sex hormones II Flashcards
Progesterone is produced by
corpus luteum
MOA of progesterone
Progesterone acts on nuclear protein receptors, which interact with DNA.
function of progesterone in the uterus
- converts endometrium to a secretory state
- maintains pregnancy
- suppresses contractility during pregnancy
Progestins come in what two types
- 19-nortestosterones
- progesterone derivatives
Uses of progestins
- contraception
- prevent endometrial hyperplasia in HRT
List the Antiprogestins
- Mifepristone
- Danazol
MOA of Mifepristone
- progesterone/glucocorticoid receptor antagonist
uses of Mifepristone
terminate pregnancy
use for Danazol
endometriosis
What is the combination pills: estrogen and progestin that you should know
Drospirenone/ethinyl estradiol (Yasmin, Yaz)
use of combination oral contraceptives
-
inhibit ovulation
- no LH surge
- Cause changes in cervical mucosa and endometrium that decreases implantation.
what part of the combination oral contraceptives initiates bleeding at the end of the cycle with its withdrawal
progestin
estrogen: progestin ratio is important. E:P ratio, estrogen stays the same and progestin increases content at each stage. List the three stages
- 1 stage: monophasic
- 2 stages: biphasic
- 3 stages: triphasic
estrogen given in off period of seasonique due to
- estrogen decreases uterine bleeding
Yaz is a comibination of ethinyl estradiol and drospirenone . MOA of drospirenone
a mineralcorticoid antagonist
advantages of ethinyl estradiol and drospirenone
- less water retention (bloating): FDA approved for PMDD
MOA of Natazia
bioidentical E2
Use for Progestin-only mini pills
- 87-98% effective for birth control
- used for adolescents and breast feeding mothers
- (prevents estrogen effects on bone growth)
- used for adolescents and breast feeding mothers
progestin-only long term therapy causes
early breakthrough bleeding, later amenorrhea
adverse effects of combination oral contraceptives
- common
- weight gain
- nausea
- edema
- depression
- breakthrough bleeding
- progestin alone or too little estrogen
- cardiovascular
- clotting
- women over 35 or smoker
- mild HTN
- migrain
- MI/stroke
- clotting
- Teratogenesis
- Fertility suppressed
combination oral contraceptive benefits
- effective contraceptives
- ovarian and endometrial CA
contraindications of combination oral contraceptive
- absolute:
- thromboembolic phenomena
- estrogen-dependent neoplasms
- relative:
- liver disease
drug interactions with combination oral contraceptive
- P450 inducers will reduce effectiveness
-
antibiotics can reduce effectiveness
- stop enterohepatic circulation
ovarian steroids and gonadotropin levels in menopause
- reduced ovarian response to gonadotropins
- decreased ovarian steroids: estrogen and progesterone
- increased gonadotropins: FSH, LH
list the major menopausal symptoms
- vasomotor problems: hot flashes
- Genito-urinary problems: vaginal dryness, atrophy, pain
- osteoporosis
- heart disease
Hormone replacement therapy for women with h/o hysterectomies
estrogen only
adverse effects of Hormone replacement therapy
- breast cancer (1.25 fold)
- cardiovascular
- gallbladder disease (2.5 fold)
general guidelines for giving Hormone replacement therapy
- < 10 years after menopause = HRT has more benefits vs risks
- > 10 years after menopause = HRT not so great
- **before prescribing, know risks of HRT, inform patient and choose appropriate tx individually
actions of androgens
- virilizing
- spermatogenesis
- sexual development
- anabolic
- increase in bone density
- increase amino acid incorporation into muscle
- puberty: development of secondary sexual characteristics in male
androgen use in men
testicular deficiency
androgen use in women
female hypopituitarism (estrogens and androgens)
andogen use in both sexes
-
hypoproteinemia of nephrosis
- proteins lost in urine, helpful because it increase anabolic activity of liver to make more proteins
adverse effects of exogenous androgens in men
decreased spermatogenesis
- in testes, need high level of testosterone, if you bring in testosterone, will get negative feedback and loss of LH
adverse effects of exogenous androgens in women
- masculinization
- pseudohermaphroditism of fetus in pregnant women
adverse effects of exogenous androgens in both sexes
- oily skin, acne
- decreased HDL
- psychological changes
list the Androgen Receptor Antagonists
- Flutamide
- spironolactone
use for Androgen Receptor Antagonist: Flutamide
- used in prostate CA with long-acting GnRH agonist
- Used to suppress ‘tumor flare’ when beginning long-acting GnRH therapy.
Use for spironolactone: high dose
- high dose antiandrogen
- use
- hirsutism in women
- precocious puberty
List the 5 alpha reductase inhibitors
- Finasteride
- Dutasteride
- MOA: no Dihydrotestosterone
uses of 5 alpha reductase inhibitors
- benign prostatic hyperplasia
- male pattern baldness
adverse effects of 5 alpha reductase inhibitors
- impotence
- teratogenic
