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IC > Gonadal Hormones > Flashcards

Gonadal Hormones Flashcards

1
Q

Hypothalamic- pituitary-gonadal axis

A

Hypothalamus secretes Gonadotropin releasing GnRH

Anterior pituitary releases gonadotropins- FSH and LH

Gonads- ovaries release estrogen and progesterone and testes release testosterone

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2
Q

GnRH

A

pulsatile release stimulates pituitary gonadotrophs to release LH and FSH

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3
Q

GnRH non pulsatile release

A

inhibits LH and FSH

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4
Q

FSH

A

spermatogenesis, follicular development

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5
Q

LH

A

steroidogenesis

testosterone secretion

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6
Q

Gonadorelin

A

synthetic GnRH
Peptide- 1/2 life 4 minutes
Must be administered parantally

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7
Q

Analogs of GnRh

A

more potent and longer acting
Leuprolide, goserelin, dafarelin (and other relins)
t1/2- 4 hrs

parenteral adminstration

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8
Q

Antagonists of GnRH

A

Ganirelix (and other relix’s)

parenteral administration

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9
Q

Usage of GnRH analogs

A

stimulation of gonadotropins
female and male infertility

or suppression of gonadotropins (agonist and antagonists)- endometriosis, uterine fibroids, prostate cancer, precocious puberty

Toxicity- hypersensitivity, menopausal symptoms, gynecomastia

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10
Q

Urofillotropin

A

Derived from urine of post menopausal women
FSH analog

parenteral

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11
Q

Fillotropin alpha

A

recombinant FSH

parenteral

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12
Q

Lutropin alpha

A

recombinant LH

parenteral

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13
Q

Chorionic gonadotropins

A

produced by placenta LH&raquo_space; FSH

  • hcg
  • choriogonadotropin alpha is recombinant version

parenteral

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14
Q

hMG

A

human menopausal gonadotropin
menotropin with FSH and LH activity

parenteral

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15
Q

Gonadotropin use

A

ovulation induction- collecting eggs, infertility, obesity, assisted reproduction. risk of ovarian hyperstimulation syndrome and multiple pregnancies

male infertility- start with hCG (less expensive) and then hMG
requires 4-6 months of treatment to detect sperm

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16
Q

Estradiol

A

E2
major product of ovary

other estrogens are estrone and estriol

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17
Q

estropipiate

A

purified crystalline estrone

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18
Q

estrogen esters

A

metabolically resistant prohormones with imrpoved bioavailability and t1/2

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19
Q

conjugated estrogens

A

equine estrogens (horses) sulfate sodium salts blended to standardized activity. high potency

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20
Q

ethinyl estradiol

A

synthetic estrogen
undergoes extensive hepatic metabolism
more active than natural estrogens

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21
Q

diethylstilbesterol

A

nonsteroidal estrogen
was used to prevent pregnancy complications but caused teratogenic effects - adenocarcinoma of vagina in daughters of pts who were treated with this

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22
Q

esterified esterogens

A

manufactured from soybeans and yams consisting primarily of estrone and equiline
metabolic conversion of estrone to estradiol

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23
Q

bisphenol

A

estrogen

leaches from plastics

24
Q

genistein

A

isoflavone phytoestrogen

derived from soybeans

25
Q

estrogens mechanism

A

bind to intracellular estrogen receptors- alpha and beta located in nucleus
receptor ligand complex initiates gene transcription by binding to estrogen response element (ERE)

-activity varies by tissue, interaction of estrogen with receptor, ERE, concentration of estrogen

26
Q

Uses for estrogen

A

primary hypogonadism
hormonal contraception
ovarian suppression for dysmenorrhea, endometriosis
post menopausal hormone therapy

27
Q

Formulations of estrogen

A

often with progestin
oral, injxn, transdermal, vaginal ring, troche

oral will have 1st pass metabolism

28
Q

estrogen side effects

A

nausea, breast tenderness, hyperpigmentation, increased migrains, accelerated blood clotting
cancer- uterine and breast cancer
uterine bleeding in post menopausal bleeding (only use estrogen + progestin for post menopausal with uterus)

29
Q

Progestins

A

all progesterin agents also have antiestrogenic activity and antimineralocorticoid activity

bind to intracellular progesterone receptors and initiates gene transcription

30
Q

Use of progestins

A

hormonal contraception, ovarian suppression for dysmenorrhea, endometriosis, post menopausal hormone replacement

31
Q

Progestins AE

A

increase blood pressure

androgenic agents may decrease plasma HDL

32
Q

Progestin agents

A 
progesterone- IM
medroxyprogesterone acetate- long doa, IM or PO
norethindrone
levonorgesterl
desogestrol
drospirenone
33
Q

Mechanism of hormonal contraception

A

suppress FSH and LH surge through negative feedback (except progestin only mini pill)
Thicken cervical m ucus
Decrease fallopian tube motility

34
Q

Oral contraceptives

A

21 days on, 7 days placebo
Most are thinyl estradiol
progestins include norethindrone, l-norgesterel, desogestrel

35
Q

AE of oral contraceptives

A

venous thromboembolism

36
Q

peri- and postmenopausal hormone therapy

A

decrease hot flashes, vaginal dryness, prevent osteoporosis, prevent atherosclerosis, prevent dementia

risks- heart disease, stroke, breast cancer (esp E + P), uterine cancer (unopposed E), inc triglycerides

use for shortest period and lowest dose to achieve treatment goals

37
Q

Selective estrogen receptor modulators (SERMS)

A

partial agonist-antagonists

38
Q

Tamoxifen

A

SERM
breast cancer

also Toremifene

39
Q

Raloxifene

A

used for osteoporosis

40
Q

Bazedoxifene

A

SERM

menopausal symptoms

41
Q

Clomiphene

A

ovulation induction, oral drug (compared to other drugs)

increase LH and FSH release by blocking negative feedback by estrogen

42
Q

Estrogen antagonist

A

fulvestrant- used in tamoxifen resistant breast cancer

43
Q

Mefipristone

A

Progesterone antagonist
Postcoital contraceptive
Abortifacient, in compination with misoprostol or PGE1
Also a glucocorticoid antagonist

44
Q

Aromatase inhibitor

A

Used for breast cancer in post menopausal women to block estrogen production by peripheral tissues

Anstrazole- nonsteroidal
Letrozole-nonsteroidal
Exemestane-steroid, irreversible

45
Q

Danazol

A

Derivative of 17a ethinyl testosterone with weak progestin, androgen, and glucocorticoid activity used to suppress ovarian function

46
Q

Androgenic agents

A

difference is between routes of administration and how much anabolic activity relative to androgenic effects

testosterone has equal anabolic and androgenic effects

47
Q

Oral androgenic agents

A

methyltestosterone
fluoxymetstrone
oxandrolone (more anabolic)

48
Q

IM androgenic agents

A

testosterone esters

49
Q

Transdermal patch androgenic agents

A

testosterone

50
Q

Use for androgens

A

androgen replacement
gynecologic disorders
anabolic agents after trauma (oxandrolone)
growth stimulation (boys with delayed puberty, but can cause premature closure of epiphyses) , osteoporosis in men, aging

51
Q

AE of androgens

A

acne, gynecomastia (aromatase makes testosterone into estradiol), testicular atrophy via feedback inhibition, masculinization in females, sodium retention, psych dependence, inc aggression

52
Q

Androgen suppression and antiandrogens used for

A

prostate cancer

53
Q

Steroid synthesis inhibitors

A

ketoconazole, abiraterone, finasteride, dutasteride

used for prostate cancer and in men with excess testosterone secretion

54
Q

cyproterone

A

androgen receptor inhibitors

used for hirsutism in women and excessive sexual desire in men

55
Q

flutamide

A

competitive androgen receptor antagonist

56
Q

spironolactone

A

androgen receptor inhibitor

competes with DHT and aldosterone

IC (31 decks)

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