Progestins, estrogens & androgens Flashcards

1
Q

Role of FSH

A

stimulate estrogens and follicular growth

-always inhibitory to Pit/Hypothalamus

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2
Q

Role of LH

A

stimulate ovulation, progesterone

-inhibitory early, stimulatory mid-cycle

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3
Q

aromatase enzyme

A

present in granulosa cells of ovaries

  • synthesizes estradiol and estrone from testosterone and androstenedione
  • also called CYP19A1
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4
Q

estrogens: main and action

A
  • estradiol-17B
    actions: stim growth and dev of the mammary gland
  • promote endometrial proliferation during follicular phase
  • promote proliferation of the vag epithelium
  • block reabsorption of bone
  • increase HDL and decrease LDL
  • increase risk of thromboembolism
  • increase incidence of endometrial/breast ca
  • increase progesterone receptors
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5
Q

progestins: main and actions

A
  • progesterone
  • promotes endometrial dev during luteal phase
  • main determinant of the onset of menstration
  • decreases amt of cervical mucus and increases viscosity
  • increases body temp
  • stim growth and dev of mammary gland during pregnancy
  • uterine effects are essential for maintenance of preg
  • weak mineralocortiocoid antagonist
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6
Q

general properties of estrogens and progestins

A

progesterone and estradiol are rapidly inactivated when taken orally

  • synthetic analogs are more useful but then cross-rxn with other steroid receptors and act as agonists or antagonists
  • many routes
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7
Q

drospirenone

A

-progesterone analog with increased activity as MC antagonist and androgen antagonist

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8
Q

ulipristal

A
  • selective progesterone receptor modulator (SPRM)
  • postcoital contraceptive
  • more effective than norgestrel and maintains efficacy longer
  • can be agonist or antagonist, dep on tissue
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9
Q

diethylstilbestrol (DES)

A

-non-steroidal estrogen, 1st

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10
Q

Hormones that can be used for contraception

A

-P, E, SPRM

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11
Q

Hormones that can be used for suppression of the hypothalamic-pituitary gonadal axis

A

P, E

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12
Q

hormones that can be used for hormone replacement therapy

A

P, E, SERM

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13
Q

hormones that can be used for abortion

A

P antagonists

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14
Q

hormones that can be used for ovulation induction

A

E antagonists, aromatase inhibitors

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15
Q

hormones that can be used for breast ca therapy

A

SERM, aromatase inhibitors

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16
Q

copper IUD

A
  • among the most effective methods of contraception
  • copper is spermicidal
  • in theory, could prevent implantation, but fertilization would have had to occurred prior to insertion
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17
Q

norethrindrone

A

a progesterone analog

  • used as an oral contraceptive agent
  • also present in IUD
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18
Q

medroxyprogesterone acetate

A

Depo-provera

  • IM injection q 3 mo
  • progesterone analog used as contraception
  • decreased bone density
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19
Q

norgestrel

A

-progestin analog
-present in IUD
-present in post coital contraceptives (plan B)
(higher dose than routine contraception, prevents ovulation)

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20
Q

progestin analog MOA

A
  • prevent fertilization by decreasing amount and increasing the viscosity of cervical mucous
  • prevent ovulation by inhibiting gonadotropin secretion
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21
Q

progestin analog SE

A
  • h/a

- abnormal bleeding

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22
Q

progestins and estrogens as contraceptive agents

A

-oral
21 on, 7 off
-usually contain norethindrone and ethinyl estradiol
-monophasic (constant E & P for 21 days)
-biphasic (constant E for 21 days, progesterone low for 1-10, increased 11-21)
-triphasic (constant E 21 days, low P 1-7, increased 7-14, increased again 15-21)

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23
Q

drospirenone/ethinyl estradiol

A

oral drug

  • Yaz
  • can prevent acne?
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24
Q

MOA of P& E combos

A
  • P and E prevent ovulation by inhibiting the hypothalamus and pituitary
  • no change in LH/FSH
  • progestins prevent fertilization by decreasing the amount and increasing the viscosity of cervical mucus
25
Q

P & E combos

SE

A
  • nausea, h/a
  • not recommended for migraines
  • CV effects like thromboembolism and MI, mostly smokers and those 35 yo and older
  • decreased glucose tolerance, (weight gain, acne, hirsutism d/t androgen activity)
26
Q

health benefits of P & E combos

A
  • decreased ovarian cysts and benign fibrocystic breast disease
  • decreased endometrial and ovarian ca
  • increased HDL and LDL
27
Q

which drugs reduce efficacy of contraceptives

A
  • rifampin antibiotics

- some anticonvulsants

28
Q

MOA for postcoital contraceptive

A
  • suppresses hypothalamic-pituitary-gonadal axis and inhibits ovulation
  • may prevent implantation and promote bleeding
29
Q

SE for postcoital contraceptives

A

N/V

  • h/a
  • dizziness
  • breast tenderness
  • leg cramping
30
Q

MOA of ulipristal as post coital

A
  • inhibits ovulation by antagonizing actions of progesterone on the granulosa cell progesterone receptor, needed for follicular rupture
  • also a progesterone agonist in the HP axis and delays LH surge
  • need rx
31
Q

other uses for progestins

A

-suppress HPG axis in rx of dysmenorrhea, endometriosis

32
Q

other uses for P/E combos

A
  • replacement therapy in ovarian dysfunction

- replacement in postmenopause and postmenopausal osteoporosis

33
Q

clomiphene/fulvestrant

A

antagonist of estrogen receptors

  • all antagonists
  • induction of ovulation. when given in the early follicular phase of the menstral cycle, they antagonize the inhibitory effects of estrogen on the pituitary and hypothalamus
34
Q

tamoxifen

A

SERM, antagonist at breast

-used for relief of post menopausal symptoms, rx osteoporosis, estrogen-dep breast ca.

35
Q

raloxifene

A

SERM, antagonist at breast. neutral at endometrium and vag

-used for relief of post menopausal symptoms, rx osteoporosis, estrogen-dep breast ca.

36
Q

ospemifene

A

SERM, antagonist at breast, neutral and endometrium

-recently approved for rx of vag atrophy in post-menopausal women,

37
Q

bazedoxifene

A

SERM, antagonist at breast, endometrium. neutral to CV system.
-with conjugated estrogens, approved for rx of postmenopausal symptoms. takes advantage of agonist on bone and antagonist on breast and endometrium

38
Q

anastrazole

A
  • aromatase inhibitors
  • inhibit conversion of androgens to estrogens
  • oral
  • useful in the rx of breast ca or other d/o where estrogen action needs to be inhibited
  • only post menopausal women
  • can also induce ovulation
39
Q

exemestane

A
  • aromatase inhibitors
  • inhibit conversion of androgens to estrogens
  • oral
  • useful in the rx of breast ca or other d/o where estrogen action needs to be inhibited
  • only post menopausal women
  • can also induce ovulation
40
Q

SE of aromatase inhibitors

A

arthralgia, hot flashes, post menopausal symptoms

41
Q

mifepristone/RU 486

A

oral progesterone receptor antagonist

  • used for abortions and post coital contraception: antagonizes progesterone actions everywhere
  • GC antagonist and can be used in rx of cushings/dm II
42
Q

role of aromatase in males

A

converts testosterone to estradiol

43
Q

how do males produce dihydrotestosterone

A

-5 a reductase (SRD5A2)

44
Q

actions of androgens

A
  • virilization of the urogenital tract during dev
  • puberty
  • maintenance of secondary sexual characteristics and accessory organs
  • essential for spermatogenesis
  • promote anabolic reactions
45
Q

testosterone oral/transdermal vs IM

A

-esters must be given IM

46
Q

which androgens have increased SE

A
  • 17A alkylated androgens (such as danazol, methyltestosterone)
  • more SE, includes hepatic toxicity
47
Q

uses of androgen therapy

A
  • replacement therapy in male hypogonadism

- rx of some catabolic stats such as muscle wasting in AIDS

48
Q

SE of androgen therapy

A
  • virilization for pre-pubertal males
  • feminization of males bc precursors to androgens
  • azoospermia and decreased testicular size (bc decreased FSH)
  • edema, jaundice, hepatic ca (exacerbated by 17alpha agents)
49
Q

finasteride

A
  • 5alpha reductase inhibitor used to treat syndromes of androgen excess or androgen dependent d/o: BPH, prostate ca, hirsutism, congenital adrenal hyperplasia, precocious puberty
  • may cause persistent sexual dysfunction
50
Q

dutasteride

A
  • 5alpha reductase inhibitor used to treat syndromes of androgen excess or androgen dependent d/o: BPH, prostate ca, hirsutism, congenital adrenal hyperplasia, precocious puberty
  • may cause persistent sexual dysfunction
51
Q

flutamide

A

androgen receptor antagonist used to treat syndromes of androgen excess or androgen dependent d/o: BPH, prostate ca, hirsutism, congenital adrenal hyperplasia, precocious puberty

52
Q

bicalutamide

A

androgen receptor antagonist used to treat syndromes of androgen excess or androgen dependent d/o: BPH, prostate ca, hirsutism, congenital adrenal hyperplasia, precocious puberty

53
Q

nilutamide

A

androgen receptor antagonist used to treat syndromes of androgen excess or androgen dependent d/o: BPH, prostate ca, hirsutism, congenital adrenal hyperplasia, precocious puberty

54
Q

LH and CG as diagnostic agents

A

LH: ovulation
CG: pregnancy

55
Q

FSH as therapeutic agents

A

-induce follicular growth. IM

56
Q

CG as therapeutic agent

A

-induce ovulation, IM inj

57
Q

gonadorelin

A
  • synthetic GnRH, wild-type
  • stim gonadotropin secretion. for ex, delayed puberty in boyd and girls, anovulatory d/o in women
  • admin single injection or in pulsatile (stimulatory)
58
Q

cetrorelix

A

GnRH antagonist

  • rx of precocious puberty in boys and excess androgens
  • rx endometriosis and dysmenorrhea
  • stop gonadotropin secretion in ovulation-induction protocols
59
Q

luprolide

A
  • long acting GnRH agonist
  • after initial stimulation of gonadotropin secretion, suppresses it
  • used to suppress gonadotropin secretion like antagonist