Fitzy's drugs that antagonize receptors; 4.8 Flashcards
What are bicalutamide, flutamide, and nilutamide? (what are the -lutamides?)
-lutamide = Non-Steroidal Anti-Androgens (NSAAs)
Which of the NSAAs is older and has more side effects?
Flutamide
How do NSAAs work?
NSAAs inhibit ligand binding and translocation of androgen receptors from the cytoplasm to the nucleus
What is seen with hormone levels with NSAAs?
Increased release of FSH and LH → increased testosterone synthesis…but no receptors so it doesn’t do anything
When are NSAAs used?
Early prostate cancer with radiation
Metastatic prostate cancer with GnRH analogs
GnRH analogs are used long-term. Are NSAAs used long-term?
NO…there would be bad side effects
What are the common side effects of NSAAs?
Acutely: diarrhea, N/V
Delayed: Low testosterone, reversible liver function anomalies
What are the categories of anti-estrogens?
Progestins
Estrogen receptor antagonists
What are the progestins?
Hydroxyprogesterone
Medroxyprogesterone
Megestrol
What are the two classifications of estrogen receptor antagonists?
Selective ER Down-regulators (SERDs)
Selective ER Modulators (SERMs)
How do SERDs work?
SERDs are competitive antagonists in every tissue
What is an example of a SERD?
Fulvestrant
How is fulvestrant given?
Fulvestrant is given IM in the butt monthly
What enzyme metabolizes fulvestrant? Does this cause any drug interactions?
CYP3A4 metabolizes fulvestrant…but it has NOT been determined to have drug interactions
What are examples of SERMs?
Raloxifene
Tamoxifen
Toremifene
Which SERM is an antagonist in breast tissue and an agonist in uterine tissue?
Toremifene
Which SERM is an antagonist in breast AND uterine, but is an agonist in bone?
Raloxifene
Which SERM is both an antagonist and partial agonist in breast, and then an agonist in BOTH uterus and bone?
Tamoxifen
How are SERMs taken? Do they work faster or slower than SERDs?
SERMs are taken orally and peak in 4-7 hours…compared to fulvestrant which peaks in 7 days
Which estrogen receptor drug is used in ER+ breast cancer in premenopausal women?
Tamoxifen is used with a GnRH analog
can also be used for prevention
When would raloxifene, toremifene, or fulvestrant be used?
The non-tamoxifen SERMs and the SERD are used in metastatic ER+ breast cancer treatment if the the disease progresses after tamoxifen or aromatase inhibitor therapy
What side effects are common to all estrogen receptor drugs?
Hot flashes N/V Menstrual irregularities Vaginal bleeding Dermatitis
Besides the normal side effects, what are some possible consequences of tamoxifen treatment?
Endometrial cancer (2-3x) Stroke (w/ long term use)
Besides the normal side effects, what other side effects are common with fulvestrant?
GI symptoms Headache Back pain Pharyngitis Injection site reactions
