Estrogens/Progestins Pharmacology

What are estrogens?

estradiol > estrone > estriol

What is the most potent estrogen?

estradiol

What is the hormonal control of the menstrual cycle?

GnRH from anterior pituitary secrete FSH and LH

What is the process of the menstrual cycle?

each follicle contains ovum (immature egg), during ovulation it releases egg for fertilization, ovum travels through fallopian tubes to uterus where fertilized ovum is implanted into uterus

What are gonadotropins?

secreted by anterior pituitary = FSH, LH

What is GnRH?

secreted by hypothalamus

Where are estrogens/progesterones secreted from?

by ovary, placenta, cervix, and adrenal cortex

How is estrogen secreted during the menstrual cycle?

GnRH stimulates FSH release which stimulates follicle development/estrogen production and secretion

What does estrogen cause?

proliferative phase/endometrial regeneration, cervical mucus pH increase = conducive to sperm passage, LH surge mid-cycle

How is progesterone released during the menstrual cycle?

LH triggers ovulation, ruptured follicle becomes corpus luteum which secretes progesterone

What does progesterone cause?

secretory phase, endometrium suitable for fertilized egg to implant, cervical mucus viscous/interferes with sperm passage

What is the purpose of follicular phase?

estrogen synthesis

What is the purpose of the luteal phase?

progesterone and estrogen synthesis

What does high levels of progesterone/estrogen cause?

feedback inhibition of FSH/LH release

What occurs during pregnancy?

progesterone causes feedback inhibition of GnRH/FSH/LH release, thickened cervical mucus, supports endometrial growth/uterine environment to maintain pregnancy, chorion secretion

What is the purpose of chorion in pregnancy?

secretes hCG and becomes placenta

What does the placenta secrete during pregnancy?

estrogen, progesterone, gonadotropins = FSH/LH in small quantities

What occurs during lactation?

progesterone controls development of alveoli mammary glands, estrogen stimulates milk production

What are reproductive effects of estrogen?

promote growth/development of female reproductive organs, reproduction/endometrial lining, stimulates synthesis of progesterone receptors, regulate menstrual cycle in absence of pregnancy

What are non-reproductive/CV effects effects of estrogen?

increase HDL/TG, decrease LDL

What are non-reproductive effects of estrogen?

increase bone strength by decrease bone resorption, increase protein metabolism by liver, increase blood coag = VTE risk

What is the effect of female sex hormones during pre-puberty?

support overall organ development and bone growth

What is the effect of female sex hormones at puberty?

menstruation begins, maturation of reproductive organs, secondary sexual characteristics, accelerated growth

What is the effect of female sex hormones post puberty?

reproduction = pregnancy, childbirth, lactation

What is the effect of female sex hormones in menopausal women?

cessation of menstruation, bone loss

What is the purpose of estrogens/progesterones as contraceptives?

prevent conception and prevent implantation

What is the main mechanism for estrogens/progesterones as contraceptives?

negative feedback on LH/FSH = prevent ovulation, inhibit sperm mobility by causing thick/viscous cervical mucus

What are the secondary mechanisms for estrogens/progesterones as contraceptives?

abnormal ovum transport, abnormal endometrium growth = reduce implantation

What is amenorrhea?

absence of periods

What is oligomenorrhea?

irregular menstruation

What is infertility?

inability to get pregnant

What is infertility due to?

low female sex hormone levels

What is the purpose of anti-estrogens for infertility?

prevent feedback inhibition of FSH/LH release by binding estrogen receptors in pituitary/hypothalamus/ovary/endometrium/cervix

What are conditions associated with infertility?

PCOS, endometriosis

What is PCOS?

enlarged ovaries/cysts on outer edges of uterus, androgen excess = hair growth/acne, obesity, irregular menstruation

What is endometriosis?

abnormal growth of endometrial tissue outside uterus = physical barrier, egg can't get through fallopian tubes

What is menopause?

permanent cessation of menstruation due to loss of ovarian follicular function including oocyte maturation and steroidogenesis

What is menopause characterized by?

vaginal dryness, hot flashes, UTI, bone loss