3.4.2 Reproductive Pharmacology Flashcards
What are the aromatase inhibitors?
competitive (anastrozole, letrozole)
Irreversible (exemestane, formestane)
What are the three SERMs?
Tamoxifen (antagonist in breast), clomiphene (antagonist in hypothalmus/pituitary), raloxifene (antagonist in ___)
What does the hypothalmus use to upregulates anterior pituitary production of LH/FSH?
GnRH
What are some of the anti-androgens?
What are the uses of aromatase inhibitors?
Early/advanced breast carcinoma
Where is LH and FSH clinical pharmacology typically used?
Ovulation induction
Male infertility
What are the different receptor agonists of estrogen?
Natural
Synthetic - Steriodal (ethinyl E2, mestronol, quinestrol) and Non-steriodal (Diethylstilbestrol, chlorotrianisene, methallenestrill)
In what medical condition is there a lack of release of GnRH from the hypothalmus?
Kallman Syndrome
Describe the release of GrRH
Pulsatile
When is GnRH clinical pharmacology used?
Progressive precocious puberty
Prostate cancer
Endometriosis
Assisted reproduction
Uterine leiomyomata (fibroids)
Male/female infertility
What are the uses of estrogen agonists?
What are the clinical toxicity effects of GnRH in females? males?
Females: symptoms of menopause, ovarian cysts (temporary), osteoporosis
Males: Hot flushes, sweats, edema, gynecomastia, osteoporosis
What are the two forms of progesterone and their functions?
What are the 8 functions of estrogens?
What are the receptor agonist/antagonists of progesterone?
What are the four potential sites of pharmacological intervention?
The highlighted
Clinical uses of progesterone?
What are the 3 areas of reproductive pharm applications?
Replacement therapy for hormone deficiency
As antagonists for dz’s caused by excess production of pituitary hormones
As diagnostic tools for identifying several endocrine abnormalities
What are the four different receptor antagonists of estrogen?
Tamoxifen, clomiphene, raloxifene, fulvestrant
What are the agonists of FSH?
Menotropins, Urofollitropin, Follitropin alpha/beta
What are the roles of FSH/LH in males and females? What are their feedback regulation mechanisms?
What are the adverse effects and contraindications of estrogen?
Estrogen dependent neoplasm (breast, endometrium)
Undiagnosed genital bleeding
Hx of thromboembolitic disorders
Pregnant women
What are the toxicities and contraindications of FSH/LH?
OHSS and multiple pregnancies
HA, depression, edema, precocious puberty
hot flushes, sweats, edema, typical symptoms of menopause
What is the androgenic effect?
How would agonists/antagonists work on GnRH?
What is changed in the GnRH agonists?
The glycine residue is changed to prevent cleavage
What is the therapeutic use of androgens?
Androgen replacement therapy: mimic the normal testosterone concentration?
What are the three different forms of estrogen and their potency?
Estradiol - E2 (100%), Estriol - E3 (10%), Estrone - E1 (1%)
What are some of the adverse effects of androgens?
What is the agonist of LH? (taken off US market in 2012 b/c the drug company didn’t want to produce it)
Lutropin alpha
What two ways can GnRH be manipulated pharmacologically?
Control pulstile release or inhibit receptor
