Lecture 2/3

Question 1

What is the MOA of estrogen ?

Answer 1

Secreted because of FSH
prevents follicular development and ovulation

Increase endometrium lining

Question 2

What is the MOA of progestin ?

Answer 2

inhibits ovulation
Thickens cervical mucus ( les sperm transport)
Slows the tubal transport
maintains the lining and highly part of the luteal phase

Question 3

Which of the following estrogens in CHC products is a synthetic version of the estrogen produced by the human fetal liver?

Answer 3

Estetrol (E4)

Question 4

What is the primary advantage of ethinyl estradiol (EE) over other forms of estrogen in CHC products?

Answer 4

Longer half-life and increased potency

Question 5

What are the estrogen made by the body ?

Answer 5

estrone 1
estradiol 2
Estriol 3
Esterol 4

Question 6

Which estrogen is released bythe placenta during pregnancy ?

Answer 6

E3

Question 7

Where and when is Estrone 1 made ?

Answer 7

ovaries, after menopause

Question 8

What is special regarding the 3rd progestin?

Answer 8

less andregenic, same progestin, estrogenic effect

Question 9

What are the non-contraceptive benefits of combined hormonal contraceptives?

Answer 9

improve cycle control
inhibits ovulation
lower risk of colorectal cancer
good effect on bone mineral density

Question 10

Which hormones has a procoagulant effect ?

Answer 10

Estrogen and dose- dependent

Question 11

What are the risks that increases VTE while being on CHC ?

Answer 11

in the 1st year
thrombophilia
older, age, obesity, recent surgery
6 weeks after delivery

Question 12

What are the risks that increases MI or Stroke while being on CHC?

Answer 12

doses more than 50 ug EE
smoking, >35 years old
hypertension

Question 13

What is the connection between breast cancer and CHC ?

Answer 13

None , unknown

Question 14

What are the effect of CHC to BP ?

Answer 14

Increases BP

Question 15

How can CHC be linked to diabetes ?

Answer 15

progestin can compete with insulin receptors

Question 16

Name 1st gen progestin ?

Answer 16

norethindrone,
ethynodiol

Question 17

Name 2nd gen CHC ?

Answer 17

norgestrel,
levonorgestrel

Question 18

Name 3rd gen CHC ?

Answer 18

desogestrel,
norgestimate,
norelgestromin,
etonorgestrel

Question 19

What are the the risks of combined hormonal contraceptives.

Answer 19

VTE , MI, Breast Cancer
BP, Diabetes, TG, gallbladder and migraines

Question 20

Name 4th gen CHC ?

Answer 20

Drospirenone

Question 21

which of the CHC has the lower androgenic activities ?

Answer 21

3rd gen CHC
desogestrel,
norgestimate,
norelgestromin,
etonorgestrel

Question 22

Which of the CHC has the most progesterone and androgenic ?

Answer 22

2nd gen CHC
norgestrel,
levonorgestrel

Question 23

What are contraindications to CHC ?

Answer 23

major one : >35 years + smoking
breastfeeding

Question 24

What are the contraindications for drospirenone ?

Answer 24

renal or liver failure, adrenal disease, drugs that
increase K+ levels (ie ACE inhibitors, spironolactone)

Question 25

What is the most common SE of CHC ?

Answer 25

Breakthrough bleeding

Question 26

What are the SE due to estrogen ?

Answer 26

nausea § breast tenderness § fluid retention/edema § headaches/migraines § chloasma § poor contact lens fit

Question 27

What are the SE due to progesterone

Answer 27

mood: depression, PMS, fatigue § breast tenderness § bloating § fluid retention § increased appetite § headache/migraines

Question 28

What proportion of unintended pregnancies are among contraceptive users?

Answer 28

50%

Question 29

Your professor in a seminar asks you to pick a 19-nortestosterone derivative progestin found in combined hormonal contraceptives which maintains progesterone selectivity but has less androgenic activity compared to a 2nd generation progestin. You would tell her the following progestin has these features:

Answer 29

3rd gen CHC : Desogestrel

Question 30

Which type of congestion would be beneficial for patient that has acne?

Answer 30

Antiandrogenic , cyproterone 4th gen, drospirenone

Question 30

What are the non-contraceptive of the benefits of CHC?

Answer 30

Cycle control: less painful menstrual cycle, less menstrual loss Acne control Inhibited ovulation: lower risk of the topic, pregnancies or overian cysts Lower risk of ovarian and endometrial cancer Positive effects on bone density Symptom control in perimenopause

Question 31

Why is there medical risk of VTE with CHC?

Answer 31

It contains estrogen, which is a dose dependent proCOAGULANT effect, and fubronolytic balance

Question 32

What is the most potent synthetic estrogen in reproductive years ?

Answer 32

Estradiol E2

Question 33

When is the risk of VTE highest for patient on CHC ?

Answer 33

In the first year of use Pregnancy Peripartum period

Question 34

Why does the third generation progestin have an increased rate of VTE compared to second gen progestin ?

Answer 34

Because second generation have more androgenic properties that adds to counteract the coagulant effect of estrogen

Question 35

What are the risk factors for patients are taking CHC for MI or stroke?

Answer 35

Does related more than 50 µg of estrogen synthetic hormone Smoking and over the age of 35 and hypertension

Question 36

What are the contradictions of a patient whose fourth generation CHC drospirenone?

Answer 36

Since it is an anti-mineral cortical steroid Renal and liver failure, adrenal disease, drugs that increase potassium levels like ace inhibitors, and spironolactone .

Question 37

What are the signs for deficiencies in estrogen?

Answer 37

Break through bleeding mood changes, menopausal symptoms like vaginal dryness Hypomenorrhea

Question 38

What can you expect in a patient who has low progesterone levels ?

Answer 38

Late breakthrough bleeding/spotting Heavy period Delayed menses

Question 39

Which of the sex hormones goes through enterohepatic recirculation ?

Answer 39

EE - synthetic estrogen

Question 40

What is the CYP for the metabolism of estrogen & progestins ?

Answer 40

CYP 3A4

Question 41

Which drug interactions should you pay attention to when a patient is on CHC

Answer 41

Anticonvulsant Antimicrobial : rifampin Lamotrigine

Question 42

What is the drug interaction between Lamotrigine and CHC?

Answer 42

CHC induces a metabolism of lamotrigine and clearance and results in a loss of seizure control Lamotrigine may need to be adjusted after starting and after discontinuation

Question 43

Why does antibiotics affect CHC?

Answer 43

And the fact of micro biome, which and then interferes with her hepatic recirculation of EE

Question 44

What level of synthetic estrogen should you to sit there? My patient starting on CHC ?

Answer 44

All we start with a low dose of EE less than 35 µg Patient is over 35 years old considered EE lesson 20 µg

Question 45

What are the type of altered hormone free interval regimen?

Answer 45

Shorten hfi Extended cycle (continue, extended cycle)

Question 46

What is the rationale for shortening hfi ?

Answer 46

There are list of pregnancy since fsh levels may have not been suppressed during the 70 days hfi

Question 47

What is your recommendation for patient and continuous cHc having more spotting and break through bleeding?

Answer 47

Use monophasic products

Question 48

What is something to keep in mind when recommending contraceptive patches?

Answer 48

Potentially increase of VTE compared to oral contraceptive, the patient weight is over 90 kg. because they have 3rd gen

Question 49

How long can a patient wear vaginal contraceptive range?

Answer 49

Technically, four weeks equal 28 days Or three weeks and remove for one week free interval

Question 50

It’s a patient from the vaginal ring more than three hours. What do they do?

Answer 50

No longer viable and 7 days of back up

Question 51

What is the MOE of estetrol/dropirenone CHC ?

Answer 51

Estetrol E4 —> selective and binds to ER in the nucleus and membrane

Question 52

What are the advantages of estetrol/ drospironone ?

Answer 52

Less risk of VTE, weak estrogen effects on the mammary glands , not metabolize by CYP

Question 53

When does the CHC start to work ?

Answer 53

7 days

Question 54

When would you need back up contraceptive ?

Answer 54

First trial : Sunday/Quick start / missed dose

Question 55

How long does a side effect last for CHC after initiation?

Answer 55

Within 3 months

Question 56

What are the warning times after contraceptive oral use?

Answer 56

ACHES - abdominal pain, chest pain, headaches, eye problems, severe leg pains

Question 57

What should the patient do if they missed more than 1 pill in week 2 or 3 ?

Answer 57

Take 1 pill and finish cycle No HFI

Question 58

What should a pt do is they missed > =3 pills in week 2-3 ?

Answer 58

Take one pill No HFI 7 days back up or EC if unprotective sex in last 5 days

Question 59

When should we follow up on a patient after the initiation of CHC ?

Answer 59

1-3 months

Question 60

What is the cause and the recommendation where a pt has BTB from a monophasic CHC ?

Answer 60

if early : Due to the deficiency in estrogen Take a break and INCREASE the dose of EE Late : due to progestin , take biphasic next time

Question 61

What should you do is the pt mentions water retention after CHC ?

Answer 61

Estrogen ADR —> lower EE Progestin ADR —> change progestin to drospirenone

Question 62

If the pt experiments BTB after 3 months of CHC ? Solutions ?

Answer 62

Find the cause ( both estrogen and progestin deficiency) Early in the cycle = Increase the dose of EE Late in the cycle = change progestin Stop the pill for 3-4 days to see if it is resolved