gonadal Flashcards

1
Q

primary female steroid hormone

increase feedback inhibition of FSH and LH

A

estrogen

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2
Q

MOA

1) developmental actions - 2nd sex organs/ characteristics and menstrual cycle
2) metabolic - bone
3) blood coagulability increase (Factors 2, 7, 9, 10)
4) lipid profile - decrease LDL cholesterol
5) sensitizes myometrium to oxytocin at term
6) maintain normal structure of skin and blood vessels

A

estrogen

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3
Q

estrogen receptors

A

ER alpha and ER beta

nuclear receptor

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4
Q

natural estrogen preparations

A

estradiol
estrone
estriol

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5
Q

synthetic steroidal estrogen preparation

A

ethinylestradiol

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6
Q

synthetic non steroidal estrogen preparation

A

diethylstilbestrol

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7
Q

therapeutic uses of estrogen

A

1) gonadal dysgenesis
2) hormone replacement therapy (HRT) - conj. estrogens, ethinylestradiol, progestin, tibolone
3) combo oral contraceptives

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8
Q

ADR

1) hepatic adenoma
2) thromboembolism, stroke
3) breast cancer (prolonged use)
4) endometrial cancer

A

estrogen

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9
Q

used in pregnant women - increase in clear cell adenocarcinoma of vagina and cervix in female offspring

A

diethylstilbestrol

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10
Q

breast cancer, endometrial cancer, pregnancy, liver dz, heavy smoker, hx of thromboembolic disorders

A

estrogen CI

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11
Q

selective estrogen receptor down regulator (SERD)

A

fulvestrant

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12
Q

MOA: inhibits ER dimerization - ER interaction with DNA prevented receptor degradation enhanced

A

fulvestrant

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13
Q

Use: tx of metastatic treats cancer unresponsive to tamoxifen

A

fulvestrant

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14
Q

estrogen antagonists

A

anastrozole
letrozole (reversible)
exemestane (irreversible)

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15
Q

MOA: aromatase inhibitor - decrease estrogen synthesis

A

estrogen antagonists

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16
Q

Use: estrogen - dependent, post menopausal breast cancer (ER +), advanced breast cancer: in case tamoxifen failure

A

estrogen antagonists

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17
Q

partial estrogen agonist

A

clomiphene

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18
Q

MOA: decrease feedback inhibition - increase FSH and LH - increase ovulation - pregnancy (follicular maturation enhanced)

A

clomiphene

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19
Q

Use: fertility drug

ADR: increase multiple births, ovarian hyper stimulation syndrome, increase risk of ovarian/endometrial cancer

A

clomiphene

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20
Q

Selective estrogen receptor modulators (SERMS)

A

tamoxifen

raloxifene

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21
Q

estrogen antagonists in breast, blood vessels

anti estrogen action - inhibit breast cancer cells and hot flashes

A

tamoxifen

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22
Q

E receptor agonists (bone)
antagonist (breast)
partial agonist (endometrium, uterus bone, liver, pituitary)
estrogen agnostic action: stimulation of endometrial proliferation (cancer risk)

A

tamoxifen

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23
Q

ADR: increase risk of endometrial cancer, hot flashes, increase risk of venous thromboembolism

A

tamoxifen

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24
Q

Used: estrogen dependent breast cancer (post mastectomy) and for prophylaxis in high risk patients

A

tamoxifen

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25
Q

E receptor agonist (bone)
antagonist breast and uterus
estrogen partial agonist in bone and CVS
distinct DNA target - raloifene response element

A

raloxifene

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26
Q

Use: postmenopausal, breast cancer, no increase cancer risk

A

raloxifene

27
Q

ADR: hot flushes, DVT, pulmonary embolism

A

raloxifene

28
Q

major natural progestin
increase body temp (.5-1 degrees C)
regular maturation of the endometrium
increase feedback inhibition of gonadotropins especially LH

A

progesterone

29
Q

synthetic progestin

A

medroxyprogesterone
norethindrone
desogestrel
megesterol acetate

30
Q

Uses: contraception, HRT, dysfunction uterine bleeding, endometriosis, threatened/habitual abortion

A

progesterone

31
Q

SE: increased HDL and decreased LDL, glucose intolerance, break through bleeding, androgenic (hirsutism and acne), weight gain, depression

A

progesterone

32
Q

anti progestin

1) antiprogestional +
2) antiglucocorticoids +
3) anti androgenic activity

A

mifepristone

33
Q

MOA:

1) partial agonist and competitive antagonists at progesterone receptor
2) attenuates midcycle Gn surge from pituitary - delay in follicular develop - delay/failure of ovulation
3) blocks progesterone support to endometrium
4) induces menstruation

A

mifepristone

34
Q

Uses:

1) termination of pregnancy (<7 wks)
2) cervical ripening
3) induce labor
4) postcoital contraceptive
5) cushings syndrome

A

mifepristone

35
Q

inhibits LH and FSH surge

inhibits steroid enzymes and gonadal fxn

A

danazol

36
Q

Uses:

1) endometriosis
2) fibrocystic breast dz
3) hereditary angioneurotic edema

A

danazol

37
Q

oral contraceptives

A

estrogen + progestin - suppresses midcycle LH surge - prevent ovulation

38
Q

interactions of oral contraceptives

A

decrease contraceptive effectiveness when used with antimicrobials and enzyme inducers

39
Q

benefits of oral contraceptives

A

decreases risk of endometrial and ovarian cancer, dysmenorrhea, endometriosis, pelvic inflammatory dz, osteoporosis

40
Q

serious A/E of oral contraceptives

A

thromboembolism
hepatomas
increase risk of breast cancer

41
Q

natural androgens

A

testosterone

dihydrotestosterone

42
Q

weak androgens

A

androstenedione

dihydro androstenedione

43
Q

Uses for androgens

A

1) testicular failure
2) delayed puberty (to achieve grow spurt)
3) hypopituitarism
4) male hypogonadism (increase muscle mass and RBC)
5) anemias (fanconi, sickle, hemolytic, aplastic)
6) illicit in athletes
7) hereditary angioneurotic edema

44
Q

PK: converted to dihydrotestosterone by 5 alpha reductase

phys: large doses - suppress gonadotropins

A

androgens

45
Q

SE: excessive masculinization, premature closure of epiphysis, cholestatic jaundice, aggression, dependence, oligospermia, azospermia

A

androgens

46
Q

17- alkyl derivatives: resist 1st mass
lipid soluble esters of testosterone
transdermal testosterone: by pass 1st pass
gels, buccal tablets, implanted pellets

use with caution in CHF, epilepsy, migraine

A

testosterone preparations

47
Q

17 alkyl derivatives testosterone preparations

A

methyl testosterone

fluoxymesterone

48
Q

lipid soluble ester of testosterone preparations

A

undecanoate
propionate
enathate

49
Q

androgen antagonists

A

flutamide
leuprolide
finasteride / dutasteride

50
Q

competitive androgen receptor blocker

used for androgen receptor positive prostate cancer

increases LH secretion by blocking feedback inhibition

A

flutamide

51
Q

GnRH analog: repository form used for androgen receptor positive prostate cancer

increase androgen levels in combo

A

leuprolide

52
Q

inhibit both type 1 and 2 5 alpha reductase enzyme - preventing conversion of testosterone to dihydrotestosterone

A

finasteride / dutasteride

53
Q

Uses in BPH and male pattern baldness

A

finasteride / dutasteride

54
Q

non competitive androgen receptor antagonists

A

cyproterone acetate - used fro hirsutism in females

55
Q

anabolic steroids

A

nandrolone
oxymetholone
stanozolol
methandienone

56
Q

uses for anabolic steroids

A

1) catholic state: severe trauma, major surgery
2) renal insufficiency: decrease urea prod and dialysis freq
3) osteoporosis: elderly males
4) anemia: hypoplastic, hemolytic, malignancy associated
5) to improve athletic performance (illegal)

57
Q

1) Gn preparations: menotropins, urofollitropin, HCG, recombinant FSH
2) GnRH antagonists: cetrolrelix
3) GnRH agonists: clomiphene and leuprolide

A

TX for aiding IVF

58
Q

synthetic Gn: gonadorelin

GnRH agonist: leuprolide

A

tx for infertility pulsatile tx

59
Q

prostate cancer drugs

A

GnRH antagonists: cetrolrelix

GnRH agonists: flutamide and leuprolide

60
Q

Breast cancer drugs

A

SERMs: tamoxifen
SERDs: fuluestrant
aromatase inhibitor: letrozole

61
Q

endometrial cancer drugs

A

progesterone

62
Q
Used in premenopausal breast cancer 
endometrial hyperplasia endometrial cancer risk 
no bone loss, fractures
venous thromboembolism risk 
improves lipid profile
A

SERMS

63
Q

not used in premenopausal women
no cancer risk
accelerates bone loss, predisposes to fractures
no increase of such risk

A

AIs

64
Q

Why does exogenous androgen cause infertility?

A

it inhibits FSH and LH

leydig cells synthesize less androgen
Sertoli cells then reduce synthesis of androgen binding protein
seminiferous tubules degenerate - no sperm

prevention: transdermal androgen patches applied to scrotum