65: Estrogens & Progestins Flashcards
LH –>
FSH –>
theca cell
granulosa cell
estrogen and progesterone exert both negative and positive feedback to regulate gonadotropin release. positive feedbcack occurs…
mid-ovarian cycle which induces ovulation
- high frequency low amplitude LH secretion
- estrogen rises
- endometrial proliferation
follicular phase (1-13)
estrogen induced gonadotropin surge
ovulation (d. 14)
- rise in estrogens and progesterone
- endometrial differentiation under control of progesterone
luteal phase (15-28)
if implantation does not occur…
steroidogenesis is not maintained and endometrial lining is shed
endometrial proliferation v differentiation
estrogen
progesterone
progesterone also prepares for implantation, decreases uterine contractions
increase LDL increase fat deposition
progesterone - also increases fasting glucose levels
estrogen decreases LDL and increases HDL and triclycerides
estrogen also antiresorptive in bone, increases plasma prtns from liver and increases expression of coagulation factors and decreases antithrombin in blood
key regulator during follicular phase =
luteal phase =
estrogen
progesterone
- decreases uterine contractions and porstaglandin production
- maintains relaxin secretion
- increases viscosity of cervical mucous
progesterone
synthetic steroidal estrogens
ethinyl estradiol
mestranol
risks from using estrogen in HORMONE REPLACEMENT THERAPY
increased risk CAD, Stroke, PE, invasive BC
decreased risk colorectal CA, hip fracture
MOA estrogens as contraceptive
suppress ovulation via negative feedback
MOA estrogen as acne treatment
suppress steroidogenesis and decrease free testosterone concentrations by increasing levels of SHBG
4 pharmacological uses of estrogen
hypogonadism
HRT
contraception
acne
key adverse effects of estrogen
breast tenderness
endometrial hyperplasia
increased blood coagulation
cancer risks
- HRT combo therapy
- HRT estrogen monotherapy
- contraceptive
increased risk invasive BC
increased risk of endometrial CA
reduced risk of ovarian and endometrial CA
adverse effects of estrogen : what is their rationale? endometrial hyperplasia cholestasis increaseed blood coagulation migraine cancer bloating
- estrogen induced endometrial proliferation
- changes in cholesterol bile salt ration and changes in hepatic bile caniculi function
- decreases antithrombin and increases factors II, VII, IX, X
- potential sign of increased blood coagulation
- endometrial and breast CA
- loss of intravascular fluid
never give ______ alone for birth control
estrogen
- commonly combined with estrogen for HRT
- used as a long acting contraceptive (depo-provera)
medroxyprogesterone
-combinational or progestin only contraception
norethindrone or norgestrel
____ less efficacious in suppressing ovulation
progestins
but work just as well in contraception because of increasing mucous viscosity as well
therapeutic uses of progestins:
- contraceptive
- HRT
- dysmenorrhea
- endometriosis
- alone or in combo with estrogen
- decrease risk of endometrial hyperplasia caused by estrognes
- decrease endometrial mass and decrease prostaglandin production
- decrease endometrial proliferation by regulating ER expression and stimulating differentiation of endometrial cells
key adverse effects progestins
- breakthrough bleeding - changes in enometrial vasculature
- impaired glucose tolearnace (increased fasting glucose)
- changes in lipid metabolism (opposite effect on LDL and HDL compared to estrogen*) (increase LDL and decrease HDL)
adverse effects related to 19-nortestosterone effects
- acne
- hirsutism
because of teh androgenic effects of synthetic progestins (19 nor testosterone derivative)
birth control treat acne with ____, cause acne with _____
estrogen
19 nor compounds
“type” of hormone birth control and related hormone
A. oral pill B. injectable C. implantable D. IUD E. Transdermal F. Vaginal Rign
A = estrogens and progestins or progestins alone (monthly, quarterly, or yearly)
B= estrogens and progestins or progestins alone (monthly or quarterly)
C= progestins alone (3 year)
D = progestins alone or copper (5 year)
E = estrogens and progestins (monthly)
G = estrogens and progestins (monthly)
oral pill can never be…
estrogen alone
mechanism of action for hormone birth control
suppress LH and FSH surge
alter cervical mucus
alter endometrium
emergency contraceptives (2) which is favored?
levlen - hormone combo
plan B - leonorgestrel (progestin only) **favored because lower failure rate
contraindications of estrogen containing contraceptives
history of breast cancer or cancer of female reproductive tract
thromboembolic disorders
liver disease
history of cardiovascular disease
smokers 35 yo+
interactions with hormone birth control
- HIV agents
- St Johns wort (induce hormone metabolism)
- anticonvulsants
- antibiotics lower contraceptive effectiveness
