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Pharm > Sex Steroids and HRT > Flashcards

Sex Steroids and HRT Flashcards

1
Q

All sex hormones in humans share a common ________

A

synthetic pathway
(they are structurally related to adrenal steroids)

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2
Q

Estrogens (E) are …

A

female sex hormone, mainly E2

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3
Q

Progestins (P) are …

A

hormones that promote gestation, mainly progesterone

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4
Q

Androgens are ..

A

male sex hormones, mainly testosterone (T)

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5
Q

Native hormones have good/poor oral bioavailability?

A

POOR
(rapidly metabolized in liver)

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6
Q

Synthetic derivatives of hormones have good/poor bioavailability?

A

GOOD
(orally effective with longer DOA)

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7
Q

Active metabolites of E and T are …

A

used as drugs

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8
Q

What kind of receptors do sex hormones have?

A

nuclear transcription factor receptors
(effects by protein synthesis)
Distinct E, P and T R (response elements provide specificity)
Drugs may be agonists or antagonists of these R

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9
Q

Estrogens stimulate growth of

A

endometrium

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10
Q

Progestins inhibit

A

endometrial growth

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11
Q

Progestins maintain

A

vascular supply and secretory capacity and pregnancy

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12
Q

progesterone withdrawal leads to

A

menstruation (or absorption)

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13
Q

E and P decline markedly at menopause but are still produced at low levels by

A

non-ovarian tissues

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14
Q

Estrogen physiological effects

A
  1. sexual maturation, 2nd sex characteristics
  2. stimulation of long bone growth, closure of epiphyses
  3. decrease bone resorption throughout adulthood
  4. improves lipid profiles
  5. increase risk of blood clotting and thromboembolic diseases (stimulates liver enzymes involved in clotting)
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15
Q

Uses of Estrogen as replacement therapy

A
  1. hypogonadism/
    hypopituitarism (low dose for growth promotion, THEN higher doses for epiphyseal closure and sex dev at puberty) ** setting where estrogen alone is safe **
  2. postmenopausal or after oophorectomy (in combo w/ progestins)
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16
Q

Uses of estrogen as suppressive therapy

A
  1. birth control (in combo with progestins)
  2. menstrual disorders
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17
Q

estrogens can be used for _____ therapy and ______ therapy

A

replacement; suppressive

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18
Q

What are 3 available preparations of estrogen?

A
  1. estradiol
  2. conjugated estrogens
  3. Ethinyl estradiol (EE2)
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19
Q

Estradiol has three forms and include:

A

oral, IM, topical

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20
Q

What two things is estradiol mainly used for?

A

HRT, hypogonadism

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21
Q

Oral estradiol is orally bioavailable, rapidly absorbed and evades …

A

the extensive hepatic first pass metabolism of conventional estradiol

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22
Q

Explain estradiol IM form

A

it is a slow-release “depot” forms (FA esters) – slow release of estrogen over time

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23
Q

What are some examples of topical form of estradiol?

A

vaginal cream, transdermal patches

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24
Q

What is the main use for conjugated estrogens?

A

HRT

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25
Q

Admin of conjugated estrogens include?

A

oral, IV, IM, vaginal

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26
Q

Is conjugated estrogen a natural prep?

A

YES, it is the most common of several natural preps
(it contains conjugates of E3 active metabolites – estrone and estriol)

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27
Q

Ethinyl estradiol (EE2) is synthetic estrogen used in

A

nearly ALL oral contraceptives and HRT

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28
Q

What is the benefit of the ethinyl group in ethinyl estradiol?

A

increases oral bioavailability, slows clearance, increases potency (relative to estradiol)

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29
Q

conjugated estrogens are natural/synthetic?

A

natural

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30
Q

ethinyl estradiol is natural/synthetic?

A

synthetic

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31
Q

MC side effects of estrogen?

A

Nausea, Edema = MC
also, breast tenderness, hyperpigmentation

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32
Q

Other side effects of estrogen include:

A
  1. migraine headaches
  2. liver disease, insulin resistance
  3. increased risk of blood clotting/TE disease (mainly from higher doses)
33
Q

What is a side effect of estrogen if used in males?

A

gynecomastia, feminization

34
Q

A side effect of estrogen includes cancer risk, explain.

A

Elevated risk of endometrial hyperplasia/cancer (ONLY if estrogen is used alone). This is REDUCED by progestins – so E should NOT be used alone

35
Q

Estrogen use is contraindicated in:

A

breast cancer, or any other estrogen-responsive tumor

36
Q

Progestin uses include _____ therapy and _____ therapy

A

replacement; suppressive

37
Q

how is progestin used in replacement therapy?

A

post menopausal use with estrogens as protective factor

38
Q

how is progestin used in suppressive therapy? 3 main uses …

A
  1. birth control (either alone or in combo with E)
  2. uterine bleeding from endometrial hyperplasia
  3. endometriosis and accompanying dysmenorrhea
39
Q

What are the available preps for progestin?

A
  1. Progesterone
  2. Medroxyprogesterone acetate
  3. norethindrone
40
Q

Progesterone comes in various forms including:

A

IM, creams, suppositories, slow release from IUD, orally bioavailable micronized powder

41
Q

Medroxyprogesterone acetate is a ____ progesterone

A

synthetic

42
Q

Medroxyprogesterone acetate is structurally related to progesterone as it:

A

retains the 19-methyl group and C20-21 structure

43
Q

what kind of effects do Medroxyprogesterone acetate produce?

A

progesterone-like effects, with little/no androgen or estrogen activity

44
Q

what are the forms of Medroxyprogesterone acetate?

A

oral, IM

45
Q

Norethindrone is a prototype synthetic progestin that is structurally related to

A

testosterone (C18)
(LACKS the C20-21 structure)

46
Q

how does Norethindrone differ from testosterone?

A

it lacks the 19-methyl group
(NOR refers to)

47
Q

Norethindrone is orally effective, more progesterone-like with decreased androgen activity …

A

compared to others in this class that have more androgen-like effects

48
Q

adverse effects of all progestins include:

A

menstrual changes
nausea
bloating
potenital teratogen

49
Q

what are the side effects of nor-progestins, androgenic?

A

acne
weight gain
masculinization
altered libido
worsened lipid profile

50
Q

Postmenopausal HRT may be used for …

A
  1. short-term use
  2. longer-term use
51
Q

Use of short-term postmenopausal HRT …

A

alleviated symptoms at onset of menopause

52
Q

What symptoms (that occur with menopause onset) can be alleviated with short-term use of postmenopausal HRT?

A
  1. vasomotor - hot flashes, sweating, palpitations
  2. urogenital atrophy -incontinence, painful intercourse, UTIs
  3. psychological -mood changes, depression, loss of libido
53
Q

Use of longer-term postmenopausal HRT

A

to prevent/treat osteoporosis-related increased risk of fractures (suppression of RANK-L)

54
Q

Estrogen/progestin combos may be continuous or cyclic for postmenopausal HRT and include:

A
  1. conjugated estrogens + medroxyprogesterone = MC
  2. ethinyl estradiol + norethindrone = synthetic agents
55
Q

when can estrogen be used alone for postmenopausal HRT?

A

if uterus has been removed

56
Q

Side effects of HRT include:

A
  1. return of menstrual bleeding, breast swelling and tenderness
  2. increased cancer and CV disease risk
57
Q

how are the side effects of HRT mitigated?

A

via local admin (vaginal)

58
Q

benefits of long-term HRT include:

A
  1. reduce risk of osteoporosis/hip fx
  2. reduction of colorectal cancer risk
  3. protect from Alzheimer’s disease risk
59
Q

risk of long-term HRT

A
  1. E+P increased risk of heart disease, strokes, PE -reverse when HRT is d/c
  2. E increases risk of endometrial cancer (adding progestin reduces this risk)
  3. E+ P increased breast cancer risk
60
Q

recommendations for HRT

A
  1. short-term use <5 years of E+P for menopause onset symptoms is probably safe but consider pt history
  2. NOT recommended for long-term use, especially in older women
61
Q

SERMs =

A

selective estrogen response modifiers

62
Q

are SERMS orally effective?

A

yes

63
Q

are SERMs non-steroidal analogs?

A

yes

64
Q

SERMs have mixed ..

A

agonist-antagonist properties on estrogen receptors

65
Q

each SERM drug stabilizes

A

a different receptor conformation (which can yield estrogen AGONIST effects in some tissues and estrogen ANTAGONIST effects in others)

66
Q

SERM prototypes include:

A

raloxifene, tamoxifen

67
Q

the main uses of protoype SERMs include

A

osteoporosis
breast cancer tx and prevention

68
Q

newer SERMS are used for

A

treating postmenopausal dyspareunia and hot flashes

69
Q

Raloxifene uses:

A
  1. tx of postmenopausal osteoporosis, improves lipid profiles
  2. for prevention of breast cancer
70
Q

Raloxifene LACKS the following cancer risks

A

lacks uterine cancer risk (as seen w/ estrogen and tamoxifen)

lacks breast cancer risk (as seen w/ estrogen)

71
Q

Does Raloxifene cause or relieve hot flashes? why?

A

CAUSES – due to its antagonist effects

72
Q

does Raloxifene increase or decrease clotting/thrombosis? why?

A

increases and causes leg cramps – due to its agonist effect

73
Q

Tamoxifen is used as an

A

anti-estrogen

74
Q

Tamoxifen, an anti-estrogen, treats

A

ER+ advanced/metastatic breast cancer

ALSO used for breast cancer PREVENTION

75
Q

agonist effects of tamoxifen decrease osteoporosis and heart disease risk but …

A

are not approved for these uses

76
Q

does tamoxifen increase endometrial cancer risk?

A

yes, via agonist action in the uterus

77
Q

does tamoxifen increase risk of thrombotic disease?

A

yes

78
Q

does tamoxifen cause menopausal symptoms?

A

yes

Pharm (6 decks)

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