Week 11: Estrogens and Anti-Estrogens Flashcards

1
Q

Effects of estrogen

A
  • increases bone density
  • normal skin and blood vessel structure
  • decrease lipid levels
  • reduces bowel motility
  • enhances coagulability of blood
  • edema (effects RAAS)
  • stability of the thermoregulatory center
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2
Q

How does estrogen work to prevent pregnancy?

A
  • suppresses LH which manipulates the hormones and prevents ovulation
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3
Q

Explain monophasic, biphasic, and triphasic estrogen treatment

A

Monophasic - same hormone dose every day - given to help even out hormone levels

Biphasic - hormone dose changes every 14 days

Triphasic - hormone dose changes every 7 days (mimics a normal cycle)

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4
Q

Estrogens cautions/CIs

A
  • over age 35 and a smoker
  • uncontrolled HTN
  • venous thrombosis
  • any GYN cancer
  • hx of CVA
  • cirrhosis
  • migraine w/ aura
  • ischemic heart disease or risk factors
  • pregnancy
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5
Q

Considerations when prescribing estrogen

A
  • start at the lowest estrogen dose while maintaining cycle control
  • Ethinyl estradiol 20-35mg (20mg - low dose; > 30mg - high dose)
  • if intact uterus, NEED estrogen AND progesterone (if estrogen only, increase risk of endometrial cancer)
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6
Q

Contraceptive start methods

A

First Day Start
- pills started on the first day of the menstrual cycle
- no backup method needed
Sunday Start
- first pill taken on the Sunday following the start of menses
- backup method for first 7 days
Quick or ‘Same Day’ start
- first pill taken on the day of the office visit
- backup method for first 7 days

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7
Q

Advantages of oral contraception (combined estrogen & progestorone)

A
  • highly effective
  • rapidly reversible
  • regulates menstrual bleeding
  • decreased menstrual blood loss and dysmenorrhea
  • reduction in risk of ovarian and endometrial CA
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8
Q

Topical patch (Ortho Evra)

A
  • applied weekly for 3 weeks and 1 week off
  • no 1st pass effect
  • increased failure rate for women weighing more than 198 pounds
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9
Q

Vaginal Ring (NuvaRing)

A
  • placed in vagina and left in place for 3 weeks, and then left off for 1 week
  • better cycle control and decreased breakthrough bleeding compared to OC
  • lower systemic exposure to estrogen
  • if out for more than 3 hours-use backup method for 7 days
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10
Q

Drug interactions with COC (combined oral contraceptives)

A
  • metabolism is increased by any drug that increased liver microsomal enzyme activity: anticonvulsants
  • decreased COC effects
  • Rifampin is the only antibiotic proven to reduce serum EE and progestin levels
  • Griseofulvin (antifungal) - associated with contraceptive failure (limited data)
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11
Q

Indications for estrogen treatment in menopause

A
  • vasomotor symptoms - systemic treatment (oral, transdermal, topical gels)
  • genitourinary symptoms (vaginal dryness, burning, vulvar itching/burning, recurrent UTIs - localized/vaginal treatment (intravaginal creams, tablets, rings)
  • *consider type of estrogen and route of administration as well as need for progestin**
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12
Q

Types of Estrogen products

A
  • Conjugated equine estrogens (CEEs) - estrone - derived from pregnant mare urine
  • Synthetic conjugated estrogens - phytoestrogens - plant based (soy, yams)
  • Micronized 17-beta estradiol - bioidentical to premenopausal estrogen
  • Esterified estrogen - conjugated estrogen
  • Ethinyl estradiol (EE) - more potent than others - used in very low doses (5mcg - unless symptoms are severe) - titrate up if symptoms are not relieved by low dose
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13
Q

Vaginal estrogen treatment in Menopause

A

Local treatment

  • used in low doses for vaginal atrophy
  • no recommended to use higher dose in those who need GU symptom treatment only
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14
Q

Estrogen ADR (in menopause)

A
  • breast soreness
  • H/A
  • Elevated blood pressure
  • exacerbation of diabetes - hyperglycemia
  • cholestasis
  • thromboembolic event - blood clotting
  • endometrial hyperplasia can develop as a result of estrogen being prescribed in women without an intact uterus
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15
Q

Contraindications to menopausal hormone therapy (MHT)

A
  • hx of breast cancer
  • CAD
  • Venous thromboembolic event (DVT/PE)
  • Stroke/TIA
  • Active liver dz
  • unexplained vaginal bleeding
  • high risk endometrial cancer
    • if pt has hx of migraine w/ aura - transdermal formulation is preferred
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16
Q
  • Selective Estrogen Receptor Modulator (SERM)
A
  • Anti-estrogen
  • Estrogen agonists and antagonist in various tissues
  • Agonist in bone: prevents bone loss, improves bone mineral density, decreases vertebral fx risk.
  • Antagonist in breast: reduces risk of breast CA
  • increase risk of thromboembolism and hot flashes
  • no effect on the endometrium or heart disease risk
17
Q

Ospemifene (Osphena)

MOA / indication

A

class: selective estrogen receptor modulator (SERM)
MOA: increases thickness and moisture of vaginal mucosa
Indication: dyspareunia, vaginal dryness
-potential increased risk of endometrial CA if intact uterus

18
Q

Raloxifene (Evista) MOA / indication

A

SERM

  • estrogen antagonist in breast: reduce risk of breast ca
  • 2nd line tx for osteoporosis bone loss