Sex hormones Flashcards
(135 cards)
1
Q
Leuprolide drug class?
A
Long acting GnRH agonist
2
Q
Cetrorelix drug class?
A
GnRH antagonist
3
Q
Menotropin/ Humegon drug class?
A
FSH
4
Q
Pregnyl drug class?
A
LH
5
Q
What are the endogenous estrogens? (3)
A
Estradiol, estrone, estriol
6
Q
Ethinyl estradiol drug class?
A
Estrogens
7
Q
Premarin drug class?
A
Estrogens
8
Q
Estradiol drug class?
A
Estrogens
9
Q
Tamoxifen drug class?
A
Antiestrogens
10
Q
Raloxifene drug class?
A
Antiestrogens
11
Q
Clomiphene drug class?
A
Antiestrogens
12
Q
Anastrozole drug class?
A
Aromatase inhibitors
13
Q
Medroxyprogesterone (Provera) drug class?
A
Progestins (progesterone derivative)
14
Q
Levonorgestrel drug class?
A
Progestins (19-nortestosterone, has both progestin and androgenic activity)
15
Q
Mifepristone drug class?
A
Antiprogestins
16
Q
Drospirenone/ ethinyl estradiol drug/ drug class?
A
Yasmin/ Yaz, combined oral contraceptive
17
Q
Testoderm transdermal drug class?
A
Androgens
18
Q
Flutamide drug class?
A
Anti-androgens
19
Q
Spironolactone drug class?
A
Anti-androgens
20
Q
Finasteride drug class?
A
5alpha-reductase inhibitors
21
Q
What hormone drives follicular development during the follicular/ proliferative phase?
A
FSH
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
23
Q
What follows the LH surge? (2)
A
Ovulation and luteinization
24
Q
What hormone maintains the corpus luteum (CL) during the luteal/ secretory phase?
A
LH
25
What hormones maintains the endothelium during the luteal/ secretory phase?
Progesterone/ estrogen
26
What progression of hormone loss leads to menstruation?
Loss of LH = loss of CL = loss of P+E
27
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?
Ovarian hyperstimulation syndrome
28
What symptoms/ complications can accompany ovarian hyperstimulation syndrome? (5)
Thromboembolisms, hypovolemia, fever, +/- shock, death
29
What is defined as a reduced ovarian response to gonadotropins (including decreased ovarian steroids and decreased gonadotropins)?
Menopause
30
HA, palpitations, night sweats, insomnia, and hot flashes are examples of what type of problems seen with menopause?
Vasomotor
31
What are the targets for HRT in menopause? (3)
Genito-urinary problems (loss of trophic effect of estrogen), osteoporosis, heart disease
32
What are the uses of HRT in females? (3)
Menopause (E + P), girls with no ovarian development or removal of ovaries prior to menopausal age (E+P), hysterectomies (E only)
33
What guidelines should be followed for HRT in the treatment of hot flashes/ night sweats in menopause?
Lowest dose for shortest duration
34
Although Raloxifene is still an option for HRT, why is it not first line?
Prevents osteoporosis and breast cancer BUT does NOT affected CHD/ hot flashes
35
What administration route of HRT is the best for osteoporosis and hot flashes?
Transdermal therapy
36
What type of HRT is the best to decrease vaginal thinning and irritation?
Estrogen cream
37
What are the adverse effects of HRT in females? (4)
```
Breast cancer (E+P), endometrial cancer (E only)
CV, gallbladder disease
```
(only a small risk for breast cancer but reason for bad rep)
38
When has HRT been shown to have the most beneficial effects and lowest risk of causing breast cancer?
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)
39
What is the MOA for Leuprolide?
Suppresses release of LH and FSH ~3 weeks, after initial surge
40
What is the DOC for endometriosis and precocious puberty?
Leuprolide
41
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)?
Leuprolide
42
What are the side effects of Leuprolide and Cetrorelix? (2)
Menopausal sxs, testicular atrophy (shuts down HPG axis)
43
What are the contraindications to use of Leuprolide and Cetrorelix? (2)
Pregnancy, breast feeding
44
If Leuprolide is used in the treatment of metastatic prostate cancer, what else must be done?
Treat with antiandrogen at start of treatment (due to initial tumor flare)
45
What is the MOA for Cetrorelix?
Suppresses release of LH at low doses and FSH at higher doses ~4-5 days, no initial surge
46
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?
Cetrorelix
47
What is the MOA of menotropins/ Humegon?
HRT
48
What drug is used for the treatment of pituitary or hypothalamic hypogonadism with infertility?
Menotropins/ Humegon
49
Menotropins/ Humegon induces spermatogenesis in hypogonadotropic hypogonadal men after how long?
Months
50
Menotropins/ Humegon stimulates the ovaries and estrogen production after how long?
9-12 days
51
In what order to you give FSH and LH for infertility treatment in women?
Give FSH then LH to induce ovulation
*F for FSH, Females, First
52
In what order to you give FSH and LH for infertility treatment in men?
Give LH then FSH to induce spermatogenesis
53
What are the side effects of menotropins/ Humegon (FSH) and Pregnyl (LH)? (3)
Ovarian hyperstimulation syndrome, multiple births, gynecomastia in men
54
What is the contraindication to treatment with Menotropins/ Humegon (FSH) and Pregnyl (LH)?
Sex-steroid dependent CA
55
What is the MOA of Pregnyl?
Binds to LH receptor resulting in LH effects
56
What is the important pharmacokinetic property of Pregnyl (compared to endogenous LH)?
Longer half life
57
What is Pregnyl used for?
Reversing infertility by increasing T for up to 1 year in men and inducing ovulation in women
58
What is the MOA for endogenous estrogens?
Nuclear receptors
| interact with DNA = inc mRNA and protein synthesis = effects of hormone, takes time for onset/ sx to digress
59
How are endogenous estrogens metabolized?
Metabolized in liver and undergo enterohepatic circulation
60
What is the benefit of endogenous estrogens undergoing enterohepatic circulation?
Reverse conjugations and increase bioavailability
61
What is the role of estrogen on the uterus?
Endometrial growth
62
What is the role of estrogen on puberty?
Close epiphyses
63
What is the role of estrogen on bone?
Maintenance
64
What is the role of estrogen on blood clotting?
Increased synthesis of clotting proteins and platelet adhesiveness
65
What is the role of estrogen on metabolism? (2)
Increase hormone binding proteins (SHBG, CBG, TBG)
| Increase HDL/ decrease LDL
66
Which form of synthetic estrogen is given as a cream/ patch?
Estradiol
67
Which form of synthetic estrogen is given as oral contraceptives?
Ethinyl estrogens
68
Which form of synthetic estrogen is given as HRT?
Conjugated estrogens (Premarin)
69
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?
Synthetic estrogens
70
Although dose dependent, what are the SEs of synthetic estrogens? (2)
Migraines, thromboembolism/ accelerated blood clotting
71
What are the contraindications to synthetic estrogens? (3)
Estrogen-dependent neoplasms (breast CA)
History of thromboembolic disorders
Pregnancy
72
What is the MOA for Tamoxifen, Raloxifene, and Clomiphene?
Selective estrogen receptor modulator (SERM)
73
Where is Tamoxifen an agonist/ antagonist?
Agonist in uterus and bone (prevents bone loss)
| Antagonist in breast
74
What is the DOC for palliative and prophylactic treatment of estrogen-dependent breast CA in premenopausal women?
Tamoxifen (antiestrogen)
(competes with estrogen for receptor in breast
75
What are the side effects of Tamoxifen? (3)
Increased risk of uterine cancer, hot flashes, N/V
76
Where is Raloxifene an agonist/ antagonist?
Agonist in bone and liver
| Antagonist in breast and uterus
77
What drug is used in the prevention of postmenopausal osteoporosis?
Raloxifene
78
What are the side effects of Raloxifene? (3)
Hot flashes, DVT, leg cramps
79
Where is Clomiphene an agonist/ antagonist?
Antagonist in hypothalamus
| Agonist elsewhere
80
What is the DOC for initial infertility treatment in women with intact HPG axis?
Clomiphene
| stimulates LH and FSH
81
What is the primary side effect of Clomiphene?
Multiple pregnancies
| others: hot flashes, HA, constipation, allergic rxn, hair loss, +/- enlarged ovaries
82
Do aromatase inhibitors inhibit other steroid synthesis?
No
83
What is the MOA for Anastrozole?
Inhibits aromatase activity to prevent production of estriol, estrone, and estradiol?
84
What is the DOC for treatment of breast CA in postmenopausal women?
Anastrozole
85
When is Anastrozole 2nd line treatment for advanced breast CA?
Postmenopausal women whose disease progressed during Tamoxifen therapy
(ovarian ablation to make premenopausal women postmenopausal)
86
What are the side effects of Anastrozole? (2)
Menopausal sxs (even if postmenopausal), GI sx
87
What are the contraindications of Anastrozole? (2)
Premenopausal women, pregnancy
88
What is the MOA for endogenous progesterone?
Acts on nuclear receptor
89
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?
Progesterone
90
Progesterone drug class?
Progestins (progesterone derivative)
91
What drug is Plan B?
Levonorgestrel
92
What is the MOA of Progesterone, Medroxyprogesterone (Provera) and Levonorgestrel (Plan B)?
Progesterone receptor agonists
93
What drugs are used for oral contraceptives (alone or in combo), prevention of endometrial hyperplasia with HRT, and when estrogen is contraindicated?
Progestins (Progesterone, Provera, Levonorgestrel)
94
What are the side effects of progestins? (3)
Decreased BP, decreased HDL, depression/ drowsiness
95
What is the MOA of Mifepristone?
Blocks progestin binding to progesterone/ glucocorticoid receptor (antagonist)
96
What drug is used for pregnancy termination (in combo with prostaglandins) and to prevent implantation (within 72 hours)
Mifepristone
97
What are the side effects of Mifepristone? (2)
GI sxs, vaginal bleeding
98
Why is Mifepristone not first choice for emergency contraception?
Excessive SEs
99
What are the contraindications to Mifepristone? (3)
Pregnancy, breast feeding, current glucocorticoid therapy
100
What is most important in the effectiveness of combo oral contraceptives?
E:P ratio (mimics physiologic hormonal cycle and decreases SEs)
101
Normal combo oral contraceptives follow a 21/ 7 day pattern but newer pills result in longer cycles of what combo? (3)
84 on/ 7 off, 84 on/ estrogen only, always on
102
What is the MOA for combined oral contraceptives?
Inhibits LH surge and prevents ovulation, progestin changes cervical mucus and endometrium = decreased implantation
103
What is a benefit of combined oral contraceptives aside from effective contraception?
Decreased risk for ovarian/ endometrial CA
104
```
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?
```
Combined oral contraceptives
105
What are the specific side effects of combined oral contraceptives with longer cycle times? (2)
Increased breakthrough bleeding (> 1st year), hard to tell if pregnant
106
What are the absolute contraindications to combined oral contraceptives? (3)
ASCVD, thromboembolitic phenomena (any clotting disorder), estrogen depdendent cancers
(others: pregnancy, >35 yo smoker, uncontrolled HTN (bc causes HTN), DM)
107
What is a relative contraindication to combined oral contraceptives?
Liver disease
108
What are the possible drug interactions seen with combined oral contraceptives?
P450 inducers, antibiotics
109
What component of Yaz is the mineralocorticoid antagonist and why is this beneficial?
Drospirenone- decreases water retention
| other component = ethinyl estradiol
110
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?
Yasmin, Yaz
111
When are the following contraceptive drugs used?
| Plan B, Preven, Mifespristone
Post-coital emergency (most effective within 72 hours)
112
Are the following contraceptive drugs combo or progestin-only?
Natazina
NuvaRing
Combo
113
What combo contraceptive provides a 3 week supply of hormone control?
NuvaRing
114
What combo contraceptive produces E2 in vivo, allowing for production of bioidentical hormones?
Natazina
115
What type of contraceptive drugs result in early breakthrough bleeding followed by amenorrhea?
Progestin only
116
What progestin-only contraceptive has 87-98% effectiveness and are used during breastfeeding?
Mini pills
| during breast feeding, mother releases estrogen = combo effect
117
What progestin- only contraceptive is given as 1 injection per 3 months?
Depo-provera
118
What progestin-only contraceptive is implanted in the arm and lasts for 3 years?
Implanon and Nexplanon
119
What progestin-only contraceptive is an IUC and lasts for 5 years?
Minera
120
The following are actions of what endogenous hormone?
Virilizing (androgenic) effects
Anabolic effects
Puberty
Testosterone (androgens)
121
What is the MOA of Testoderm transdermal?
Testosterone receptor agonist
122
Besides testicular deficiency (hypogonadism), what are other uses of Testoderm transdermal? (4)
Female hypopituitarism (+ estrogen), hypoproteinemia of nephrosis, negative nitrogen balance, F-to-M gender affirming treatment
123
For males and females, oily skin, acne, decreased HDL, psych changes (aggression, depression, altered sex drive, psychosis) are side effects of what drug?
Testoderm transdermal
124
For males, decreased testosterone/ spermatogenesis is a side effect of what drug?
Testoderm transdermal
125
For females, masculinization and pseudohermaphtoditism of fetus in pregnant women are side effects of what drug?
Testoderm transdermal
126
What is the MOA for Flutamide?
Blocks androgen receptor
127
When is Flutamide used for treatment of prostate cancer?
With a long-acting GnRH agonist (prevents tumor flare at start of treatment)
128
What is the SE of Flutamide?
Reversible hepatotoxicity (so only use short-term)
129
Is spironolactone high or low dose antiandrogen?
High dose
130
What is the MOA of Spironolactone?
Mineralocorticoid antagonist- prevents T synthesis and blocks androgen receptor
131
What are the uses of Spironolactone? (4)
```
Women: hirsutism, PCOS, PMS
Precocious puberty (not DOC)
```
132
What is the MOA of Finasteride?
Inhibits 5alpha- reductase (no conversion of T to DHT)
133
What are the uses of Finasteride? (3)
BPH, male pattern baldness, suppresses male sex accessory organs w/o affecting libido
134
What are the SEs of Finasteride? (2)
Gynecomastia, ED
135
What is a contraindication to Finasteride?
Pregnancy
