Pharmacology Flashcards

1
Q

What are the clinical uses of estrogens?

A

Treat female hypogonadism
HRT
Prevents bone loss
Component of hormonal contraceptives

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2
Q

What are the clinical uses of progesterones?

A
Hormonal contraceptives (alone or with estrogen)
Component of HRT to lower risk of endometrial cancer
Assisted reproductive technology
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3
Q

What enzyme converts testosterone to DHT?

A

5α-reductase

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4
Q

What drugs inhibit 5α-reductase?

A

Finasteride

Dutasteride

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5
Q

Why do supraphysiologic levels of testosterone lead to testicular atrophy and decreased spermtogenesis?

A

Inhibit LH/FSH

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6
Q

Paradoxically, supraphysiologic doses of testosterone can result in gynecomastia. Why does this occur?

A

Aromatization of testosterone to estrogen

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7
Q

What are the sites of action of anti-androgens?

A

GnRH receptor
CYP17 (17α-hydroxylase)
5α-reductase
Androgen receptor

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8
Q

What drug is a GnRH analog?

A

Leuprolide

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9
Q

What is the anti-androgen MOA of ketoconazole?

A

Inhibits desmolase
Inhibits 17α-hydroxylase
(synthesis inhibitor)

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10
Q

What drugs are androgen receptor antagonists?

A

Bicalutamide

Spironolactone

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11
Q

What is the anti-androgen MOA of leuprolide?

A

GnRH analog

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12
Q

What is the anti-androgen MOA of dutasteride?

A

Inhibits 5α-reductase

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13
Q

What is the anti-androgen MOA of bicalutamide?

A

Androgen receptor antagonist

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14
Q

What is the anti-androgen MOA of finesteride?

A

Inhibits 5α-reductase

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15
Q

What class of drug(s) can be used to treat prostate cancer?

A

GnRH agonist

Androgen receptor antagonist

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16
Q

What is the anti-androgen MOA of spironolactone?

A

Androgen receptor antagonist

17
Q

When would you use a 5α-reductase inhibitor to treat BPH?

A

Very large prostate

Intolerance of α-1 blockers

18
Q

How can you treat precocious puberty in boys?

A

GnRH agonist

19
Q

A woman with PCOS has hirsutism, what anti-androgen drug can be given to treat this condition?

A

Spironolactone

20
Q

What drugs are SERMs?

A

Tamoxifen
Raloxifene
Clomiphene

21
Q

Detail the antagonist actions of tamoxifen.

A

Breast cancer receptors

Hot flases

22
Q

Detail the agonist actions of tamoxifen.

A

Endometrial receptors
Venous thrombosis
Prevents osteoperosis

23
Q

Compare/contrast raloxifene with tamoxifen.

A

Raloxifen is like tamoxifen, however, it does not have agonist activity at the endometrium

24
Q

What is clomiphene used for?

A

Induces ovulation- selectively blocks estrogen receptors at pituitary which increases FSH/LH output

25
Q

What drug is a pure estrogen receptor antagonist?

A

Fulvestrant

26
Q

Estrogen is not used alone to treat menopausal symptoms. What is given with estrogen and why?

A

Progesterone

Decreased risk of endometrial cancer

27
Q

What drugs are aromatase inhibitors?

A

Anastrozole

Exemestane

28
Q

What are aromatase inhibitors used to treat?

A

Breast cancer that is ER positive

29
Q

What is the MOA of anastrozole?

A

Aromataste inhibitor

30
Q

What drug is a competitive inhibitor of progestins at progesterone receptors used to terminate pregnancy?

A

Mifepristone

31
Q

What drug is administered with mifepristone and what is its MOA?

A

Misoprostol- PGE1 analog

32
Q

What is the MOA of exemestane?

A

Aromatase inhibitor

33
Q

What is the MOA of estrogen-progesterone OCPs that inhibits ovulation?

A

Inhibit LH/FSH, thus prevent estrogen surge. Without the estrogen surge there is no LH surge and no ovulation.

34
Q

How do OCPs inhibit pregnancy?

A

Inhibit ovulation
Progesterones-
Thicken cervical mucus
Inhibit endometrial proliferation

35
Q

What is the MOA of mifepristone?

A

Inhibits progestins

36
Q

A drug with β2-agonist activity will have what effect at the uterus?

A

Relaxation

37
Q

What drugs are uterine β2-agonists given to decrease contraction frequency during labor?

A

Terbutaline

Ritodrine