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Sex hormones Flashcards

1
Q

Leuprolide drug class?

A

Long acting GnRH agonist

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2
Q

Cetrorelix drug class?

A

GnRH antagonist

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3
Q

Menotropin/ Humegon drug class?

A

FSH

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4
Q

Pregnyl drug class?

A

LH

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5
Q

What are the endogenous estrogens? (3)

A

Estradiol, estrone, estriol

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6
Q

Ethinyl estradiol drug class?

A

Estrogens

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7
Q

Premarin drug class?

A

Estrogens

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8
Q

Estradiol drug class?

A

Estrogens

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9
Q

Tamoxifen drug class?

A

Antiestrogens

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10
Q

Raloxifene drug class?

A

Antiestrogens

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11
Q

Clomiphene drug class?

A

Antiestrogens

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12
Q

Anastrozole drug class?

A

Aromatase inhibitors

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13
Q

Medroxyprogesterone (Provera) drug class?

A

Progestins (progesterone derivative)

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14
Q

Levonorgestrel drug class?

A

Progestins (19-nortestosterone, has both progestin and androgenic activity)

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15
Q

Mifepristone drug class?

A

Antiprogestins

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16
Q

Drospirenone/ ethinyl estradiol drug/ drug class?

A

Yasmin/ Yaz, combined oral contraceptive

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17
Q

Testoderm transdermal drug class?

A

Androgens

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18
Q

Flutamide drug class?

A

Anti-androgens

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19
Q

Spironolactone drug class?

A

Anti-androgens

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20
Q

Finasteride drug class?

A

5alpha-reductase inhibitors

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21
Q

What hormone drives follicular development during the follicular/ proliferative phase?

A

FSH

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22
Q

During ovulation, there is high/ sustained levels of what hormone which leads to positive feedback on LH release and the LH surge?

A

Estrogen

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23
Q

What follows the LH surge? (2)

A

Ovulation and luteinization

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24
Q

What hormone maintains the corpus luteum (CL) during the luteal/ secretory phase?

A

LH

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25
Q

What hormones maintains the endothelium during the luteal/ secretory phase?

A

Progesterone/ estrogen

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26
Q

What progression of hormone loss leads to menstruation?

A

Loss of LH = loss of CL = loss of P+E

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27
Q

What is the term for sudden ovarian enlargement with increased vascular permeability leading to a rapid accumulation of fluid in the peritoneal, pleural and pericardial cavities?

A

Ovarian hyperstimulation syndrome

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28
Q

What symptoms/ complications can accompany ovarian hyperstimulation syndrome? (5)

A

Thromboembolisms, hypovolemia, fever, +/- shock, death

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29
Q

What is defined as a reduced ovarian response to gonadotropins (including decreased ovarian steroids and decreased gonadotropins)?

A

Menopause

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30
Q

HA, palpitations, night sweats, insomnia, and hot flashes are examples of what type of problems seen with menopause?

A

Vasomotor

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31
Q

What are the targets for HRT in menopause? (3)

A

Genito-urinary problems (loss of trophic effect of estrogen), osteoporosis, heart disease

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32
Q

What are the uses of HRT in females? (3)

A

Menopause (E + P), girls with no ovarian development or removal of ovaries prior to menopausal age (E+P), hysterectomies (E only)

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33
Q

What guidelines should be followed for HRT in the treatment of hot flashes/ night sweats in menopause?

A

Lowest dose for shortest duration

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34
Q

Although Raloxifene is still an option for HRT, why is it not first line?

A

Prevents osteoporosis and breast cancer BUT does NOT affected CHD/ hot flashes

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35
Q

What administration route of HRT is the best for osteoporosis and hot flashes?

A

Transdermal therapy

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36
Q

What type of HRT is the best to decrease vaginal thinning and irritation?

A

Estrogen cream

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37
Q

What are the adverse effects of HRT in females? (4)

A 
Breast cancer (E+P), endometrial cancer (E only)
CV, gallbladder disease

(only a small risk for breast cancer but reason for bad rep)

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38
Q

When has HRT been shown to have the most beneficial effects and lowest risk of causing breast cancer?

A

E only and < 10 years after onset of menopause

(typically ~50-59 yo, healthy women in first few years of menopause who need HRT to relieve sxs should have no fears about use and benefits outweigh risks)

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39
Q

What is the MOA for Leuprolide?

A

Suppresses release of LH and FSH ~3 weeks, after initial surge

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40
Q

What is the DOC for endometriosis and precocious puberty?

A

Leuprolide

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41
Q

Aside from endometriosis and precocious puberty (DOC), what drug can be used for IVF, sex-dependent CA, and gender affirmation (stops puberty until child decides gender)?

A

Leuprolide

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42
Q

What are the side effects of Leuprolide and Cetrorelix? (2)

A

Menopausal sxs, testicular atrophy (shuts down HPG axis)

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43
Q

What are the contraindications to use of Leuprolide and Cetrorelix? (2)

A

Pregnancy, breast feeding

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44
Q

If Leuprolide is used in the treatment of metastatic prostate cancer, what else must be done?

A

Treat with antiandrogen at start of treatment (due to initial tumor flare)

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45
Q

What is the MOA for Cetrorelix?

A

Suppresses release of LH at low doses and FSH at higher doses ~4-5 days, no initial surge

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46
Q

What is the primary drug used for the treatment of IVF, but can also be used for endometriosis, precocious puberty, sex-dependent cancers, and gender affitmation?

A

Cetrorelix

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47
Q

What is the MOA of menotropins/ Humegon?

A

HRT

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48
Q

What drug is used for the treatment of pituitary or hypothalamic hypogonadism with infertility?

A

Menotropins/ Humegon

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49
Q

Menotropins/ Humegon induces spermatogenesis in hypogonadotropic hypogonadal men after how long?

A

Months

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50
Q

Menotropins/ Humegon stimulates the ovaries and estrogen production after how long?

A

9-12 days

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51
Q

In what order to you give FSH and LH for infertility treatment in women?

A

Give FSH then LH to induce ovulation

*F for FSH, Females, First

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52
Q

In what order to you give FSH and LH for infertility treatment in men?

A

Give LH then FSH to induce spermatogenesis

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53
Q

What are the side effects of menotropins/ Humegon (FSH) and Pregnyl (LH)? (3)

A

Ovarian hyperstimulation syndrome, multiple births, gynecomastia in men

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54
Q

What is the contraindication to treatment with Menotropins/ Humegon (FSH) and Pregnyl (LH)?

A

Sex-steroid dependent CA

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55
Q

What is the MOA of Pregnyl?

A

Binds to LH receptor resulting in LH effects

56
Q

What is the important pharmacokinetic property of Pregnyl (compared to endogenous LH)?

A

Longer half life

57
Q

What is Pregnyl used for?

A

Reversing infertility by increasing T for up to 1 year in men and inducing ovulation in women

58
Q

What is the MOA for endogenous estrogens?

A

Nuclear receptors

interact with DNA = inc mRNA and protein synthesis = effects of hormone, takes time for onset/ sx to digress

59
Q

How are endogenous estrogens metabolized?

A

Metabolized in liver and undergo enterohepatic circulation

60
Q

What is the benefit of endogenous estrogens undergoing enterohepatic circulation?

A

Reverse conjugations and increase bioavailability

61
Q

What is the role of estrogen on the uterus?

A

Endometrial growth

62
Q

What is the role of estrogen on puberty?

A

Close epiphyses

63
Q

What is the role of estrogen on bone?

A

Maintenance

64
Q

What is the role of estrogen on blood clotting?

A

Increased synthesis of clotting proteins and platelet adhesiveness

65
Q

What is the role of estrogen on metabolism? (2)

A

Increase hormone binding proteins (SHBG, CBG, TBG)

Increase HDL/ decrease LDL

66
Q

Which form of synthetic estrogen is given as a cream/ patch?

67
Q

Which form of synthetic estrogen is given as oral contraceptives?

A

Ethinyl estrogens

68
Q

Which form of synthetic estrogen is given as HRT?

A

Conjugated estrogens (Premarin)

69
Q

What drugs stimulate pubertal development in hypogonadic girls, decrease uterine bleeding, suppress ovulation in dysmenorrhea, and are used in male-to-female gender affirming treatment?

A

Synthetic estrogens

70
Q

Although dose dependent, what are the SEs of synthetic estrogens? (2)

A

Migraines, thromboembolism/ accelerated blood clotting

71
Q

What are the contraindications to synthetic estrogens? (3)

A

Estrogen-dependent neoplasms (breast CA)
History of thromboembolic disorders
Pregnancy

72
Q

What is the MOA for Tamoxifen, Raloxifene, and Clomiphene?

A

Selective estrogen receptor modulator (SERM)

73
Q

Where is Tamoxifen an agonist/ antagonist?

A

Agonist in uterus and bone (prevents bone loss)

Antagonist in breast

74
Q

What is the DOC for palliative and prophylactic treatment of estrogen-dependent breast CA in premenopausal women?

A

Tamoxifen (antiestrogen)

(competes with estrogen for receptor in breast

75
Q

What are the side effects of Tamoxifen? (3)

A

Increased risk of uterine cancer, hot flashes, N/V

76
Q

Where is Raloxifene an agonist/ antagonist?

A

Agonist in bone and liver

Antagonist in breast and uterus

77
Q

What drug is used in the prevention of postmenopausal osteoporosis?

A

Raloxifene

78
Q

What are the side effects of Raloxifene? (3)

A

Hot flashes, DVT, leg cramps

79
Q

Where is Clomiphene an agonist/ antagonist?

A

Antagonist in hypothalamus

Agonist elsewhere

80
Q

What is the DOC for initial infertility treatment in women with intact HPG axis?

A

Clomiphene

stimulates LH and FSH

81
Q

What is the primary side effect of Clomiphene?

A

Multiple pregnancies

others: hot flashes, HA, constipation, allergic rxn, hair loss, +/- enlarged ovaries

82
Q

Do aromatase inhibitors inhibit other steroid synthesis?

83
Q

What is the MOA for Anastrozole?

A

Inhibits aromatase activity to prevent production of estriol, estrone, and estradiol?

84
Q

What is the DOC for treatment of breast CA in postmenopausal women?

A

Anastrozole

85
Q

When is Anastrozole 2nd line treatment for advanced breast CA?

A

Postmenopausal women whose disease progressed during Tamoxifen therapy

(ovarian ablation to make premenopausal women postmenopausal)

86
Q

What are the side effects of Anastrozole? (2)

A

Menopausal sxs (even if postmenopausal), GI sx

87
Q

What are the contraindications of Anastrozole? (2)

A

Premenopausal women, pregnancy

88
Q

What is the MOA for endogenous progesterone?

A

Acts on nuclear receptor

89
Q

What endogenous hormone acts on the uterus to convert the endometrium to a secretory state to maintain pregnancy and also plays a role in the endocervical glands, breasts, and thermogenic action?

A

Progesterone

90
Q

Progesterone drug class?

A

Progestins (progesterone derivative)

91
Q

What drug is Plan B?

A

Levonorgestrel

92
Q

What is the MOA of Progesterone, Medroxyprogesterone (Provera) and Levonorgestrel (Plan B)?

A

Progesterone receptor agonists

93
Q

What drugs are used for oral contraceptives (alone or in combo), prevention of endometrial hyperplasia with HRT, and when estrogen is contraindicated?

A

Progestins (Progesterone, Provera, Levonorgestrel)

94
Q

What are the side effects of progestins? (3)

A

Decreased BP, decreased HDL, depression/ drowsiness

95
Q

What is the MOA of Mifepristone?

A

Blocks progestin binding to progesterone/ glucocorticoid receptor (antagonist)

96
Q

What drug is used for pregnancy termination (in combo with prostaglandins) and to prevent implantation (within 72 hours)

A

Mifepristone

97
Q

What are the side effects of Mifepristone? (2)

A

GI sxs, vaginal bleeding

98
Q

Why is Mifepristone not first choice for emergency contraception?

A

Excessive SEs

99
Q

What are the contraindications to Mifepristone? (3)

A

Pregnancy, breast feeding, current glucocorticoid therapy

100
Q

What is most important in the effectiveness of combo oral contraceptives?

A

E:P ratio (mimics physiologic hormonal cycle and decreases SEs)

101
Q

Normal combo oral contraceptives follow a 21/ 7 day pattern but newer pills result in longer cycles of what combo? (3)

A

84 on/ 7 off, 84 on/ estrogen only, always on

102
Q

What is the MOA for combined oral contraceptives?

A

Inhibits LH surge and prevents ovulation, progestin changes cervical mucus and endometrium = decreased implantation

103
Q

What is a benefit of combined oral contraceptives aside from effective contraception?

A

Decreased risk for ovarian/ endometrial CA

104
Q 
The following side effects are for what class of drugs? 
Weight gain, nausea, edema, depression, breakthrough bleeding, CV problems (clotting, mild HTB, migraine, MI/ stroke), teratogenesis, and fertility?
A

Combined oral contraceptives

105
Q

What are the specific side effects of combined oral contraceptives with longer cycle times? (2)

A

Increased breakthrough bleeding (> 1st year), hard to tell if pregnant

106
Q

What are the absolute contraindications to combined oral contraceptives? (3)

A

ASCVD, thromboembolitic phenomena (any clotting disorder), estrogen depdendent cancers

(others: pregnancy, >35 yo smoker, uncontrolled HTN (bc causes HTN), DM)

107
Q

What is a relative contraindication to combined oral contraceptives?

A

Liver disease

108
Q

What are the possible drug interactions seen with combined oral contraceptives?

A

P450 inducers, antibiotics

109
Q

What component of Yaz is the mineralocorticoid antagonist and why is this beneficial?

A

Drospirenone- decreases water retention

other component = ethinyl estradiol

110
Q

What drug is used as birth control but also results in decreased water retention/ less bloating and is therefore also used as a treatment for PMDD?

A

Yasmin, Yaz

111
Q

When are the following contraceptive drugs used?

Plan B, Preven, Mifespristone

A

Post-coital emergency (most effective within 72 hours)

112
Q

Are the following contraceptive drugs combo or progestin-only?
Natazina
NuvaRing

113
Q

What combo contraceptive provides a 3 week supply of hormone control?

114
Q

What combo contraceptive produces E2 in vivo, allowing for production of bioidentical hormones?

115
Q

What type of contraceptive drugs result in early breakthrough bleeding followed by amenorrhea?

A

Progestin only

116
Q

What progestin-only contraceptive has 87-98% effectiveness and are used during breastfeeding?

A

Mini pills

during breast feeding, mother releases estrogen = combo effect

117
Q

What progestin- only contraceptive is given as 1 injection per 3 months?

A

Depo-provera

118
Q

What progestin-only contraceptive is implanted in the arm and lasts for 3 years?

A

Implanon and Nexplanon

119
Q

What progestin-only contraceptive is an IUC and lasts for 5 years?

120
Q

The following are actions of what endogenous hormone?
Virilizing (androgenic) effects
Anabolic effects
Puberty

A

Testosterone (androgens)

121
Q

What is the MOA of Testoderm transdermal?

A

Testosterone receptor agonist

122
Q

Besides testicular deficiency (hypogonadism), what are other uses of Testoderm transdermal? (4)

A

Female hypopituitarism (+ estrogen), hypoproteinemia of nephrosis, negative nitrogen balance, F-to-M gender affirming treatment

123
Q

For males and females, oily skin, acne, decreased HDL, psych changes (aggression, depression, altered sex drive, psychosis) are side effects of what drug?

A

Testoderm transdermal

124
Q

For males, decreased testosterone/ spermatogenesis is a side effect of what drug?

A

Testoderm transdermal

125
Q

For females, masculinization and pseudohermaphtoditism of fetus in pregnant women are side effects of what drug?

A

Testoderm transdermal

126
Q

What is the MOA for Flutamide?

A

Blocks androgen receptor

127
Q

When is Flutamide used for treatment of prostate cancer?

A

With a long-acting GnRH agonist (prevents tumor flare at start of treatment)

128
Q

What is the SE of Flutamide?

A

Reversible hepatotoxicity (so only use short-term)

129
Q

Is spironolactone high or low dose antiandrogen?

130
Q

What is the MOA of Spironolactone?

A

Mineralocorticoid antagonist- prevents T synthesis and blocks androgen receptor

131
Q

What are the uses of Spironolactone? (4)

A 
Women: hirsutism, PCOS, PMS 
Precocious puberty (not DOC)
132
Q

What is the MOA of Finasteride?

A

Inhibits 5alpha- reductase (no conversion of T to DHT)

133
Q

What are the uses of Finasteride? (3)

A

BPH, male pattern baldness, suppresses male sex accessory organs w/o affecting libido

134
Q

What are the SEs of Finasteride? (2)

A

Gynecomastia, ED

135
Q

What is a contraindication to Finasteride?

Pharm II (13 decks)

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