Contraceptives

Question 1

Estrogens

Answer 1

Estradiol, estriol, estrone

Question 2

Progestin

Answer 2

Progesterone

Question 3

Major site of synthesis

Answer 3

Ovarian granulosa cells

Corpus luteum

Question 4

Estrogens Special Effects

Answer 4

• Reduced bone resorption
• Metabolic effect
• Pro-coagulatory effects

Question 5

Progestins Special Effects

Answer 5

• Basal body temperature

* Endometrial and cervical secretion

Question 6

Synthetic (and conjugated) compounds

Answer 6

Estrogens: ethinyl estradiol; mestranol
Progestins:
A. ester of progesterone
medroxyprogesterone acetate
B. 19-nortestosterone
norethindrone — moderate androgenic
norgestimate & levonorgestrel – low androgenic

Question 7

Contraceptive Preparations (3 types)

Answer 7

Estrogen+progestin
Progestin Alone
Post-coital

Question 8

Combined Contraceptives

Answer 8

Multiple mechanisms of action
Prevent ovulation (Negative feedback on FSH  and LH)
Thickened cervical mucus
Endometrial changes to prevent implantation

Question 9

Lunelle

Answer 9

Estradiol cypionate + medroxyprogesterone acetate
Injection given every 28-33 days
50% of women experience withdrawal bleeding that begins 20-25 days after injection
15% may experience no bleeding at all
>99% effective

Question 10

NuvaRing

Answer 10

Etonogestrel/Ethinyl estradiol
A flexible ring about 2 inches in diameter 
 that is inserted into the vagina
Remains in the vagina for 3 weeks, then
 is removed for 1 week
99% effective

Question 11

Ortho Evra

Answer 11

ethinyl estradiol and norelgestromin
A transdermal patch that delivers E + P
Worn continuously for 7 days before being replaced with new patch
Regimen followed for 3 weeks followed by a patch- free week
99% effective; Less effective in women weighing over 198 lbs.
Patch risk: three times higher blood clots due to the 60%more estrogen than a normal pill

Question 12

Continuous estrogen/progestin combination pills

Answer 12

No scheduled menstrual bleeding

Increased risk of unrecognized pregnancy

Question 13

Estrogen Adverse effects

Answer 13

GI disturbances
Weight gain
Migraine headache
Fluid retention
Breast tenderness
Increased blood clots 
Endometrial cancer (for HRT)

Question 14

Progestins Adverse effects

Answer 14

Breakthrough bleeding
Mild depression
Weight gain

Question 15

Yasmin®, Yaz® or Ocella®

Answer 15

synthetic progestin drospirenone, plus ethinylestradiol
drospirenone can elevate the body’s potassium levels and lead to hyperkalemia, thus serious and potentially fatal heart problems

Question 16

Progestin alone therapy

Answer 16

Mechanisms of action: prevent ovulation, thickening of cervical mucus, endometrial changes, 97-98% effective
Therapeutic indication: Estrogens contradicted or poorly tolerated

Question 17

Postcoital contraception

Answer 17

Ethinyl estradiol/levonorgestrel (Preven)
Plan B levonorgestrel
Mechanisms of action (not clear)
Delays or prevents ovulation
Endometrial changes that prevent implantation
Not effective if already pregnant
1st dose within 72 hrs, 2nd dose 12 hrs later

Question 18

Clomiphene (Clomid)

Answer 18

Fertility drug
Mechanism of action:
estrogen receptor antagonist
Inhibits negative feedback effects 
on hypothalamus and anterior pituitary
Induces ovulation

Question 19

Mifepristone (RU-486, Mifeprex)

Answer 19

Contragestation
competitive antagonist of progesterone and glucocorticoid receptors
Uses: Medical abortion (early pregnancy)
Administered after implantation; leads to endometrial shedding

Question 20

Selective estrogen receptor modulators (SERMs)

Answer 20

Mimic the effects of estrogen in some organs but act as antagonists in others

Question 21

Tamoxifen (Nolvadex)

Answer 21

Estrogen antagonist in breast tissue, inhibits proliferation of breast cancer

Question 22

Raloxifene (Evista)

Answer 22

Estrogen antagonist in breast and uterin, agonist in bone

• -prevent postmenopausal osteoporosis
• -reduce the risk of invasive breast cancer in postmenopausal women

Question 23

Femara (Letrozole)

Answer 23

aromatase inhibitor, reduces estrogen production

First line treatment for breast cancer with or without positive response to estrogen

Question 24

Hormonal replacement therapy

Answer 24

Primary Hypogonadism
Postmenopausal Hormonal Therapy based on estrogen
Alleviation of hormone-withdrawal symptoms
hot flashes, night sweats, etc.
Prevention of osteoporosis
Estrogen decreases bone resorption