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Pharm Block 4 > gonadal > Flashcards

gonadal Flashcards

(64 cards)

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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
E receptor agonist (bone) antagonist breast and uterus estrogen partial agonist in bone and CVS distinct DNA target - raloifene response element
raloxifene
26
Use: postmenopausal, breast cancer, no increase cancer risk
raloxifene
27
ADR: hot flushes, DVT, pulmonary embolism
raloxifene
28
major natural progestin increase body temp (.5-1 degrees C) regular maturation of the endometrium increase feedback inhibition of gonadotropins especially LH
progesterone
29
synthetic progestin
medroxyprogesterone norethindrone desogestrel megesterol acetate
30
Uses: contraception, HRT, dysfunction uterine bleeding, endometriosis, threatened/habitual abortion
progesterone
31
SE: increased HDL and decreased LDL, glucose intolerance, break through bleeding, androgenic (hirsutism and acne), weight gain, depression
progesterone
32
anti progestin 1) antiprogestional + 2) antiglucocorticoids + 3) anti androgenic activity
mifepristone
33
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
mifepristone
34
Uses: 1) termination of pregnancy (<7 wks) 2) cervical ripening 3) induce labor 4) postcoital contraceptive 5) cushings syndrome
mifepristone
35
inhibits LH and FSH surge | inhibits steroid enzymes and gonadal fxn
danazol
36
Uses: 1) endometriosis 2) fibrocystic breast dz 3) hereditary angioneurotic edema
danazol
37
oral contraceptives
estrogen + progestin - suppresses midcycle LH surge - prevent ovulation
38
interactions of oral contraceptives
decrease contraceptive effectiveness when used with antimicrobials and enzyme inducers
39
benefits of oral contraceptives
decreases risk of endometrial and ovarian cancer, dysmenorrhea, endometriosis, pelvic inflammatory dz, osteoporosis
40
serious A/E of oral contraceptives
thromboembolism hepatomas increase risk of breast cancer
41
natural androgens
testosterone | dihydrotestosterone
42
weak androgens
androstenedione | dihydro androstenedione
43
Uses for androgens
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
PK: converted to dihydrotestosterone by 5 alpha reductase phys: large doses - suppress gonadotropins
androgens
45
SE: excessive masculinization, premature closure of epiphysis, cholestatic jaundice, aggression, dependence, oligospermia, azospermia
androgens
46
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
testosterone preparations
47
17 alkyl derivatives testosterone preparations
methyl testosterone | fluoxymesterone
48
lipid soluble ester of testosterone preparations
undecanoate propionate enathate
49
androgen antagonists
flutamide leuprolide finasteride / dutasteride
50
competitive androgen receptor blocker used for androgen receptor positive prostate cancer increases LH secretion by blocking feedback inhibition
flutamide
51
GnRH analog: repository form used for androgen receptor positive prostate cancer increase androgen levels in combo
leuprolide
52
inhibit both type 1 and 2 5 alpha reductase enzyme - preventing conversion of testosterone to dihydrotestosterone
finasteride / dutasteride
53
Uses in BPH and male pattern baldness
finasteride / dutasteride
54
non competitive androgen receptor antagonists
cyproterone acetate - used fro hirsutism in females
55
anabolic steroids
nandrolone oxymetholone stanozolol methandienone
56
uses for anabolic steroids
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
1) Gn preparations: menotropins, urofollitropin, HCG, recombinant FSH 2) GnRH antagonists: cetrolrelix 3) GnRH agonists: clomiphene and leuprolide
TX for aiding IVF
58
synthetic Gn: gonadorelin | GnRH agonist: leuprolide
tx for infertility pulsatile tx
59
prostate cancer drugs
GnRH antagonists: cetrolrelix | GnRH agonists: flutamide and leuprolide
60
Breast cancer drugs
SERMs: tamoxifen SERDs: fuluestrant aromatase inhibitor: letrozole
61
endometrial cancer drugs
progesterone
62
``` Used in premenopausal breast cancer endometrial hyperplasia endometrial cancer risk no bone loss, fractures venous thromboembolism risk improves lipid profile ```
SERMS
63
not used in premenopausal women no cancer risk accelerates bone loss, predisposes to fractures no increase of such risk
AIs
64
Why does exogenous androgen cause infertility?
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

Pharm Block 4 (18 decks)

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