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Pharm > Estrogens > Flashcards

Estrogens Flashcards

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
Q

Progesterone ______GnRH frequency.

A

Decreases GnRH frequency

Increases the amplitude of LH

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26
Q

In the CNS, what does progesterone do?

A

Increases depressant and hypnotic actions

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27
Q

What effect does progesterone have on the reproductive tract?

A

Increases the endometrium!

Decreases the action of E2

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28
Q

Half life of progesterone?

A

5 minutes

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29
Q

What are the types of hormonal contraceptives?

A

Progestin-only pill (aka the mini pill)

Progestin-Estrogen Pill

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30
Q

Northindrone

A

Progestin-only pill

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31
Q

Norethindrone or norgestrel are…

A

Less effective than combo pill.
Must be taken at same time, every day.
Used during pregnancy as estrogen reduces breast milk production.

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32
Q

What are the Long Term Reversible Method options for Progestin-Only BC?

A

Implants: Etonogestrel
Injection: MPA (wt gain and bone loss)
IUS: Levonorgestrel (Minera) 5 years

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33
Q

Etonogestrel (Implanon)

A

3 year implant

LT Reversible Method

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34
Q

Medrooxyprogesterone Acetate (MPA)

A

3 months
Injection
Causes wt gain, bone loss

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35
Q

Levonorgestrel (Minera)

A

5 yers

IUD,

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36
Q

At very LOW doses, what does the progestin pill do?

A

Inhibits ovulation in half of cycles

Thickens the cervical mucus (reduces sperm viability and penetration)

37
Q

At medium doses, what does the progestin pill do?

A

Inhibits ovulation in 97% of the cycles

Thickens the cervical mucus

38
Q

At high doses, what does the Progestin-Only pill do?

A

Completely inhibits ovulation

Thickens the cervical mucus

39
Q

Anovulatory cycles causes by progestin-only pill causes…

A

Interference with implantation of the blastocyst

40
Q

Ethinyl Estradiol (EE) = combo pill

A

Mestranol

Mestranol is Metabolized into EE

41
Q

Side effects of Combo BC:

A

Irregular menstrual bleeding
Amenorrhea
Headaches
Bloating

42
Q

Low Dose Combo Pill

A

Contain as little as 20 mcg of EE nd 100 mcg of progestin

43
Q

Continuous Pills of CBC

A

Seasonique (30 EE and 150 levonorgestrel - progestin) cuts cycle to one every 3 mo

44
Q

EE and Mestranol

A

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
Q

The 17alpha ethinyl group on mestranol inhibits…

A

Hydroxylation and glucuronization in metabolism

46
Q

The 3 methyl Group in mestranol inhibits..

A

Sulfation

47
Q

High levels of progestin = Levonorgestrel aka PLAN B

A

70-80% effective

Side effects:
Nausea
Abdominal pain
Fatigue, headache
Vomiting, menstrual changes
Deterioration in glucose tolerance, increases in plasma insulin
48
Q

Combo pill used as emergency contraceptive

A

Side effects worse than plan B

PREVEN, YUZPE

49
Q

Copper T IUD

A

Highly effective and for ongoing contraceptive

50
Q

Ulipristal Acetate (Ella)

A

Alternative to levonorgestrel

Take one dose within 5 days

selective PR modulator (SPRM)

51
Q

Mifipristone

A

Effective within 5 days
An anti-progestin
Disrupts follicular maturation, mid-cycle LH surge, alters the endometrium

52
Q

Hormone replacement therapy:

A

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
Q

Estrogen Alone HRT: Estrones

A

Estropipate

Conjugated Equine Estrogens (CEE)

54
Q

Estradiol (E2) Estrogen-alone HRT

A

Naturally present in premenopausal women

55
Q

Estriol (E3) Estrogen-Alone HRT

A

A weak natural estrogen elevated during pregnancy

56
Q

Estriol (E3) HRT

A

Does not increase risk of breast or endometrial cancers, asa it is not converted into estrone

57
Q

Estrogen and Progestin HRT

A

Prempo = CEE plus MPA

Indicated for women with a uterus and postmenopausal symptoms

58
Q

Why is progestin added to HRT COMBO?

A

Progestin is added to prevent endometrial hyperplasia from unopposed estrogen

59
Q

What are risks associated with Estrogen-Progestin HRT?

A

Venous thromboembolism
Coronary event
Pulmonary embolism

Should not be initiated or continued in postmenopausal women from prevention of CV disease

60
Q

SERM : Selective Estrogen Receptor Modulator

A

Acts as agonist and antagonist

61
Q

Tamoxifen

A

SERM
Nonsteroidal
Antagonist on BREAST
Agonist on UTERINE AND BONE

Treatment of ER+ breast cancer

62
Q

Hepatic metabolism of Tamoxifen (SERM), produces…

A

Produces highly active 4-hydroxytamoxifen

63
Q

Tamoxifen effects:

A

Decreases total cholesterol, LDL, lipoproteins
Does not increase HDL and TG

Side effects:
HOT FLASHES
ENDOMETRIAL CARCIMONA
DVT
PULM EMBOLISM
64
Q

Toremifene

A

Structurally similar to tamoxifen, similar properties/indications/toxicities

65
Q

Raloxifene

A

Nonsteroidal
Partial agonist on bone
Antagonist on uterus and breast

66
Q

What is raloxifene used for?

A

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
Q

Clomiphene

A

Older partial agonist

Used as ovulation-inducing agent

68
Q

Bazedoxifere

A

Approved as HRT and for osteoporosis

Used in combo with conjugated estrogens

69
Q

Fulvestrant

A

Analog of estradiol (estrogen antagonist)
- no known estrogenic activity

Indicated for ER pos breast cancer, if resistant to tamoxifen

70
Q

Side effects of fulvestrant

A

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
Q

Mifipristone

A

A PR and GR antagonist
Luteolytic properites

USED FOR MEDICAL ABORTIONS 7 weeks into pregnancy, effective emergency contraceptive

72
Q

Misoprostol

A

Prostaglandin E1

- added to induce uterine contractions

73
Q

Mechanism of Mifepristone

A

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
Q

Side effects of Mifepristone

A

Prolonged bleeding

75
Q

Aromatase Inhibitors (AI) TYPE 1

A

Irreversible, steroidal

Exemestane - similar to androstenedione

76
Q

Exemestane

A

Type I - aromatase inhibitor

77
Q

Exemestane is used for

A

Postmenopausal women with ER pos early breast cancer
More effective than tamoxifen

Irreversible binds to aromatase (converts testosterone -> estradiol)

78
Q

Formestane

A

Similar to exemestane (Type I AI)

  • weak androgen
  • mild AI
  • poor bioavailability
79
Q

Type II Aromatase Inhibitor

A

Reversible, non-steroidal

80
Q

Anastrozole

A

For ER+ breast cancer as first line treatment following tamoxifen

Tamoxifen resistant cancer rarely responds to anastrozole

Causes hot flashes

81
Q

Letrozole

A

Type II AI
Reversible, Nonsteriodal

ER+ breast cancer
Blocks estrogen production, increase FSH, stimulates follicle growth

82
Q

SERMs

A

Tamoxifen
Raloxifene
Bazedoxifene
Clomiphene

83
Q

Anti-estrogen

A

Fulvestrant

84
Q

Aromatase Inhibitor

A

Anastrozole
Letrozole
Exemestane

85
Q

Formestane

A

Aromatase Inhibitor

86
Q

Anti-Progestin

A

Mifepristone (misoprostol)

87
Q

Progestin

A

Norethindrone
Levonorgestrel
Medroxyprogesterone Acetate (MPA)

88
Q

SPRM

A

Ulipristal

89
Q

Estrogens

A

Ethinyl Estraadiol (EE)
Mestranol
Conjugated Equine Estrogens (CEE)

Pharm (6 decks)

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