Hormones Pharm part I, Linger Flashcards

(49 cards)

1
Q

What are the estrogens we have for drugs

A

conjugated E- premarin
estradiol valerate
ethinyl estradiol
mestranol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what are the progestin drgus

A

desogestrel(inactive etonogestrel(active)
drospinenone
medroxyprogresterone, norethindrone, norgestimate
norgestrel (L-norgestrel, levonorgestrel)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

what are the E and P inhibitors

A

Mifepristone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

what are the selective E R modulators

A

raloxifene
tamoxifen
toremifene

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what are the selective E R downregulators

A

clomiphene

fulvestrant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what are the aromatase inhibitors

A

anastrazole
exemestane
letrozole

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

how do synthetic E work

A

bind to the SHBG and lower affinity to albumin so there is more unfound E around

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

why are vaginal and transdermal modes for effective for giving E

A

because avoid the first pass metabolism of the liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

MOA E

A

binds ER and activates gene transcription

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

how do E Receptros work

A

homodimerize and bind promoter regions or bind to other transcription factors which bind to the promoter regions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

endometrial effects of E

A

bleeding and shedding

continuous exposure will lead to hyperplasia of the endometrium leading to abnormal bleeding patterns

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

metabolic effects of E

A

decrease rate of bone resoprtion because promotes apoptosis of osteoclasts
stimulate adipose tissude production of letpin
stimulates increase production of the cortisol globulin, thyroxine binding globulin, sex hormone binding protein
increase HDL and TG, reduce LDL

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

vascular effects of E

A

enhance coagulability of blood
increases factors II CII IX and X, decrease antithrombin III
icnrease plasminogen

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

When do we use E for Tx

A

primary hypogonadism
postmenopausal hormone replacement
suppress ovulation in patients with intractable dysmenorrhea or suppress ovarian function in cases of hirsutism and excessive ovary androgen secretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

E and P replacement decreases risk of what

A

osteoporotic fractures of hip vertebrae, and wrist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

adverse effects estrogens

A

uterine bleeding, breast and endometrial cancer

nausea, breast tenderness, hyperpigmentation, increased migraine frequency, cholestasis, gallbladder disease and HTN

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

how is endometrial hyperplasia from administration of E prevented

A

give progestin too

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

does adding P to E Tx prevent breast cancer

A

not, may actually increase risk of breast cancer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Contraindications to E

A

patients with E dependent neoplasms (endometrial carcinoma and breast cancer)
patients with unDx genital bleeding, liver disease, history of thromboembolic disorder and heavy smokers

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

what sideeffects are decreased in transdermal preparations of e

A

does not increase renin levels, corticosteroid binding substrate and thyroxine binding substrate

21
Q

Where is P naturally made

A

in ovary (corpus luteum), testis and adrenal Cx

22
Q

how are pharmacokinetics of P different than E

A

rapid regardless of PO or IM

23
Q

MOA progesterone

A

activates gene transcription via nuclear R

24
Q

isoforms of Progesterone R

25
physiologic effects of progesterone
- dec frequency of GnRH pulses - onset menstruation with its abrupt decline - maintains pregnancy and mammary gland development - stimulates lipoprotein lipase and favors fat deposition - increases basal insulin levels and insulin response to glucose - promotes glycogen storage and ketogenesis - can compete for mineralocorticoid R (dec in Na reabsorption)
26
clincal uses of progestins
HRT and hormone contraception | long term ovarian suppression
27
how are progestins used for Dx testing
can be used to test E secretion | causes bleeding after 5-7 days progesterone if endometrium has been stimulated by E
28
dosage and drug used for long term ovarian suppression
150mg medroxyprogesterone acetate IM every 90 days
29
adverse effects of progestins
breakthrough bleeding increase BP reduce HDL in women
30
2 types of oral contraception preparations
combinations E and P or just P without E
31
what is monophaseic? bi? tri?
mono is constant dose of both E and P in pills biphasic changes once triphasic changes twice
32
what hormones are in the transdermal preparation of contraception
ethinyl estradiol and norelgestromin
33
adverse effects with ransdermal patch
breast discomfort, dysmenorrhea, nausea, vomiting and skin irritation
34
What drugs are in the NuvaRing
ethinyl estradiol and etonogestrel
35
adverse effects for injectable preparations for contraceptin
unpredictable spotting or bleeding return of fertility can take 18 mo after last injection increased risk atherosclerosis
36
What drug is in IUD and how long is it effective
levonorgestrel | effective for 5 years
37
with IUD at increased risk for
ovarian cyst
38
what drug is in the implantable contraceptions
eronogestrel good for 3 years bleeding abnormalities are common
39
what drugs are in the day after pills
E alone P alone E and P P R modulators
40
adverse effects of day after pills
nausea, vomiting, HA, dizziness, breast tenderness, abdominal and leg cramps
41
what is in plan B
levonorgestrel
42
how does plan B work
not sure | cannot reverse pregnancy that has already occurred (post implantation)
43
What is Ella and how does it work
Ulipristal acetate, partial agonist at P R, inhibits ovulation when taken up to 5 days after intercourse, may block implantation
44
adverse effects Ella
HA and abdominal pain
45
main MOA E and P contraceptive pills
selective inhibition of pituitary function (negative feedback) change cervical mucus, uterine endometrium and motility of uterine tubes
46
effects of E and P on ovary
depress ovarian function
47
effects oe E and P on uterus
prolonged use may cause hypertrophy of cervix and polyp formationl glandular atropy and decreased bleeding are common depending on preparation
48
E and P contraception effects on breast
stimulate enlargement and suppress lactation
49
other effects of E and P contraception
mood changes increased urinary exretion of free cortisol, increased renin, increased aldosterone increased coagulability of blood increase certain lipids