Estrogens and Progestins Flashcards
Two cells of steroidogenesis in females
regulatory molecules (2)?
Theca
Granulosa
gonadotropins, LH and FSH
Steroidogenesis regulated by what?
feedback regulation
Estrogen and Progesterone exert what types of feedback?
both NEGATIVE AND POSITIVE
Positive occurs MID-OVARIAN CYCLE (day 14)
Phases of Menstrual Cycle
associated hormones (2)? What does each control?
Follicular - estrogen rises, low amplitude LH secretion
Ovulation - estrogen induced gonadotropin surge
Luteal - rise in estrogen and progesterone,
progesterone controls DIFFERENTIATION
Estrogen controls PROLIFERATION
Endogenous steroids bind to?
INTRACELLULAR RECEPTORS - modulate transcriptional activity
AGONISTS/ANTAGONISTS COMPETE FOR INTRACELLULAR SITES
Estrogen effects - HPG Axis? Endometrium? Metabolic? Development? Menstrual cycle?
feedback regulation on HPG axis
proliferation of endometrium
Good cholesterol effects
Anti-resorptive for bone
Increase plasma proteins from liver
Increase coagulation factors, decrease anti-thrombin
Ovary, fallopian tubes, uterus, vagina, breast development
FOLLICULAR PHASE of cycle
Progesterone effects - - HPG Axis? Endometrium? Metabolic? Development? Menstrual cycle? Cervical Glands?
feedback regulation on HPG axis
DIFFERENTIATION of endometrium, decrease uterine contraction
Bad cholesterol effects
Increase fasting glucose
Ovary, fallopian tubes, uterus, vagina, breast development
LUTEAL PHASE of cycle
INCREASE CERVICAL MUCOUS VISCOSITY
Natural steroidal estrogens
Estradiol
Estrone
Estriol
Conjugated equine estrogens
Synthetic steroidal estrogens
Chemical modification has what effect?
Ethinyl estradiol
Mestranol
INCREASES HALF-LIFE
ethinyl group - DECREASES 1st PASS EFFECT
Dosing of natural vs synthetic
HIGHER DOSAGE FOR NATURAL ESTROGENS
Estrogen therapy in hypogonadism goals
promote development of female sex characteristics
Estrogen therapy in hormone replacement goals
HPG axis - feedback on gonadotropins
Endometrium proliferation
Anti-resorption of bone
Development
maintain bone density, suppress hot flashes, suppress urogenital atrophy
Estrogen Risks and Benefits
increased risk of coronary heart disease, stroke, PE, invasive breast cancer
decreased risk of colorectal cancer, hip fracture
Estrogen therapy in contraception goals
NEGATIVE FEEDBACK PRESSURE ON HPG AXIS
progestins are not as effective
Estrogen therapy in acne treatment
may suppress steroidogenesis
increase SHBG production in liver - DECREASING FREE TESTOSTERONE
ESTROGENIC COMPONENT, not progestin component suppresses acne
Adverse effects of estrogen
breast tenderness
endometrial hyperplasia
increased blood coagulation
nausea, cholestasis, migraine, cancer, bloating
Progestin use as contraceptive
alone or in combination with estrogen
negative feedback on HPG axis
Increases cervical mucous viscosity
Mechanisms of Progestin use in Hormone replacement therapy, dysmenorrhea, and endometriosis
HRT - decrease risk of endometrial hyperplasia
Dysmenorrhea - decrease endometrial mass, decrease prostaglandin production
Endometriosis - decrease proliferation
Adverse Effects of progestins
Adverse related to 19-nor compounds
breakthrough bleeding
impaired glucose tolerance
changes in lipid metabolism
19-Nor compounds – acne, hirsutism
Mechanism of Action of Birth control
suppress LH and FSH
Alter cervical mucous
Alter endometrium
Oral pill - hormones? Injectable? Implantable? IUD? Transdermal? Vaginal Ring?
oral - estrogens and progestins or progestins alone
injectable - estrogens and progestins or progestins alone
implantable - progestins alone
IUD - progestins + copper
Transdermal - estrogens and progestins
Vaginal ring - estrogens and progestins
Emergency contraception effectiveness
Combined - 25% failure
Progestin only - 12% failure
Contraceptive Hormone Adverse Effects - 3 categories? Name some from each
Mild - nausea, mastalgia, breakthrough bleecding, edema, headache, withdrawal bleeding, serum protein changes
Moderate - breakthrough bleeding, weight gain, skin pigmentation, acne, hirsutism, vaginal infections, amenorrhea
Severe - thromboembolic disease, MI, cerebrovascular disease, GI, depression, cancer?
Non-contraceptive benefits of hormone birth control
reduced ovarian/endometrial cancer
reduce dysmenorrhea, endometriosis
decrease ectopic pregnancy
decrease benign breast disease
increase Hb concentrations
Suppress acne/hirsutism
Contraindications of estogen containing contraceptives
known or suspected breast cancer or female reproductive tract cancer
thromboembolic disorders
liver disease
history of CV disease
smokers aged 35 and older
Interactions of contraceptives
HIV agents, anti-convulsants, St. Johns Wort - INDUCE METABOLISM
Anti-biotics LOWER EFFECTIVENESS
