sex hormones Flashcards

1
Q

compare forms of estrogen

A

estradiol (E2) = primary
estrone (E1) = less active
ethinyl estradiol = MORE potent

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2
Q

what estrogen HRT is indicated for patients with intact uterus, no uterus, and at moderate CVD risk?

A

intact = estrogen + progestin
absent = estrogen
moderate CVD risk = avoid PO

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3
Q

what conditions is estrogen HRT contraindicated?

A

breast cancer
liver disease
stroke, CVD, high CVD risk
DVT

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4
Q

what drugs are progestins?

DPM2N3

A
Drospirenone
Progesterone
Megestrol
Medroxyprogesterone
Norethindrone
Norgestrel
Norgestimate
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5
Q

what is the MOA of progestins?

A

act on receptor of others (estrogen, androgen, mineralocorticoids)
suppresses ovulation by (-) feedback

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6
Q

How does progestin provide contraception?

A

suppress ovulation by dec. GnRH
Matures endometrial lining
Dec. transit of sperm (thickens mucus)

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7
Q

compare deficiency and excess of estrogen on endometrium

A

def: early cycle breakthrough bleeding; hypomenorrhea/amenorrhea
excess: other effects…

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8
Q

compare deficiency and excess of progestin on endometrium

A

def: late cycle bleed; hypermenorrhea
excess: hypOmenorrhea/amenorrhea

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9
Q

What women are CI for estrogen + progestin?

A

CVD, DVT/PE, Afib, stroke

smokers >35 YO

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10
Q

compare dosage forms of contraceptives

A

monophase = traditional
multiphasic = mimic natural hormone changes, may have less side effects
extended interval = placebo pills q3mos, less frequent menses, may improve endometriosis, PMDD
continuous = no placebo pills; PREVENTS menstruation; may improve endometriosis, PMDD

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11
Q

which progestins are most androgenic?

A

2nd generation
norgestrel
leveonorgestrel

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12
Q

which progestins are less androgenic?

A

norgestimate

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13
Q

what drug is anti-androgenic?

A

drospirenone

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14
Q

name androgens

A

testosterone
oxandrolone
methyltestosterone
danazol

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15
Q

describe dermatological effects of androgens

A

male pattern baldness, inc. sweat and sebum (acne!), hair growth (hirsutism in females)

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16
Q

how is testosterone administered/

A

parenterally

17
Q

what are uses of modified androgens?
methyltestosterone
oxandrolone
danazol

A
methyltestosterone = hypogonadism
oxandrolone = weight gain
danazol = endometriosis
18
Q

what classes of agents are “down regulators”?

A

GnRH antagonists = degarelix, cetrorelix, ganirelix

GnRH agonists = leuprolide, goserelin, nafarelin

19
Q

what is the MOA and use of GnRH antagonists?

A

dec. LH and FSH to dec. sex hormones

use: hormone dependent cancers

20
Q

what agents are “synthesis inhibitors”?

A
17-hydroxylase inhibitors:
abiraterone, spironolactone
5-alpha reductase inhibitors:
finasteride, dutasteride
aromatase inhibitors:
anastrozole, letrozole, exemestrane
21
Q

differentiate between abiraterone and spironolactone uses

A
abiraterone = POTENT- used for castration, resistant metastatic prostate cancer
spironolactone = weak - used for hirsutism in females or transgender
22
Q

what are 5 alpha reductase inhibitors used for? What AEs are associated with them?

A

treat BPH and male pattern baldness

AEs: impotence, dec. libido

23
Q

what are aromatase inhibitors used for? what AEs are associated with them?

A

estrogen-dependent cancers (breast)

AEs: similar to menopause

24
Q

What agents are “receptor modulators”

A
SERMs = tamoxifen, raloxifene, clomiphene
SPRMs = Ullipristal
25
Q

what are the four classes of anti-hormonal agents?

A

down regulators
synthesis inhibitors
receptor modulators
receptor antagonists

26
Q

What are the MOA and use of ullipristal?

A

agonist of HPA to suppress ovulation + alter endometrium

use: emergency contraception

27
Q

what is clomiphene used for?

A

infertility - it’s an antagonist of negative feedback in order to stimulate ovulation

28
Q

compare agonist/antagonist activities of tamoxifen

A

ag: bone, cholesterol, uterus
ant: breast

29
Q

compare agonist/antagonist activities of raloxifene

A

ag: bone, cholesterol
ant: breast, uterus

30
Q

what agents are receptor antagonists?

A
estrogen = fulvestrant
progestin = mifepristone
androgen = bicalutamide, flutamide, enzalutamide, nilutamide
31
Q

what are uses for estrogen R antagonists?

A

breast cancer

32
Q

what is the use of mifepristone?

A

(with misopristol) for medical abortion

33
Q

what are uses of androgen receptor antagonists?

A

prostate cancer