Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm II Unit III > 1 Sex Hormones > Flashcards

1 Sex Hormones Flashcards

1
Q

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

A

Suppress gonadotropin (FSH/LH) release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What drugs are the long-acting GnRH agonists?

A

Leuprolide (Lupron)

Goserelin (Zoladex)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

MOA for Long-Acting GnRH agonists

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

GnRH antagonists

A

Cetrorelix (Cetrotide)

Ganirelix (Antagon)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

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

A

Menopausal symptoms

Testicular atrophy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

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

A

FSH

—> increased estrogen
—> endometrial development and thickening

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

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

A

Estrogen
LH release

LH surge —> ovulation —> Luteinization

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

How does menstruation occur?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Role of FSH in Women and Men

A

Women: develops overian follicles and supports estrogen synthesis

Men: stimulates spermatogenesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is Urofollitropin (uFSH, Bravelle)?

A

purified FSH

no longer on the market

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Contraindications for the use of gonadotropins

A

Sex steroid-dependent cancers

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What are the different endogenous estrogens?

A

Estradiol
Estriol
Estrone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

How do estrogens work?

A

Upon nuclear receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

How are estrogens metabolized?

A

Conjugated by the liver and excreted in bile

Enterohepatic circulation reverses conjugation and increases bioavailability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Estrogen Functions:

On the ovaries

A

Prepare for ovulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Estrogen Functions:

On the uterus

A

Endometrial growth

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Estrogen Functions:

On vaginal epithelium

A

Proliferation, maintenance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Estrogen Functions:

On endocervical glands

A

Mucus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Estrogen Functions:

On breasts

A

Growth during pregnancy and puberty

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Estrogen Functions:

On puberty

A

Growth and maturation, closes epiphyses

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Estrogen Functions:

On bones

A

Maintenance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Estrogen Functions:

On blood clotting

A

Increased synthesis of clotting proteins

Increased platelet adhesiveness

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

Estrogen Functions:

On metabolism

A

Liver (clotting factors and hormone binding proteins: SHBG, CBG, TBG)
Increased HDL
Decreased LDL
Na+ and H2O retention

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

How are exogenous estrogens administered?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

What are exogenous estrogens used for?

A

Oral contraception

Postmenopausal hormone replacement therapy (HRT)

Stimulating pubertal development in hypogonadic girls

Decreased uterine bleeding

Suppressing ovulation in dysmenorrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

What are the adverse effects of estrogen use?

A

Endometrial hyperplasia***

Nausea and breast tenderness

Migraines***

Gallbladder disease***

HTN***

THROMBOEMBOLISM*******
Thrombophlebitis, increased platelet aggregation, accelerated blood clotting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

Contraindications for estrogen use

A

ESTROGEN-DEPENDENT NEOPLASMS

THROMBOEMBOLIC DISORDERS

Undiagnosed genital bleeding

Uncontrolled HTN

Liver disease

Smoking and over 35

Pregnancy

39
Q

MOA for Clomiphene (Clomid)

A

SERM

Antagonizes negative feedback of estrogen in hypothalamus

Used in initial infertility therapy - stimulates LH/FSH, inducing ovulation

40
Q

Main side effect of Clomiphene (Clomid)

A

MULTIPLE PREGNANCIES

41
Q

DOC for initial treatment of infertility in women

A

Clomiphene (Clomid)

42
Q

How is Fulvestrant (Faslodex) used?

A

Full estrogen receptor antagonist (Antiestrogen)

Used to treat estrogen-dependent breast cancer

43
Q

DOC for breast cancer in premenopausal women?

A

Tamoxifen (Novaldex)

44
Q

Where are SERMs?

A

Selective Estrogen Receptor Modulators

Tamoxifen
Clomiphene
Raloxifene
Toremifene

45
Q

How does Tamoxifen (Novaldex) work?

A

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
Q

What makes Raloxifene different from other SERMs?

A

Is better antiestrogen for those with osteoporosis

Not as likely to cause uterine cancer as tamoxifen

47
Q

Which SERM is the best for maintaining HDL?

A

Toremifene

48
Q

MOA for Aromatase Inhibitors

A

Block production of estrogens but do not inhibit other steroid synthesis

Anastrozole (Arimidex)
Letrozole (Femara)
Exemestane (Aromasin)

49
Q

What are the indications for aromatase inhibitors

A

DOC for breast cancer in postmenopausal women

Advanced BC after tamoxifen failure

50
Q

Adverse effects of aromatase inhibitors

A

Diarrhea, abdominal pain, N/V, HOT FLASHES, joint pain

51
Q

Contraindications for aromatase inhibitors

A

PREmenopausal women

Pregnancy Cat X - known teratogen, MUST NOT be prescribed

52
Q

What are the biological functions of progesterone?

A

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
Q

Similar to estrogens, progesterone is not _______ so different formulations are used

A

Not orally active

54
Q

What are the different types of progestins used?

A

19-nortestosterones - have both progestin and androgenic activity

Progresterone derivatives - have varying levels of androgen activity

55
Q

Uses for progestins

A

Contraception - with estrogen or alone

Prevent endometrial hyperplasia in HRT

Treatment of other problems when estrogens are contraindicated

56
Q

Adverse effects of progestins

A

Possible increase in BP

High doses may reduce plasma HDL levels (19-nortestosterones)

Depression and drowsiness

57
Q

What are the two antiprogestins?

A

Mifepristone (RU 486, Mifeprix)

Danazol (Danocrine)

58
Q

Progesterone/glucocorticoid receptor antagonist used to terminate pregnancy (w/ prostaglandins) and prevent implantation

A

Mifepristone (RU 486, Mifeprix)

59
Q

Side effects of Mifepristone

A

Vomiting, diarrhea, abdominal or pelvic pain, and vaginal bleeding

60
Q

Weak progestin and androgen used to suppress ovarian function in the treatment of endometriosis

A

Danazol (Danocrine)

61
Q

What are the side effects of Danazol?

A 
Weight gain
Edema
Acne and oily skin
Hirsutism
Deepening voice
HA
Flush
Libido changes
Cramps
62
Q

What do we need to know about oral contraceptives?

A
  1. They work by suppressing ovulation (no LH surge)***
  2. Common side effects
  3. That they are combo pills
63
Q

How do combination oral contraceptives work

A

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
Q

Most commonly used estrogen in combination oral contraceptives

A

Ethinyl estradiol or mestranol

65
Q

Most commonly used progestin in combination oral contraceptives

A

Levonorgestrel or norethindrone

66
Q

Why did original combo oral contraceptives have many side effects?

A

High amounts of estrogen - now we use a lot less

67
Q

______ is more important that the amount of estrogen in oral contraceptives

A

The Estrogen/Progestin ratio

68
Q

Newer combo pills that provide longer cycle times or no cycle at all

A

Seasonale (84 on, 7 off - combo pill)

Seasonique (84 on, 7 off - estrogen only)

Lybrel - always on pill

69
Q

Downsides of the newer, longer cycle COCs?

A

Increased breakthrough bleeding (esp during first year)

Hard to tell if you are pregnant

70
Q

What is special about Yasmin/Yaz?

A

Uses ethinyl estradiol and DROSPIRENONE (a mineralcorticoid antagonist)

Less water retention (FDA approved for PMDD)

Very little or anti-androgenic properties

71
Q

What is special about Natazia

A

Bioidentical hormones (uses dienogest as progestin)

72
Q

What’s in the NuvaRing?

A

Etonogesterel and ethinyl estradiol

73
Q

Common side effects of COCs

A

Weight gain
Nausea
Edema
Depression

Breakthrough bleeding (esp if progestin alone or two little estrogen)

74
Q

High-dose, levonorgestrel-only pill taken within 72 hours of intercourse

A

Plan B

Preven is similar but also has ethinyl estradiol

Can also take multiple regular COCs

75
Q

How can mifepristone be used for post-coital contraception?

A

Can be used to prevent implantation if administered within 72 hours after intercourse

76
Q

More serious adverse effects of COCs

A

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
Q

What are the benefits of COCs?

A 
Reduced risk for:
Ovarian and endometrial cancer
Ovarian cysts
Benign breast disease
Ectopic pregnancy
Iron deficiency, RA, PMS
78
Q

Absolute contraindications for COCs

A 
Thromboembolic phenomena
Thrombophlebitis
Cerebrovascular disorders
Estrogen-dependent neoplasms
Pregnancy
79
Q

Relative contraindications to COCs

A 
Liver disease
Adolescents prior to epiphyseal closure
Asthma, eczema
Migraine, HTN
DM
Optic neuritis, retrobulbar neuritis
Seizure disorders
Smoking and >35 years old
80
Q

What drugs can reduce the effectiveness of COCs?

A

P450 inducers (phenytoin, rifampin, carbamazepine)

Antibiotics (decreases enterohepatic circulation)

81
Q

COCs decrease the effectiveness of what key medication?

A

WARFARIN

Also:
Anticoagulants
Anticonvulsants
Tricyclic antidepressants
Guanethidine
Oral hypoglycemics
82
Q

Menopausal symptoms

A

Vasomotor problems: HA, palpitations, night sweats, insomnia, HOT FLASHES***

Genito-urinary problems: vaginal dryness, atrophy, pain

Osteoporosis: decrease in bone mass

Heart disease

83
Q

Adverse effects of HRT

A

Endometrial cancers (progestins reduce)

Breast cancer - small risk

Gallbladder disease

Cardiovascular

84
Q

General guidelines for HRT

A

< 10 years after menopause = HRT has more benefits than risk

> 10 years after menopause = HRT is not so great

85
Q

What are the virilizing (androgenic) effects of androgens?

A

Spermatogenesis

Sexual development

86
Q

What are the anabolic effects of androgens?

A

Increased bone density
Increased amino acid incorporation into muscle
Increased red blood cell mass
Antagonize catabolic effects of glucocorticoids

87
Q

During puberty, _______ are responsible for the development of secondary sexual characteristics in males

A

Androgens

88
Q

What are the two androgen drugs?

A

Testosterone (injection)

Methyltestosterone (oral)

89
Q

How are androgens used in men v women

A

Men - testicular deficiency

Women - female hypopituitarism (estrogens and androgens)

Both sexes - hypoproteinemia of nephrosis, negative nitrogen balance patients (BURNS***)

90
Q

Side effects of androgens

A

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
Q

What are the two androgen receptor antagonists?

A

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
Q

What are the 5a-Reductase Inhibitors

A

Finasteride (Propecia) and Dutasteride (Avodart)

Inhibit 5a-reductase —> no DHT

Suppresses male sex accessory organs WITHOUT AFFECTING LIBIDO

93
Q

What are 5a-Reductase inhibitors used for?

A

BPH
Male pattern baldness

Can cause gynecomastia and ED and are teratogenic

Pharm II Unit III (4 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions