Estrogens and androgens Flashcards Preview

Pharmacology > Estrogens and androgens > Flashcards

Flashcards in Estrogens and androgens Deck (42):
1

Estradiol

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

2

estrone

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

3

Estriol

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

4

ADRs of estrogen

nausea and breast tenderness

5

How should estrogen therapy be used for intact uterus?

progesterone in combo with estrogen

6

How should estrogen therapy be used for hysterectomy?

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

7

what are the SERMS

tamoxifen, raloxifene (Evista), Clomiphene (Clomid)

8

MOA of SERMS

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

9

Clinical use of tamoxifen

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

10

ADRs of tamoxifen

nausea, hot flashes, endometrial hyperplasia, and malignancy

11

Raloxifene (evista) use

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

12

Adrs of raloxifene

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

13

Clomiphene use

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

14

ADRs of clomiphene

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

15

progesterone produced in response to

LH in females and males

16

where is progesterone produced?

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

17

What does progesterone do

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

18

What is the major clinical use of progesterone

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

19

Progesterone ADRs

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

20

What is medroxyprogesterone adr

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

21

Contraceptive MOA

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

22

Progestin only contaceptives

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

23

How often is injectable progestin given

every 3 months

24

What can injectable progestin cause

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

25

Advantages of progestin implants

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

26

Complications with contraceptives

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

27

Advantages of contraceptives

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

28

ADRs of contraceptives

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

29

androgens

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

30

what is testosterone synthesized by?

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

31

What are androgens required for?

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

32

Schematic of testosterone secretion

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

33

Therapeutic uses of androgens?

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

34

Clinical uses of androgens?

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

35

ADR of danazol

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

36

PO testosterone

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

37

Testosterone available?

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

38

ADRs of testosterone in children?

abnormal sexual maturation and growth disturbances

39

Other ADRs of androgens

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

40

Antiandrogen options

finasteride (proscar), and dutasteride (avodart)

41

When are antiandrogens used

for tx BPH, also male pattern baldness

42

dosage of antiandrogens

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