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Gonadal Hormones Flashcards

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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

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A

estrogen

leaches from plastics

24
Q

genistein

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A

isoflavone phytoestrogen

derived from soybeans

25
estrogens mechanism
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
Uses for estrogen
primary hypogonadism hormonal contraception ovarian suppression for dysmenorrhea, endometriosis post menopausal hormone therapy
27
Formulations of estrogen
often with progestin oral, injxn, transdermal, vaginal ring, troche oral will have 1st pass metabolism
28
estrogen side effects
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
Progestins
all progesterin agents also have antiestrogenic activity and antimineralocorticoid activity bind to intracellular progesterone receptors and initiates gene transcription
30
Use of progestins
hormonal contraception, ovarian suppression for dysmenorrhea, endometriosis, post menopausal hormone replacement
31
Progestins AE
increase blood pressure | androgenic agents may decrease plasma HDL
32
Progestin agents
``` progesterone- IM medroxyprogesterone acetate- long doa, IM or PO norethindrone levonorgesterl desogestrol drospirenone ```
33
Mechanism of hormonal contraception
suppress FSH and LH surge through negative feedback (except progestin only mini pill) Thicken cervical m ucus Decrease fallopian tube motility
34
Oral contraceptives
21 days on, 7 days placebo Most are thinyl estradiol progestins include norethindrone, l-norgesterel, desogestrel
35
AE of oral contraceptives
venous thromboembolism
36
peri- and postmenopausal hormone therapy
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
Selective estrogen receptor modulators (SERMS)
partial agonist-antagonists
38
Tamoxifen
SERM breast cancer also Toremifene
39
Raloxifene
used for osteoporosis
40
Bazedoxifene
SERM | menopausal symptoms
41
Clomiphene
ovulation induction, oral drug (compared to other drugs) | increase LH and FSH release by blocking negative feedback by estrogen
42
Estrogen antagonist
fulvestrant- used in tamoxifen resistant breast cancer
43
Mefipristone
Progesterone antagonist Postcoital contraceptive Abortifacient, in compination with misoprostol or PGE1 Also a glucocorticoid antagonist
44
Aromatase inhibitor
Used for breast cancer in post menopausal women to block estrogen production by peripheral tissues Anstrazole- nonsteroidal Letrozole-nonsteroidal Exemestane-steroid, irreversible
45
Danazol
Derivative of 17a ethinyl testosterone with weak progestin, androgen, and glucocorticoid activity used to suppress ovarian function
46
Androgenic agents
difference is between routes of administration and how much anabolic activity relative to androgenic effects testosterone has equal anabolic and androgenic effects
47
Oral androgenic agents
methyltestosterone fluoxymetstrone oxandrolone (more anabolic)
48
IM androgenic agents
testosterone esters
49
Transdermal patch androgenic agents
testosterone
50
Use for androgens
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
AE of androgens
acne, gynecomastia (aromatase makes testosterone into estradiol), testicular atrophy via feedback inhibition, masculinization in females, sodium retention, psych dependence, inc aggression
52
Androgen suppression and antiandrogens used for
prostate cancer
53
Steroid synthesis inhibitors
ketoconazole, abiraterone, finasteride, dutasteride used for prostate cancer and in men with excess testosterone secretion
54
cyproterone
androgen receptor inhibitors | used for hirsutism in women and excessive sexual desire in men
55
flutamide
competitive androgen receptor antagonist
56
spironolactone
androgen receptor inhibitor | competes with DHT and aldosterone

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