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Estrogens Flashcards

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1
Q

E1

A

Estrone
18 Carbon Steroid

Medium Potency

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2
Q

E2

A

Estradiol

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3
Q

E3

A

Estriol

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4
Q

Premenopausal women have…

A

E2 (estradiol) released by the granulosa cells in the ovaries

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5
Q

In pregnant, the estrogen produced is…

A

Estriol (E3) by the placenta’s syncytiotrophoblasts - fetal liver

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6
Q

In post-menopausal women, what produces estrogen?

A

Adipose stroma cells

- E1 (estrone)

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7
Q

In men, what produces estrogens?

A

The testes
E1 (estrone)
E2 (estradiol)

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8
Q

ER alpha receptor

A

Expressed in endometrium

70% of breast cancer pts have overexpression

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9
Q

ER beta

A

Expressed in the:
Kidney
Brain

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10
Q

E2 (estradiol) binds what receptors?

A

Both receptors (alpha and beta)

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11
Q

E1 prefers to bind to which receptor?

A

ER alpha

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12
Q

E3 prefers to bind to what receptor

A

ER beta

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13
Q

Estrogen does ___ to bones.

A

Increases bone formation!

Increases HT, decreases muscle mass

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14
Q

Estrogen does ____ to HDL and ____ to VDL.

A

Increases HDL, VLDL, TG
Decreases LDL, total cholesterol

Increases metabolism of fat!

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15
Q

Estrogen ___ coagulation factors.

A

Increases coagulation factors.

Increases platelet adhesiveness.

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16
Q

Estrogen ___ to cortisol binding globulin (CBG), thyroxine binding globulin (TBG), and sex hormone binding globulin (SHBG).

A

Increases CBG, TBG, SHBG

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17
Q

What does estrogen do to GI functioning?

A

Decreases GI functioning
Increases cholesterol in the bile

Increases risk of gallstone formation

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18
Q

Progesterone (P4) is a …

A

Precursor of other steroids

P5 (Pregnenolone) is converted to P4

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19
Q

Progesterone is involved in…

A

Menstrual cycle, pregnancy and embryogenesis

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20
Q

Where does progesterone come from in non-pregnant vs. pregnant individuals?

A

Non-preg:
- corpus luteum, granulosa lutein cells, stimulated by LH

Pregnant:
- corpus luteum but stimulated by hCG

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21
Q

During the 2nd and 3rd month of pregnancy, what does the placenta secrete?

A

Estriol (E3) and progesterone

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22
Q

Two types of progesterone receptors include:

A

PR-B = stimulates epithelial cell proliferation

PR-A = opposes estrogen-induced proliferation

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23
Q

What induces PR expression in the endometrium?

A

Estrogen level rising!

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24
Q

What are the metabolic effects of progesterone?

A

Increases insulin levels

Increases LDL

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25
Progesterone ______GnRH frequency.
Decreases GnRH frequency Increases the amplitude of LH
26
In the CNS, what does progesterone do?
Increases depressant and hypnotic actions
27
What effect does progesterone have on the reproductive tract?
Increases the endometrium! Decreases the action of E2
28
Half life of progesterone?
5 minutes
29
What are the types of hormonal contraceptives?
Progestin-only pill (aka the mini pill) Progestin-Estrogen Pill
30
Northindrone
Progestin-only pill
31
Norethindrone or norgestrel are...
Less effective than combo pill. Must be taken at same time, every day. Used during pregnancy as estrogen reduces breast milk production.
32
What are the Long Term Reversible Method options for Progestin-Only BC?
Implants: Etonogestrel Injection: MPA (wt gain and bone loss) IUS: Levonorgestrel (Minera) 5 years
33
Etonogestrel (Implanon)
3 year implant | LT Reversible Method
34
Medrooxyprogesterone Acetate (MPA)
3 months Injection Causes wt gain, bone loss
35
Levonorgestrel (Minera)
5 yers | IUD,
36
At very LOW doses, what does the progestin pill do?
Inhibits ovulation in half of cycles Thickens the cervical mucus (reduces sperm viability and penetration)
37
At medium doses, what does the progestin pill do?
Inhibits ovulation in 97% of the cycles | Thickens the cervical mucus
38
At high doses, what does the Progestin-Only pill do?
Completely inhibits ovulation Thickens the cervical mucus
39
Anovulatory cycles causes by progestin-only pill causes...
Interference with implantation of the blastocyst
40
Ethinyl Estradiol (EE) = combo pill
Mestranol Mestranol is Metabolized into EE
41
Side effects of Combo BC:
Irregular menstrual bleeding Amenorrhea Headaches Bloating
42
Low Dose Combo Pill
Contain as little as 20 mcg of EE nd 100 mcg of progestin
43
Continuous Pills of CBC
Seasonique (30 EE and 150 levonorgestrel - progestin) cuts cycle to one every 3 mo
44
EE and Mestranol
Mestranol is converted to 17-alpha-EE in the liver This conversion increases the oral effectiveness of these estrogens. The modifications to EE increase the ORAL BIOAVAILABILITY.
45
The 17alpha ethinyl group on mestranol inhibits...
Hydroxylation and glucuronization in metabolism
46
The 3 methyl Group in mestranol inhibits..
Sulfation
47
High levels of progestin = Levonorgestrel aka PLAN B
70-80% effective ``` Side effects: Nausea Abdominal pain Fatigue, headache Vomiting, menstrual changes Deterioration in glucose tolerance, increases in plasma insulin ```
48
Combo pill used as emergency contraceptive
Side effects worse than plan B PREVEN, YUZPE
49
Copper T IUD
Highly effective and for ongoing contraceptive
50
Ulipristal Acetate (Ella)
Alternative to levonorgestrel Take one dose within 5 days selective PR modulator (SPRM)
51
Mifipristone
Effective within 5 days An anti-progestin Disrupts follicular maturation, mid-cycle LH surge, alters the endometrium
52
Hormone replacement therapy:
To make up for decline in estrogen-progestin after menopause Relieving symptoms postmenopausally - vasomotor problems, hot flashes, night sweats - vaginal atrophy - osteoporosis Women who want to take it..do it for lowest dose and shortest period!
53
Estrogen Alone HRT: Estrones
Estropipate | Conjugated Equine Estrogens (CEE)
54
Estradiol (E2) Estrogen-alone HRT
Naturally present in premenopausal women
55
Estriol (E3) Estrogen-Alone HRT
A weak natural estrogen elevated during pregnancy
56
Estriol (E3) HRT
Does not increase risk of breast or endometrial cancers, asa it is not converted into estrone
57
Estrogen and Progestin HRT
Prempo = CEE plus MPA Indicated for women with a uterus and postmenopausal symptoms
58
Why is progestin added to HRT COMBO?
Progestin is added to prevent endometrial hyperplasia from unopposed estrogen
59
What are risks associated with Estrogen-Progestin HRT?
Venous thromboembolism Coronary event Pulmonary embolism Should not be initiated or continued in postmenopausal women from prevention of CV disease
60
SERM : Selective Estrogen Receptor Modulator
Acts as agonist and antagonist
61
Tamoxifen
SERM Nonsteroidal Antagonist on BREAST Agonist on UTERINE AND BONE Treatment of ER+ breast cancer
62
Hepatic metabolism of Tamoxifen (SERM), produces...
Produces highly active 4-hydroxytamoxifen
63
Tamoxifen effects:
Decreases total cholesterol, LDL, lipoproteins Does not increase HDL and TG ``` Side effects: HOT FLASHES ENDOMETRIAL CARCIMONA DVT PULM EMBOLISM ```
64
Toremifene
Structurally similar to tamoxifen, similar properties/indications/toxicities
65
Raloxifene
Nonsteroidal Partial agonist on bone Antagonist on uterus and breast
66
What is raloxifene used for?
Prevention and treatment of osteoporosis in postmenopausal women and breast cancer Does not increase LDL, like tamoxifen Does not simulate endometrium, therefore less uterine cancer risk Effects are diminished by: Estrogens Cholesterol lowering drug (decreases absorption)
67
Clomiphene
Older partial agonist | Used as ovulation-inducing agent
68
Bazedoxifere
Approved as HRT and for osteoporosis | Used in combo with conjugated estrogens
69
Fulvestrant
Analog of estradiol (estrogen antagonist) - no known estrogenic activity Indicated for ER pos breast cancer, if resistant to tamoxifen
70
Side effects of fulvestrant
More potent than tamoxifen, degrades the ER alpha receptor May cross placenta and cause abnormalities Side effects include GI symptoms, headache, hot flashes, pharyngitis
71
Mifipristone
A PR and GR antagonist Luteolytic properites USED FOR MEDICAL ABORTIONS 7 weeks into pregnancy, effective emergency contraceptive
72
Misoprostol
Prostaglandin E1 | - added to induce uterine contractions
73
Mechanism of Mifepristone
Blocks uterine PR - decrease hCG - decrease progesterone secretion from corpus luteum - further decidual breakdown - increase prostaglandins from uterus, leads to expulsion of detached blastocyst
74
Side effects of Mifepristone
Prolonged bleeding
75
Aromatase Inhibitors (AI) TYPE 1
Irreversible, steroidal Exemestane - similar to androstenedione
76
Exemestane
Type I - aromatase inhibitor
77
Exemestane is used for
Postmenopausal women with ER pos early breast cancer More effective than tamoxifen Irreversible binds to aromatase (converts testosterone -> estradiol)
78
Formestane
Similar to exemestane (Type I AI) - weak androgen - mild AI - poor bioavailability
79
Type II Aromatase Inhibitor
Reversible, non-steroidal
80
Anastrozole
For ER+ breast cancer as first line treatment following tamoxifen Tamoxifen resistant cancer rarely responds to anastrozole Causes hot flashes
81
Letrozole
Type II AI Reversible, Nonsteriodal ER+ breast cancer Blocks estrogen production, increase FSH, stimulates follicle growth
82
SERMs
Tamoxifen Raloxifene Bazedoxifene Clomiphene
83
Anti-estrogen
Fulvestrant
84
Aromatase Inhibitor
Anastrozole Letrozole Exemestane
85
Formestane
Aromatase Inhibitor
86
Anti-Progestin
Mifepristone (misoprostol)
87
Progestin
Norethindrone Levonorgestrel Medroxyprogesterone Acetate (MPA)
88
SPRM
Ulipristal
89
Estrogens
Ethinyl Estraadiol (EE) Mestranol Conjugated Equine Estrogens (CEE)

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