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Reproductive and Post-reproductive Health Quiz
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Which of the following best describes the action of tamoxifen in breast tissue?
- A Aromatase inhibitor in breast tissue You picked ✕
- B Oestrogen receptor agonist in breast tissue You picked ✕
- C Oestrogen receptor antagonist in breast tissue You picked ✓
- D Progesterone receptor antagonist in breast tissue You picked ✕
- E Selective progesterone receptor modulator in breast tissue You picked ✕
Correct!
Incorrect
The answer is C: Oestrogen receptor antagonist in breast tissue
Explanation
Why C is correct
See Tamoxifen and Raloxifene (SERMs). Option C is correct. Tamoxifen is a selective oestrogen receptor modulator (SERM): a drug that binds the oestrogen receptor but acts as an antagonist (a blocker) in some tissues and an agonist (an activator) in others. In breast tissue it is an antagonist: it competes with oestrogen for the receptor, so growth signals that oestrogen would normally give to the cell are reduced. That is the basis for its use in oestrogen-receptor-positive breast cancer (cancer whose cells carry oestrogen receptors and depend on oestrogen to grow). The same drug behaves like an oestrogen in the endometrium and in bone, which is why the tissue matters in the question and why tamoxifen has a different adverse-effect profile from an aromatase inhibitor. The BNF recommends tamoxifen as the initial adjuvant endocrine therapy in premenopausal women and in men with oestrogen-receptor-positive invasive breast cancer. A simple memory aid is that tamoxifen blocks the receptor in the breast, while anastrozole removes the oestrogen supply.
- Drug type: tamoxifen is a selective oestrogen receptor modulator (SERM).
- In breast tissue: it is an antagonist that competes with oestrogen for the receptor.
- Elsewhere: it acts like an oestrogen in the endometrium and bone.
- Use: oestrogen-receptor-positive breast cancer.
Why the other options are incorrect
- A. Aromatase inhibitor in breast tissue: This is the action of aromatase inhibitors such as anastrozole, which stop oestrogen being made. Tamoxifen leaves oestrogen production alone and instead occupies the receptor. Your answer
- B. Oestrogen receptor agonist in breast tissue: Tamoxifen does act as an oestrogen agonist in some tissues, such as the endometrium and bone, but not in the breast. That is the point of a selective oestrogen receptor modulator, and the breast is where it blocks the receptor. Your answer
- D. Progesterone receptor antagonist in breast tissue: Tamoxifen acts on the oestrogen receptor, not the progesterone receptor. A progesterone receptor antagonist would be a drug such as mifepristone, which has a different place in treatment. Your answer
- E. Selective progesterone receptor modulator in breast tissue: A selective progesterone receptor modulator is a drug such as ulipristal. Tamoxifen is a selective oestrogen receptor modulator, so it belongs to a different class that acts on a different receptor. Your answer
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