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Pharm Exam III > Sex Hormones > Flashcards

Sex Hormones Flashcards

1
Q

Long acting GnRH agonists

A

Leuprolide

Goserelin

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2
Q

GnRH agonist drugs

A
  • Continuous administration suppresses release of LH and FSH (after initial surge)
  • used in IVF, sex steroid-dependent cancers, endometriosis, precocious puberty
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3
Q

GnRH antagonists (Cetrorelix and ganirelix)

A
  • suppress LH and FSH

- Used in IVF, sex steroid-dependent CA, endometriosis, precocious puberty

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4
Q

Long acting GnRH agonists and antagonists differences

A
  • Only 4-5 days of antagonist treatment vs. 3 weeks of agonist to suppress gonadotropins
  • No initial surge of gonadotropins in antagonist treatment
  • (agonist only) metastatic prostate CA-problems during start of treatment (use anti androgen**)
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5
Q

Long acting GnRH agonists and antagonists mutual side effects

A
  • Menopausal symptoms

- Testicular atrophy

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6
Q

Follicle stimulating hormone (FSH) use in women

A

Develops ovarian follicles and supports estrogen synthesis

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7
Q

FSH use in men

A

Stimulates spermatogenesis

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8
Q

Human menopausal gonadotropins (hMG)

A

FSH & LH (aka menotropins)

-Used for FSH

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9
Q

Urofollitropin (uFSH, Bravelle)

A

Purified FSH

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10
Q

Luteinizing hormone (LH)

A
  • Stimulates ovulation
  • Stimulates luteinization of follicles
  • Steroid production (women=progesterone synthesis; men=testosterone synthesis)
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11
Q

hCG (Pregnyl)

A

Used instead of LH, has same actions

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12
Q

Use of gonadotropins-general

A

Reversing infertility

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13
Q

Use for gonadotropins-men

A
  • Inducing spermatogenesis
  • LH increases testosterone (for up to a year)
  • FSH then induces spermatogenesis (takes months)
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14
Q

Use for gonadotropins-women

A
  • IVF (ART)

- FSH (9-12 days) stimulates ovaries and estrogen production, single dose of LH give to induce ovulation

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15
Q

Side effects of gonadotropins

A
  • Uncomplicated ovarian enlargement
  • Ovarian hyperstimulation syndrome**
  • Multiple births (20%)**
  • Gynecomastia**

(HA, depression, edema,, precocious puberty)

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16
Q

Gonadotropins contraindications

A

Sex steroid-dependent CA

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17
Q

Estrogens major endogenous ones

A
  • Estradiol
  • Estriol
  • Estrone
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18
Q

Estrogens mechanism

A

Nuclear receptors

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19
Q

Estrogens Metabolism

A
  • Conjugated by liver (excreted in bile)

- Enterohepatic circulation (reverses conjugation, increases bioavailability)

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20
Q

Estrogen function-ovary

A

prepare for ovulation

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21
Q

Estrogen function-uterus

A

endometrial growth

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22
Q

Estrogen function-Vaginal epithelium

A

Proliferation, maintenance

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23
Q

Estrogen function-endocervical glands

A

Mucous

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24
Q

Estrogen function-breasts

A

growth (pregnancy and puberty)

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25
Q

Estrogen function-puberty

A

Growth and maturation, closes epiphyses

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26
Q

Estrogen function-Bone

A

maintenance

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27
Q

Estrogen function-blood clotting

A

Synthesis of clotting proteins, increases platelet adhesiveness

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28
Q

Estrogen function-metabolic

A
  • Liver (clotting factors and hormone binding proteins: SHBG, CBG, TB)
  • Increases HDL and decreases LDL
  • Na and H2O retention
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29
Q

Exogenous estrogens

A
  • Naturally occurring estrogens are not orally active, so oral forms have been developed
  • Synthetic–>oral contraceptives
  • Conjugated–>HRT
  • Estradiol—>creams/patches
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30
Q

Exogenous estrogens-uses

A
  • Oral contraception**
  • Postmenopausal hormone replacement therapy (HRT)
  • Stimulating pubertal development in hypogonadic girls**
  • Decrease uterine bleeding
  • Suppressing ovulation in dysmenorrhea
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31
Q

Estrogen adverse effects

A
  • Endometrial hyperplasia
  • Nausea and breast tenderness
  • Migraines**
  • Gallbladder disease
  • HTN
  • Thromboembolism, thrombophlebitis; increased platelet aggregation; accelerated blood clotting
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32
Q

Estrogens contraindications

A
  • Estrogen dependent neoplasms (ex: breast CA)**
  • Undiagnosed genital bleeding
  • Uncontrolled HTN
  • Liver disease
  • Thromboembolic disorders**
  • Smoking AND over 35
  • pregnancy
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33
Q

Antiestrogens (Tamoxifen [Novaldex])

A
  • selective estrogen receptor modulator (SERM)

- Might decrease HDL-Toremifene (Fareston) is better for this

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34
Q

Tamoxifen-antagonist

A
  • Breast: used as palliative and prophylactic treatment in breast CA (reduces risk of further breast CA)
  • DOC in premenopausal women
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35
Q

Tamoxifen-agonist

A
  • Bone: limits bone loss
  • Uterus: May increase risk of uterine CA
  • Raloxifene (Evista) is better for this –> for osteoporosis
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36
Q

Antiestrogens (Clomiphene [Clomid])

A
  • SERM
  • Antagonizes negative feedback of estrogen in hypothalamus**
  • Stimulates LH & FSH, inducing ovulation
  • Multiple pregnancies** (5-10%)
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37
Q

Antiestrogens (Fulvestrant [Faslodex])

A

Full estrogen receptor antagonist

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38
Q

Aromatase inhibitors (Anastrozole, Letrozole, and Exemastane)

A
  • Exemastane is irreversible

- Do not inhibit adrenal steroid synthesis

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39
Q

Aromatase inhibitors Indications

A
  • DOC-breast cancer treatment in postmenopausal women**

- Advanced breast cancer after tamoxifen failure in postmenopausal women

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40
Q

Aromatase inhibitors adverse effects

A
  • GI disturbances
  • Hot flashes
  • Joint pain
41
Q

Aromatase inhibitors contraindications

A
  • Premenopausal women

- Pregnancy cat X

42
Q

Progesterone

A
  • Produced by corpus luteum

- Produced by fetal/placental unit in pregnant women

43
Q

Progesterone mechanism

A

Nuclear receptor

44
Q

Progesterone biological functions-uterus

A
  • Converts endometrium to a secretory state*
  • Maintains pregnancy*
  • Suppresses contractility during pregnancy
45
Q

Progesterone biological functions-endocervical glands

A

Regulates cervical mucus

46
Q

Progesterone biological functions-breasts

A

Lobuloalveolar development at the end of the mammary ducts during pregnancy and puberty

47
Q

Progesterone biological functions-Thermogenic action

A

-Increases body temperature

48
Q

Progestins preparations

A
  • Same as estrogens, progesterone is not orally active; so different formulations
  • 19-nortestosterones (have both progestin and androgenic activity)
  • Progesterone derivatives (have varying levels of androgen activity)
49
Q

Progestins uses

A
  • Contraception**
  • Prevent endometrial hyperplasia in HRT**
  • Treatment of other problems when estrogens are contraindicated
50
Q

Progestins side effects

A
  • Possible increased BP
  • High doses may reduce plasma HDL levels (19-nortestosterones)
  • Depression and drowsiness
51
Q

Antiprogestins-Mifepristone

A

Progesterone/glucocorticoid receptor antagonist

52
Q

Mifepristone uses

A
  • Terminate pregnancy (w/prostaglandins)**

- Prevent implantation

53
Q

Mifepristone side effects

A
  • GI disturbances
  • Pelvic pain
  • Vaginal bleeding
54
Q

Antiprogestins-Danazol

A
  • Weak progestin and androgen

- Suppresses ovarian function

55
Q

Danazol uses

A

-Used to treat endometriosis**

56
Q

Danazol side effects

A
  • Weight gain
  • Edema
  • Acne and oily skin
  • Hirsutism
  • Deepening voice
  • HA
  • Flush
  • Libido changes
  • Cramps
57
Q

Contraception options

A
  • Combination pills: estrogen and progestin

- Drospirenon/ehinyl estradiol

58
Q

Combination oral contraceptives

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
59
Q

Combination oral contraceptives-estrogen

A

-Commonly ethinyl estradiol or mestranol

60
Q

Combination oral contraceptives-Progestins

A

Commonly levonorgestrel or norethindrone

61
Q

In combination oral contraceptives, what is more important?

A

Ratio is more important than amount

  • Minimal amounts**
  • Mimic normal hormonal cycle and minimize side effects**
62
Q

E:P ratio in combination oral contraceptives

A
  • Estrogen stays the same: increase progestin content at each stage
  • 1 stage–>mono phasic
  • 2 stages–>biphasic
  • 3 stages–>triphasic
63
Q

Combination oral contraceptives-Seasonale cycle

A

84 on, 7 off

64
Q

Combination oral contraceptives-Seasonique cycle

A

84 on, 7 estrogen only

65
Q

Combination oral contraceptives-Lybrel cycle

A

Always on pill

66
Q

Combination oral contraceptives-adverse effects

A
  • Increased breakthrough bleeding (especially during 1st year)
  • Hard to tell if you are pregnant
67
Q

Estradiol/drospirenone (mineralcorticoid antagonists; Yasmin, Yaz) advantages

A
  • Less water retention-FDA approved fro PMDD**

- Very little androgenic properties

68
Q

Natazia

A
  • Takes advantage of estradiol vale rate to produce E2 in vivo–>bioidentical hormones**
  • Uses dienogest as progestin, weird 4 cycle regimen
69
Q

NuvaRing

A

A vaginal ring containing a 3-week supply of etonogesterel and ethinyl estradiol

70
Q

Progestin only-mini pills

A
  • 87-98% effective for birth control**

- Used for teens and breast feeding

71
Q

Progestin only: Depo-Provera

A

3 month depot injection of medroxyprogesterone

72
Q

Progestin only: Implanon

A
  • Single silastic tube implanted in arm

- >99% effective-3 years

73
Q

Progestin only: Mirena

A
  • Intrauterine contraceptive (IUC) containing levonorgesterel
  • 99.9% effective-up to 5 years
74
Q

Post coital (emergency)-Plan B

A
  • Levonorgestrel-only pill
  • Taken within 72 hours after sex
  • Better the sooner it is taken
  • Available w/o a prescription to adults 18 years or older
75
Q

Post coital (emergency)-Preven

A

Similar to Plan B but it also has ethyinyl estradiol as well

76
Q

Post coital (emergency)-Mifepristone (RU-486, Mifeprix)

A

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

77
Q

Adverse effects of combination oral contraceptives

A
  • Common is weight gain, nausea, edema, depression
  • Breakthrough bleeding: progestin alone or too little estrogen
  • Cardiovascular problems (clotting [women over 35, smoking], mild HTN, migraine, MI/stroke)**
  • Cholestatic jaundice and gallbladder disease
  • Teratogenesis**
  • Fertility (can be suppressed for 3 months)
78
Q

Combination oral contraceptive benefits

A
  • Effective contraception
  • Reduced risk for ovarian and endometrial cancer (50% reduction even after 2 years of treatment, protection lasts 15 years after discontinuation)

(also ovarian cysts, benign breast disease, ectopic pregnancy, iron deficiency, rheumatoid arthritis, PMS, etc.)

79
Q

Combination oral contraceptive absolute contraindications

A
  • Thrombophlebitis
  • Thromboembolic phenomena**
  • Cerebrovascular disorder
  • Estrogen-dependent neoplasms**
  • Pregnancy
80
Q

Combination oral contraceptive relative contraindications

A
  • Liver disease**
  • teens prior to epiphyseal closure
  • Asthma; eczema
  • Migraine; HTN
  • Diabetes
  • Optic neuritis (retrobulbar neuritis)
  • Seizure disorders
  • Smoking and over 35 yo
81
Q

Combination oral contraceptive drug interactions

A
  • P450 inducers reduce effectiveness (phenytoin, rifampin, carbamazepine, etc.)
  • Antibiotics can reduce effectiveness (stops enterohepatic circulation)

(oral contraceptives decrease effectiveness of anticoagulants, anticonvulsants, tricyclic antidepressants, guanethidine, oral hypoglycemics)

82
Q

HRT-options/considerations

A
  • Younger patients w/HRT appear to not have as many side effects (within 10 years)
  • Hysterectomies-estrogen only**
  • Used in girls w/no ovarian development
  • Raloxifene does NOT affect CHD, but does prevent osteoporosis and breast CA , but no effect on hot flashes
83
Q

HRT-routes of administration

A
  • Creams for urogenital tract

- Transdermal good for osteoporosis w/less CHD effects

84
Q

HRT adverse effects

A
  • Endometrial CA-progestins produce
  • Breast CA-small risk**
  • Gallbladder disease
  • Cardiovascular**
85
Q

HRT advantages

A
  • Menopausal symptoms
  • Osteoporosis
  • Heart disease
86
Q

HRT concerns

A
  • Breast CA?

- Strokes

87
Q

Androgens virilizing (androgenic) effects

A
  • Spermatogenesis

- Sexual development

88
Q

Androgens anabolic effects

A
  • Increased bone density
  • Increased amino acid incorporation into muscle
  • Increased Red blood cell mass
  • Antagonize catabolic effects of glucocorticoids
89
Q

Androgens puberty effects

A

-Development of secondary sexual characteristics in males

90
Q

Androgen uses (testosterone and methyl testosterone) men

A

Testicular deficiency

91
Q

Androgen uses women

A

-Female hypopituitarism (estrogens and androgens)

92
Q

Androgen uses both sexes

A
  • Hypoproteinemia of nephrosis

- Negative nitrogen balance patients

93
Q

Androgen side effects-men

A
  • Decreased spermatogenesis

- May exacerbate prostate CA

94
Q

Androgen side effects-women

A
  • Masculinization

- Pseudohermaphroditism of fetus in pregnant women

95
Q

Androgen side effects-both sexes

A
  • Baldness
  • Fluid retention, edema
  • Oily skin, acne**
  • Decreased HDL*, increased LDL
  • Psychological changes
96
Q

Androgen receptor antagonists-Flutamide (Eulexin), others

A
  • Used in prostate CA w/long-acting GnRH agonist

- Hepatotoxic-reversible

97
Q

Androgen receptor antagonists-Spironolactone (Aldactone)

A
  • Mineralcorticoid antagonist
  • High doses antiandrogen
  • Uses: Hirsutism* and PMS in women, Precocious puberty*
98
Q

5 alpha-reductase inhibitors (Finasteride & Dutasteride)

A
  • Inhibits 5 alpha-reductase (no DHT)**
  • Suppresses male sex accessory organs w/o affecting libido
  • Uses: benign prostatic hyperplasia, male pattern baldness**
  • Teratogenic

Pharm Exam III (11 decks)

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