor
44
Androgen receptor antagonists are used in the treatment of _______
Hirsutism (growth of coarse, dark hair in areas where women typically grow fine hair or no hair at all)
45
Androgen receptor antagonist examples
Flutamide, bicalutamide, nilutamide, enzalutamide and spirinolactone
46
Progesterone receptor antagonist examples
Mifepristone (RU-486), misoprostol (prostaglandin analogue), asoprisnil
47
Two common classes of oral contraceptives
Progestin only and estrogen-progestin combo
48
What are the cons of orally administered natural estrogens?
Poor solubility Extensive first pass metabolism Very short half life
49
How is bioavailability administered estrogens increased?
Small particles/micronized Transdermal administration Synthetic estrogens Conjugated estrogens
50
Common example of synthetic estrogen
Ethinyl estradiol
51
Estrogen action in pituitary gland
Regulate LH and FSH release
52
Estrogen action in ovary
Stimulate follicular growth
53
Estrogen action in uterus
Stimulate growth and proliferation of non-secretory endometrium
54
Estrogen action in vagina
Change in skin tone
55
Estrogen action in cervix
Increase thin mucosa (favoring sperm) Develop and maintain genitalia Develop and maintain secondary sex characteristics
56
Estrogen action in bones
Maintain calcium content/ decreased resorption
57
Estrogen action in liver
Improved cholesterol profile
58
Estrogen action in blood
Increase in coagulation
59
Progestin only contraception is ___ - ___ % effective
96-98%
60
Progestin only contraception MOA
Primary: Alter frequency of GnRH pulsing and decrease anterior pituitary gland responsiveness to GnRH Secondary: Alter cervical mucus, endometrial receptivity and tubal peristalsis
61
True or false: Patients taking progestin only contraceptives experience typical menstruation
False. They do not normally experience menstruate, but sometimes experience spotting
62
True or false: In estrogen-progestin contraceptives are mostly combos of synthetic estrogen and synthetic or conjugated progestin
True. The synthetic estrogen used is either ethinyl estradiol or mestranol
63
True or false: Patients taking estrogen-progestin contraceptives experience typical menstruation
True. These are typically used for 21 days with off period of 7 days
64
How effective are estrogen-progestin combo contraceptives?
99% effective
65
What are the four forms of contraception?
Natural Barrier; condoms, spermicides Hormonal; the pill, plan B Sterilization; vasectomy, hysterectomy
66
What are the two types of emergency contraception?
Mifepristone (RU-486) and levonorgestrel
67
Emergency contraceptive MOAs
Prevention or delay of ovulation Changed rate of tubal transport of ovum Changes in endometrium unfavorable to implantation
68
Why is inhibition of spermatogenesis difficult?
Even a 99% reduction will still result in sufficient number of viable sperm for fertilization
69
What is the goal of male contraception?
Reversibly suppress endogenous sperm production
70
Menopause results in a large reduction of what two hormones?
Estrogen and progesterone
71
Menopause results in a large increase of what two hormones?
LH and FSH
72
Androgen replacement therapy is effective in treatment of _______
Hypogonadism

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