women's health Flashcards
hypothalamus releases _______ onto anterior pituitary. AP releases ______ and ______
GnRH; gonadotrophs LH and FSH
what two cells does FSH work on? what does it do in each cell?
1) . stimulates development of ovarian follicles (granulosa cells)
2) . regulate spermatogenesis in testes (Sertoli cells)
what three things does LH do?
1) . causes ovulation and formation of corpus luteum in the ovary
2) . stimulates production of estrogen and progesterone by the ovary
3) . stimulates testosterone production by the testes
DHEA turns into ______________ by 3beta-hydroxysteroid dehydrogenase
androstenedione
androstenedione turns into _____________ (testes) and then that turns into ________ (ovaries)
testosterone; 17 beta-estradiol
in the ___________ cell, cholesterol turns into pregnenolone and then ____________
granulosa; progesterone
progesterone travels from the ____________ cell to the ________ cell to make ___________
granulosa; theca; androgens
androgens in the ________ cell travels to the __________ cell to be converted to ________
theca; granulosa; estrogens
what is the enzyme that converts androgens to estrogens?
aromatase
what enzyme is lacking during menopause? this causes lack of what hormone?
aromatase (bc granulosa cells are lacking); estrogen cant be made, only progesterone
estradiol is secreted by ______ and is ______ potent. this is the _________ estrogen in _____________ women
ovary; most potent; primary; pre-menopausal
what are the three types of estrogens?
estradiol (17 beta-estradiol), estrone, estriol
estrone is a __________ of estradiol; it has the __/___ potency of estradiol
metabolite; 1/3
estriol is a ____________ of estradiol. it is the primary estrogen after __________
metabolite; menopause
estrogen increases levels of what four clotting factors? what does this increase for pts?
2, 7, 9, 10; increases risk of blood clots
estrogen _________ HDL and _________ LDL
increases; decreases
estrogen decreases rate of bone ___________: _________ osteoblast activity (____________ osteocyte survival) and decreases number and activity of ___________. this effect on bone is important for _______________
resorption; increases and increases; osteoclast; homeostasis
estrogen is important for closure of what plates in males and females? starts closing upon 2 years of puberty in what sex?
epiphyseal; females
estrogen promotes __________ and _____ atherogenesis (in terms of blood vessels)
vasodilation; slows
estrogen binds to receptors in the ___________. when receptors are activated, they increase or decrease ____ __________
nucleus; gene transcription
what are the two types of estrogen receptors? does it matter which one we are targeting with drugs?
alpha and beta; no
where are ER alpha receptors found?
female reproductive tract, mammary gland, hypothalamus, endothelial cells, and vascular smooth muscle
where are ER beta receptors found?
highly expressed in prostate and ovaries; lower expression in lung, brain, bone, and vasculature
what two hormones share the same MOA?
estrogen and progestin
natural estrogens are derived from what two sources?
plant: saw palmetto or soybeans
animal: pregnant mares are a major commercial source of estrogen
what is the type of synthetic estrogen used for hormone replacement/contraception? what is different about this compared to estrogen the body normally makes?
ethinyl estradiol (prolonged DOA and higher potency)
micronized products have a large surface area for rapid absorption. what does this do for a drug?
increases its bioavailability
what does the ethinyl component in estrogen do to metabolism?
it inhibits first-pass metabolism (cleared more slowly)
estrogens undergo _______ hepatic metabolism and _____________ recirculation
rapid; enterohepatic (liver will see these substances twice)
what are estrogens highly protein bound to?
sex hormone binding globulin
what two ways is estrogen excreted? in what form is it excreted?
in the urine as estradiol, estrone, and estriol; in breast milk too, decreases the quality/quantity of human milk
estrogen has what impact on blood pressure?
increases it, because increases angiotensinogen synthesis and increases angiotensin II
why can estrogen cause thromboembolic disorders and gallbladder disease?
thromboembolic- increase hepatic synthesis of clotting factors
GB disease- increase cholesterol excretion in bile leading to gallstones
what are five contraindications to estrogens?
1) . estrogen dependent tumor (breast cancer or high risk of it)
2) . undiagnosed vaginal bleeding (could be due to CA)
3) . liver disease
4) . thromboembolic disease (anyone with hx of clots)
5) . heavy smokers (inc risk of blood clots)
clinical use of estrogen (weeds):
Contraception Dysmenorrhea Acne Primary hypogonadism Postmenopausal hormonal therapy Relieves genitourinary atrophy Relieves vasomotor instability Osteoporosis Insomnia and fatigue Mood changes Sexual function
what is the natural form of progestogen? what is this produced in response to? what secreted this in both males and females?
progesterone; LH
males: secreted by the testes
females: secreted by corpus luteum mostly during second half of menstrual cycle and placenta
what body organ synthesizes a small amount of progesterone in males and females?
adrenal cortex
MOA of progestogen?
same as all other steroid hormones
what is the main goal of progestogen?
promotes development of secretory endometrium to support implantation and embryo development
what does progestogen inhibit?
production of gonadotropin, preventing further ovulation
if conception occurs, does progestogen continue to be secreted?
yes, it maintains endometrium and reduces uterine contractions
what happens to progesterone production if there’s no conception?
corpus luteum progesterone production stops quickly and menstruation starts
what are the 7 progestogens?
Progesterone Medroxyprogesterone Levonorgestrel Norethindrone Norgestrel Norgestimate Drospirenone
what are the uses of progestogen: (5)
1) . contraception- alone or in combo with estrogen
2) . Hormone replacement therapy along with estrogen
3) . vasomotor symptoms- postmenopausal women who can’t use estrogen
4) . dysmenorrhea
5. endometriosis and infertility
ADRs of progestogens
HAs, inc appetite, inc weight gain, depression, fatigue, hair loss, acne/oily skin
breast fullness/tenderness is a sign of an ADR from what drug/hormone?
estrogen
acne and hirsutism are signs of ADRs for what drug/hormone?
progestin
cyclic weight gain and cyclic headache are signs of ADRs for what drug/hormone?
estrogen
what are the types of hormonal contraception? (7)
1) . minipill (progestin only)
2) . implant
3) . long acting IM injection
4) . combined oral pill
5) . 91-day oral combo
6) . combination patch
7) . contraceptive vaginal ring
what are the types of contraception (in general)? (6)
1) . periodic abstinence
2) . mechanical barriers
3) . hormonal contraception
4) . IUD
5) . sterilization (female/male)
6) . emergency contraception
what are the top four BEST contraceptive methods (two reversible/two irreversible)
reversible: Nexplanon/implant (0.05%), IUD (0.2-0.8%)
irreversible: vasectomy, female sterilization
what five methods of contraception are the middle tier in terms of effectiveness? what are their percent chance of pregnancy?
injectable, pill, patch, ring, diaphragm (6-12%)
what six things are categorized as the least effective contraceptive methods? what are their percent chance of pregnancy?
male condom (18%), female condom (21)%, withdrawal (22%), sponge, fertility awareness based methods, spermicide (28%)
what is the pharmacologic effect of hormonal contraception- estrogen and progestin?
estrogen/progestin inhibit LH/FSH and prevent estrogen surge (no estrogen surge = no LH surge = no ovulation
factors in selecting contraception (7)
1) . personal preference
2) . effect on menstrual pattern/bleeding
3) . childbearing plans
4) . pattern of sexual activity
5) . partner influences/concerns
6) . ability to acquire/use effectively
7) . tolerance for the medication
Nexplanon: rod coated with _________, provides contraception for ___ years. once pts get it removed, they return to ovulation _______ (usually within _______)
progestin; 3; return to ovulation quickly; 3 weeks of removal
what is the IM injection for contraception? how many days does it last? what hormone does it use?
medroxyprogesterone; 90 day; progestin
ADRs for IM injection (5, one main one)
1) . DELAY in return to fertility (6-12 months)
2) . amenorrhea or irregular bleeding
3) . weight gain
4) . HA
5) . acne
boxed warning for IM injection
women who have used for at least 5 years have significantly reduced BMD of lumbar spine/femoral neck (particularly after 15 yrs and if started before age 20)
is the boxed warning for IM injection reversible?
almost completely reversible, even after 4 or more years of drug
what are the two types of oral progestin?
norgestrel or norethindrone
a “missed dose of minipill” means you’re outside a ___ hr window. what do you do after a missed dose?
three; must use back up method for 48 hours
what are combo pills made up of?
estrogen- ethinyl estradiol
progestin- norgestimate, desogestrol, dienogest, ethyodiol (BEST)
-drospirenone (might have hyperkalemia)
-norgestrel, levonorgestrel, norethindrone (more ADRs)
what is the monophasic pill formulation? what are the two drug names?
constant dose every day for 21 days (estrogen/progestin), 7 days of no hormones +/- iron; ortho-cyclen, yasmin