Gonadal Hormones and Inhibitors Flashcards
Clinical applications of ethinyl estradiol
Hypogonadism in girls, women
OCP, parenteral contraceptive (combined with a progestin)
Intractable dysmenorrhea or uterine bleeding
Moderate toxicities of ethinyl estradiol
Breakthrough bleeding, nausea, breast tenderness
Serious toxicities of ethinyl estradiol
Thromboembolism, gallbladder disease, hypertriglyceridemia, migraine headache, HTN, depression
In postmenopausal women: breast cancer, endometrial hyperplasia
Mestranol
A prodrug that is converted to ethinyl estradiol, contained in some contraceptives
Long-acting estrogens administered IM and used for hypogonadism in young females
Estrogen esters (eg, estradiol cypionate)
What type of hormonal receptors does norgestrel activate?
Progesterone
Clinical uses of norgestrel
Contraception: oral in combination with estrogen, as an IUD, or as a postcoital contraceptive
Adverse effects of norgestrel
weight gain, reversible decrease in bone mineral density (high doses)
MOA of Tamoxifen
Estrogen antagonist in breast tissue and CNS
Estrogen agonist effects in endometrium, liver, and bone
Clinical use of tamoxifen
prevention and adjuvant treatment of hormone-responsive breast cancer
Adverse effects of tamoxifen
Hot flushes, thromboembolism, endometrial hyperplasia
SERM approved for osteoporosis and prevention of breast cancer in selected patients
Raloxifene
MOA of raloxifene
Antagonist effects in breast, CNS, and endometrium;
agonist effects in the liver
SERM used for ovulation induction
Clomiphene
MOA of clomiphene
Estrogen antagonist in pituitary –> increases LH, FSH secretion
MOA of fulvestrant
Estrogen receptor antagonist in all tissues. IM admin.
What is fulvestrant used for?
Adjuvant treatment of hormone-responsive breast cancer that is resistant to first-line anti estrogen therapy
Aromatase inhibitors used in adjuvant treatment of hormone-responsive breast cancers
Anastrozole, Letrozole, and exemastane (irreversible)
Adverse effects of aromatase inhibitors
Hot flushes, musculoskeletal disorders, reduced bone mineral density Joint symptoms (arthralgia, arthritis, arthritis, cervical spondylosis, osteoarthritis, and disk herniation)
GnRH agonist; used in controlled ovarian hyperstimulation and also for the treatment of precocious puberty in children and short-term (
Leuprolide
GnRH antagonists used for controlled ovarian hyperstimulation
Ganirelix, cetrorelix
Weak cytochrome P450 inhibitor and partial agonist of progestin and androgen receptors
Danazol
What is danazol used for?
Endometriosis, fibrocystic breast disease
Adverse effects of danazol
Acne, hirsutism, weight gain, menstrual disturbances, hepatic dysfunction
MOA of finasteride, dutasteride
5alpha-reductase inhibitors
What is finasteride used for?
BPH, male-pattern hair loss
Possible side effects of finasteride
Rarely, impotence, gynecomastia
Competitive inhibitors of androgen receptors
flutamide, bicalutamide, nilutamide (bicalutamide and nilutamide have lower risk of hepatotoxicity)
Adverse effects of flutamide?
Gynecomastia, hot flushes, impotence, hepatotoxicity
What type of cancer can ketoconazole be used to to treat?
Advanced prostate cancer that is resistant to first-line anti androgen drugs
