EXAM #5: ESTROGENS & PROGESTIN II

Question 1

What adverse effects are associated with progestins?

Answer 1

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

Question 2

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

Answer 2

1) Acne
2) Hirsutism

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

Question 3

What is birth control?

Answer 3

Combined estrogen-progestin or progestin only drugs

Question 4

What can birth control drugs never be composed of?

Answer 4

Estrogen alone

Question 5

What is the most common type of injectable BC?

Answer 5

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

• Monthly
• or Quarterly

Question 6

What are implantable BC methods composed of?

Answer 6

Progestin only

Question 7

How long can an implantable BC stay implanted?

Answer 7

3 years

Question 8

What is the composition of IUD BC?

Answer 8

Progestins only

Question 9

How long can an IUD stay in?

Answer 9

5 years

Question 10

How often are vaginal rings and transdermal BC placed?

Answer 10

Monthly

Question 11

What is the general MOA of BC?

Answer 11

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

Question 12

Give an example of a progestin only BC.

Answer 12

Nor-QD

Question 13

What hormone is in “Depo-provera?”

Answer 13

Medroxyprogesterone

Question 14

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

Answer 14

Higher doses for emergency contraception

Question 15

How long after intercourse can one take Plan-B?

Answer 15

72 hours

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

Question 16

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

Answer 16

8%

Question 17

What are the mild adverse effects associated with contraceptives?

Answer 17

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

Question 18

What are the moderate adverse effects of contraceptives?

Answer 18

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

Question 19

What are the severe adverse effects of contraceptives?

Answer 19

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

Question 20

What are the benefits of contraceptives?

Answer 20

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

Question 21

What are the contraindications to estrogen containing contraceptives?

Answer 21

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

Question 22

What are the drugs that induce hormone metabolism?

Answer 22

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

Question 23

What effect do antibiotics have on contraceptives?

Answer 23

Decreased efficacy

Question 24

What is the clinical indication for Clomiphene?

Answer 24

Fertility drug

Question 25

What is the MOA of Clomiphene?

Answer 25

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

Question 26

What is a partial agonist?

Answer 26

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

Question 27

What adverse effects are associated with Clomiphene?

Answer 27

1) Hot flashes | 2) Multiple births

Question 28

When in the menstrual cycle is Clomiphene given?

Answer 28

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

Question 29

What are SERMS?

Answer 29

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

Question 30

What is the function of SERMS in bone?

Answer 30

Suppress bone resorption (agonist) *I.e. estrogen receptor agonism will reduce osteoporosis

Question 31

What is the function of SERMS in the endometrium?

Answer 31

Proliferation (partial agonist) *This is an unintended adverse effect and can lead to development of endometrial hyperplasia and endometrial CA*

Question 32

What is the function of SERMS in pituitary and breast?

Answer 32

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

Question 33

List the two SERMS.

Answer 33

Tamoxifen | Raloxifene

Question 34

What is the clinical indication for Tamoxifen?

Answer 34

ER+ Breast Cancer

Question 35

What adverse effects are associated with Tamoxifen?

Answer 35

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

Question 36

How does Raloxifene differ from Tamoxifen?

Answer 36

NO partial agonist effects on endometrium

Question 37

What are the clinical indications for Raloxifene?

Answer 37

1) Breast cancer | 2) Post-menopausal bone loss

Question 38

What key adverse effect is associated with Raloxifene?

Answer 38

Hot flashes

Question 39

What are the clinical indications for dananzol?

Answer 39

1) Endometriosis | 2) Breast fibrocystic disease

Question 40

What is the MOA of dananzol?

Answer 40

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

Question 41

What adverse effects are associated with dananzol?

Answer 41

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

Question 42

What is the MOA of anaztrozole and letrozole?

Answer 42

Aromatase inhibitors that prevent conversion of Testosterone to Estrogen

Question 43

What are the indications for anaztrozole and letrozole?

Answer 43

ER+ breast cancer

Question 44

What adverse effects are associated with anaztrozole and letrozole?

Answer 44

- GI disturbances - Hot flashes - Lethargy

Question 45

List the anti-progesterone drugs.

Answer 45

Mifepristone | Ulipristal

Question 46

What is the MOA of Mifepristone?

Answer 46

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

Question 47

What is the clinical use of Mifepristone?

Answer 47

Abortifacient (less than 7 weeks/ first trimester) *Followed by misoprostol (synthetic prostaglandin, which further increases uterine contractions) 48 hours later*

Question 48

What is the clinical indication for Uliprastal?

Answer 48

Emergency contraception

Question 49

What is the MOA of Uliprastal?

Answer 49

Partial progesterone agonist

Question 50

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

Answer 50

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