[PHARM] MHT, SERMs and TSECs [Segars] Flashcards

1
Q

What are the hallmark symptoms of menopause?

A

Hot flashes

Night sweats

Vaginal dryness

Sleep disturbances

Mood/cognitive issues

Urinary incontinence

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2
Q

Thinking look a good DO, what are some other systems are are likey affected during menopause?

A

Bone effects (osteopenia, osteoporosis, fractures)

Cardiovascular effects (ACS/MI/CVD)

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3
Q

What is the primary therapy for menopausal symptoms?

A

Estrogen

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4
Q

What is a significant consideration to make when a woman has menopausal symptoms but ALSO has an intact uterus?

A

In addition to estrogen, must also be on a PROGESTIN

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5
Q

What are the (4) available estrogenic forms of menopausal hormone therapy?

A

Estradiol

Conjugated Estrogens [CE]

Esterified Estrogens [EE]

Estropipate

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6
Q

What are the (3) available progestinic drugs?

A

Medroxyprogesterone [MPA]

Methyltestosterone

Progesterone

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7
Q

What is the MOA of estrogen?

A

Estrogen binds to estrogen receptors (ER’s; alpha/beta) in various tissues

They are transferred into the nucleus, which increases protein production and results in physiological responses

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8
Q

WILL BE A TEST QUESTION

Women with an intact uterus that has menopausal symptoms that is taking estrogen must also be on a???

Why?

A

PROGESTIN

Due to increased risk of endometrial hyperplasia/carcinoma from unopposed tissue proliferation w/ prolonged duration

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9
Q

What were some of the major HARMS that were identified in women on combined estrogen and progestin use in postmenopausal women?

A

Increased incidence of:

  • Coronary heart disease
  • Dementia
  • Stroke
  • Venous thromboembolism
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10
Q

What were some of the major BENEFITS that were identified in women on combined estrogen and progestin use in postmenopausal women?

A
  • Better controlled diabetes
  • Lower incidence in all fractures
  • Lower incidence of colorectal cancer
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11
Q

What were some of the major HARMS that were identified in women on ONLY estrogen use in postmenopausal women?

A

Increased incidence of…

  • Dementia
  • Stroke
  • Thromboembolism
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12
Q

What were some of the major BENEFITS that were identified in women on ONLY estrogen use in postmenopausal women?

A

Decreased incidence of:

  • Breast cancer
  • All fractures
  • Diabetes better controlled
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13
Q

MHT very effectively minimizes/treats ____________ and ______________

A

MHT very effectively minimizes/treats vasomotor symptoms and vaginal changes

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14
Q

MHT should NOT be used to…

A

MHT should NOT be used to prevent CVD or dementia

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15
Q

In terms of MHT dosage and duration, what are the key facts you should remember?

A

Use the lowest dose possible

Treat for the shortest duration possible

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16
Q

What does:

SERM

TSEC

Stand for?

A

SERM= Selective estrogen receptor modulators

TSEC= Tissue selective estrogen complexes

17
Q

What are the (2) SERM drugs?

A

Ospemifene

Clomiphene

18
Q

What is the one TSEC?

A

Bazedoxifene

19
Q

What is the ONE indication for Ospemifene?

A

Moderate-to-severe DYSPAREUNIA

(painful intercourse)

20
Q

What is the MOA of ospemifene?

A

Functions as ESTROGEN AGONIST by binding to ER’s in vagina, but also anti-estrogenic on breast

  • Increases superficial cell growth
  • Increases vaginal secretions
  • Decreases vaginal pH
  • Reduces pain/discomfort during vaginal intercourse
21
Q

What are the side effects of Ospemifene?

A

Post menopausal like symptoms

  • Worsening hot flashes/sweating
  • Estrogenic-similar effects on coagulation
  • Endometrial thickening and even hyperplasia
22
Q

Contraindications for Ospemifene?

A

Thomboembolic diseases

Unusual vaginal bleeding

Estrogen-related neoplasias

23
Q

What are the indications of Bazedoxifene?

A
  • Moderate to severe vasomotor symptoms associated with menopause in women with a uterus
  • Prevention of post-menopausal osteoporosis
24
Q

What is the MOA of bazedoxifene?

A

Antagonastic activity in endometrium and in breast tissue

Estrogenic physiologic effects particularly in the bone

Destroys HER2 malignant cells

25
Q

What are the SE of bazedoxifene?

A

ALL estrogen-related effects (due to CE component)

26
Q

What is the ONE anti-estrogenic drug?

A

Clomiphene

27
Q

What is the indication for clomiphene?

A

Infertility in anovulatory women

28
Q

What is the MOA of clomiphene?

A

BLOCKS inhibitory actions of estrogen on the hypothalamus GnRH and pituitary gonadotropin release

29
Q

SE of clomiphene?

A

Multiple births

Ovarian cysts

Hot flashes

Luteal-phase dysfunction