E3: Sex Hormones Flashcards
What kind of drug is Leuprolide?
A long acting agonist of GnRH
What does leuprolide do and when is it used?
- Continuous administration suppresses release of LH and FSH after initial surge
- Used in IVF, endometriosis, precocious puberty, sex steroid dependent cancers, and gender affirmation
What kind of drug is Cetrorelix?
GnRH antagonist
What is cetrorelix used for?
Suppressing LH and FSH, used in the same situations as Leuprolide
What are the main differences between long acting GnRH agonists and antagonists?
- Antagonists suppress gonadotropins in 4-5 days while agonist require 3 weeks
- No initial surge of gonadotropins in antagonist treatment
- When treating prostate cancer with an agonist, need to coadminister with antiandrogen
What are the adverse effects of long acting GnRH antagonist/agonist?
Menopausal symptoms and testicular atrophy
What is Human menopausal Gonadotropin (hMG?used for?
Used as FSH in infertility
What is human chorionic gonadotropin used for?
-Used instead of LH, has the same actions
What are the uses of gonadotropins in men?
LH increases testosterone, FSH induces spermatogenesis
What are the uses of gonadotropins in women?
FSH stimulates ovaries and estrogen production, single dose of LH given to induce ovulation
What are the adverse effects of gonadotropins?
-Ovarian hyperstimulation syndrome
-multiple births
-gynecomastia
-uncomplicated ovarian enlargement
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What is it called when a patient has sudden ovarian enlargement, increased vascular permeability, rapid accumulation of fluid in the peritoneum, hypovolemia, shock, fever, thromboembolisms, and death?
Ovarian hyperstimulation syndrome
What are the contraindications of gonadotropins?
Sex-steroid dependent cancers
What is the MOA of estrogens?
Nuclear receptors
What is the metabolism of estrogens?
Metabolized by the liver and undergo enterohepatic circulation
What are the uses of estrogens?
-oral contraception, postmenopausal HRT, and stimulating pubertal development in hypogonadic girls
What are the adverse effects of estrogen?
-migraines, thromboembolism, endometrial hyperplasia, nausea, HTN, and gallbladder disease
What are the contraindications of estrogens?
Estrogen dependent neoplasms and thromboembolic disorders
What is the MOA of Tamoxifen?
- Seletive estrogen receptor modulator (SERM)
- Antiestrogen
- Has both antagonist and agonist effects
What is the DOC for palliative and prophylactic treatment of breast cancer in premenopausal women?
Tamoxifen
What are the agonist effects of Tamoxifen?
- Bone: Limits bone loss
- Uterus: many increase risk of uterine cancer
What antiestrogen just does not increase the risk of uterine cancer and is frequently use for osteoporosis?
Raloxifene
What is the MOA of Clomiphene?
- Antiestrogen
- SERM
- Antagonizes negative feedback of estrogen in hypothalamus
What is Clomiphene often used for?
Initial infertility therapy (stimulates LH and FSH)
-Causes multiple pregnancies 5-10% of the time