Chapter 29: Reproduction Flashcards
Once testosterone is released from sex-hormone binding globulin and goes into the cell, what does testosterone become to inflict increased androgenic change?
–(5-alpha-reductase)–> dihydrotestosterone,
which makes dimer with androgen receptor and causes transcription
How does each of the following affect FSH/LH during feedback?
1) estrogen
2) testosterone
3) activin
4) inhibin
5) GnRH
1) + at ovulation causing surge, - all other times
2) -
3) + (just FSH)
4) - (just FSH)
5) + when pulsatile, - when continuous
Role of LH on sex hormones in the male
Increase testosterone synthesis in Leydig cells
Role of LH on sex hormones in the female
increase androgen synthesis in Thecal cells
Role of FSH on sex hormones in the male
increases androgen binding protein, inhibin, and activin in Sertoli cells
Role of FSH on sex hormones in the female
converts androgens–(aromatase)–> estrogens and increases inhibin and activin in granulosa cells
2 common endocrine-related causes of infertility
polycystic ovarian syndrome (because increased androgens) and prolactinomas (because prolactin supresses estrogen via GnRH antagonism)
3 hypotheses for Polycystic Ovarian Syndrome
1) LH hypothesis: increased LH –> increases androgens –> prevents normal follicle growth and secretion –> no estrogen trigger
2) Insulin theory: increased insulin –> decreases sex hormone-binding globulin production –> increases free testosterone
3) Ovarian hypothesis: thecal cell dysregulation
What kind of estrogen is predominant in the postmenopausal woman?
estrone (produced by adipose tissue, less potent)
What drug selectively inhibits type II 5-alpha-reductase to treat BPH (most effective for large prostates) and alopecia, but can cause decreased libido and ED?
finasteride
What drug inhibits both type I and II 5-alpha-reductase to treat BPH, but can cause decreased libido and ED?
dutaseride
What are the most effective for ER+ breast cancer treatment, but cause osteoporotic fractures?
anastrozole, letrozole, exemestane, formestane
What are the reversible competitive inhibitors of aromatase, used to treat breast cancer?
anastrozole, letrozole
What are the irreversible inhibitors of aromatase, used to treat breast cancer?
exemestane, formestane (it STAINS it = irreversible)
What drug is an estrogen receptor antagonist in breast tissue and partial agonist in endometrium and bone, and is good (along with general breast cancer treatment) for therapy after lumpectomy? It should NOT be prescribed with DVT/pulmonary embolism.
tamoxifen
What drug is an estrogen receptor antagonist in the hypothalamus and anterior pituitary and partial agonist in ovaries, increasing FSH and LH? The FSH can cause multiple follicles to grow, so side effects are ovarian cysts and hypertrophy.
clomiphene
What treats female infertility due to an ovulatory disorder by inducing ovulation?
clomiphene
What SERMs are agonists in bone, thus treating osteoporosis?
bazedoxifene and raloxifene
What drug treats vulvovaginal dryness and atrophy?
ospemifene
What drug is an agonist in bone and antagonist in both breast and endometrial tissue?
raloxifene
What is a pure estrogen receptor antagonist, used to treat ER+ metastatic breast cancer in postmenopausal women?
fulvestrant (ful = FULL ER antagonist)
What is a androgen receptor antagonist used to treat prostate cancer and BPH, but can cause hepatotoxicity?
flutamide
What is a androgen receptor antagonist used to treat hirsutism, acne, and hypertension, but can cause hyperkalemic metabolic acidosis? It has both anti-androgen AND progesterone effects.
spironolactone
What inhibits progesterone binding to receptor, causing death of the decidua and detachment of a blastocyst? It blocks glucocorticoid receptors at higher concentrations, so may be useful for ectopic ACTH syndrome too.
mifepristone
What inhibits progesterone binding to receptor and may treat endometriosis and fibroids?
asoprisnil
What 4 effects do oral contraceptives have in preventing transport of egg and sperm?
1) estrogens supress LH surge –> no ovulation
2) alter tubal peristalsis
3) decrease endometrial receptivity
4) decrease cervical mucus secretions
What two cancers might oral contraceptives decrease?
endometrial cancer (WITH progesterone), ovarian cancer
What progestin is used as emergency contraception and has high androgenic activity?
levonorgestrel
What is part of an 84 day-7 day combo pack (hint: the progestin has high androgenic activity?
ethinyl estradiol and levonorgestrel
What are important side effects in oral contraceptives?
DVT, embolism (esp in smokers), stroke, gallbladder disease, DVT, breakthrough bleeding
What oral contraceptive combo is available as a vaginal ring that’s kept in for 21 days?
ethinyl estradiol and etonogestrel (eton = EYTAN gonna propose w/ ring soon)
What oral contraceptive combo is available as a transdermal patch that is changed weekly?
ethinyl estradiol and norelgestromin (ROAMIN around TRANSatlantic)
What is used as a progesterone only contraceptive and in post-menopausal women, and injectable every 3 months? Side effects are breakthrough spotting and irregular periods.
medroxyprogesterone acetate
What is a progesterone only contraceptive used as a silastic implant changed every 3 years?
etonogestrel
What is best used transdermally (bypass liver) to treat hypogonadism in men, but can cause acne, gynecomastia, BPH, and prostate cancer?
testosterone enanthate, testosterone cypionate
What is best used transdermally (bypass liver) for male contraception, but can cause weight gain, polycythemia, and increased prostate size with progestin? By what method?
testosterine enanthate, testosterone undecanoate (by decreasing GnRH release –> decreases LH, FSH –> decreases spermatogenesis)
