pharmacology Flashcards

1
Q

function of estrogen in endometrium

A

growth of endometrial glands, thickening of endometrium, emergence of spiral arteries from the basal layer.

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2
Q

function of estrogen in menstrual cycle

A

acts as a positive feedback signal thus leading to a massive surge of fsh and lh that causes ovulation

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3
Q

fuct of estrogen in female repro system

A

development of female secondary sex characteristics during puberty, like the growth of breasts and widening of the hips, as well as distribution of fat on the buttocks, hips, and thighs.

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4
Q

5 systemic functions of estrogen

A
  1. inhibits osteoclastic activity
  2. lowers ldl levels
    3.vasolidation by keeping blood vessels flexible
  3. increases blood cogulation and clotting factos
  4. increases synthesis of progesterone receptors
  5. increases cognition and sense of well-being
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5
Q

most potent form of estrogen

A

17-b estradiol

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6
Q

form of estrogen in postmenopause

A

estrone

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7
Q

estrogen form during preg

A

estriol

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8
Q

synthetic estrogen include

A

ethinyl estradiol; diethylstilbestrol, or DES; and mestranol.

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9
Q

sysnthetic estroegen can be given via what route

A

orally, via transdermal patches, vaginal creams, or intramuscular injection.

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10
Q

5 indications of synthetic estrogen

A
  1. primary hypogonadism
    2.hrt
    3.premature ovarian failure or surgical removal of oavries
  2. primary amenorrhea
    5.hormonal contraceptives along with progesterone
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11
Q

adverse effects of synthetic estrogens

A
  1. vaginal bleeding, breast tenderness.
  2. increased risk of breast and endometrial cancer
    3.nausea
  3. thromboembolic events
  4. peripheral edema
  5. hypertension
    8.uterine bleeding
    9.hyperpigmentation
  6. migraines
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12
Q

adverse effect of diethylstillbestrol

A

women given these during preg, thier daughter can develop infertility, ectopic preg, vaginal adenocarcinoma, and vaginal adenosis

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13
Q

5 estrogen synthetics contraindications

A
  1. estrogen dependent neoplasm( endometrium and breast cancer)
    2.Undiagnosed genital bleeding
    3.Liver disease
  2. History of thrombo-embolic disorder
  3. Heavy smokers
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14
Q

name 5 serts

A

tamoxifen,
raloxifene, and
clomiphene.
TOREMIFINE
OSPEMIFENE

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15
Q

tamoxifen and raloxifene indications

A

breast cancer, osteoporosis

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16
Q

5 tamoxifen se

A

endometrial hyperplasia, increased risk of endometrial cancer, endometrial polyps,
thromboembolic events, hot flashes

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17
Q

2 se of raloxifene

A

hot flashes, increased thromboembolic events

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18
Q

raloxifene preferred over tamoxifene?

A

raloxifene do not stimulate estrogen receptors of the emdometrium

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19
Q

clomiphene moa

A

estrogen antagonist in the hypothalamus, preventing the normal negative feedback, and thus increases FSH and LH output from the pituitary and ultimately stimulates ovulation.

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20
Q

clomiphene indications

A

induce ovulation and treat infertility

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21
Q

clomiphene se

A

hot flashes,
ovarian enlargement,
Risk of ovarian cancer(prolong use)
multiple pregnancies due to multiple ovulation, and
visual disturbances.
Headaches, constipation, allergic reactions

Deprssion,fatigue and weight gain
Breast soreness,
urinary frequency.

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22
Q

TOREMIFINE use?

A

treatment of metastatic breast cancer

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23
Q

OSPEMIFENE use?

A

Treatment of dyspareunia (painful sexual intercourse) related to menopause.

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24
Q

purely antagonists in all tissues that acts on estrogen receptor antagonist

A

fulvestrant

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25
Q

when is fullvestrant used

A

Used in tamoxifene resistant patients of breast cancer

26
Q

se of fullvestrant

A

hot flashes, headache, injection site rxn

27
Q

arotomase inhibitors more effective in post or premenopausal women

A

post menopausal women

28
Q

arotomaze inh used in

A

advanced breast cancer that is er+

29
Q

arotamase inh are of -types

A

type 1 steriodal- irreveribly bind to arotamase
type 2 non steriodal - reversibly bind to arotamase
both are competetive inhibitors

30
Q

type 2 arotomase ihb agents names

A

anastrozole and letrozole,

31
Q

type 1 arotamase ihb agent name

A

exemestane

32
Q

route for arotomase inh

A

peroral

33
Q

s.e of arotomase inh

A

cvs disease,
osteopenia,
osteoporosis in hips and lumbar spine which can lead to fractures

symptoms similar to those that precede menopause, like hot flashes, night sweats, vaginal dryness, and loss of libido.

Joint symptoms like arthralgia, arthrosis, arthritis, and disk herniation can also occur.

34
Q

letrozole se

A

nausea, and hair thinning, but it has less cardiovascular side effect

35
Q

exemestane se

A

nausea, diarrhea, fatigue, as well as visual disturbance

36
Q

danazol moa

A

Inhibits several enzymes involved in gonadal steroid synthesis.
Inhibitor of gonadal function

Suppress mid cycle surge of LH AND FSH🡪Suppress ovarian function

37
Q

contraindication of danazol

A

Pregnancy (Urogenital abnormalities in offspring)
Breast feeding
Hepatic dysfunction (Risk of hepatocellular damage)

38
Q

progestrin is a -carbon steriod

A

21

39
Q

progestrins produced in

A
  1. gonads
  2. adrenal cortex
    3.ovarian corpus leutum in the 1st ten weeks of pregnancy
  3. placenta during pregnancy
40
Q

normal effects of progestrone on repro system

A
  1. prevent endometrial shedding
  2. decreased uterine motility
    3.inhibition of immulogical rejection of the fetus
  3. secretory changes in the endometrium
    5.thickens cervical mucus thus making it hostile to further sperm
    6.induces preg likes changes in the vagina
  4. proliferation of breast preparing them for lactation working tog with estrogen
41
Q

systemic effects of progestrone

A

1.fat deposition
2.glycogen storage
bone stregth
skin elastic
3. competes with aldosterone so dec na reabsorption
4. increase body temp
5. depression

42
Q

2 kinds of progestins

A

progestrone-derivatives and testosterone derivatives

43
Q

eg of progesterone derivatives

A

medroxyprogesterone, hydroxyprogesterone,
megestrol acetate, dihydrogesterone.

44
Q

eg of older testerone derivatives

A

danazol norgestrel, levonorgestrel, and ethynodiol

45
Q

eg of newer testerone derivatives

A

desogestrel, norgestimate, and etonogestrel, gestodene

46
Q

indication for newer testerone derivatives

A

women who experience side effects such as
acne, depression or breakthrough bleeding with the older drugs.

47
Q

bad effect of newer testosterone derivatives

A

increases the risk of thromboembolic events

48
Q

indications for progestrins

A
  1. contraceptives with or w/o estrogens
  2. hrt along with estrogen to prevent endometrial hyperplasia/growth and to relieve post menopausal symtoms
  3. secondary amenorrhea
  4. dysfunctional and abnormal uterine bleeding
  5. endometriosis
  6. ovarian supression in cases of dysmennorrhea
  7. endometroid carcinoma
49
Q

what test is it used for

A

progestin or medroxyprogesterone is given to patients for 10 days to see if its induces mentrual period in week following the withdrawal of the therapy. ammenorhea occurs in patients with endometrium scarring and if estrogen levels are low.

50
Q

route for progestins

A

orally,im, intrauterine device, transdermal implant

51
Q

toxicity of progestins at typical doses

A

fluid retention
increase blood pressure, fatigue,
mood changes
depression,
breast discomfort, changes in libido
menstrual irregularities

52
Q

progestins se at high doses

A

reversible decrease in bone density
delay the resumption of ovulation after termination of the therapy.

53
Q

older testerone derivative

A

virilization

54
Q

2 antiprogestins

A

mifepristone, uripristal

55
Q

mifepristone use

A

surgical terminal of preg effective within 50 days of preg
sensitizes the uterus to prostaglandin use

56
Q

antiprogestins moa

A

competeitve inh at progesterone receptors

57
Q

ulipristal use

A

emergency birth control within 5 days of intercourse, uterine fibroids

58
Q

mifepristone given duirng follicular phase vs luteal phase

A

fp-slowing of follicular development and delay/failure of
ovulation.
lp-prevents secretory changes hence causing uterine contractions

59
Q

mifepristol se

A

nausea, vomitting, diarhea, unable to induce complete abortion,

60
Q

uripristal moa

A

on the ovary
(by suppressing or delaying ovulation) and on the
endometrium (by decreasing endometrial thickness).

61
Q

se of uripristal

A

headache, nausea and abdominal pain, hot flushes.

62
Q
A