Estrogen and Progestins Flashcards
what progestin is progesterone derived? (others are 19-nor cmds)
medroxyprogesterone acetate (MPA)
what are the estrogen drugs
conjugated equine estrogens
diethylstilbestrol
estradiol
ethinyl estradiol
mestranol
what cells are required for estradiol synthesis
theca and granulosa
when does positive feedback from estrogen and progesterone occur? (otherwise its negative feedback)
mid-ovarian cycle (day 14) - induces ovulation
what phase is estrogen first synthesized? when is this phase?
follicular phase
- first 1/2 (days 1-13)
what induces ovulation
LH and FSH spike (day 14)
what phase is estrogen and progesterone synthesized
Luteal phase
2nd half (15-28 day)
what promotes proliferation of endometrial cells
estrogen
what promotes differentiation of the endometrium and supports implantation and decreases uterine contractions
progesterone
when does estrogen peak
day 11-13 –> causes LH surge
when does progesterone peak
luteal phase
natural water-soluble estrogen sulfate
conjugated equine estrogens
synthetic steroid estrogens
chemically modified estradiol
ethinyl estradiol
mestranol
1st synthetic non steroidal estrogen
DES
how can estrogen be used for hypogonadism
promotes development of ovaries, fallopian tubes, uterus, vagina, breasts
how can estrogen be used as a hormone replacement therapy
Target HPG axis and endometrium
Metabolic effects:
-bone: antiresorptive
Development:
- ovaries, fallopian tubes, uterus, vagina, breast
*decrease bone resorption/vasomotor sx/urogenital atrophy
what are risk of using hormone replacement therapy
Coronary heart disease
Stroke
PE
invasive breast cancer
decreases: colorectal cancer, hip fractures
how can estrogen be used to prevent contraception
Negative feedback pressure on HPG axis - suppression of LH/FSH surge
- inhibit ovulation
How can estrogen be used for acne tx
- may suppress steroidogenesis
- increase SHBG production by liver and decrease free testosterone concentrations
- Liver: increase plasma proteins
Adverse effects of estrogen are related to what physiological effects?
- breast tenderness
- endometrial hyperplasia
- increased blood coagulation
- endometrial proliferation
- blood: increase expression of coag factros, decreases AT
- development: breast
other SE of estrogen
- Nausea
- cholestasis
- migraine (sign of altered blood coag)
- cancer (endometrial and breast)
- bloating (loss of intravascular fluid)
HRT combination therapy has an increase risk of what cancer
invasive break canser (likely due to progestin not estrogen)
HRT estrogen monotherapy has increase risk of what cancer (only do if someone had a hysterectomy or early on during hypogonadism)
endometrial
contraceptive therapy has a reduced risk for what cancers
ovarian and endometrial cancer
Progestin that is commonly combined with estrogen for HRT
used as a long acting contraceptive
medroxyprogesterone (MPA)
combinational or progestine only hormone cnotraception
19-nortestosterone derivative
norgesterel
norethindrone
how can progesterone be used as a contraceptive agent (alone or in combo)
negative feedback on HPG axis (steoidgenesis and ovulation)
increase cervical mucous viscosity
How can progestins be used as HRT
***decrease risk of endometrial hyperplasia cuased by estrogens
How can progestins be used for dysmenorrhea
UTerus smooth muscle:
- decrease uterine contractions
- decrease prostaglandin production
- decrease endometrial mass
how can progestins be used for endometriosis
- decrease endometrial proliferation by regulating ER expression
and stimulating differentiation of endometrial cells.
SE of progestin related to key physiological effects
- breakthrough bleeding
- impaired glucose tolerance
- increase fasting glucose levels - change in lipid metabolism
- Lipids: increase LDL, increase fat deposition
other important SE related to 19-nortestosterone effects
- acne
2. hirsutism
how does estrogen effect lipids
decrease LDL
increase HDL
increase TG
MOA of BC
- inhibit ovulation
- inhibit follicle develoment
- disrupt normal endometrial growth and development
- change viscosity of cervical mucus
what type of oral use and parenteral use does progesterone only BC have
oral: monophasic, emergency
parenteral: injectable, implantable
what type of oral use and parenteral use does combined BC have
Oral: monophase, multiphasic, extended, emergency
parenteral: transdermal, injectable
what is postcoital BC
emergency
what percent of expected pregnancies were prevented when taken within 72 hours of intercourse
50%
when are you most loikely to get pregnant
1-2 days before ovulation (30%)
Contraindications for estrogen containing contraceptives
- known or suspect breast cancer or cancer of female reproctive tract (reduce risk of ovarian and endometrial cancer)
- Thromboembolitic disorders
- Liver disease
- history of CV disease
- Smokers 35 y/o or older
what drug interactions do estrogen containing BC have?
- HIV agents, anticonvulsants and St. John’s wort induce hromone metabolism
- antibiotics lower contraceptive effectiveness
what is the most effective BC
Implanon = 0.05
combo oral contraception
describe the difference in T1/2 of estradiol and estradiol ethinyl
Estradiol ethinyl = longer
decreases 1st pass effect
