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Pharm 6 > female reproductive and infertility > Flashcards

female reproductive and infertility Flashcards

1
Q

target cells of FSH and LH

A

FSH: Sertoli and granulosa cells
LH: Leydig and theca cells

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2
Q

inhibin and activin

A

inhibin: from Sertoli and granulosa cells, inhibits anterior pituitary release of FSH (not LH)
activin: same source, but activate ant pit release of FSH (not LH)

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3
Q

PCOS sx and cause

A

anovulation, oligo-ovulation, inc plasma androgen -> hirsutism, dysmenorrhea, acne
theories:
1- inc freq and amplitude of LH pulses = stimulates theca cells to make androgen
2- inc insulin secretion = dec sex hormone binding globulin = inc free testosterone
3- theca cell dysregulation of sex steroid synthesis

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4
Q

prolactinoma

A

benign lactotroph adenoma in ant pit -> suppressed estrogen synth by GnRH-block, dec gonadotroph sensitivity to GnRH
sx: gynecomastia, galactorrhea, dysmenorrhea, etc.

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5
Q

hypogonadism

A

sex hormone production impaired before adolescence -> no sexual maturation
inc FSH and LH

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6
Q

menopause

A

exhaustion of ovarian follicles -> dec estrogen and inhibins, inc FSH and LH

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7
Q

GnRH agonist MOA

A

continuous administration suppresses FSH and LH since they are released in a pulsatile manner
*R is in ant pit

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8
Q

leuprolide

A

continuous GnRH agonist

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9
Q

goserelin

A

continuous GnRH agonist

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10
Q

naferelin

A

continuous GnRH agonist

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11
Q

cetrorelix

A

GnRH antagonist

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12
Q

ganirelix

A

GnRH antagonist

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13
Q

uses of GnRH replacements

A 
hormone-dep tumors: prostate, some breast ca
endometriosis pain ?
central precocious puberty
PCOS
controlled ovarian hyperstimulation
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14
Q

anastrozole

A

competitive aromatase inhibitor

reversible

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15
Q

letrozole

A

competitive aromatase inhibitor

reversible

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16
Q

exemastene

A

covalently-binding aromatase inhibitor

irreversible

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17
Q

formestane

A

covalently-binding aromatase inhibitor

irreversible

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18
Q

uses and ADR of aromatase inhibitors

A

ER+ metastatic breast ca: tx and prevention of recurrence

ADR: estrogen suppression -> osteoporosis

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19
Q

tamoxifen

A

SERM w agonistic effect on endometrium and bone, antagonistic effect on breast
for breast ca
4-6x inc risk endometrial ca, so not given >5 yr (switch to aromatase-inh)

20
Q

raloxifene

A

SERM w agonistic effect on bone, antagonistic effect on endometrium and breast
mgmt of post-meno osteoporosis and breast ca prevention

21
Q

clomiphene

A

SERM w antagonistic effect in hypothal and ant pit, partial agonist in ovaries = inc release GnRH and gonadotropins -> stimulates follicle growth and ovulation
use: ovulation induction
ADR: inc ovary stimulation, multiple pregnancies

22
Q

locations of ER receptors

A

all are cytoplasmic/ nuclear
ERa - endometrium, breast ca cels, ovarian cells, hypothalamus
ERb - kidney, brain, bone, heart

23
Q

flutamide

A

androgen-R antagonist

24
Q

spironolactone

A

androgen-R antagonist

25
Q

MOA androgen-R antagonist

A

competitively inhibit binding of endogenous androgens to receptor = blocks action of DHT and testosterone

26
Q

uses of androgen-R antagonists

A

metastatic prostate ca, severe BPH
spironolactone: K-sparing diuretic (aldosterone blocker), female hirsutism, male pattern baldness (but causes loss of libido)

27
Q

mifepristone

A

progesterone-R antagonist to induce abortion up to 63 days of pregnancy
prog stabilizes uterine lining, promotes decidua prep - inhibition -> decay of decidua, detachment of blastocyst

28
Q

misoprostol

A

PG analogue given with mifepristone to stimulate uterine contractions

29
Q

ethinyl estradiol and mestranol

A

estrogens for HRT and acne, also in combo OCPs
ADR: HTN (inc AT2 d/t inc angiotensinogen activity), thomboembolic d/o (inc hepatic synth of clotting factors), gall bladder dz (inc cholesterol excretion in bile)

30
Q

2 types of OCP

A

combo estrogen-progestin pills

progestin-only pills

31
Q

MOA of estrogen-progestin pills

A

suppress GnRH, LH, FSH = no follicular development or ovulation
also altered tubal peristalsis, dec endometrial receptivity, dec cervical mucus secretions

32
Q

ADR of estrogen-progestin pills

A

unopposed estrogen: inc risk endometrial ca (reduce risk w progestin), DVT, and PE
inc risk GB d/z (stasis)
don’t give to women >45 and smoke

33
Q

androgenic activity of estrogens

A

highest: norgestrel, levonorgestrel
lower: norethindrone
lowest: norgestimate, ethynodiol
anti-androgen: drosperinone (inc CV/ thromboembolic risk)

34
Q

combo OCP drug interactions

A

abx like penicillin, tetracyclines - dec effect estrogen
estrogen can inh metabolism of: cyclosporine, antidepressants, glucocorticoids
estrogen inc synthesis of vit-K-dep clotting factors, antagonizes warfarin effect

35
Q

norgestrel and norethindrone

A

progestin-only pills, used when estrogen contraindicated

pts won’t menstruate but may have spotting

36
Q

medroxyprogesterone acetate

A

“depot” progestin, used for sex offenders to dec sexual drive and stop spermatogenesis

37
Q

levonorgestrel and etonorgestrel

A

progestin implants

*levo also emergency contraception (plan B) - most efficacious with fewest ADRs

38
Q

ADR progestin only

A

androgenic effect -> acne, hirsutism, inc libido, oily skin

39
Q

MOA plan B (levonorgestrel)

A

blocks LH surge, disrupting ovulation and produces endometrial changes not conducive for implantation

40
Q

PCOS tx

A

estrogen-progestin contraceptive (stop ovarian testosterone production)
anti-androgen (spironolactone)
metformin to reduce insulin resistance -> regular ovulation and T levels
GnRH analogues

41
Q

female infertility tx

A

clomiphene citrate

42
Q

prolactinoma tx

A

DA-R agonist: cabergoline, bromocriptine

43
Q

breast and endometrium ca tx

A

SERM, aromatase inhibitors

44
Q

endometriosis tx

A

OCP, GnRH analogs (continuous)

Danazol - androgen analog (suppresses FSH, LH -> hypoestrogenic state)

45
Q

menopause tx

A

hormone replacement therapy

Pharm 6 (5 decks)

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