Pharmacology Flashcards

1
Q

Which H exerts antiproliferative effects on the endometrium by promoting endometrial secretion rahter than proliferation?

A

Progestins

progesterone

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2
Q

Which enzyme converts T –> DHT?

A

5a-reductase

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3
Q

Which form is more biologically active, T or DHT?

A

DHT

10x greater affinity for androgen R

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4
Q

What is the phenotype of males that lack the 5a-reductase enzyme?

A

Phenotypically female

cant activate a program of male differentiation during development

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5
Q

When E enters the cell, what does it do to estrogen R’s?

A

Dimerizes them

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6
Q

The E-ER complexes binds to what on the promotr regions of DNA to change the txn of specific genes?

A

ERE’s

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7
Q

Which reactant is used to make progesterone and 17-OHpregnenolone?

A

Pregnenolone

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8
Q

Progesterone uses what enzyme to be converted into 17-OHprogesterone?

A

17a-hydroxylase

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9
Q

From which molecule is Androstenedione made from?

A

Dehydroepiandrosterone

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10
Q

Which enzyme converts androstenedione to estrone?

A

Aromatase

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11
Q

Which enzyme converts T –> estradiol?

A

Aromatase

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12
Q

Estrone and Estradiol belong to what class of H’s?

A

Estrogens

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13
Q

Androstenedione and T belong to what class of H’s?

A

Androgens

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14
Q

What happens to the gonadotroph release of LH and FSH if GnRH is administered continuously?

A

Suppressed

GnRH is normally pulsatile

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15
Q

What doe sthe corpus luteum produce after ovulation, which causes the endometrium to become secretory rather than proliferative?

A

P

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16
Q

This is a complex syndrome characterized by annovulation and increased levels of plasma androgens.

A

PCOS

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17
Q

What are the Sx to PCOS?

A

Annovulation, hirsutism, masculinization

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18
Q

In addition to an E-P contraceptive to suppress ovarian production of T, what drug is typically given to lower the masculinization in PCOS?

A

Anti-androgen, like Spironolactone

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19
Q

What are the 2 DOC to suppress PRL secretion form a prolatinoma?

A

Cabergoline

Bromocriptine

20
Q

What is the MOA for the following drugs to treat prostate CA?

Leuprolide, Goserelin, nafarelin

A

GnRH agonists

21
Q

What are the 2 GnRH antagonists used for the Tx of prostate CA?

A

Cetrorelix, Ganirelix

“you need to relix that prostate…”

22
Q

What is the drug that is used for prostate CA that INHIBITS the 5a-reductase enzyme?

A

Finasteride

23
Q

What is the drug that is used for prostate CA that is an androgen R antagonist?

A

Flutamide

24
Q

Exemestane, Formestant, Anastrozole, and Letrozole inhibit what enzyme for the treatment of breast CA?

A

Aromatase

25
Q

Which 2 aromatase inhibitors act by competitive inhibition of aromatase?

A

Anastrozole and Letrozole

26
Q

Which 2 aromatase inhibitors act by covalently binding to aromatase?

A

Exemstane

Formestant

27
Q

What is the estrogen R antagonist that is used in the treatment of breast CA that increases the risk for endometrial CA?

A

Tamoxifen

28
Q

What is the estrogen R antagonist in the breast that does NOT increase the risk for endometrial CA?

A

Raloxifene

29
Q

What is the SERM used to induce ovulation by acting as a E receptor antagonist in the hypothalamus and anterior pit gland, and as a partial agonist in the ovaries?

A

Clomiphene

30
Q

What is the 1 indication for flutamide?

A

Metastatic prostate CA

31
Q

This is a progesterone receptor antagonist that is used to induce 1st-trimester abortion.

A

Mifepristone (RU-486)

32
Q

What was the big deal of unopposed estrogen in early contraceptives?

A

Unopposed E –> ↑↑ endometrial growth –> risk of endometrial CA

33
Q

What are contraceptives now given with in addition to E, to prevent the risk of endometrial CA?

A

Progestin

34
Q

What class do the following drugs belong to?

Ethyndiol, norgestamate, gestodene, desogestrel

A

3rd generation progestins

35
Q

What is the advantage of 3rd generation progestins?

A

They have a very low androgen receptor cross-reactivity

36
Q

In addition to ↓ the risk of endometrial CA, what is the other advantage of using progestins in contraceptives?

A

Lighter periods because progestins inhibits the proliferative growth of the endometrium

I feel like progestins is that 1 guy at the surprise birthday party who makes everyone be quiet. Like everyone is having a good time waiting for the birthday guy/girl to arrive, getting a little sloshed, but then there’s that one guy who quiets everyone down and makes them hide. Yeah, it’s important and once the guest arrives (in this case, the fertilized egg) everything will go through as planned but he’s kinda a buzz-kill.

37
Q

What are the 2 rare adverse effects of long-term contraceptive use?

A
DVT formation (and PE)
↑ Gallbladder disease (cuz E's ↑ biliary concentration of cholesterol)
38
Q

What is the most effective morning-after pill?

A

Levonorgestrel 075mg

39
Q

Within what time frame is Levonorgestrel most effective?

A

Within 120 hours

40
Q

What is the 1 hormone u only need to give for hormone therapy for a post-hysterectomy pt?

A

Estrogen

dont need progestin cuz u dont got any uterus ya hurr?

41
Q

A 35 year old obese woman presents to the office with a history of type 2 diabetes. She informs you that she has noticed the top of her head is losing hair and she is developing facial hair. You suspect PCOS and decide to treat her symptoms, but are worried because the drug of choice for her masculization may exasterbate what complication of her pre-existing diabetes?

A. Breast atrophy
B. Hyperkalemia
C. Facial hair
D.  Urinary retention
E.  HTN
A

B. Hyperkalemia

42
Q

Ron Weasley and Hermione Granger presents to the office complaining of infertility. You find that the sperm cell count is A-OK in the man but the woman is complaining of oligomenorrhea and loss of peripheral vision. What is the best drug of choice for her suspected problem?

A. Spironolactone
B. Fluroquinolones
C. Tamoxifen
D.  Cabergoline
E.  Octreotide
A

D. Cabergoline

43
Q

A 55 year old man complains of dysuria. A DRE reveals an enlarged prostate with no nodules. In order to treat his BPH, you decide to use a drug that directly inhibits the 5 α-reductase enzyme. Which drug shall you use?

A. Finasteride
B. Tamoxifen
C.  Anastrozole
D.  Flutamide
E.  Bromocriptine
A

A. Finasteride

44
Q

An 18 year old female presents to the office concerned that she and her boyfriend just had sex for the first time and the condom broke. She is not using any other birth control methods and is requesting the morning after pill. During what time frame is levonorgestrel most effective?

A.

A

D.

45
Q

A 56 y/o female presents with a lump in her breast. After many studies you find that the breast mass is estrogen dependent and decide to use a drug that covalently binds to aromatase. Which drug do you have in mind?

A.  Anastrozole
B.  Letrozole
C.  Formestane
D.  Sprinolactone
E.  Furosemide
A

C. Formestane