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Pharm II Unit III > 1 Sex Hormones > Flashcards

1 Sex Hormones Flashcards

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1
Q

Because GnRH release is typically pulsatile, continues exogenous GnRH administration will…

A

Suppress gonadotropin (FSH/LH) release

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2
Q

What drugs are the long-acting GnRH agonists?

A

Leuprolide (Lupron)

Goserelin (Zoladex)

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3
Q

MOA for Long-Acting GnRH agonists

A

Continuous administration suppresses release of LH and FSH (after initial surge)

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4
Q

What might you use long-acting GnRH agonists for?

A

(Leuprolide and goserelin)

Used in IVF, sex steroid-dependent cancers (ie PROSTATE CANCER), endometriosis, precocious puberty

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5
Q

GnRH antagonists

A

Cetrorelix (Cetrotide)

Ganirelix (Antagon)

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6
Q

What are GnRH antagonists used for?

A

Suppress LH/FSH

Used for the same purposes as long-acting GnRH agonists - IVF, sex steroid-dependent cancers, endometriosis, precocious puberty

BUT, only need 4-5 days of antagonist vs 3 weeks of agonist

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7
Q

How are long-acting GnRH agonists and GnRH antagonists different?

A

Only 4-5 days of antagonist treatment needed vs 3 weeks of agonist to suppress gonadotropin

No initial surge of gonadotropin with antagonist treatment

(Agonist only) Metastatic prostate cancer - problems during start of treatment (use antiandrogen)

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8
Q

Mutual adverse effects of long-acting GnRH agonists and GnRH antagonists

A

Menopausal symptoms

Testicular atrophy

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9
Q

During the follicular/proliferative phase of the menstrual cycle, ______ drives folliculogenesis

A

FSH

—> increased estrogen
—> endometrial development and thickening

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10
Q

During ovulation, high, sustained levels of ______ cause a positive feedback on ____ release

A

Estrogen
LH release

LH surge —> ovulation —> Luteinization

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11
Q

What maintains the corpus luteum during the secretory phase of the menstrual cycle?

A

LH (that’s why it’s called the Luteal phase)

Meanwhile, progesterone and estrogen maintain the endometrium

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12
Q

How does menstruation occur?

A

Loss of LH —> loss of CL —> loss of progesterone and estrogen

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13
Q

Role of FSH in Women and Men

A

Women: develops overian follicles and supports estrogen synthesis

Men: stimulates spermatogenesis

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14
Q

What is used to replace FSH?

A

Human menopausal gonadotropin (hMG) - aka menotropins

Contain FSH and LH but used as you would FSH

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15
Q

What is Urofollitropin (uFSH, Bravelle)?

A

purified FSH

no longer on the market

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16
Q

What does LH do in Women and Men?

A

Women: Stimulates ovulation and luteinization of follicles, and responsible for estrogen/progesterone synthesis

Men: Testosterone synthesis

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17
Q

What is used instead of LH?

A

hCG (human chorionic gonadotropin; Pregnyl)

Has same actions as LH, but works by binding to the same receptor

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18
Q

How are gonadotropins used in men?

A

To reverse infertility

To induce spermatogenesis, give LH to increase testosterone (for up to a year), then FSH to induce spermatogenesis (takes months)

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19
Q

How are gonadotropins used in women?

A

For IVF (ART)

Give FISH first (9-12 days) to stimulate ovaries and estrogen production, then a single dose of LH to induce ovulation

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20
Q

Why is the hCG diet a bad fucking idea?

A

No conclusive evidence for any benefit compared to only the 500 cal/day diet

You gain the weight right back when you stop

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21
Q

Side effects of gonadotropin use

A

Uncomplicated ovarian enlargement

OVARIAN HYPERSTIMULATION SYNDROME (most serious - medical emergency)

MULTIPLE BIRTHS in 20%

Gynecomastia

HA, depression, edema, precocious puberty

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22
Q

Contraindications for the use of gonadotropins

A

Sex steroid-dependent cancers

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23
Q

What are the different endogenous estrogens?

A

Estradiol
Estriol
Estrone

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24
Q

How do estrogens work?

A

Upon nuclear receptors

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25
How are estrogens metabolized?
Conjugated by the liver and excreted in bile Enterohepatic circulation reverses conjugation and increases bioavailability
26
Estrogen Functions: On the ovaries
Prepare for ovulation
27
Estrogen Functions: On the uterus
Endometrial growth
28
Estrogen Functions: On vaginal epithelium
Proliferation, maintenance
29
Estrogen Functions: On endocervical glands
Mucus
30
Estrogen Functions: On breasts
Growth during pregnancy and puberty
31
Estrogen Functions: On puberty
Growth and maturation, closes epiphyses
32
Estrogen Functions: On bones
Maintenance
33
Estrogen Functions: On blood clotting
Increased synthesis of clotting proteins | Increased platelet adhesiveness
34
Estrogen Functions: On metabolism
Liver (clotting factors and hormone binding proteins: SHBG, CBG, TBG) Increased HDL Decreased LDL Na+ and H2O retention
35
How are exogenous estrogens administered?
Naturally occurring estrogens are not orally active, so oral forms have been developed Ethnyl estradiol —> synthetic used in oral contraceptives Conjugated estrogens (Premarin) —> HRT Estradiol (Estraderm) —> creams/patches
36
What are exogenous estrogens used for?
Oral contraception Postmenopausal hormone replacement therapy (HRT) Stimulating pubertal development in hypogonadic girls Decreased uterine bleeding Suppressing ovulation in dysmenorrhea
37
What are the adverse effects of estrogen use?
Endometrial hyperplasia*** Nausea and breast tenderness Migraines*** Gallbladder disease*** HTN*** THROMBOEMBOLISM********* Thrombophlebitis, increased platelet aggregation, accelerated blood clotting
38
Contraindications for estrogen use
ESTROGEN-DEPENDENT NEOPLASMS THROMBOEMBOLIC DISORDERS Undiagnosed genital bleeding Uncontrolled HTN Liver disease Smoking and over 35 Pregnancy
39
MOA for Clomiphene (Clomid)
SERM Antagonizes negative feedback of estrogen in hypothalamus Used in initial infertility therapy - stimulates LH/FSH, inducing ovulation
40
Main side effect of Clomiphene (Clomid)
MULTIPLE PREGNANCIES
41
DOC for initial treatment of infertility in women
Clomiphene (Clomid)
42
How is Fulvestrant (Faslodex) used?
Full estrogen receptor antagonist (Antiestrogen) Used to treat estrogen-dependent breast cancer
43
DOC for breast cancer in premenopausal women?
Tamoxifen (Novaldex)
44
Where are SERMs?
Selective Estrogen Receptor Modulators Tamoxifen Clomiphene Raloxifene Toremifene
45
How does Tamoxifen (Novaldex) work?
Selective estrogen receptor modulator (SERM) As an antagonist: • Used as palliative and prophylactic tx for BC in PREmenopausal women - reduces risk of further BC As an agonist: • Limits bone loss • May increase risk of uterine cancer May also decrease HDL (but Toremifene better for this)
46
What makes Raloxifene different from other SERMs?
Is better antiestrogen for those with osteoporosis Not as likely to cause uterine cancer as tamoxifen
47
Which SERM is the best for maintaining HDL?
Toremifene
48
MOA for Aromatase Inhibitors
Block production of estrogens but do not inhibit other steroid synthesis Anastrozole (Arimidex) Letrozole (Femara) Exemestane (Aromasin)
49
What are the indications for aromatase inhibitors
DOC for breast cancer in postmenopausal women Advanced BC after tamoxifen failure
50
Adverse effects of aromatase inhibitors
Diarrhea, abdominal pain, N/V, HOT FLASHES, joint pain
51
Contraindications for aromatase inhibitors
PREmenopausal women Pregnancy Cat X - known teratogen, MUST NOT be prescribed
52
What are the biological functions of progesterone?
Converts endometrium to a secretory state —> maintains pregnancy, suppresses contractility during pregnancy Regulates cervical mucus Lobuloalveolvar development at the end of the mammary ducts during pregnancy and puberty Increases body temperature
53
Similar to estrogens, progesterone is not _______ so different formulations are used
Not orally active
54
What are the different types of progestins used?
19-nortestosterones - have both progestin and androgenic activity Progresterone derivatives - have varying levels of androgen activity
55
Uses for progestins
Contraception - with estrogen or alone Prevent endometrial hyperplasia in HRT Treatment of other problems when estrogens are contraindicated
56
Adverse effects of progestins
Possible increase in BP High doses may reduce plasma HDL levels (19-nortestosterones) Depression and drowsiness
57
What are the two antiprogestins?
Mifepristone (RU 486, Mifeprix) Danazol (Danocrine)
58
Progesterone/glucocorticoid receptor antagonist used to terminate pregnancy (w/ prostaglandins) and prevent implantation
Mifepristone (RU 486, Mifeprix)
59
Side effects of Mifepristone
Vomiting, diarrhea, abdominal or pelvic pain, and vaginal bleeding
60
Weak progestin and androgen used to suppress ovarian function in the treatment of endometriosis
Danazol (Danocrine)
61
What are the side effects of Danazol?
``` Weight gain Edema Acne and oily skin Hirsutism Deepening voice HA Flush Libido changes Cramps ```
62
What do we need to know about oral contraceptives?
1. They work by suppressing ovulation (no LH surge)*** 2. Common side effects 3. That they are combo pills
63
How do combination oral contraceptives work
Inhibit ovulation (no LH surge)**** Change cervical mucus (block sperm) Change endometrium (decrease implantation) Progestin withdrawal initiates bleeding at the end of the cycle
64
Most commonly used estrogen in combination oral contraceptives
Ethinyl estradiol or mestranol
65
Most commonly used progestin in combination oral contraceptives
Levonorgestrel or norethindrone
66
Why did original combo oral contraceptives have many side effects?
High amounts of estrogen - now we use a lot less
67
______ is more important that the amount of estrogen in oral contraceptives
The Estrogen/Progestin ratio
68
Newer combo pills that provide longer cycle times or no cycle at all
Seasonale (84 on, 7 off - combo pill) Seasonique (84 on, 7 off - estrogen only) Lybrel - always on pill
69
Downsides of the newer, longer cycle COCs?
Increased breakthrough bleeding (esp during first year) | Hard to tell if you are pregnant
70
What is special about Yasmin/Yaz?
Uses ethinyl estradiol and DROSPIRENONE (a mineralcorticoid antagonist) Less water retention (FDA approved for PMDD) Very little or anti-androgenic properties
71
What is special about Natazia
Bioidentical hormones (uses dienogest as progestin)
72
What’s in the NuvaRing?
Etonogesterel and ethinyl estradiol
73
Common side effects of COCs
Weight gain Nausea Edema Depression Breakthrough bleeding (esp if progestin alone or two little estrogen)
74
High-dose, levonorgestrel-only pill taken within 72 hours of intercourse
Plan B Preven is similar but also has ethinyl estradiol Can also take multiple regular COCs
75
How can mifepristone be used for post-coital contraception?
Can be used to prevent implantation if administered within 72 hours after intercourse
76
More serious adverse effects of COCs
Cardiovascular problems (inc clotting, esp in women over 35 and smokers; mild HTN; migraine; MI/Stroke) Cholestatic jaundice and gallbladder disease Teratogenesis Fertility can be suppressed for 3+ months
77
What are the benefits of COCs?
``` Reduced risk for: Ovarian and endometrial cancer Ovarian cysts Benign breast disease Ectopic pregnancy Iron deficiency, RA, PMS ```
78
Absolute contraindications for COCs
``` Thromboembolic phenomena Thrombophlebitis Cerebrovascular disorders Estrogen-dependent neoplasms Pregnancy ```
79
Relative contraindications to COCs
``` Liver disease Adolescents prior to epiphyseal closure Asthma, eczema Migraine, HTN DM Optic neuritis, retrobulbar neuritis Seizure disorders Smoking and >35 years old ```
80
What drugs can reduce the effectiveness of COCs?
P450 inducers (phenytoin, rifampin, carbamazepine) Antibiotics (decreases enterohepatic circulation)
81
COCs decrease the effectiveness of what key medication?
WARFARIN ``` Also: Anticoagulants Anticonvulsants Tricyclic antidepressants Guanethidine Oral hypoglycemics ```
82
Menopausal symptoms
Vasomotor problems: HA, palpitations, night sweats, insomnia, HOT FLASHES*** Genito-urinary problems: vaginal dryness, atrophy, pain Osteoporosis: decrease in bone mass Heart disease
83
Adverse effects of HRT
Endometrial cancers (progestins reduce) Breast cancer - small risk Gallbladder disease Cardiovascular
84
General guidelines for HRT
< 10 years after menopause = HRT has more benefits than risk > 10 years after menopause = HRT is not so great
85
What are the virilizing (androgenic) effects of androgens?
Spermatogenesis | Sexual development
86
What are the anabolic effects of androgens?
Increased bone density Increased amino acid incorporation into muscle Increased red blood cell mass Antagonize catabolic effects of glucocorticoids
87
During puberty, _______ are responsible for the development of secondary sexual characteristics in males
Androgens
88
What are the two androgen drugs?
Testosterone (injection) Methyltestosterone (oral)
89
How are androgens used in men v women
Men - testicular deficiency Women - female hypopituitarism (estrogens and androgens) Both sexes - hypoproteinemia of nephrosis, negative nitrogen balance patients (BURNS*******)
90
Side effects of androgens
Men - decreased spermatogenesis, may exacerbate prostate cancer Women - masculinization, pseudohermaphrodism of fetus Both sexes - baldness, oily skin, acne, fluid retention, edema, decreased HDL, increased LDL, psychological changes
91
What are the two androgen receptor antagonists?
Flutamide (Eulexin) • Androgen receptor antagonist • Used is PROSTATE CANCER w/ long-acting GnRH agonist • Hepatotoxic Spironolactone • Mineralocorticoid antagonist • High doses—>antiandrogen • Used for Hirsutism and PMS in women and for precocious puberty
92
What are the 5a-Reductase Inhibitors
Finasteride (Propecia) and Dutasteride (Avodart) Inhibit 5a-reductase —> no DHT Suppresses male sex accessory organs WITHOUT AFFECTING LIBIDO
93
What are 5a-Reductase inhibitors used for?
BPH Male pattern baldness Can cause gynecomastia and ED and are teratogenic

Pharm II Unit III (4 decks)

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