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Pharm Sem 4 > Block 2 > Flashcards

Block 2 Flashcards

1
Q

what is the mechanism of action of estrogen

A

diffuse across membrane
bind to intracellular receptors
hormone receptor complex binds to a hormone response element

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2
Q

what is the effect of estrogen on the bone

A

decreases osteoclast activity

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3
Q

what is the effect of estrogen on the RAAS system

A

increases angiotensinogen

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4
Q

what is the effect of estrogen having high enterohepatic circulation

A

increases the synthesis of clotting factors and plasma angiotensinogen

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5
Q

does estrogen or progesterone have a favorable effect on the lipid profile

A

estrogen: increases HDL, decreases LDL

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6
Q

what are 7 uses of estrogen

A

primary hypogonadism in females
androgen dependent prostatic tumors
menopause hormonal therapy
hirsutism
PCOS
acne
menopause hormonal therapy

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7
Q

what drug can be used in women with a history of breast cancer when estrogens are contraindicated

A

Paroxetine (SSRI)

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8
Q

name 5 adverse effects of estrogen use

A

increased risk of endometrial/breast cancer
thromboembolism
migraine
postmenopausal bleeding
edema

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9
Q

estrogen use is contraindicated in situations such as (6)

A

liver disease
untreated hypertension
porphyria cutanea tarda
thromboembolism disorders
high risk for breast cancer
estrogen dependent neoplasms/endometrial hyperplasia

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10
Q

name 5 uses of progesterone

A

contraception
menopause hormone therapy
endometrial hyperplasia/cancer
increase appetite (megestrol acetate in cancer or AIDS)
prevent recurrent miscarriages

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11
Q

what is the effect of progesterone on bone

A

can cause osteoporosis

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12
Q

what is the effect of progesterone on the lipid profile

A

increases LDL, decreases HDL

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13
Q

adverse effects of progesterone use include (5)

A

changes in libido
hirsutism
acne
osteoporosis
change in libido

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14
Q

what are 2 examples of drugs which act as antiestrogens

A

Clomiphene
Fulvestrant

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15
Q

what is the mechanism of action of fulvestrant

A

increases intracellular degradation of ERalpa receptor which protecting ERbeta–>decreases estrogen effect

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16
Q

Fulvestrant, an antiestrogen, is used in what 2 conditions

A

breast cancer in women resistant to Tamoxifen and aromatase inhibitors
breast cancer with endometrial risk

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17
Q

what is the mechanism of action of Clomiphene

A

partial agonist at estrogen receptors causes interference of negative feedback on the hypothalamus and pituitary, leading to increased FSH/LH, allowing for an increase in ovulation and pregnancy

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18
Q

what is Clomiphene used for

A

infertility (ovulation induction)

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19
Q

what are 3 adverse effects of Clomiphene, an antiestrogen

A

multiple births
visual disturbances
increased risk of ovarian cancer/ovarian enlargement

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20
Q

what are 2 examples of selective estrogen receptor modulators

A

Tamoxifen
Raloxifene

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21
Q

what is the mechanism of action of selective estrogen receptor modulators

A

estrogenic in some issues, antiestrogenic in others

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22
Q

what is the mechanism of action of tamoxifen, a selective estrogen receptor modulator

A

competitive antagonist for estrogen receptors in breast tissue
agonist in bone and endometrium

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23
Q

how is tamoxifen metabolism

A

it’s a prodrug converted to active form in the liver by CYP2D6/3A4

24
Q

what is tamoxifen, a selective estrogen receptor modulator, used for

A

estrogen receptor positive breast cancer

25
Q

what are 5 adverse effects of tamoxifen

A

thromboembolism/pulmonary embolism
increased risk for endometrial cancer
hypercalcemia
cataracts
bone pain

26
Q

what is the mechanism of action of Raloxifene, a selective estrogen receptor modulator

A

agonist effect on bone
antagonist effect on endometrium and breast

27
Q

what are 2 uses of Raloxifene, a selective estrogen receptor modulator

A

prevention of osteoporosis in postmenopausal women
reduce risk of invasive breast cancer in postmenopausal women

28
Q

what is an adverse effect of Raloxifene, a selective estrogen receptor modulator

A

thromboembolism

29
Q

what is Toremifene used for

A

metastatic breast cancer

30
Q

-ozole is a suffix used for what drug class
what are 2 other drugs in this class

A

aromatase inhibitors
Exemestane, Testolactone

31
Q

what is the mechanism of action of aromatase inhibitors

A

block the conversion of androgens–>estrogen leads to increase in GnRH with increases FSH and LH

32
Q

name 3 uses of aromatase inhibitors

A

estrogen dependent postmenopausal breast cancer
metastatic breast cancer
ovulation induction

33
Q

name 2 adverse effects of aromatase inhibitors

A

osteoporosis with prolonged use
acne

34
Q

what drug class is used for prepubertal cryptorchism

A

gonadotropins (FSH/LH)

35
Q

what drug class can be used to aid with infertility in hypogonadal men

A

gonadotropins (FSH/LH)

36
Q

what are 3 adverse effects of gonadotropin use

A

multiple pregnancies
ovarian hyperstimulation syndrome
gynecomastia

37
Q

what is the mechanism of action of gonadotropin agonists

A

pulsatile release increases FSH/LH release
continuous release increases FSH/LH release for 7-10 days, then decreases

38
Q

what is an example of a gonadotropin analog

A

gonadorelin

39
Q

what type of action does gonadorelin have

A

short acting gonadotropin–>increased FSH and LH release

40
Q

what are the uses of gonadorelin, a short acting gonadotropin

A

diagnosis of hypogonadism
infertility

41
Q

what type of drug action does goserelin have

A

long acting continuous release–>decreased FSH/LH

42
Q

in what 5 situations is goserelin, a long acting gonadotropin analog, used

A

endometriosis
uterine leiomyoma
precocious puberty
breast/ovarian cancer
early pubertal transgender adolescents

43
Q

what are 3 adverse effects of gonadotropin analogues

A

symptoms of menopause
gynecomastia in men
osteoporosis with long term use

44
Q

GnRH receptor antagonists have the suffix ___

A

-relix

45
Q

what is the mechanism of action of combined oral contraceptives

A

negative feedback to reduce levels of FSH/LH –> decreased ovulation, atrophy of glands, slowing of tubal motility and ova transport, thickens cervical mucus

46
Q

in combined oral contraceptive pills, estrogen reduced __, progesterone reduced __

A

estrogen reduces FSH
progesterone reduces LH

47
Q

what are 5 uses of combined oral contraceptives

A

endometriosis
hirsutism
PCOS
reduce endometrial/ovarian/colorectal cancer
primary dysmenorrhea

48
Q

if severe adverse effects such as __ (4) occur with combined oral contraceptive use, use must be immediately withdrawn

A

thromboembolism
hepatic adenoma
depression
increased risk of breast cancer/cerebrovascular disorders

49
Q

combined oral contraceptive use is contraindicated if a patient has __ (9)

A

thromboembolic disease
coronary disease
cerebrovascular disease
smoking
migraines
undiagnosed vaginal bleeding
mild hypertension
gallbladder disease
convulsive disorders

50
Q

combined oral contraceptives should be avoided with use of what other drugs

A

enzyme inducers
antibiotics

51
Q

mini pills are classified as __ only pills

A

progesterone

52
Q

what is the mechanism of action of mini pills (progesterone only pills)

A

decrease frequency of GnRH release–>decreased midcycle LH surge
thickening of cervix mucus

53
Q

__ drugs are used when estrogen is contraindicated

A

mini (progesterone only)

54
Q

in what 5 cases are mini pills uses

A

chronic smokers
hepatic disease
hypertension
psychosis
history of thromboembolism

55
Q

what are 2 adverse effects of mini pill (progesterone only) use

A

doesn’t completely suppress ovulation–>irregular fertile periods
amenorrhea

56
Q
A

Pharm Sem 4 (2 decks)

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