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Pharmacology > Estrogens and androgens > Flashcards

Estrogens and androgens Flashcards

1
Q

Estradiol

A

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

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2
Q

estrone

A

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

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3
Q

Estriol

A

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

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4
Q

ADRs of estrogen

A

nausea and breast tenderness

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5
Q

How should estrogen therapy be used for intact uterus?

A

progesterone in combo with estrogen

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6
Q

How should estrogen therapy be used for hysterectomy?

A

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

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7
Q

what are the SERMS

A

tamoxifen, raloxifene (Evista), Clomiphene (Clomid)

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8
Q

MOA of SERMS

A

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

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9
Q

Clinical use of tamoxifen

A

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

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10
Q

ADRs of tamoxifen

A

nausea, hot flashes, endometrial hyperplasia, and malignancy

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11
Q

Raloxifene (evista) use

A

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

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12
Q

Adrs of raloxifene

A

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

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13
Q

Clomiphene use

A

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

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14
Q

ADRs of clomiphene

A

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

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15
Q

progesterone produced in response to

A

LH in females and males

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16
Q

where is progesterone produced?

A

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

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17
Q

What does progesterone do

A

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

18
Q

What is the major clinical use of progesterone

A

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

19
Q

Progesterone ADRs

A

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

20
Q

What is medroxyprogesterone adr

A

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

21
Q

Contraceptive MOA

A

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
Q

Progestin only contaceptives

A

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
Q

How often is injectable progestin given

A

every 3 months

24
Q

What can injectable progestin cause

A

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

25
Q

Advantages of progestin implants

A

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

26
Q

Complications with contraceptives

A

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

27
Q

Advantages of contraceptives

A

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

28
Q

ADRs of contraceptives

A

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

29
Q

androgens

A

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

30
Q

what is testosterone synthesized by?

A

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

31
Q

What are androgens required for?

A

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

32
Q

Schematic of testosterone secretion

A

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
Q

Therapeutic uses of androgens?

A

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
Q

Clinical uses of androgens?

A

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

35
Q

ADR of danazol

A

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

36
Q

PO testosterone

A

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

37
Q

Testosterone available?

A

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

38
Q

ADRs of testosterone in children?

A

abnormal sexual maturation and growth disturbances

39
Q

Other ADRs of androgens

A

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

40
Q

Antiandrogen options

A

finasteride (proscar), and dutasteride (avodart)

41
Q

When are antiandrogens used

A

for tx BPH, also male pattern baldness

42
Q

dosage of antiandrogens

A

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

Pharmacology (61 decks)

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