[PHARM] MHT, SERMs and TSECs [Segars] Flashcards
What are the hallmark symptoms of menopause?
Hot flashes
Night sweats
Vaginal dryness
Sleep disturbances
Mood/cognitive issues
Urinary incontinence
Thinking look a good DO, what are some other systems are are likey affected during menopause?
Bone effects (osteopenia, osteoporosis, fractures)
Cardiovascular effects (ACS/MI/CVD)
What is the primary therapy for menopausal symptoms?
Estrogen
What is a significant consideration to make when a woman has menopausal symptoms but ALSO has an intact uterus?
In addition to estrogen, must also be on a PROGESTIN
What are the (4) available estrogenic forms of menopausal hormone therapy?
Estradiol
Conjugated Estrogens [CE]
Esterified Estrogens [EE]
Estropipate
What are the (3) available progestinic drugs?
Medroxyprogesterone [MPA]
Methyltestosterone
Progesterone
What is the MOA of estrogen?
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
WILL BE A TEST QUESTION
Women with an intact uterus that has menopausal symptoms that is taking estrogen must also be on a???
Why?
PROGESTIN
Due to increased risk of endometrial hyperplasia/carcinoma from unopposed tissue proliferation w/ prolonged duration
What were some of the major HARMS that were identified in women on combined estrogen and progestin use in postmenopausal women?
Increased incidence of:
- Coronary heart disease
- Dementia
- Stroke
- Venous thromboembolism
What were some of the major BENEFITS that were identified in women on combined estrogen and progestin use in postmenopausal women?
- Better controlled diabetes
- Lower incidence in all fractures
- Lower incidence of colorectal cancer
What were some of the major HARMS that were identified in women on ONLY estrogen use in postmenopausal women?
Increased incidence of…
- Dementia
- Stroke
- Thromboembolism
What were some of the major BENEFITS that were identified in women on ONLY estrogen use in postmenopausal women?
Decreased incidence of:
- Breast cancer
- All fractures
- Diabetes better controlled
MHT very effectively minimizes/treats ____________ and ______________
MHT very effectively minimizes/treats vasomotor symptoms and vaginal changes
MHT should NOT be used to…
MHT should NOT be used to prevent CVD or dementia
In terms of MHT dosage and duration, what are the key facts you should remember?
Use the lowest dose possible
Treat for the shortest duration possible
What does:
SERM
TSEC
Stand for?
SERM= Selective estrogen receptor modulators
TSEC= Tissue selective estrogen complexes
What are the (2) SERM drugs?
Ospemifene
Clomiphene
What is the one TSEC?
Bazedoxifene
What is the ONE indication for Ospemifene?
Moderate-to-severe DYSPAREUNIA
(painful intercourse)
What is the MOA of ospemifene?
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
What are the side effects of Ospemifene?
Post menopausal like symptoms
- Worsening hot flashes/sweating
- Estrogenic-similar effects on coagulation
- Endometrial thickening and even hyperplasia
Contraindications for Ospemifene?
Thomboembolic diseases
Unusual vaginal bleeding
Estrogen-related neoplasias
What are the indications of Bazedoxifene?
- Moderate to severe vasomotor symptoms associated with menopause in women with a uterus
- Prevention of post-menopausal osteoporosis
What is the MOA of bazedoxifene?
Antagonastic activity in endometrium and in breast tissue
Estrogenic physiologic effects particularly in the bone
Destroys HER2 malignant cells
What are the SE of bazedoxifene?
ALL estrogen-related effects (due to CE component)
What is the ONE anti-estrogenic drug?
Clomiphene
What is the indication for clomiphene?
Infertility in anovulatory women
What is the MOA of clomiphene?
BLOCKS inhibitory actions of estrogen on the hypothalamus GnRH and pituitary gonadotropin release
SE of clomiphene?
Multiple births
Ovarian cysts
Hot flashes
Luteal-phase dysfunction
