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88 Cards in this Set
- Front
- Back
What inhibits FSH and LH (gonadotropin) release in a woman?
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Estrogens
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_____ cells of ovary release estrogen
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granulosa
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surge of what stimulates ovulation
a) LH c) FSH c) estrogen |
a) LH
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Why does ant pit stop making gonadotropins during cycle?
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corpus luteum makes estrogen and progesterone
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What are phyto-estrogens?
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plant estrogen
(used as dietary supplement or cream used to enlarge breasts) |
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What is conjugation?
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conversion of compound to large bulky compoiund that is more water soluble and more easily excreted.
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Three Natural Human Estrogens
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17b estradiol (principal ovarian estrogen)
Estriol (principal placental estrogen) Estrone (metabolite of 17b estradiol and major ovarian and postmenopausal estrogen) |
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How are hormones transported to target tissues?
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complexed with proteins
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Estrogens are carried by ____
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sex hormone-binding globulin
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Progesterone is carried by _____
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corticosteroid-binding globulin
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Actions of Estrogens
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Reg of repro tract, pit and breasts during cycle
role in some tumor growth Incr water and Na retention Decr bowel motility |
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Effects of Estrogen
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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 |
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Estrogen's effect on LDL formation
a) inhibits b) stimulates c) no effect |
a) inhibits
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Estrogen's effect on HDL production
a) inhibits b) stimulates c) no effect |
b) stimulates
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Estrogen's effect on blood clotting factors production
a) inhibits b) stimulates c) no effect |
b) stimulates
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What progestins have weak progestational activity?
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17a-, 20a-, and 20b-hydroxypro-gesterone
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Progesterone concentrations rise rapidly in ______ phase of menstrual cycle
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luteal
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Progesterone's effect on temperature during luteal phase of cycle
a) increases b) decreases c) no effect |
a) increases
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Progesterone's effect on HDL production
a) increases b) decreases c) no effect |
b) decreases
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Progesterone's effect on LDL production
a) increases b) decreases c) no effect |
a) increases
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Progesterone'e effect on Na and H2O retention?
a) increases b) decreases c) no effect |
b) decreases
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Progesterone's effect on endometrial lining?
a) maintains it b) sloughs it c) no effect |
a) maintains it
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Conditions calling for HRT with Estrogens and progesterone
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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) |
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What is clomiphene citrate used for?
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Ovulation induction
Infertility |
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Natural estrogens (3)
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Estradiol (most potent)
Estrone Estriol |
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Problems with administering natural estrogens
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Low oral potency
Poorly absorbed and rapidly inactivated by liver |
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Conjugated Estrogens Prepared from pregnant mare’s urine (3)
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Estrogen
Equilin (found in horses but not humans) Estrone |
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Pluses to conjugated estrogens
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Water soluble with virtually no estrogenic activity until activated by hydrolyzation
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Synthetic Steroidal Estrogens
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Ethinyl estradiol
Mestranol (converted to ethnyl estradiol by liver) Estropipate Quinestrol |
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Which estrogens are Used predominantly as oral contraceptives
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Synthetic Steroidal Estrogens
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Parenteral Synthetic Steroidal Estrogens
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Estradiol cypionate
Estradiol valerate Polyestradiol phosphate |
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Synthetic Non-Steroidal Estrogens
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Diethylstilbesterol
Chlorotrianisene Dienestrol |
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Progestins
(maybe disregard this card) |
Progesterone
17a-hydroxyprogesterone Medroxyprogesterone acetate Megestrol acetate Hydroxyprogesterone caproate Levonorgestrel Norgestrel Norethindrone Norethindrone acetate Norethynodrel Ethynodiol diacetate |
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Most effective reversible method
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Combination Oral Contraceptives
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Failure rate of combination oral contraceptives
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is less than 0.7 per 100 women
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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 |
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What decreases the incidence of adverse side effects of combination oral contraceptives
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low dose estrogen
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Most common formulations consist of 21 days of combination with how many days off for withdrawal bleeding?
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7
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Oral Contraceptives: MOA
Progestin primarily suppresses a) LH b) FSH c) estrogen |
a) LH
(prevents menstruation) |
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Oral Contraceptives: MOA
Estrogen suppreses a) LH b) FSH c) progestin |
b) FSH
(prevents emergence of dominant follicle) |
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Oral Contraceptives: MOA
What is estrogen's effect on endometrium? |
stabilizes
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Oral Contraceptives: MOA
What is estrogen's effect on progestin? |
postentiates the progestin action
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Oral Contraceptives: MOA
Progestin's effect on endometrium? |
makes endometrium not receptive to ovum implantation
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Oral Contraceptives: MOA
Which is the dominant hormone? |
progestin
(endomeetrial effect is profoudly "progestational") |
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Combination Oral Contraceptives Prevent pregnancy by ___
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inhibiting ovulation
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Combination Oral Contraceptives
Early follicular phase FSH concentrations and midcycle peaks of FSH and LH are a) observed b) not observed |
b) not observed
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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
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Combination Oral Contraceptives
Missing how many doses during a cycle substantially increases risk of pregnancy? |
two or more
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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 |
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Combination Oral Contraceptives:
They protect against ovarian cancer , but may cause what cancer? |
endometrial
(Controversial.. later slide says it reduces endometerial cancer) |
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Combination Oral Contraceptives:
50% decrease in _____ breast disease |
fibrocystic
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21 active pills, 2 days placebo, 5 days of 10 mg ethinyl estradiol alone
a) Mircette b) Seasonale c) Ovcon d) Yasmin |
a) Mircette
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a) Mircette
b) Seasonale c) Ovcon d) Yasmin |
d) Yasmin
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84 consecutive hormonal pills followed by 7 days placebo
a) Mircette b) Seasonale c) Ovcon d) Yasmin |
b) Seasonale
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chewable pills (COC)
a) Mircette b) Seasonale c) Ovcon d) Yasmin |
c) Ovcon
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Combination Oral Contraceptives - Side Effects
Risk of idiopathic venous thrombosis (2-6 fold greater) is related to a) combination b) dose |
b) dose
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Combination Oral Contraceptives - Side Effects
Increased BP is related more to a) progestin b) estrogen c) LH d) FSH |
b) estrogen
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Combination Oral Contraceptives - Side Effects
Cervical cancer risk in some users (use greater than how many yrs?) |
5
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Combination Oral Contraceptives - Side Effects
Effect on milk production a) increases b) decreases |
b) decreases
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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 |
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Problems with Progestin-Only Contraception
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Slightly higher failure rate (2-3 per 100 women-yrs)
Higher incidence of irregular bleeding Suppresses FSH and LH to variable degrees |
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Progestin-Only Contraception produces endometrial
a) hypertrophy b) hypotrophy c) atrophy |
c) atrophy
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Medroxyprogesterone is not approved in the USA b/c why?
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breast tumors in beagles
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Progestin-Only Contraception can be used in the USA for what conditions?
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treatment of advanced endometrial and renal carcinoma and endometriosis
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Side effects of Progestin-Only Contraception
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Breakthrough bleeding, spotting
Amenorrhea Edema Weight gain Bloating Mood changes Decreased HDL and increased LDL |
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Which Oral Contraceptive?
Endometriosis- |
need strong progestin to create a pseudo-pregnancy state
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Which Oral Contraceptive?
Functional ovarian cysts |
high dose monophasic pill may be more effective
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Which Oral Contraceptive?
Androgen excess |
high estrogen/progestin ratio to reduce free testosterone and inhibit 5 alpha reductase activity
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Which Oral Contraceptive?
Breastfeeding |
progestin only pill
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Transdermal: what's it called?
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Ortho Evra
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What's in Ortho Evra?
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Delivers 20 mcg ethinyl estradiol and 150 mcg on norelgestromin daily
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What's NuvaRing?
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Vaginal contraceptive ring
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What's in NuvaRing?
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15 mcg ethinyl estradiol and 120 mcg of desogestrel
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What's the failure rate of Nuva Ring?
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Failure rate of typical use: 8%
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What's Depo Provera?
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150 mg IM q 3 months
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how long does Depo Provera last?
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Contraceptive level maintained for 14 weeks
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What is mechanism of DepoProvera?
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Thickens cervical mucous
Blocks LH surge Initiate treatment during first week of menses |
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Advantages of Depo Provera
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Long acting
Estrogen-free Safe during breast feeding Increases milk quality |
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Disadvantages of Depo Provera
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Irregular bleeding (70% in first year)
Breast tenderness Weight gain Depression Slow return of menses after stopping use Decreases HDL |
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Postcoital Contraception must be given in what time frame?
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72 hours
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How does pstcoital contraception work
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Endometrium is made nonreceptive to implantation by high dose of hormone
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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 |
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________ acts as an antiestrogen at the hypothalamus to increase pulse frequency of LH
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Clomiphene
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Endometriosis results from what?
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ectopic endometrial cell implants outside the uterus
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Goal of therapy for endoetriosis
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to induce a hormone-poor environment (especially low estrogen) to inhibit growth of implants
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Agents used to treat endometriosis include
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Danazol
Progestins Gonadotropin-releasing hormone or analogs |
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What does Danazol do?
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Inhibits either LH/FSH surge
Produces amenorrhea and relief of pain without decreasing basal concentrations of gonadotropins or estrogen |
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What's Tamoxifen?
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therapy that reduces estrogen
Antiestrogen |