Hormones and Contraceptives

Question 1

MOA of Ethinyl estradiol

Answer 1

synthetic estrogen. Has ethinyl groups (triple bonds) which greatly decrease hepatic metabolism.

In conjunction with progestins, drop FSH and LH levels to prevent ovulation and pregnancy.

Question 2

MOA of levonorgestrel

Answer 2

synthetic progestin. Thickens cervical mucus to stop sperm. Blocks ovulation 70% of the time.

Progesterone = Pro-pregnancy
breast development, pregnancy maintenance, inhibits uterine contraction, alters carb metab, stimulates fat uptake and bad lipid profile.

Question 3

MOA of norgestrel

Answer 3

synthetic progestin. Thickens cervical mucus to stop sperm. Blocks ovulation 70% of the time.

Progesterone = Pro-pregnancy
breast development, pregnancy maintenance, inhibits uterine contraction, alters carb metab, stimulates fat uptake and bad lipid profile.

Question 4

MOA of mestranol

Answer 4

synthetic estrogen.

In conjunction with progestins, drop FSH and LH levels to prevent ovulation and pregnancy.

Question 5

MOA of mifepristone

Answer 5

antiprogestin. Blocks binding of progesterone to its receptors. Stimulates uterine contractions. Used to terminate pregnancy or as delivery inducer. (must be less than 49 days into pregnancy to abort)

Question 6

MOA of fluoxymesterone

Answer 6

testosterone derivative. Oral delivery, short acting. Alkylation of 17-a psoition allows oral admin becuase it decreses hepatic metabolism.

Question 7

MOA of testosterone transdermal patches

Answer 7

better than oral or injection.

Question 8

MOA of danazol

Answer 8

androgen. Used to treat endometriosis and PMS. Weakly androgenic. IM injection. Long acting.

Question 9

ADE of testosterone supplementation?

Answer 9

Makes ladies into dudes and dudes into ladies.

virilizing females.
Feminizing males because testot converted to estradiol.
Suppression of LH and FSH decereases testis, spermatogen.
Decreases HDL and increases LDL increasing CHD risk.

Question 10

MOA of cyproterone acetate

Answer 10

Competes with DHT for androgen repceptor to prevent translocation to nucleus.
IM injection, long acting. Used to treat acne, baldness, hirsutism.

Question 11

ADE of cyproterone acetate

Answer 11

inhibits libido

Question 12

MOA of flutamide

Answer 12

androgen receptor antagonist. Treats prostate cancer.

Question 13

ADE of flutamide

Answer 13

Hepatic toxicity and must be taken 3x daily

Question 14

MOA of onapristone

Answer 14

antiprogestin. a more pure antagonist.. Used to terminate pregnancy. (must be less than 49 days into pregnancy)

Question 15

MOA of anastrozole

Answer 15

aromatase inhibitor. non-steroidal. used after tamoxifen failure. Decreases estrogen to extremely low levels by inhibiting conversion of adrenal androgens to estrogens.

Question 16

MOA of letrozole

Answer 16

aromatase inhibitor. non-steroidal. used after tamoxifen failure. Decreases estrogen to extremely low levels by inhibiting conversion of adrenal androgens to estrogens.

Question 17

MOA of testosterone cypionate derative

Answer 17

testosterone derivative.

Question 18

MOA of copper IUD

Answer 18

one of the most effective contraceptives. Copper is spermacidal. Effective for 15-20 years.

Question 19

ADE of copper IUDs

Answer 19

copper can cause cramping and progestin-irrugular bleeding. High initial cost, low overall. Must be inserted by physician.

Question 20

MOA of vaginal contraceptive rings

Answer 20

one of the most effective contraceptives. Inserted by patient.

Question 21

ADE of vaginal contraceptive rings

Answer 21

discomfort, headaches, vaginal discharge. Not effective for 7 days.

Question 22

Which hormone would make myometrium smooth muscle hyperpolarized: estrogen or progesterone? What effect does this have?

Answer 22

Progesterone is elevated in pregnancy. It hyperpolarizes uterine smooth muscle membranes making them non-excitable and preventing release of arachidonic acid, preventing prostaglandins from being made.

Question 23

What effect does estrogen have on myometrium gap junctions?

Answer 23

estrogen increases the number of gap junctions that couple the myometrial muscle cels. This also increases the receptors for contractile agonists, making contraction more likely

Question 24

What do tocolytics do?

Answer 24

prevent contraction –> prevent premature parturition and delay delivery for brief periods

Question 25

What do oxytocics do?

Answer 25

induce contractions. –>labor. control postpartum uterine hemorrhage. Therapeutic abortion

Question 26

What are the 3 natural estrogens?

Answer 26

estradiol (most potent and principal ovarian steroid)
estrone
estriol (least potent, placental steroid and made from estradiol and estrone in liver and adipose)

Question 27

What are the differences between selective estrogen receptor modulators and antiestrogens?

Answer 27

SERM = selective estrogen receptor modulator. Produce estrogen effects only where beneficial (bone, brain, liver) and avoid breast and endometrium. Ex. tamoxifen.

Antiestrogens (clomiphene) antagonize all tissues and are used as ovulation inducing agents.

Question 28

How are the majority of estrogens and androgens transported in blood?

Answer 28

bound to sex hormone binding globulin (SHBG)

Question 29

How would administration of estrogen affect SHBG and free androgen levels?

Answer 29

estrogen will increase SHBG, decreasing free angrogen levels

Question 30

How is progesterone primarily transported in blood?

Answer 30

bound to transcortin

Question 31

What effect do estrogens have on lipid profile?

Answer 31

increase HDL, decrease LDL and lower incidence of CHD in pre-menopausal women. Estrogens do increase risk of stroke+DVT though because of increased clotting factors.

Question 32

What effect do estrogens have on bone resorption? How?

Answer 32

decrease bone resorption and oppose osteoporosis by decreasing activity and number of osteoclasts

Question 33

What effect do estrogens have on hepatic proteins and clotting factors?

Answer 33

increases TBG, transcortin, SHBG and clotting factors.

Question 34

Usually giving estrogen is a bad idea for cancer. It can stimulate progression of endometrial and breast tumors. When is it helpful?

Answer 34

prostate cancer.

Question 35

What effect does progesterone have on carb metab?

Answer 35

increases basal insulin levels and promotes glycogen storage.

Question 36

What effect does progesterone have on lipid profile?

Answer 36

Opposite of estrogen. Decreases HDL and increases LDL. Also stimulates LPL (fat transfer from lipoproteins to tissue) Increase risk of CHD.

Question 37

Which hormone is responsible for the spike in body temperature at ovulation?

Answer 37

progesterone

Question 38

What is the minipill?

Answer 38

progestin only pill.

Question 39

A patient asks what the most effective forms of contraception are

Answer 39

Sterilization, IUDs, progestin implants, —> least effective = barriers like condoms and diaphragms

Question 40

In addition to antibiotics, what other drugs can cause oral contraceptives to fail?

Answer 40

rafampin, anti-HIV agents, anticonvulsants, and St. John’s wort.

Question 41

Compare DHT to tesetosterone.

Answer 41

DHT is made by 5a-reductase. It is more potent and binds 10x tighter than testosterone

Question 42

ADEs of progesterone?

Answer 42

GI, menstrual disorders, bad lipid profiles, depression, acne, weight gain

Question 43

ADE of letrozole

Answer 43

non-steroidal AIs can cause cataracts.
Hot flashes, Nausea, Hair thinning (no effect on adrenal steroids/thyroid function). arthralgia/diarrhea but less gyn Sx then tamoxifen.

Question 44

ADE of anastrozole

Answer 44

non-steroidal AIs can cause cataracts.
Hot flashes, Nausea, Hair thinning (no effect on adrenal steroids/thyroid function). arthralgia/diarrhea but less gyn Sx then tamoxifen.