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Leuprolide
71%
183/257
Anastrozole
12%
31/257
Clomiphene
4%
9/257
Tamoxifen
5%
14/257
Cyproterone
13/257
Select Answer to see Preferred Response
Flutamide is a non-steroidal antiandrogen that acts as a competitive inhibitor at testosterone receptors. It is used in combination with a GnRH analog, such as leuprolide, in the treatment of advanced prostate cancer. It is given in a continuous manner as to act as an antagonist. The inhibitory effect of flutamide on the tumor's testosterone receptors is beneficial to halt the progression of prostate cancer. However, there is also an unwanted increase in systemic testosterone levels seen with flutamide monotherapy due to reduced negative feedback at the level of the pituitary. The addition of a leuprolide counters this unwanted increase in testosterone levels by decreasing the release of LH and FSH from the anterior pituitary, thereby reducing androgen production. Note that upon administration of leuprolide, there is an initial surge n LH and FSH before achieving suppression. Combination flutamide/leuprolide therapy has side effects associated with reduced androgen levels, including hot flashes, gynecomastia, and impotence. Incorrect Answers: Answer 2: Anastrozole is an aromatase inhibitor that prevents peripheral conversion of androgens to estrogens. Its primary use is in estrogen-receptor positive breast cancer in post-menopausal women. Answer 3: Clomiphene has been demonstrated to increase testosterone levels; this would oppose the competitive inhibition effect of flutamide and potentially lead to an undesired stimulation of prostate cancer cells. Answer 4: Tamoxifen is a selective estrogen receptor modulator (SERM) and is primarily used in the treatment of estrogen-receptor positive breast cancer. Answer 5: Cyproterone is an antiandrogen that works by the same mechanism as flutamide; therefore, addition of this agent would not be expected to yield as much benefit as incorporation of a complementary therapy, such as a GnRH agonist.
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