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Pharmacology > Gonadal > Flashcards

Gonadal Flashcards

1
Q

concept: Describe clinical presentation in 17 alpha-hydroxylase deficiency

A

decreasd androgens, cortisol
increased mineralcorticoids

XY - cryptorchidism and indistinct genitalia – give androgens, glucocorticoids and anti hypertensives
XX - outwardly female with normal internal but no secondary charcteristics — give estrogens and anti hypertensives

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2
Q

concept: 21 hydroxylase deficiency

A

decreased BP icnreased K, increased renin and volume depletion

pseudohermaphroditism in females

tx: fliuds, salt repletion and give cortisl to decreased ACTH

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3
Q

concept: 11 hydrozxylase deficiency

A

increased sex hormones, decreased cortisol and mineralcorticoids but increased 11 deoxycorticosterone

increased BP
overmasculinization
tx: estrogens and HTN (same as 11)

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4
Q

Which is the most potent: estriol, estrone, estradiol

A

estradiol because has the most letters

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5
Q

concept: effects of estronge on a) coagulation b) lipid profile c) hormone levels d) cholesterol

A

a) procoagulation state - increases II, VII, IX, X, XII and decreases antithrombin II, prot C and S
b) favours lipid profile
c) increases binding protein; free level fo hormone unaffected
d) increases cholesterol in bile - formation of gall stone

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6
Q

List the clinically used estrogens please

A 
estradiol
conjugated estrogen
ethinyl estradoil
quinestrol
estrone
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7
Q

What is mestranol

A

prodrug converted to ethinyl estradiol (in some contraceptives)

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8
Q

Benefits of HRT please

A

reduced hot flashed
reudeced bone fracture and loss
decreased urogenital atrophy

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9
Q

A/se of HRT/estrogens

A 
thromboembolism
changes in lipid/carb metabolism
increased risk of high bp
increased incidence of breast and endometrial cnacers
migraine
cholestasis
mood changes
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10
Q

What is Diethylstilbestrol (DES)?

A

a nonsteroidal estrogen agonist

‘‘des daughters’’

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11
Q

Name the absolute contraindications of estrogen use!!!

A

1) history of thromboembolism
2) breast and endometrial cancer
3) pregnancy
4) liver disease

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12
Q

Tamoxifen - repeat from boen

A

antag @ breat
ag @ bone
ag @ liver
ag @ endometrium

USED @ breast cancer treatment

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13
Q

a/se of tamoxifen

A

antag - hot flushes
ag - thrombosis
increased risk of endometrial cacners

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14
Q

Toremifene

A

used in metastatic breast cancer

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15
Q

Raloxifene

A

antag @ breast
ag @ bone
no effect @ endo

therefore, no increased risk of endometrial cancer, hurahh!!

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16
Q

Use of Raloxifene

A

prophylaxis vrs breast cancer in high risk patients

prevention fo osteoporosis

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17
Q

Name an estrogen receptor antagonist in all tissues

A

Fulvestrant

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18
Q

used of Fulvestrant

A

estrogen receptor antag

used @ breast cancer in tamoxifen resistant patients

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19
Q

a/se of fulvestrant

A

hot flushes
injection site reactions
headache

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20
Q

List the aromatase inhibitors

A

letrozole
anastrozole
exemestane - irreversible

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21
Q

Use of letrozole, anastrozole, exemestane

A

aromatase inhibitors

second line for breast cancer to tamoxifen

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22
Q

MOA Clomiphene

A

estrogen antag @ hypothalamus and anterior pituitary –> prevents feedback inhibito fo GnRh by hypothalamus –> continued release of GnRH from hypothalamus –> LH and FSH from pituitary –> ovulation

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23
Q

Uses of clomiphene

A

treatment of infertility

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24
Q

A/se of clomiphene

A

ovarian hyperstimulation syndrome
ovarian elargment
multiple pregnancy
visual disturbances

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25
Q

affect of progesterone on gallbladder…rando

A

decreases gall bladder contraction

26
Q

effects of progesterone at high levels

A

suppresses gonadotropin secretion – anovulation

27
Q

List the progestins

A

medroxyprogesterone and NORgestrel and NORethindrone

28
Q

List the antiprogestins

A

mifepristone

SHARK flashback –> used to treat inoperable ectpoic ACTh syndrome (inhibits glucocorticoi and progesterone receptors)

29
Q

List some newer preps with less androgenic effects than classic progesterones ( medroxyprogesterone, norgestrol and nor ethindrone)

A

desoGESTREL
norelGESTROmine
etonoGESTREL
norGESTimate

GESTROL - less like a gentlemen. . . .

30
Q

What is DROSPIRENONE?

A

spironolactone ( aldosterone antaga with some anti androgenic activity)

used to treat acne in feamles

31
Q

acne in females treatment

A

drospirenone - spironolactone derivaitive (hirsutism, aldosternoisn, diuretic) that antagonizes aldosterone

32
Q

a/se progestins @ long term use

A 
weight gain
depression
oedema
acne
decreasd HDL
hypertension
thrombophlebitis
cholestatic juandice
33
Q

Mifepristone MOA

A

competitive inhibitor of progesterone and glucocorticoids

34
Q

uses of mifepristone

A

morning after pill - abortificant

inoperable ectopic ACTH syndrome

35
Q

Danazol = ?

A

inhibitor P450 in gonadal steroid synthesis

partial agonist of progestin, androgen, glucocorticoids

36
Q

Use of danazol

A

endometriosis

fibrocystic disease of breast

37
Q

a/se danazol

A

parial agonist at progestin, andronge, glucocorticoids

hepatitis - abnormal liver function

since a modified androgen – masculizing effects ie acne (despiranone), hirsutism (spironolactone), menstrual distoruabcnes

38
Q

which is more potent androstenedione, testosterone, DHT

A

DHT

39
Q

Compare and contrast the actions of testosterone and DHT

A

testosterone:

  • wolffian duct
  • boen formation
  • muscle growth
  • spermatogenesis

VRS

DHT

  • growth of external genitalia
  • prostate growth
  • scalp hair loss - remember jerrys story abotu this
  • acne – OCP
  • facial/body hair
40
Q

List synthetic androgens please

-OLONE

A 
oxandrolone
stanozolol
fluxymesterone** this one is bolded
oxymetholone
nandrolone
OLONE
41
Q

how can you use androgens to be clinically helpful?

A

hypogonasim
increase bone density
increase muscle mass (positive nitrogen balance)
some cases of aplastic anaemia

42
Q

admin route of androgens

A

oxandrolon, stanozolol, fluxymesterone, oxymetholon, nandrolone

transdermal
IM

43
Q

one bolded a/se of androgens

A

hepatic adenomas

44
Q

List the androgen receptor antagonists

U-T-AMIDE

A

flutamide
bicalutamide
nilutamide
UTAMIDE

45
Q

use of flutamide, bicalutamide, nilutamide

LUTAMIDE

A

used with GnRH analogs to decrease initial tumour flare ups of prostate carcinoma

46
Q

Finasteride MOA

A

5 alpha reductase inhibitors –> inhibits conversion of testosterone to DHT

47
Q

use of finasteride

A

BPH

promotes hair growth

48
Q

a/se finasteride

A

gynecomastia and impotence

49
Q

Ketoconazole

A

inhibits 17, 20 desmolase

(no gonadal no adrenal hormones)

cushing, prostate cancer

50
Q

GnRH analogs list please

A

leuprolide
goserelin
nafarelin

51
Q

continuous does of leuprolide, goserelin and nafarelin

A

down regulates GnRH receptors in pituiturat

52
Q

Used of leuprolide, goserelin and nafarelin

A

prostate cancer
uterine fibroids
precocious puberty

53
Q

list other drugs with anti androgenic action

A

spironlactone ( hirsutism, aldosternosim, diuretic)
cimetidine
cyproterone acetate

54
Q

uses of : leuprolide and flutamide

A

flutamide (androgen receptor antag)
leuprolide (GnRH analog)

prostate cancer

55
Q

Bicalutamide

A

a nonsteroidal antiandrogenic
prostate cancer
hirsutism

56
Q

Nilutamide

A

used for prostate cance

57
Q

SHARK: prostate cancer

A

leuprolide
flutamide
nilutamide

58
Q

Spironolactone and cyropterone

A

hirsutism

59
Q

BPH and male patterned baldness

A

finasteride (5alpha reductase inhibitor)

60
Q

Ketoconazole

A

inhibits 17,20 desmolase

treats cushing and met prostati cancer.

61
Q

How do finasteride and dutasteride help with benign prostatic hyperplasia?

A

5 alpha reductase inhibitors that decrease size of prostate

62
Q

How do terazosin, doxazosin, tamsulosin, and alfuzosin help in BPH?

A

reduce tension fo prostatic smooth muscle in prostate, capsule, neck

Pharmacology (70 decks)

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