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.Pharmacology > Part 17: Gonadal Hormones > Flashcards

Part 17: Gonadal Hormones Flashcards

1
Q

the gonadal hormones are also known as ____

A

sex hormones

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2
Q

t/f sex hormones are involved in more than just reproduction

A

t

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3
Q

LH and FSH are secreted by the ____ gland to act on the ___ and ___

A

pituitary; testes & ovaries

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4
Q

stimulation of ovaries & testes by LH and FSH causes them to release ___

A

estrogens and androgens

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5
Q

sex hormones exist in a ___ feedback system

A

negative

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6
Q

androgens and estrogens cause negative feedback by looping back to the ___ and ___ glands

A

pituitary and hypothalamus

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7
Q

the frequency of ____ from the hypothalamus detrmines which pituitray hormone is released

A

pulsatile release of gonadotropin releasing hormone

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8
Q

what releases GnRH?

A

hypothalamus

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9
Q

what releases LH and FSH?

A

pituitary gland

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10
Q

what is the role of LH?

A

androgen release, ovulation

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11
Q

what is the role of FSH?

A

follicle development & spermatogenesis

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12
Q

which hormone will be released by pituitary if there is a high frequency of GnRH release from the hypothalamus?

A

LH

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13
Q

which hormone will be released by pituitary if there is a low frequency of GnRH release from the hypothalamus?

A

FSH

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14
Q

which hormones are released from the pituitary if there is constant release of GnRH from the hypothalamus?

A

neither FSH or LH

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15
Q

give 2 examples of what synthetic GnRH can be used to treat

A

infertility; some types of hormone sensitive cancer

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16
Q

what is the main role of FSH in males?

A

starting puberty and sperm maturation

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17
Q

____ is the primary hormone that stimulate the making of testosterone

A

LH

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18
Q

where is testosterone made?

A

Leydig cells of the testes

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19
Q

testosterone is made from ___

A

cholesterol

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20
Q

testosterone circulates in the blood by being bound to ___ protein

A

sex hormone binding globulin (SHBG)

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21
Q

testosterone binds to ___ receptors

A

intracellular androgen receptors

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22
Q

once inside target cells, testosterone is converted to ___ by ___ enzymes

A

dihydrotesterone (DHT); 5-alpha reductases

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23
Q

which is a higher potency agonist at androgen receptors, testosterone, or DHT?

A

DHT

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24
Q

the activated androgen-receptor complex is translocated to the ____ where it modifies gene ___ and ___ synthesis

A

nucleus, transcription; protein synthesis

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25
Q

t/f many of the androgenic effects we often associate with testosterone are actually caused by DHT

A

t

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26
Q

which androgen is responsible for the development of male secondary sex characteristics?

A

DHT

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27
Q

testosterone is important in early development and throughout life it is involved in the production and maintenance of ___, ___ , __and ___

A

muscle mass; red blood cells; bones; hair growth

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28
Q

testosterone can also be metabolized by CYP19 (aromatase) into ___

A

estradiol

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29
Q

the estrogens made from testosterone is important for ___ in males

A

bond density

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30
Q

the levels of estrogen in males is typically ____ (high or low)

A

low

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31
Q

t/f aromatase enzymes are expressed in fat cells, so obese men can express more estrogen and a decrease in testosterone

A

t

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32
Q

what are the 2 categories testosterone modulation falls into?

A

replacement or suppression therapy

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33
Q

androgen ____ therapy is used for low T syndrome

A

replacement

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34
Q

androgen ____ therapy is used for performance enhancement

A

replacement

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35
Q

androgen ____ therapy is used for treatment of prostate enlargement

A

suppression

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36
Q

androgen ____ therapy is used for treatment of hormone sensitive prostate cancer

A

suppression

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37
Q

what is low T syndrome?

A

circulating levels of testosterone are insufficient to maintain normal physiologic roles of androgens

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38
Q

t/f testosterone levels dcline with age

A

t

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39
Q

what are some of the symptoms of low T?

A

low sex drive, fatigue, hair loss, reduced muscle mass

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40
Q

t/f replacing testosterone can effectively manage low T symptoms

A

t

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41
Q

t/f the lipophilicity of steroid hormones make it possible to administer them transdermally

A

t

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42
Q

what are the benefits of transdermal testosterone?

A

slow release, easy, avoids 1st pass metabolism

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43
Q

what is a major downfall of oral testosterone treatment?

A

most will be metabolized before reaching systemic circulation

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44
Q

how is testosterone for performance typically administered?

A

high dose my IM injection

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45
Q

why is testosterone for performance typically given IM?

A

to target the muscle they want to grow and avoids 1st pass metabolism

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46
Q

what is Androderm?

A

testosterone transdermal patch

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47
Q

t/f androgens are involved in prostate enlargement

A

t

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48
Q

what is benign prostatic hyperplasia (BPH)?

A

a benign prostate enlargement

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49
Q

what is a common symptoms of enlarged prostate?

A

urinary retention

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50
Q

why does enlarged prostate cause urinary retention?

A

obstruction of the urethra

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51
Q

does prostate cancer have a high level of metastasis?

A

yes

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52
Q

ketoconazole and spironolactone are anti-androgens that work by what way?

A

inhibit testosterone biosynthesis

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53
Q

what is a concern when usifg ketoconazole to inhibit testosterone synthesis?

A

a CYP3A4 inhibitor which can lead to a lot of interactions

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54
Q

why are ketoconazole and spironolactone not commonly used as androgen suppressors?

A

they both have other systemic effects and there are drugs that are more specific to target androgen production

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55
Q

how is finasteride used as an anti-androgen?

A

inhibits the conversion of testosterone to DHT by inhibiting the 5-alpha reductase enzymes

56
Q

how does flutamide work as an anti-androgen

A

androgen receptor antagonist

57
Q

an important consideration when using finasteride or flutamide as anti-androgens is that blocking these pathways allows for more ____

A

free testosterone that can be converted into estradiol

58
Q

what is a side-effect of finasteride and flutamide as a result of increased estradiol?

A

increased breast tissue

59
Q

what are the 5 hormones involved in female reproduction?

A

progestins, estrogens, human chorionic gonadotropin (hCG), oxytocin, prolactin

60
Q

which female hormones are directly involved in the menstrual cycle and female reproductive development?

A

progestins and estrogens

61
Q

____ is a hormone produced during early embryo development, is excreted in urine and is used in at-home pregnancy tests

A

human chorionic gonadotropin (hCG)

62
Q

what hormone is involved in uterine contractions during birth?

A

oxytocin

63
Q

what hormone is involved in milk production and lactation?

A

prolactin

64
Q

what are the 4 stages of the menstrual cycle in order?

A

follicle development, ovulation, endometrium proliferation, and menstruation

65
Q

what is the important hormone during the follicular phase?

A

FSH

66
Q

follicle secrete what hormone as they develop?

A

estrogen

67
Q

increased estrogen levels results in a ____ feedback on FSH levels and ____ feedback of LH levels

A

negative; positiev

68
Q

LH spike triggers ____

A

ovulation

69
Q

after ovulation, ___ and ____ levels rise

A

progesterone and estrogen

70
Q

estrogen and progesterone is secreted by the ____

A

corpus luteum

71
Q

what is the effect of estrogen and progesterone release after ovulation?

A

endometrial changes that favour implantation of a fertilized egg

72
Q

a drop in ___ and ___ hormones initiates menstruation

A

estrogen and progesterone

73
Q

t/f estrogen and progesterone have negative feedback effects throughout most of the menstrual cycle

A

t

74
Q

during follicle development, there is a ___ feedback loop between estradiol and LH, resulting in the LH surge needed for ovulation

A

positive

75
Q

estrogen and progesterone have nagative feedback loops on ___ and ___

A

FSH and GnRH

76
Q

estrogens and progesterone are produced mainly in the ____

A

ovaries

77
Q

is testosterone produced in the ovaries?

A

yes actually

78
Q

___ is the starting material for estrogen, testosterone, and progesterone

A

cholesterol

79
Q

____ enzymes are used in the process of making estrogen

A

aromatases

80
Q

t/f there are many similarities between the male and female hormone systems, but it is teh balance of the hormones made that makes the difference

A

t

81
Q

bc androgens and estrogens are made by the same pathway, altering production of one will have an impact om the other

A

t

82
Q

what is the most common pharm modulation of estrogens and progestins?

A

hormonal contraceptives to prevent pregnancy

83
Q

estrogens and progesterones used as hormone replacement are typically dosed ___ (higher or lower) than contraceptives

A

lower

84
Q

give 2 examples of local progestin administration for birth control

A

IUD and nuva ring

85
Q

how does hormonal contraception work?

A

reinforces the negative feedback loop to prevent LH surge, which inhibits ovulation, no egg, no pregnancy

86
Q

progestin-containing contraceptives have negative feedback on ___ and ___ hormones

A

LH and FSH

87
Q

what is the main goal of hormonal contraception?

A

increase the negative feedback loop so the positive feedback loop does not occur and ovulation is prevented

88
Q

estrogen ___ the endometrium

A

increses

89
Q

progesterone ___ the endometrium

A

decreases (lighter periods)

90
Q

if estrogen was given alone, it could cause ___

A

endometrial cancer

91
Q

t/f estrogen is always given at the lowest effective dose and always with progesterone

A

t

92
Q

the continual presence of progesterone makes the uterus unfavourable for _____

A

implantation of a fertilized egg

93
Q

progesterone ____ the movement of sperm

A

slows

94
Q

progesterone ____ cervical mucus production

A

increases

95
Q

what is ethinyl estradiol?

A

an estrogen used for contraception

96
Q

t/f progestin only products need to be taken at the same time every day to maintain adequate hormone levels

A

t

97
Q

depot injections typically last ___ weeks

A

12

98
Q

IUDs like mirena last up to ___ years

A

5

99
Q

what is the most common side effect with prolonged progestins?

A

breakthrough bleeding or spotting related to the shedding of the endometrial lining

100
Q

t/f the breakthrough bleeding of progestins typically resolves over time

A

t

101
Q

t/f many patients using IUD or depot tend to cease menstruation all together

A

t

102
Q

give an example of a progestin only contraceptive

A

micronor: norethindrone

103
Q

androgenic progestins may increase ___ and ___ as side effects and non-androgenic progestins have the oppposite effects

A

weight gain & acne

104
Q

what is the active ingredient in the depo-provera shot?

A

medroxyprogesterone acetate

105
Q

what is the active ingredient is the Mirena IUD?

A

levonorgestrel

106
Q

when a contraceptive with a progestin that is highly structurally similar to progesterone, it can be metabolized into _____ in the body

A

testosterone

107
Q

when the progestin in BC is converted into testosterone, it can cause what side effects?

A

weight gain, acne, hair growth

108
Q

are non-androgenic progestins structuarlly related to progesterone? Can they be converted into testosterone?

A

no ; no

109
Q

give an example of an androgenic progestin?

A

norethindrone

110
Q

give an example of a non-androgenic progestins

A

dropirenone

111
Q

t/f the combination estrogen and progestin hormonal contraceptives are the most common birth control pills

A

t

112
Q

t/f ethinyl estradiol is commonly used, but many different progestins are used

A

t

113
Q

t/f there are many different varieties of dosing regimens

A

t

114
Q

t/f combination birth controls cause an “artificial menstrual cycle”

A

t

115
Q

what are the active ingredients in Yaz?

A

ethinyl estradiol & drospirenone

116
Q

how does combination BC like Yaz work?

A

phasic cycles of hormone levels mimic physiologic levels to maintain the menstrual cycle but prevent the LH spike that would cause ovulation

117
Q

what are some common side effects of elevated estrogen from BC? Are they reversible?

A

nausea, edema, migraines; usually resolve after prolonged use or when the dose is lowered

118
Q

what are some of the serious side effects of estrogen in BC? What increases these risks?

A

CV (MI, blood clots, stroke); smoking and being older than 35 years

119
Q

what can be done if a patient on a combo BC continues to have migraines and increased CV risk?

A

can be switched to progestin only pill

120
Q

what is the failure rate of OCs?

A

7%

121
Q

what is the failure rate of barrier methods like condoms?

A

13%

122
Q

what can cause low hormone levels leading to contraceptive failures?

A

missing pills or improper administration, drug interactions, or other physiologic changes

123
Q

t/f blood monitoring for hormone levels following BC use is possible, but not done unless there is a compelling reason

A

t

124
Q

estrogens and progestin are metabolized by ____ enzymes, meaning many drug interactions are possible

A

CYP3A4

125
Q

are CYP3A4 inducers or inhibitors more likely to decrease BC hormones?

A

CYP3A4 hormones

126
Q

if using a combo BC rather than just progesterone, you are ___ (more or less ) likely to avoid failure due to drug interactions

A

less

127
Q

the effect of enterohepatic circulation would be ____ (more or less) prominent when using an alternative dosage form like the IUD or depo shot

A

less

128
Q

t/f the Mirena also prevents egg implantation by providing a physical barrier

A

t

129
Q

the overall effectiveness of IUDs like Mirena is reported to be greater than ___

A

99%

130
Q

is antibiotic use while on BC directly linked to failure leading to pregnancy?

A

no

131
Q

what is the fail rate of depot progestin injections?

A

4%

132
Q

what is the failure rate of surgical sterilization?

A

0.1-0.5%

133
Q

what is the effect of phenytoin on BC?

A

CYP3A4 inducer (reduce circulating hormones)

134
Q

what is the effect of antibiotics on BC?

A

reduce GI enterohepatic circulation hormones and increase CYP3A4

135
Q

which antibiotic has been linked to possible contraceptive failure?

A

rifampin

.Pharmacology (55 decks)

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