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NURS 424 > Week 11 - Estrogen and Anti-Estrogens > Flashcards

Week 11 - Estrogen and Anti-Estrogens Flashcards

1
Q

Role of estrogen in the body

A
  • Primary effects are maturation and function of female reproductive system
  • Estrogen receptors in: breast, ovaries, uterus, bone, CNS, GI tract, cardiovascular tissue
  • Stabilizes endometrium to maintain regular withdrawal bleeding
  • Increases bone density
  • Results in normal skin and blood vessel structure
  • Affects lipids levels
  • Reduces bowel motility
  • Enhances coagulability of blood
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2
Q

Estrogen formulations

A

Pill, transdermal, vaginal ring

If there are no contraindications, combined oral contraception may be continued from menarche to menopause

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3
Q

Ethinyl estradiol: indications

A
  • Prevents the release of an egg (ovulation) during your menstrual cycle
  • Makes vaginal fluid thicker to prevent sperm from reaching an egg (fertilization)
  • Changes the lining of the uterus to prevent attachment of a fertilized egg
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4
Q

Ethinyl estradiol: pharmacokinetics

A
  • Metabolized by the liver
  • No significant difference in contraceptive efficacy between dosages
  • Start w/ lowest estrogen while maintaining cycle control
  • Dose may be increased if breakthrough bleeding occurs
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5
Q

Monophasic, biphasic, triphasic oral contraception therapy

A

Monophasic: each tablet contains a fixed amount of estrogen and progestin

  • Same dose of estrogen and progestin for full cycle

Biphasic: each tablet contains a fixed amont of estrogen while the amount of progestin increases in the second half of the cycle

Triphasic: amount of estrogen may be fixed or variable while the amount of progestin increases in three equal phases

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6
Q

Conditions that carry unacceptable health risks when considering estrogen oral contraceptive therapy

A
  • >35 years and smoking
  • Uncontrolled HTN
  • VTE
  • Current breast cancer
  • Cirrhosis
  • Migraine w/ aura
  • Ischemic heart disease or multiple risk factors
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7
Q

Advantages of oral contraception

A
  • Highly effective
  • Rapidly reversible
  • Regulates menstrual bleeding
  • Decreased menstrual blood loss and dysmenorrhea
  • Reduction in risk of ovarian and endometrial cancers
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8
Q

Drug interactions w/ combined oral contraception (COC)

A
  • Metabolism increased by any drug that increases liver enzyme activity
  • Anticonvulsants
  • Rifampin is the ONLY abx that reduces serum ethinyl estradiol and progestin levels
  • Griseofulvin (antifungal) associated w/ contraceptive failure
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9
Q

Estrogen in menopause: indications

A
  • Vasomotor symptoms
  • GU symptoms (vaginal dryness, vaginal burning)
  • Benefits outweight risk for healthy, symptomatic women who are within 10 years of menopause OR younger than 60 years old and do not have contraindications to treatment
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10
Q

True/False: Long-term use of estrogen during menopause is recommended for prevention of disease

A

False - NO longer recommended

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11
Q

Estrogen in menopause: formulations

A
  • Oral
  • Transdermal
  • Topical gels, emulsions, lotions
  • Intravaginal creams, tablets, rings

Consider type of estrogen and route of administration, as well as need for progestin

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12
Q

Estrogen in menopause: pharmacokinetics (oral)

A
  • Oral has greater effect on liver d/t first-pass effect
  • Oral increases liver production of clotting factors, HDL, triglycerides, and proteins such as sex hormone-binding globulin (SHBG) and thyroxine-binding globulin (TBG)
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13
Q

Estrogen in menopause: pharmacokinetics (transdermal)

A
  • Transdermal associated with lower risk of VTE and stroke
  • Less effect on serum lipids compared to comparable oral dose
  • Equally effective to oral for preserving bone density
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14
Q

Where are conjugated equine estrogens (CEEs) dervied from?

A

Pregnant mare’s urine (mostly comprised of estrone)

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15
Q

Where are synthetic conjugated estrogens derived from?

A

Plant sources (soy, yams)

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16
Q

What is structurally identical (bioidentical) to the main product of a premenopausal ovary?

A

Micronized 17-beta estradiol

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17
Q

True/False: Esterified estrogens have comparable serum estradiol/estrone levels to conjugated estrogen

A

True

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18
Q

True/False: Ethinyl estradiol is more potent than others for menopausal hormone therapy (MHT)

A

True - use in VERY low doses

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19
Q

Types of estrogen: steroidal

A

Endogenous

  • Estradiol
  • Estrone
  • Estriol
20
Q

Types of estrogen: non-steroidal

A

Exogenous

  • Phytoestrogens
  • Xenoestrogens
  • Mycoestrogens
21
Q

Ethinyl estradiol dosing

A

Start w/ low dose estrogen unless severe symptoms arise

Dose can be titrated up if symptoms are not completely relieved by low dose

22
Q

Estrogen in menopause: vaginal therapies

A
  • Commonly used in low doses for vaginal atrophy
  • Vasomotor symptoms treated w/ higher doses
  • NOT recommended to use higher vaginal estrogen doses in those who need treatment for GU symptoms only
23
Q

Estrogen in menopause: ADR

A
  • Breast soreness
  • HA
  • Elevated BP
  • Exacerbation of DM (hyperglycemia)
  • Cholestasis
  • Thromboembolic event
  • Endometrial hyperplasia
24
Q

Menopausal hormone therapy (MHT): contraindications

A
  • History of breast cancer
  • CAD
  • VTE
  • Stroke/TIA
  • Active liver disease
  • Unexplained vaginal bleeding
  • High risk endometrial cancer
25
Q

True/False: Transdermal estrogen is not as effective as oral estrogen for preserving bone density

A

False - transdermal is as effective as oral

26
Q

Raloxifene (Evista): classification

A

Selective estrogen receptor modulator (SERM)

27
Q

Bazedoxifene (Duavee): classification

A

Combination estrogen derivative with SERM

28
Q

SERM (raloxifene): MOA

A
  • Estrogen agonist in bone –> prevents bone loss, improves bone mineral density, decreases vertebral fracture risk
  • Estrogen antagonist in breast –> reduces risk of breast cancer

NO effect on heart disease or endometrium

29
Q

SERM (raloxifene): ADR

A

Increase in thromboemolism and hot flashes

30
Q

SERM (ospemifene): MOA

A
  • Increases thickness and moisture of vaginal mucosa
  • Estrogen agonist effect in endometrium
31
Q

SERM (ospemifene): indications

A
  • Dyspareunia in postmenopausal females
  • Vaginal dryness in postmenopausal females
32
Q

SERM (ospemifene): ADR

A
  • Increased risk of endometrial cancer if the uterus is intact
  • Increased risk of stroke and DVT
33
Q

Estrogen-only products: contraindications

A
  • Women with intact uterus
  • Pregnancy (unless specialist directed low hormone level)
  • Breast cancer
  • Estrogen-dependent neoplasia
  • Active DVT or pulmonary embolism
  • History of past year of stroke or MI
  • Liver dysfunction
  • Smokers
34
Q

Estrogen for contraception

A

Combination of estrogen and progestin

35
Q

Estrogen for relief of peri and postmenopausal symptoms

A
  • Start on lowest dose
  • Do not give unopposed estrogen to women with a uterus
36
Q

Estrogen for vaginal atrophy and dryness

A

Vaginal cream, tablets, or ring

37
Q

Estrogen and progesterone: effects

A
  • Positive effect on bone mass, increases serum triglycerides, improves ratio of high-density lipoprotein to low density lipoprotein
  • Stimulates coagulation and fibrinolytic pathways
38
Q

Mechanism of pregnancy prevention: estrogen

A
  • Improves efficacy by suppressing FSH release
  • Provides cycle control
39
Q

Dosing regimens OCP: “traditional”

A

21 days active drug + 7 days of inactive tablets w/ withdrawal bleed during inactive tablets

40
Q

Dosing regimens OCP: extended cycle

A

84 days of active drug then 7 days off

Withdrawal bleed once every 3 months

41
Q

OCP starting methods: first day start

A

Pills started on first day of menstrual cycle

No backup method needed

42
Q

OCP starting methods: Sunday start

A

First pill taken on the Sunday following the start of menses

Back up method for first 7 days

Menses only occur during the week

43
Q

OCP starting methods: quick or “same day” start

A

First pill taken on the day of the office visit

Back up method for first 7 days

44
Q

Estrogen topical patch: Ortho Evra patch

A
  • Patch applied weekly for 3 weeks, then 1 week off
  • Start on first day of menses
    • Can start on other days if backup method is used
  • Increased failure rate in women weighing more than 198 lbs
45
Q

Vaginal ring: NuvaRing

A
  • Ring placed in vagina, left in place for 3 weeks, left off for 1 week
  • Better cycle control and decreased breakthrough bleeding are achieved compared with OC
  • Systemic exposure to estrogen lower
46
Q

Progestin-only pills: patient education

A

If pill is taken a few hours late, a backup method is recommended for the following 48 hours

NURS 424 (35 decks)

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