Gonadal Hormones and Inhibitors Flashcards Preview

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Flashcards in Gonadal Hormones and Inhibitors Deck (36):
1

what happens when there is release of CRH

-anterior pituitary releases ACTH, MSH, beta-endorphine
-which cause a release of mineralcorticoids, glucocorticoids, and sex hormones

basically ACTH causes release of hormones from adrenal gland

2

what happens with increased dopamine

increased dopamine --> decreased prolactin --> increased GnRH --> increased spermatogenesis and ovulation

3

stimulus that causes an increase in GHRH

-increased exercise and sleep
-decreased somatostatin and glucose

4

what is general mechanism of gonadal hormones - estrogen, progesterone, and androgens

-they bind to their cytosolic receptor
-the hormone-receptor complex (HRC) then travels into the nucleus
-in nucleus, it is activated --> transcription of the steroid hormone regulated genes

5

what occurs in 17 alpha hydroxylase deficiency and symptoms it leads to

(17 years olds are salty they can't have sex)

-increase in aldosterone --> high BP and low K+

-decrease in androgens and cortisol --> cryptochordism and indistinct genitalia in males while females lack secondary sexual characteristics

6

how do you treat males and females with 17 alpha hydroxylase deficiency

males: anti hypertensives, androgens, and glucocorticoids

females: anti hypertensives, estrogen

7

what occurs in 21 hydroxylase deficiency and what symptoms it leads to

(21 year olds can only have sex)

-increase in androgens --> over masculinization and pseudo-hermaphroditism in females

-decrease in cortisol and aldosterone --> low BP, high K, high renin activity, and volume depletion

8

how do you treat 21 hydroxylase deficiency

fluids and salt repletion and give cortisol to decrease ACTH

9

what occurs in 11 beta hydroxylase deficiency and what symptoms manifest

(11 beta is similar to 21 alpha)

-increase in androgens --> over masculinazation

-decrease in cortisol and aldosterone but increase in 11-deoxycorticosterone --> high BP because of the 11-deoxycorticosterone (how it differs from 21 hydroxylase deficiency)

10

how do you treat 11 beta hydroxylase deficiency

anti hypertensives and estrogen

11

what are the main estrogen synthesized within the body

estrone
estradiol (not seen after menopause)
estriol (seen in pregnancy)

12

what are the estrogen that can administered

CEMD

Conjugated estrogen
Ethinyl estradiol
Mestranol
Diethylstilbestrol

13

what is mestranol and its importance

prodrug converted --> ethinyl estradiol (seen in some contraceptives) --> increases bioavailability and half life, decreases FSH and LH via feedback

14

what metabolizes estrogen and the importance

CYP450 metabolizes estrogen --> if given an inducer, it can decrease the effect of contraceptives since estrogen seen in contraceptives

15

clinical uses of estrogen

-long acting ones used in female hypogonadism
-oral contraceptives together with progestins
-postmenopausal HRT --> decrease hot flashes, prevent bone loss and fracture, decrease urogenital atrophy
-dysmenorrhea, uterine bleeding, prostate cancer, and acne

16

adverse effects of estrogen

-thromboembolism
-breast cancer
-endometrial hyperplasia and cancer (unless progestins added as well)

17

adverse effect seen using estrogen diethylstilbestrol during pregnancy

if pregnant with female child --> infertility and vaginal cancer

18

contraindications of estrogens

-Thromboembolism
-Breast and Endometrial cancer
-Pregnancy
-Liver Disease

19

what are the SERMs (selective estrogen receptor modulator) and mechanism

RoTTC

Raloxifene
Tamoxifen
Toremifene
Clomiphene

they exhibit agonist behavior in some tissues and antagonist in others

20

mechanism of tamoxifen and what it is used for

-estrogen receptor antagonist in breast and agonist in bone and endometrium

-used to treat breast cancer or for prophylaxis in high risk patients

21

adverse effects of tamoxifen

-risk of endometrial cancer
-hot flashes (antagonist)
-thrombosis (agonist)

22

mechanism and uses of Toremifene and Raloxifene

-Toremifene: treatment and prophylaxis of breast cancer

-Raloxifene: estrogen antagonist in breast and agonist in bone and no effect in endometrium
-prophylaxis against breast cancer
-prevention of post menopausal osteoporosis

23

estrogen antagonist in all tissue and its use

fulvestrant: treatment of breast cancer in tamoxifen resistant patients

24

adverse effect of fulvestrant

hot flushes, pain at injection site, headache

25

what are the aromatase inhibitors and their exact mechanism

inhibits conversion of androgens to estrogen

Anastrozole - reversible
Letrozole - reversible
Exemestane - irreversible aromatase inhibitor

26

use of aromatase inhibitors (name them) and their adverse effects

anastrozole, letrozole, exemestane

-used in treatment of estrogen dependent breast cancer
-AE: hot flushes, decreased bone mineral density

27

mechanism and use of clomiphene

-fertility drug used in tx of anovulatory infertility

-estrogen antagonist in hypothalamus and anterior pituitary --> prevents feedback inhibition of GnRH release by hypothalamus --> continued release of GnRH from hypothalamus --> increased LH and FSH from pituitary --> ovulation

28

adverse effect of Clomiphene

-Ovarian hyper stimulation leading to enlargement of ovary
-Multiple pregnancy

29

what are the progestins

PMNNNDD

Progesterone
Medroxyprogesterone
Norgestrel
Norethindrone
Norgestimate
Desogestrel
Drospirenone

30

what is the anti progestin

Mifepristone

31

what are the newer progestins that lack androgenic and antiestrogenic effects

MNNND

Medroxyprogesterone
Norgestrel
Norethindrone
Norgestimate
Desogestrel

32

mechanism of drospirenone

spironolactone derivative used as an oral contraceptive and antagonizes aldosterone effect --> used in females for acne

33

AE for long term use of progestins

HAD WAGE

-HDL high, low LDL, and hypertension
-Androgenic - hirsutism and acne
-Depression

-Weight gain
-Anti estrogenic - blocks lipid change
-Glucose intolerance
-Edema and acne

34

mechanism of mifeprostone

competitive inhibitor of progesterone AND glucocorticoid receptor

35

use of mifeprostone

-morning after drug abortifacient
-with prostaglandins, increases myometrial contraction

36

AE of mifeprostone

Excessive bleeding
GI effects: anorexia, abdominal pain etc

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