Gonadal Hormones

Question 1

When the primary follicle matures, it secretes

Answer 1

estrogen

Question 2

Mature follicle releases ovum and then follicle transforms into

Answer 2

Corpus Luteum

Question 3

Corpus Leuteum secretes

Answer 3

progesterone which is involved in maintenance of the endometrium

Question 4

Ovarys release what hormones

Answer 4

estrogen and progesterone

Question 5

Precursor for hormones

Answer 5

cholesterol

Question 6

Enzyme transforms non aromatic onto aromatic

Answer 6

Aromatase

Question 7

Main natural estrogen

Answer 7

estradiol

Question 8

Genistein

Answer 8

Natural compound found in plants such as soy, used OTC , used to support women undergoing menopause. It can activate estrogen receptors similar to Estadiol.

Question 9

Bisphenol A

Answer 9

Used in plastic bottles. Might have hormonal effects. Could be disruptive in developing fetuses.

Question 10

Why use synthetic estrogens?

Answer 10

estrogen has low bioavailability when taken orally. Can increase the bioavailability when used as a cream, but it is still low.

Question 11

Pharmokinetics of estrogens

Answer 11

Binds strongly to sex hormone binding globulin.
Biotransformation in the liver and excretion in bile (can compromise the liver).

Lipophilic , requires proteins for shuttling.

Cytoplasmic receptors, not transmembrane.

Binding estrogen forms complex with receptors, dimerizes then binds to DNA sequence. Different receptors than GCS, but same sequence of events.

Question 12

Physiological effects of estrogens

Answer 12

Decrease rate of bone resorption

Reduce total plasma cholesterol

Endometrial effects

stimulate production of leptin

structure and function of skin and blood vessels.

Enhance blood coagulability

Maturation

Question 13

Clinical uses of estrogens

Answer 13

hypogonadism

postmenopausal hormone therapy

hormonal contraceptive

Question 14

Estrogen side effects

Answer 14

Uterine bleeding

Cancer (slightly enhanced risk of breast cancer, but rare)

Question 15

Progestins produced by CL and synthesized in

Answer 15

ovary, testis, adrenal cortex, placenta during pregnancy

Question 16

Progestins are metabolized in the

Answer 16

liver and secreted in the urine as a glucuronide conjugate

Question 17

Progesterone favors

Answer 17

fat deposition, increased basal insulin levels and promotes glycogen storage

Question 18

Progesterone competes with

Answer 18

aldosterone and decreases sodium reabsorption

Question 19

Progesterone increases

Answer 19

body temp (indicator of ovulation)

Question 20

Synthetic progestins do not

Answer 20

usually support implantation of fertilized egg

Question 21

1:1 estrogen progesterone ratio

Answer 21

monophonic

Question 22

bi and tri phasic differs in

Answer 22

hormone levels

Question 23

continuous progestin therapy aka

Answer 23

mini pills

Question 24

Use mini pills when

Answer 24

patients don’t respond to estrogen

Question 25

Estrogens to known

Answer 25

Ethinyl Estradiol Mestranol Estradiol Valerate

Question 26

Progestins to know

Answer 26

norgestrel desogestrel norethindrone

Question 27

Main purpose of combined forms of estrogen and progesterone

Answer 27

prevent LH spike and inhibit ovulation

Question 28

Progestins mostly effect

Answer 28

endometrium and changes in the uterus

Question 29

Mini pills do not . . .

Answer 29

inhibit ovulation, but influence changes in the endometrium. Effects are purely on endometrium.

Question 30

Pharmacologic effects of hormonal contraceptives (1)

Answer 30

depression of ovarian function hypertrophy of cervix changes in cervical mucous stimulation of breasts (risk of breast cancer)

Question 31

Pharm effects of hormonal contraceptives (2)

Answer 31

change in other hormones regulated to AP increased pigmentation, changes in serum production increased coagulation beneficial changes in lipid profile change in levels of globulins (more globulins that binds steroids = less bioavailability , only active in their free form)

Question 32

Adverse effects of estrogens (mild)

Answer 32

nausea, Mastalgia, edema, headache, lack of withdrawal bleeding

Question 33

Adverse effects of estrogens (moderate)

Answer 33

abnormal bleeding when its not time for the period vaginal infections weight gain acne and hirsutism amenorrhea

Question 34

Adverse estrogen effects severe

Answer 34

cancer, depression , vasular disorders

Question 35

SERMs

Answer 35

selective estrogen receptor modulators (not called antagonist because they inhibit some receptors in some tissues, but activate in other, depends on location.

Question 36

SERMs to know

Answer 36

tamoxifen raloxifen toremifene clomifene mifepristone

Question 37

How does tamoxifen, raloxifen, and toremifene work?

Answer 37

used in patients with breast cancer after mastectomy to prevent metastasis and used in cancer that responds to increase estrogens. Could cause hot flashes, no negative impacts on bone.

Question 38

How does clomifene work?

Answer 38

blocks only estrogen receptors in the brain. (hypothalamus and Ant pit) blocks the neg feedback , so CNS keeps pumping estrogens . Why use these? In fertility clinics , to stimulate fertilization.

Question 39

Mifepristone

Answer 39

Antagonist of GCS and MCS, but mainly blocks progesterone receptors. Will be used to induce abortions often used in combinations of drugs that will stimulate uterine contractions, certain prostaglandins may increase uterine contractions.

Question 40

Androgens are produced in

Answer 40

testes or adrenal glands

Question 41

Physiological form of Testosterone

Answer 41

Dihydrotestosterone

Question 42

Taking testosterone may increase estrogens

Answer 42

aromatase does this conversion

Question 43

Physiological effects of androgens

Answer 43

maturation replacement therapy low libido (also used in females) growth stimulators (AIDS)

Question 44

Androgen side effects

Answer 44

prostatic hyperplasia sleep apnea, agressiveness Acne masculinizing effects

Question 45

Drugs that inhibit androgens will be used in treating

Answer 45

prostate cancer or prostate hyperplasia

Question 46

Dihydrotestosterone may

Answer 46

stimulate balding , so drugs may block this to prevent balding

Question 47

Inhibits synthesize of steroids way up the pathway

Answer 47

Ketoconazole, spironolactone

Question 48

Inhibits 5 alpha reductase which converts testosterone to dihydrotestosterone

Answer 48

finasteride and Dutasteride

Question 49

Directly inhibits receptors of dihydrotestosterone

Answer 49

Flutamide, cyproterone, spironolactone

Question 50

Combination given for prostate hyperplasia

Answer 50

alpha 1 antagonist and 5 alpha reductase inhibitor