Hormones Flashcards
Mixed agonists with estrogenic effects are called ___________
Selective Estrogen receptor modulator
Long-acting esters of estradiol _______________ is administered __________
Estradiol cypionate
IV
Biologic source of estrogen
Premarin
Effects of estrogen on the body
- Modifies protein levels
- Reduces LDL and Increases HDL
- Reduces bone resorption
4.Enhances the coagulability of blood
5.Inhibits the secretion of gonadotropins from the anterior pituitary
Estrogen is used for
Hypogonadism
Estrogen deficiency (POF, menopause or surgical removal of varies)
Osteoporosis
Estrogen increases the risk for _____________ and ______________ CA
Breast
Endometrial
Endometrial cancer risk can be reduced by adding ____________ to estrogen
Progestin
Dosage of estrogen must be reduced in hypogonadal girls. Why?
To prevent premature closure of epiphyses of long bones and short stature
What are dose-dependent toxicities of estrogen?
Nausea
Breast tenderness
Migraine headache
Thromboembolic events
Gall bladder disease
Hypertriglyceridemia
Hypertension
Increased clotting factors
The side effect of increased clotting factors by estrogen can be decreased by ______________
avoiding oral route
Diethylstilbestrol use is associated with ____________, ______________, and ______________ in the daughters of women who were treated for spontaneous abortion
Infertility
Ectopic pregnancy
Vaginal adenocarcinoma
Progesterone ___________________ have improved oral bioavailability
Medroxyprogesterone
Fx of progesterone
Maintenance of pregnancy
Affect carb metabolism
Suppress ovulation in high doses
Uses of progesterone
COntraceptive with estrogen
Maintain pregnancy
Toxicities of progesterone
Decrease HDL
Weight gain
Decrease in bone density
Delayed resumption of ovulation after termination of therapy
Increases the risk of breast CA
Postcoital contraceptive
L-norgestrel alone
Estrogen alone
COCP
Abortifacient
Mifepristone
Misoprostol
Endometriosis
OCP
Depot inj of medroxyprogesterone acetate
GnRH agonist
Danazol
Breast cancer
Tamoxifen
Aromatase inhibitors (e.g. anastrozole)
Osteoporosis
Estrogen
Raloxifene
Infertility
Clomiphene
hMG
hCG
GnRH analogs
Progesterone
Bromocriptine
Hirsutism
COCP
Spironolactone
Flutamide
GnRH agonists
Prostate hyperplasia
Finasteride
Norethindrone is AKA ___________
minipill
What is norethindrone?
Progesterone
For breastfeeding women
COCPs are available in
monophasic
biphasic
triphasic
quadriphasic
Postcoital contraceptives should be used within _______ hours after unprotected intercourse
72 hours
What is the action of COCP?
Inhibition of ovulation
Thickening of the cervical mucus
Affects the tubal function and endometrial lining
Using COCPs has reduced the risk of many diseases.
Ovarian cyst
Ovarian CA
Endometrial CA
PID
Ectopic pregnancy
Iron deficiency anemia
Benign breast disease
Rheumatoid arthritis
What are the toxicities of COCPs?
Thromboembolic events
Breast CA
Nausea
Breast tenderness
Headache
Skin pigmentation
Depression
Weight gain
Acne
Hirsutism
Why SERMs have agonist and antagonist effects at different sites?
Different ER dimers
ERa-ERa
ERa-ERb
ERb-ERb
Name some SERMS
Tamoxifen
Raloxifene
Clomiphene
Toremifene
Bazedoxifine
_______________ is a pure estrogen receptor antagonist
Fulvestrant
Tamoxifen is used for the tx of ______________
Hormone responsive breast cancer
What is the action of tamoxifen?
Antagonist in breast tissue
Agonist at endometrial tissue
What are the pros of tamoxifen?
Reduces risk of breast CA
Prevents osteoporosis
What are the cons of tamoxifen?
Endometrial CA (agonist)
Venous thromboembolism (agonist)
Hot flushes (antagonist)
Raloxifene is used for __________________
Clomiphene is used for __________________
Osteoporosis
Induction of ovulation
_______________ is a newer SERM for the treatment of menopausal symptoms and prophylaxis of osteoporosis
Bazedoxifene
Raloxifene reduces the risk of ______________ cancer
breast
Side effects of raloxifene
Hot flushes
Venous thromboembolism
How does clomiphene induce ovulation?
It is a partial agonist at the estrogen receptor so it increases FSH and LH output (by reducing the negative feedback)
______________ is used in tx of breast cancer resistant to tamoxifen
Fulvestrant
Name the aromatase inhibitors and their use.
Anastrozole
Letrozole
Exemestane
Used for Breast cancer
What is the mechanism of action of Danazol?
It inhibits the P450 enzyme involved in gonadal steroid synthesis
Weak partial agonist at progestin, androgen, and glucocorticoid receptors
Danazol is used for _________________ and ____________________
Endometriosis
Fibrocystic disease of the breast
GnRH analog _____________ is used for _________________ (4)
Leuprolide
Controlled ovarian hyperstimulation
Precocious puberty
Endometriosis
Fibroids
Side effect of leuprolide
Decreased bone density if used for more than 6 months
GnRH antagonist _______________ and _____________ are used for ___________________
Ganirelix
Cetrorelix
Controlled ovarian hyperstimualtion
Antiprogestins (Mifepristone) is used as an abortifacient in ____________ pregnancy
early (up to 49 days after LMP)
Most common complication of mifepristone is ______________
failure to induce abortion
Side effects of Mifepristone
N/V/D and cramping and bleeding associated with passing the pregnancy
