Pharmacology of Hormonal Contraceptives

Question 1

Estrogen receptor mechanisms?

Answer 1

Steroid/lipophilic
Binds to receptor in cytoplasm
Leads to altered gene expression and mRNA synthesis

Question 2

What is the most potent estrogen?

Answer 2

Estradiol

Question 3

What are the most common synthetic forms?

Answer 3

Ethinyl estradiol and mestanol

Question 4

Estradiol is not used because?

Answer 4

Poor oral bioavailability due to rapid first pass metabolism

Question 5

Ester does what?

Answer 5

Allows longer duration of action

Question 6

Estrogens cause what?

Answer 6

Proliferative changes in the endometrium and increase the amount of cervical mucus

Question 7

Estrogen ADME

Answer 7

wide VofD
Free drug is the active form
Estradiol is eliminated rapidly but the synthetics are eliminated slower
Into the urine
Show enterohepatic re-circulation

Question 8

Estrogen Adverse Effects

Answer 8

Increased risk of breast, endometrial, cervical, vaginal cancer
Increased risk of MI, DVT, or PE
Severe migraine, n/v, reactivation or exacerbate endometriosis

Question 9

Pregnanes Example

Answer 9

Medroxyprogesterone acetate

Question 10

Estranes Example

Answer 10

Nortestosterone

Question 11

Estranes Properties

Answer 11

Exhibit progestational, androgenic (facial hair) and other activities

Question 12

Gonanes Example

Answer 12

Norgestrel

Question 13

Gonanes Properties

Answer 13

No estrogenic effects, diminished androgenic activity

Question 14

Progestin activity on the reproductive tract development

Answer 14

Thickening of cervical mucous

Decrease progesterone at end of cycle –> menstruation

Question 15

Progestin activity on CNS

Answer 15

Induce 0.6 degrees C –> depressant activity

Question 16

Progestin activity on metabolic effects

Answer 16

Decreased effects of insulin, enhanced fat deposition

Question 17

Progestin Receptor Mechanisms

Answer 17

Lipophilic
Receptors in the cell
Leads to altered gene expression and mRNA synthesis

Question 18

Progestin ADME

Answer 18

Limited oral bioavailability due to hepatic metabolism
Broad distribution
In urine

Question 19

Progestins bind to?

Answer 19

SHBG and albumin (plasma proteins)

Question 20

Progestin adverse effects

Answer 20

Etopic pregnancy
Irregularm unpredictable spotting
Weight change
Abnormal glucose tolerance test

Question 21

Monophasic

Answer 21

21 days with hormones + 7 without

Question 22

Biphasic

Answer 22

Two different doses of hormones for 21 days

Question 23

Triphasic

Answer 23

Three different doses of hormones for 21 days

Question 24

Progestin only

Answer 24

Less effective
Needs to be taken at the SAME time every day
Irregular and unpredictable menstrual bleeding

Question 25

Combination Oral Contraceptives

Answer 25

Progestin + Estrogen Alters cervical mucous Inhospitable endometrial lining PREVENTS ovulation

Question 26

Progestin in contraceptives?

Answer 26

Thicken cervical muculs Slows sperm transport Impairs implantation in the endometrium Suppresses LH surge (ovulation)

Question 27

Estrogen in contraceptives?

Answer 27

``` Stabilizes endometerial lining Suppresses FSH (prevents a dominant follicle) ```

Question 28

Menstranol is?

Answer 28

50% less potent than ethinyl estradiol bc it has to be convert to it first

Question 29

Extended cycle OCs

Answer 29

84 hormone pills +7 days of placebo | 4 menstrual cycles per year

Question 30

Continuous cycle OCs

Answer 30

Hormones for 21 days and then low-dose E&P for 4-7 days

Question 31

Both extended and continuous cycle can lead to

Answer 31

Decreased amount of bleeding and ultimately amenorrhea

Question 32

Side effects of OCs

Answer 32

N/V MI, stroke, emboli Breast enlargement Breakthrough bleeding

Question 33

Serious Side Effects of OCs?

Answer 33

Blood clots ACHES Cancer Gall bladder

Question 34

ACHES stands for

Answer 34

``` Abdominal pain Chest pain Headaches Eye problems Swelling and leg pain (DVT) ```

Question 35

Precaution for use of COC

Answer 35

``` >35 Smoking HTN Dyslipidemia Diabetes Headaches Breast cancer Thromboembolism Obesity ```

Question 36

Obesity problem?

Answer 36

The hormones will go hide in the fat cells of the body and not cause the effects they needed