Estrogens and androgens

Question 1

Estradiol

Answer 1

most potent estrogen produced and secreted by ovaries, principle estrogen in premenopausal women

Question 2

estrone

Answer 2

metabolite of estradiol, 1/3 istrogenic potency, primary circulating estrogen after menopause

Question 3

Estriol

Answer 3

another metabolite of estradiol, significantly less potent, present during pregnancy, principle estrogen produced by placenta

Question 4

ADRs of estrogen

Answer 4

nausea and breast tenderness

Question 5

How should estrogen therapy be used for intact uterus?

Answer 5

progesterone in combo with estrogen

Question 6

How should estrogen therapy be used for hysterectomy?

Answer 6

estrogen alone, progesterone may alter the beneficial effects of estrogen on lipid parameters

Question 7

what are the SERMS

Answer 7

tamoxifen, raloxifene (Evista), Clomiphene (Clomid)

Question 8

MOA of SERMS

Answer 8

interact with estrogen receptors but have different effects depending on the tissue, selective agonism or antagonism according to tissue type

Question 9

Clinical use of tamoxifen

Answer 9

palliative treatment of metastatic breast cancer in postmenopausal women, some breast tumors regress with treatment

Question 10

ADRs of tamoxifen

Answer 10

nausea, hot flashes, endometrial hyperplasia, and malignancy

Question 11

Raloxifene (evista) use

Answer 11

prophylaxis of br ca in high risk women, prevention and tx of osteoporosis in postmenopausal women, decreases bone resorption and bone turnover, little to no effect on endometrial tissue, decrease total and LDL cholesterol

Question 12

Adrs of raloxifene

Answer 12

hot flashes, leg cramps, increase of deep venous thrombosis and pulmonary embolism

Question 13

Clomiphene use

Answer 13

tx of infertilit associated with anovulatory cycles, interferes w/ negative feedback of estrogens on hypothalamus, inc secretion of GnRH and gonadotropins leading to stimulation of ovulation

Question 14

ADRs of clomiphene

Answer 14

dose related nausea, HA, hot flashes, visual disturbances, ovarian enlargement

Question 15

progesterone produced in response to

Answer 15

LH in females and males

Question 16

where is progesterone produced?

Answer 16

in females it is secreted by corpus luteum during luteal phase an dbby placenta, in males it is secreted by testes

Question 17

What does progesterone do

Answer 17

promotes development of secretory endometrium, accommodates implantation of newly forming embryo

Question 18

What is the major clinical use of progesterone

Answer 18

contraception and treatment of hormonal deficiencies, and control of dysfunctional uterine bleeding, treatment of dysmenorrhea and management of endometriosis and infertility

Question 19

Progesterone ADRs

Answer 19

HA, depression, wt gain, changes in libido, some can cause increase in LDH cholesterol- acne, and hirsutism

Question 20

What is medroxyprogesterone adr

Answer 20

increased risk of osteoporosis, so take with calcium and only use 2 years

Question 21

Contraceptive MOA

Answer 21

for estrogens- negative feedback on release of LH/FSH, consistent levels prevent LH spike and ovulation; progestin- make cervical mucus less permeable, makes implantation more difficult

Question 22

Progestin only contaceptives

Answer 22

are less effective, but preferred when estrogen use is not desired, still prevents LH spike, used for breastfeeding women, history of clots and >35 and smokers

Question 23

How often is injectable progestin given

Answer 23

every 3 months

Question 24

What can injectable progestin cause

Answer 24

wt gain, and amenorrhea, can delay fertility for several months

Question 25

Advantages of progestin implants

Answer 25

offers long term contraception, effects reversible when removed, nearly as reliable as sterilization

Question 26

Complications with contraceptives

Answer 26

increased risk of DVT, increased MI and stroke, inc BP

Question 27

Advantages of contraceptives

Answer 27

regulation, decreased flow, improved acne, can stabilize moods, dec unplanned pregnancy

Question 28

ADRs of contraceptives

Answer 28

breakthrough bleeding, imbalance in estrogen and progestin components, nausea/vomiting, wt gain, breast tenderness, fluid retention, depression

Question 29

androgens

Answer 29

steroids with anabolic and masculinizing effects in both males and females, testosterone is the most important

Question 30

what is testosterone synthesized by?

Answer 30

leydig cells in testes of the male, thecal cells in the ovary of the female, adrenal gland of both sexes

Question 31

What are androgens required for?

Answer 31

normal maturation of male, sperm production, increased synthesis of muscle proteins and hemoglobin, dec bone resorption

Question 32

Schematic of testosterone secretion

Answer 32

secreted by Leydig cells controlled by GnRH from hypothalamus, stimulates anterior pituitary to secrete FSH/LH, LH stimulates steroidogenesis in Leydig cells, FSH causes spermatogenesis

Question 33

Therapeutic uses of androgens?

Answer 33

males with inadequate androgen secretion, tx male senile osteoporosis and chronic wasting associated with HIV or CA, adjunct therapy in severe burns, ALS, speed recovery from surgery or chronic debilitating diseases

Question 34

Clinical uses of androgens?

Answer 34

endometriosis- inhibits release of LH/FSH, and antiestrogenic activity, unapproved for increase muscle mass, strength, and endurance

Question 35

ADR of danazol

Answer 35

wt gain, acne, decreased breast size, deepening voice, increased libido, increased hair growth

Question 36

PO testosterone

Answer 36

inactivated by 1st pass, but alkylation of 17a position works- oxandrolone (oxandrin)

Question 37

Testosterone available?

Answer 37

patches, gels, buccal tabs- androderm, androgel, testim, striant, fortesa

Question 38

ADRs of testosterone in children?

Answer 38

abnormal sexual maturation and growth disturbances

Question 39

Other ADRs of androgens

Answer 39

increased LDL, dec HDL, fluid retention, premature coronary heary disease

Question 40

Antiandrogen options

Answer 40

finasteride (proscar), and dutasteride (avodart)

Question 41

When are antiandrogens used

Answer 41

for tx BPH, also male pattern baldness

Question 42

dosage of antiandrogens

Answer 42

Finasteride- 5 mg PO, Dutasteride (.5mg PO)