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88 Cards in this Set

  • Front
  • Back
What inhibits FSH and LH (gonadotropin) release in a woman?
Estrogens
_____ cells of ovary release estrogen
granulosa
surge of what stimulates ovulation

a) LH
c) FSH
c) estrogen
a) LH
Why does ant pit stop making gonadotropins during cycle?
corpus luteum makes estrogen and progesterone
What are phyto-estrogens?
plant estrogen
(used as dietary supplement or cream used to enlarge breasts)
What is conjugation?
conversion of compound to large bulky compoiund that is more water soluble and more easily excreted.
Three Natural Human Estrogens
17b estradiol (principal ovarian estrogen)
Estriol (principal placental estrogen)
Estrone (metabolite of 17b estradiol and major ovarian and postmenopausal estrogen)
How are hormones transported to target tissues?
complexed with proteins
Estrogens are carried by ____
sex hormone-binding globulin
Progesterone is carried by _____
corticosteroid-binding globulin
Actions of Estrogens
Reg of repro tract, pit and breasts during cycle

role in some tumor growth

Incr water and Na retention

Decr bowel motility
Effects of Estrogen
Incr fat depo in breasts, butt and thighs

Initiate breast development

Acc growth at puberty

Stims closure of epiphyses in the shafts of long bones

Stim synth and secretion of prolactin from pit

Incr cellular prolif of uterus in the absence of progesterone

Incr protein synth

Thickens vaginal mucosa and thinning of cervical mucus

Aids in maint of bone mass

Stims hepatic production of sex hormone-binding globulin, thyroid binding globulin, blood clotting factors
Estrogen's effect on LDL formation

a) inhibits
b) stimulates
c) no effect
a) inhibits
Estrogen's effect on HDL production

a) inhibits
b) stimulates
c) no effect
b) stimulates
Estrogen's effect on blood clotting factors production

a) inhibits
b) stimulates
c) no effect
b) stimulates
What progestins have weak progestational activity?
17a-, 20a-, and 20b-hydroxypro-gesterone
Progesterone concentrations rise rapidly in ______ phase of menstrual cycle
luteal
Progesterone's effect on temperature during luteal phase of cycle

a) increases
b) decreases
c) no effect
a) increases
Progesterone's effect on HDL production

a) increases
b) decreases
c) no effect
b) decreases
Progesterone's effect on LDL production

a) increases
b) decreases
c) no effect
a) increases
Progesterone'e effect on Na and H2O retention?

a) increases
b) decreases
c) no effect
b) decreases
Progesterone's effect on endometrial lining?

a) maintains it
b) sloughs it
c) no effect
a) maintains it
Conditions calling for HRT with Estrogens and progesterone
Menopause (estrogens, progestins)
Osteoporosis (estrogens, progestins)
Ovarian failure (estrogens, progestins)
Dysfunctional uterine bleeding (progestins,estrogens)
Luteal phase dysfunction (progestins)

Breast cancer (estrogens, progestins, antiestrogens, steroidogenesis inhibitors)
Endometrial cancer (progestins, antiestrogens
Prostate cancer (estrogens)

Endometriosis (danazol, progestins, GnRH)
Diagnostic (progestins)
What is clomiphene citrate used for?
Ovulation induction
Infertility
Natural estrogens (3)
Estradiol (most potent)
Estrone
Estriol
Problems with administering natural estrogens
Low oral potency
Poorly absorbed and rapidly inactivated by liver
Conjugated Estrogens Prepared from pregnant mare’s urine (3)
Estrogen
Equilin (found in horses but not humans)
Estrone
Pluses to conjugated estrogens
Water soluble with virtually no estrogenic activity until activated by hydrolyzation
Synthetic Steroidal Estrogens
Ethinyl estradiol
Mestranol (converted to ethnyl estradiol by liver)
Estropipate
Quinestrol
Which estrogens are Used predominantly as oral contraceptives
Synthetic Steroidal Estrogens
Parenteral Synthetic Steroidal Estrogens
Estradiol cypionate
Estradiol valerate
Polyestradiol phosphate
Synthetic Non-Steroidal Estrogens
Diethylstilbesterol
Chlorotrianisene
Dienestrol
Progestins

(maybe disregard this card)
Progesterone
17a-hydroxyprogesterone
Medroxyprogesterone acetate
Megestrol acetate
Hydroxyprogesterone caproate
Levonorgestrel
Norgestrel
Norethindrone
Norethindrone acetate
Norethynodrel
Ethynodiol diacetate
Most effective reversible method
Combination Oral Contraceptives
Failure rate of combination oral contraceptives
is less than 0.7 per 100 women
Combination Oral Contraceptives

What is the estrogen and what is the progestin?
Estrogen component is either ethinyl estradiol or mestranol (less potent)

Progestins include norethidrone, norethidrone acetate, ethynodiol diacetate, norgestrel or levonorgestrel
What decreases the incidence of adverse side effects of combination oral contraceptives
low dose estrogen
Most common formulations consist of 21 days of combination with how many days off for withdrawal bleeding?
7
Oral Contraceptives: MOA

Progestin primarily suppresses a) LH
b) FSH
c) estrogen
a) LH

(prevents menstruation)
Oral Contraceptives: MOA

Estrogen suppreses
a) LH
b) FSH
c) progestin
b) FSH

(prevents emergence of dominant follicle)
Oral Contraceptives: MOA

What is estrogen's effect on endometrium?
stabilizes
Oral Contraceptives: MOA

What is estrogen's effect on progestin?
postentiates the progestin action
Oral Contraceptives: MOA

Progestin's effect on endometrium?
makes endometrium not receptive to ovum implantation
Oral Contraceptives: MOA

Which is the dominant hormone?
progestin

(endomeetrial effect is profoudly "progestational")
Combination Oral Contraceptives Prevent pregnancy by ___
inhibiting ovulation
Combination Oral Contraceptives

Early follicular phase FSH concentrations and midcycle peaks of FSH and LH are

a) observed
b) not observed
b) not observed
Combination Oral Contraceptives

The lower concentration of FSH results in

a) decreased ovarian function
b) increased ovarian function
c) decreased pituitary function
d) increased pituitary function
a) decreased ovarian function
Combination Oral Contraceptives

Missing how many doses during a cycle substantially increases risk of pregnancy?
two or more
Seems to me that
Combination Oral contraceptives prevent pregnancy in 3 general ways. What are they?
1) inhibit follicle maturation
2) inhibits ovum implantation in endometrium
3) inhibits sperm penetration by making cervix thicker and more mucus-y
Combination Oral Contraceptives:

They protect against ovarian cancer , but may cause what cancer?
endometrial

(Controversial.. later slide says it reduces endometerial cancer)
Combination Oral Contraceptives:

50% decrease in _____ breast disease
fibrocystic
21 active pills, 2 days placebo, 5 days of 10 mg ethinyl estradiol alone

a) Mircette
b) Seasonale
c) Ovcon
d) Yasmin
a) Mircette
a) Mircette
b) Seasonale
c) Ovcon
d) Yasmin
d) Yasmin
84 consecutive hormonal pills followed by 7 days placebo

a) Mircette
b) Seasonale
c) Ovcon
d) Yasmin
b) Seasonale
chewable pills (COC)

a) Mircette
b) Seasonale
c) Ovcon
d) Yasmin
c) Ovcon
Combination Oral Contraceptives - Side Effects

Risk of idiopathic venous thrombosis (2-6 fold greater)
is related to

a) combination
b) dose
b) dose
Combination Oral Contraceptives - Side Effects


Increased BP is related more to

a) progestin
b) estrogen
c) LH
d) FSH
b) estrogen
Combination Oral Contraceptives - Side Effects

Cervical cancer risk in some users (use greater than how many yrs?)
5
Combination Oral Contraceptives - Side Effects

Effect on milk production

a) increases
b) decreases
b) decreases
Combination Oral Contraceptives - Side Effects

Contraindicated in what conditions?
History of thrombophlebitis
Coronary artery or cerebrovascular disease
Suspected pregnancy
Undiagnosed abnormal genital bleeding
Carcinoma of breast, cervix, uterus, vagina
Problems with Progestin-Only Contraception
Slightly higher failure rate (2-3 per 100 women-yrs)
Higher incidence of irregular bleeding
Suppresses FSH and LH to variable degrees
Progestin-Only Contraception produces endometrial

a) hypertrophy
b) hypotrophy
c) atrophy
c) atrophy
Medroxyprogesterone is not approved in the USA b/c why?
breast tumors in beagles
Progestin-Only Contraception can be used in the USA for what conditions?
treatment of advanced endometrial and renal carcinoma and endometriosis
Side effects of Progestin-Only Contraception
Breakthrough bleeding, spotting
Amenorrhea
Edema
Weight gain
Bloating
Mood changes
Decreased HDL and increased LDL
Which Oral Contraceptive?

Endometriosis-
need strong progestin to create a pseudo-pregnancy state
Which Oral Contraceptive?

Functional ovarian cysts
high dose monophasic pill may be more effective
Which Oral Contraceptive?

Androgen excess
high estrogen/progestin ratio to reduce free testosterone and inhibit 5 alpha reductase activity
Which Oral Contraceptive?

Breastfeeding
progestin only pill
Transdermal: what's it called?
Ortho Evra
What's in Ortho Evra?
Delivers 20 mcg ethinyl estradiol and 150 mcg on norelgestromin daily
What's NuvaRing?
Vaginal contraceptive ring
What's in NuvaRing?
15 mcg ethinyl estradiol and 120 mcg of desogestrel
What's the failure rate of Nuva Ring?
Failure rate of typical use: 8%
What's Depo Provera?
150 mg IM q 3 months
how long does Depo Provera last?
Contraceptive level maintained for 14 weeks
What is mechanism of DepoProvera?
Thickens cervical mucous
Blocks LH surge
Initiate treatment during first week of menses
Advantages of Depo Provera
Long acting
Estrogen-free
Safe during breast feeding
Increases milk quality
Disadvantages of Depo Provera
Irregular bleeding (70% in first year)
Breast tenderness
Weight gain
Depression
Slow return of menses after stopping use
Decreases HDL
Postcoital Contraception must be given in what time frame?
72 hours
How does pstcoital contraception work
Endometrium is made nonreceptive to implantation by high dose of hormone
Contragestation:

Give example,
How does it work,
what are side effects?
Mifepristone (RU 486)
Synthetic potent antiprogestin
Binds to progesterone receptor
Well tolerated
Occasional prolonged uterine bleeding
________ acts as an antiestrogen at the hypothalamus to increase pulse frequency of LH
Clomiphene
Endometriosis results from what?
ectopic endometrial cell implants outside the uterus
Goal of therapy for endoetriosis
to induce a hormone-poor environment (especially low estrogen) to inhibit growth of implants
Agents used to treat endometriosis include
Danazol
Progestins
Gonadotropin-releasing hormone or analogs
What does Danazol do?
Inhibits either LH/FSH surge

Produces amenorrhea and relief of pain without decreasing basal concentrations of gonadotropins or estrogen
What's Tamoxifen?
therapy that reduces estrogen


Antiestrogen