Progestins, Estrogens, Androgens Flashcards
follicular phase
- phase of the menstrual cycle in which female follicles develop and mature
- ends with ovulation around day 14 of the cycle
- main hormone controlling this phase is estradiol
- progesterone levels are low during this phase
luteal phase
- phase of menstrual cycle that occurs after ovulation
- formation of corpus luteum and ends with pregnancy or menstruation
- brought on by stimulatory effects of estradiol midway through cycle which stimulates LH spike
- LH spike stimulates production of progesterone
androstenedione
- androgen precursor to estrone
- produced in female theca cells
- converted to estrone in granulosa cells via action of aromatase
granulosa cells
-cells in a female required to convert androgens to various estrogens via action of aromatase
theca cells
-cells located outside of ovarian follicle who’s primary function is the conversion of cholesterol to androgens through the action of various CYP enzymes
estriol
-form of estrogen produced in the ovary
DHT (dihydrotestosterone)
-more potent form of androgen produced by the action of 5a-reductase which converts testosterone to DHT in other tissues outside of testes
aromatase
-enzyme responsible for conversion of androgens to estrogens in the granulosa cells of a female and the testes of a male
5a-reductase
-enzyme responsible for the conversion of testosterone to DHT in tissues outside of the testes
drospirenone
Progestin
- used in combo progestin/estrogen oral contraceptives
- has enhanced activity as MC antagonist and androgen antagonist
progesterone
Progestin
- most important progesterone in humans
- rapidly inactivated when given orally
- decreases the amount of cervical mucous and increases its viscosity
- main determinant of onset of menstruation
medroxyprogesterone acetate (Depo-Provera)
Progestin analog
- commonly used in progestin only contraceptives
- given as IM injections q 3 months
- MOA: prevents fertilization by dec. amount and inc. the viscosity of cervical mucous (mimics normal progesterone, but at higher doses and without interruption)
- Secondary MOA: prevents ovulation by inhibiting gonadotropin secretion (mimics inhibitory effects of progesterone on gonadotropin secretion)
- S/Fx: headaches, abn. menstrual bleeding, dec. bone density with depo-provera
norethindrone (Micronor)
Progestin
- commonly used in progestin only contraceptives or in combo oral progestin/estrogen contraceptives (monophasic to triphasic)
- given as daily oral treatment or in IUDs implanted for 1-5 years (among most effective methods)
- main MOA when progestin only: prevents fertilization by dec. amount and inc. the viscosity of cervical mucous (mimics normal progesterone, but at higher doses and without interruption)
- main MOA when combo: prevents ovulation by inhibiting gonadotropin secretion (mimics inhibitory effects of progesterone and estrogen on gonadotropin secretion)
- S/Fx: nausea, headaches, CV risks such as MI and thrombus (not recommended for smokers 35 and older), dec. glucose tolerance, weight gain, acne
norgestrel (Ovrette)
Progestin
- commonly used in progestin only contraceptives
- given as daily oral treatment or in IUDs implanted for 1-5 years (among most effective methods)
- MOA: prevents fertilization by dec. amount and inc. the viscosity of cervical mucous (mimics normal progesterone, but at higher doses and without interruption)
- Secondary MOA: prevents ovulation by inhibiting gonadotropin secretion (mimics inhibitory effects of progesterone on gonadotropin secretion)
- S/Fx: headaches, abn. menstrual bleeding, dec. bone density with depo-provera
ulipristal (Ella)
Selective Progestin Response Modulator (SPRM)
- effective oral emergency contraceptive if used within 5 days of intercourse (prescription required)
- more effective then norgestrel (plan-b)
- inhibits ovulation by antagonizing the actions of progesterone on the granulosa cell progesterone receptor (this action needed for follicular rupture)
- also a progesterone agonist in the pituitary/hypothalamus and it delays LH surge
RU 486 (mifepristone)
Progestin Receptor Antagonist
- oral, used for abortions (followed by oral prostaglandin)
- used for post-coital contraception due to antagonizing effects of progesterone receptors everywhere including endometrium (progesterone normally required for implantation and maintenance of pregnancy)
- also GC antagonist and is approved to be used as such in tx of Cushings and DM type II
FSH (Gonal-F)
Gonadotropin
- IM injection used to induce follicular growth
- commonly used prior to in vitro fertilization
CG (Pregnyl)
Gonadotropin
- IM injection used to induce ovulation
- time sensitive admin based on growth of follicle
gonadorelin
Synthetic GnRH
- stimulate gonadotropin secretion
- Tx: delayed puberty and anovulatory D/O in women.
- Single injection or pulsatile pump
luprolide
Long acting GnRH Agonist
-causes initial increases in androgen production, followed by a suppression of release of androgens (remember: give with flutamide)
cetrorilex
GnRH antagonist
- stop gonadotropin secretion
- Prepercocious puberty in boys, endometriosis and dysmenorrhea.
testosterone
Androgen
- product of the hypothalamus-pituitary-testicular axis.
- ineffective PO
- Use: replacement for hypogonadism
- Adverse: Virilization, feminization (males), azoospermia, small BALLS, edema, jaundice, hepatic carcinoma.
testosterone proprionate
Androgen
-testosterone with a carboxy group (ester form).
danazol
Androgen: 17 alpha alkylated adrogen
- product of the hypothalamus-pituitary-testicular axis.
- Contains OH group making it orally active, but increased liver toxicity
- Use: replacement for hypogonadism
- Adverse: Virilization, feminization (males), azoospermia, small BALLS, edema, jaundice, hepatic carcinoma.
methytestosterone
Androgen: 17 alpha alkylated adrogen
- product of the hypothalamus-pituitary-testicular axis.
- Contains OH group making it orally active, but increased liver toxicity
- Use: replacement for hypogonadism
- Adverse: Virilization, feminization (males), azoospermia, small BALLS, edema, jaundice, hepatic carcinoma.
dutasteride
Anti-androgen: 5-alpha reductase inhibitor
- Used to treat androgen excess or androgen dependent D/O: BPH, prostate CA, Hurtuism, CAH
- S/E: persistent sexual dysfunction
finasteride
Anti-androgen: 5-alpha reductase inhibitor
- Used to treat androgen excess or androgen dependent D/O: BPH, prostate CA, Hurtuism, CAH
- S/E: persistent sexual dysfunction
bicalutamide
Anti-androgen: Androgen receptor antagonist
- Used to treat androgen excess or androgen dependent D/O: BPH, prostate CA, Hurtuism, CAH
- S/E: persistent sexual dysfunction
flutamide
Anti-androgen: Androgen receptor antagonist
- Used to treat androgen excess or androgen dependent D/O: BPH, prostate CA, Hurtuism, CAH
- S/E: persistent sexual dysfunction
nilutamide
Anti-androgen: Androgen receptor antagonist
- Used to treat androgen excess or androgen dependent D/O: BPH, prostate CA, Hurtuism, CAH
- S/E: persistent sexual dysfunction
estradiol
estrogen
-rapidly inactivated when given orally
ethinyl estradiol
estrogen
contraceptive agent often used in combination with northindrone
-Oral (21 days on, 7 days off)
prevent ovulation by inhibiting the hypothalamus & pituitary
-mimic inhibitory effects of estrogen on gonadotropin secretion in high doses
-adverse effects: nausea, headache, thromboembolism, MI, decreased glucose tolerance, weight gain, acne, hirstism
-health benefits: decreased incidience of ovarian cyst & benign fibrocystic breast disease, & endometrial/ovraian CA, increased HDL and decreased LDL
estrone sulfate
estrogen
diethylstilbestrol
estrogen
no longer on the market
bazedoxifene
SERM
with conjugated estrogens, approved for the treatment of postmenopausal symptoms
-agonist effects on bone
-antagonist effect on breast and endometrium
tamoxifen
SERM
- relief of postmenopausal symptoms
- treatment of osteoporosis
- estrogen-dependent breast cancer
raloxifene
SERM
- relief of postmenopausal symptoms
- treatment of osteoporosis
- estrogen-dependent breast cancer
ospemifene
SERM
- treatment of vaginal atrophy in postmenopausal women
- agonist effects on vaginal epithelium
clomiphene
estrogen receptor antagonist
- induce ovulation, when given early in the follicular phase of the menstrual cycle
- antagonize the inhibitory effects of estrogen on the pituitary & hypothalamus
fulvestrant
estrogen receptor antagonist
- induce ovulation, when given early in the follicular phase of the menstrual cycle
- antagonize the inhibitory effects of estrogen on the pituitary & hypothalamus
anastrozole
aromatase inhibitor
- oral, non-steroidal
- inhibit conversion of androgens to estrogens
- useful in the treatment of breast CA or disorders where estrogen action needs to be inhibited
- only give to postmenopausal women
- can induce ovulation
- side effects: arthralgia, hot flashes, other postmenopausal symptoms
exemestane
aromatase inhibitor
- oral, steroidal
- inhibit conversion of androgens to estrogens
- useful in the treatment of breast CA or disorders where estrogen action needs to be inhibited
- only give to postmenopausal women
- can induce ovulation
- side effects: arthralgia, hot flashes, other postmenopausal symptoms
