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PHARM II, QUIZ 1 > HRT and Breast Cancer therapies > Flashcards

HRT and Breast Cancer therapies Flashcards

1
Q

Which hormones increase during menopause

A

FHS, LH

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2
Q

Oral Estrogens

A

CEE (conjugated equine estrogen + estrone sulfate)

Esterified estrogens (estrogen mixture)

Estradiol

  • Micronized for better absorption
  • Liver metabolism to estrone, less potent
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3
Q

Topical Estrogens

A

Estradial patch, emulsion, gel, spray

No first pass effect, so estrogen levels similar to pre menopausal

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4
Q

Vaginal Estrogens

A

For vaginal atrophy

CEE cream (Premarin)
Estradiol cream (Estrace)
Estradiol ring (Estring) 
Estradiol tablet (Vagifem)
*sustained release, less systemic effect*
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5
Q

Estrogen ADRs and indications

A

Indication: Relief of vasomotor symptoms

ADRs
Nausea, HA, breast tenderness, bleeding

Serious ADRs
CHD, CVA, VTE
Breast cancer
Gallbladder disease

ADRs are less likely w transdermal estrogens

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6
Q

Estrogen WARNINGS

A

Increased risk of stroke and VTE (venous thromboembolism)

Endometrial Cancer in unopposed estrogen for patients with a uterus

Breast cancer, increased risk in combined HRT over long term

Slight increased risk of Dementia in estrogen only therapy

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7
Q

Estrogen only vs Estro + Progest HRT, Risks

A

Estrogen Only

  • Higher risk of Stroke
  • About same risk of DVT

Estro + Progest

  • Higher risk of Breast Cancer
  • Higher risk of Dementia
  • Lower risk of Stroke
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8
Q

3 categories of phytoestrogens

A

Lignans
- flax

Isoflavones
- soy, garbanzo, red clover, lentils, beans

Coumestens
- Red clover, sunflower seeds, sprouts

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9
Q

Indications for Soy

A

mild reduction in vasomotor symptoms - hot flashes

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10
Q

Drug for premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD)

A

Flibanserin

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11
Q

Contraindications for Flibanserin

A

EtOH, P450 3A4 inhibitors, hepatic impairment

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12
Q

Flibanserin ADRs

A

Sedation, hypotension, syncope, CNS depression

REMS program: hypotension, syncope with EtOH use

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13
Q

At what age do the benefits of HRT outweigh the risks

A

women < 60 yrs

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14
Q

Estrogen therapy effectively treats

A

vasomotor symptoms (Sleep, Irritability, Concentration, Reduced QOL)

Vulvar and vaginal atrophy (Vaginal dryness, Dyspareunia, Atrophic vaginitis

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15
Q

General HRT guideline

A

“lowest dose, shortest period necessary”

unopposed estrogen should not be used in women with intact uterus

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16
Q

HRT and Osteoporosis

A

HRT may be used for the prevention and treatment of osteoporosis within the context of the overall benefit-versus-risk analysis of each patient.

17
Q

3 classes of breast cancer treatment

A
  1. Selective Estrogen Receptor Modulators (SERMs)
  2. Steroidal Estrogen Receptor Antagonist
  3. Aromatase Inhibitors
18
Q

SERMs

A

Tamoxifen

Toremifene

Raloxifene

19
Q

Steroidal Estrogen Receptor Antagonists

A

Fulvestrant

20
Q

Aromatase Inhibitors

A

Anastrozole

Exemestane

Letrozole

21
Q

SERMs effects on breast vs other tissues

A

Breast: ESTROGEN ANTAGONIST

Endometrium, bone, liver, coag system: ESTROGEN AGONIST

22
Q

Indications for use of Tamoxifen

A

ER+ Breast Cancers:

  1. Adjuvant therapy for breast cancer
  2. Metastatic breast cancer
  3. Reduce risk of invasive cancer from Ductal carcinoma in situ
  4. Breast cancer prevention in high risk women
23
Q

Tamoxifen ADRs

A

Menopausal symptoms

- vasomotor, vaginal atrophy, N/V, menstrual irregularities

24
Q

Tamoxifen WARNINGS

A

Increased risk DVT, PE

Increased incidence Endometrial cancer

Liver abnormalities

Ocular cataracts (high dose only)

Hypercalcemia

PREGNANCY CATEGORY D

25
Q

Tamoxifen (SERM) drug interactions

A

P450 / 3A4, 2D6 Metabolism

Warfarin
Rifampin
Anastrazole (chemo therapy)
Paroxetine, Fluoxetine, Bupropion (SSRI)

26
Q

WHAT ARE SERMS GOOD FOR

A

Reduces breast cancer risk

Lowers LDL cholesterol

Strengthens bones

27
Q

WHAT ARE SERMS BAD FOR

A

Increases uterine cancer risk

Increases clot risk

28
Q

Raloxifene (SERM) indication

A

Breast cancer prevention in high risk patients

  • slightly less effective prevention than Tamoxifen but FEWER cases uterine cancer and clots

same ADR / warning profile

29
Q

SERMs for vasomotor symptoms

A

Bazedoxifene

Ospemifene

Same SERM class ADR/Warnings

30
Q

Aromatase Inhibitor Indications

Anastrozole, Exemestane, Letrozole

A

Better efficacy than SERMs for advanced breast cancer

first-line for adjuvant breast cancer treatment in post menopausal women

an aromatase inhibitor is the best hormonal therapy to start. When treating early-stage, hormone-receptor-positive breast cancer, aromatase inhibitors have more benefits and fewer serious side effects than tamoxifen.

31
Q

Fulvestrant (SERD) Indications

A

Pure anti-estrogen - inhibits and degrades estrogen receptors

Indicated for postmenopausal women with hormone receptor–positive metastatic breast cancer that has progressed on tamoxifen

No P450 interactions

Well tolerated (Nausea, hot flashes, headaches)

PHARM II, QUIZ 1 (2 decks)

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