EXAM #5: ESTROGENS & PROGESTIN II Flashcards Preview

Pharmacology > EXAM #5: ESTROGENS & PROGESTIN II > Flashcards

Flashcards in EXAM #5: ESTROGENS & PROGESTIN II Deck (50):
1

What adverse effects are associated with progestins?

1) Breakthrough bleeding (endometrial vasculature)
2) Impaired glucose tolerance
3) Changes in lipid metabolism
- Elevated LDL
- Lowered HDL

2

What are the key adverse effects associated with 19-nortestosterone compounds?

1) Acne
2) Hirsutism

Thus, 19-nor effects of BC cause acne vs. estrogen which is protective against acne

3

What is birth control?

Combined estrogen-progestin or progestin only drugs

4

What can birth control drugs never be composed of?

Estrogen alone

5

What is the most common type of injectable BC?

Progestin alone i.e. depo-provera, which is given:
- Monthly
- or Quarterly

6

What are implantable BC methods composed of?

Progestin only

7

How long can an implantable BC stay implanted?

3 years

8

What is the composition of IUD BC?

Progestins only

9

How long can an IUD stay in?

5 years

10

How often are vaginal rings and transdermal BC placed?

Monthly

11

What is the general MOA of BC?

1) Suppress LH and FSH surge for ovulation
2) Alter cervical mucus
3) Alter endometrium

12

Give an example of a progestin only BC.

Nor-QD

13

What hormone is in "Depo-provera?"

Medroxyprogesterone

14

What is the major difference between normal contraceptive therapy and emergency contraception?

Higher doses for emergency contraception

15

How long after intercourse can one take Plan-B?

72 hours

*Note that this is the drug of choice for emergency contraception

16

What is the failure rate of oral contraception with typical use?

8%

17

What are the mild adverse effects associated with contraceptives?

- Nausea
- Mastalgia (breast tenderness)
- Breakthrough bleeding (Estrogen-mediated)
- Edema
- Headache
- Withdrawal bleed failure
- Serum protein changes

18

What are the moderate adverse effects of contraceptives?

- Breakthrough bleeding (Progestin-mediated)
- Weight gain
- Increased skin pigmentation
- Acne
- Hirsutism
- Vaginal infection
- Amenorrhea

19

What are the severe adverse effects of contraceptives?

- Thromboembolic disease
- MI
- CVA
- GI disorders i.e. cholestasis
- Depression
- ?Cancer

20

What are the benefits of contraceptives?

1) Reduced risk of ovarian and endometrial cancer
2) Reduction in dysmenorrhea/ endometriosis
3) Decreased incidence of ectopic pregnancy
4) Decreased benign breast disease
5) Increased Hb concentrations
6) Suppress acne and hirsutism

21

What are the contraindications to estrogen containing contraceptives?

1) Known/ suspected breast cancer
2) Thromboembolic disorder
3) Liver disease
4) Cardiovascular disease
5) Smoker 35 y/o+

22

What are the drugs that induce hormone metabolism?

1) HIV agents
2) Anti-convulsants
3) St. John's wort

23

What effect do antibiotics have on contraceptives?

Decreased efficacy

24

What is the clinical indication for Clomiphene?

Fertility drug

25

What is the MOA of Clomiphene?

- PARTIAL AGONIST that blocks negative feedback on LH and FSH
- Increase liklihood of ovulation

26

What is a partial agonist?

Drug that produces a lower than maximal response compared to the agonist

27

What adverse effects are associated with Clomiphene?

1) Hot flashes
2) Multiple births

28

When in the menstrual cycle is Clomiphene given?

- Follicular phase for 5x days
- Removed prior to day 14 (ovulation)

29

What are SERMS?

Selective Estrogen Receptor Modulators

*Note that the same SERM can have different actions in different tissues i.e. agonist, partial agonist, antagonist

30

What is the function of SERMS in bone?

Suppress bone resorption (agonist)

*I.e. estrogen receptor agonism will reduce osteoporosis

31

What is the function of SERMS in the endometrium?

Proliferation (partial agonist)

*This is an unintended adverse effect and can lead to development of endometrial hyperplasia and endometrial CA*

32

What is the function of SERMS in pituitary and breast?

Antagonist, which will
- Hot flashes (pituitary)
- Inhibited proliferation in breast (anti-ER+ cancer)

33

List the two SERMS.

Tamoxifen
Raloxifene

34

What is the clinical indication for Tamoxifen?

ER+ Breast Cancer

35

What adverse effects are associated with Tamoxifen?

1) Hot flashes
2) Endometrial cancer
3) Nausea/vomiting

36

How does Raloxifene differ from Tamoxifen?

NO partial agonist effects on endometrium

37

What are the clinical indications for Raloxifene?

1) Breast cancer
2) Post-menopausal bone loss

38

What key adverse effect is associated with Raloxifene?

Hot flashes

39

What are the clinical indications for dananzol?

1) Endometriosis
2) Breast fibrocystic disease

40

What is the MOA of dananzol?

Decreased estrogen concentration in blood by displacing estrogen from serum proteins and increasing estrogen clearance

41

What adverse effects are associated with dananzol?

1) Hot flashes
2) Weight gain
3) Oily skin
4) Acne
5) Hirsutism

42

What is the MOA of anaztrozole and letrozole?

Aromatase inhibitors that prevent conversion of Testosterone to Estrogen

43

What are the indications for anaztrozole and letrozole?

ER+ breast cancer

44

What adverse effects are associated with anaztrozole and letrozole?

- GI disturbances
- Hot flashes
- Lethargy

45

List the anti-progesterone drugs.

Mifepristone
Ulipristal

46

What is the MOA of Mifepristone?

Progesterone receptor antagonist i.e. it will decrease the effects of progesterone

47

What is the clinical use of Mifepristone?

Abortifacient (less than 7 weeks/ first trimester)

*Followed by misoprostol (synthetic prostaglandin, which further increases uterine contractions) 48 hours later*

48

What is the clinical indication for Uliprastal?

Emergency contraception

49

What is the MOA of Uliprastal?

Partial progesterone agonist

50

What is the benefit of Uliprastal vs. Plan-B?

Can be used 5 days post-intercourse vs. 3 days for Plan-B

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