Raloxifene Flashcards

1
Q

what is Raloxifene

A

A Selective estrogen receptor modulator

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2
Q

what does Raloxifene do

A

, produces estrogen-like effects on bone and lipid metabolism, while antagonizing the effects of estrogen on breast and uterine tissue

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3
Q

what does Ralixofene do in the bone?

A

binds to the estrogen receptors, resulting in reduced bone resorption and increased bone mineral density in postmenopausal women, slowing the rate of bone loss

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4
Q

how does Raloxifene slow the rate of bone loss

A

via activation of transforming growth factor-β3, which is a bone matrix protein with antiosteoclastic properties. In addition Raloxifene can inhibit the proliferation of preosteoclastic cells

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5
Q

what else does Raloxifene inhibit?

A

can inhibit the proliferation of preosteoclastic cells

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6
Q

what else does Raloxifene antagonise?

A

the effects of estrogen on mammary and uterine tissue

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7
Q

what does Raloxifene d in mammary and uterine tissue

A

Raloxifene prevents the transcriptional activation of genes containing the estrogen response element

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8
Q

descibe the two possibilities by which Raloxifene prevents the transcriptional activation of genes containing the estrogen response

A
  • Raloxifene’s tissue-specific estrogen agonist or antagonist activity is dependent on the structural differences between the raloxifene-estrogen receptor complex and the estrogen-estrogen receptor complex.
  • The presence of at least 2 estrogen receptors (ERα, ERβ) may determine the tissue specificity of Raloxifene.
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