Pharm Flashcards
(85 cards)
Names & Indications of estrogen
-estrols (Hexestrol & Diethylstibestrol)
Cancer therapy
HRT
Contraception
What are we trying to alter in estrogen therapy?
The estrogen response-the creation of proteins
Which pharmolocolgic agent is described as “flat and hydrophobic”?
Estrogen
Which estrogen receptor gene has a more specialized role and why?
Estrogen Receptor Gene-B: dominates in the lung and has limited tissue expression.
List the SERM corepressors
Raloxifene
Tamoxifen
Fulvestrant
What are the indications for SERMs?
They inhibit the estrogenic effects of breast cancer while maintaining bone mass.
Used in cancer therapy, HRT, and contraception
What are antihormones that inhibit activity by reducing P160 coactivator binding to estrogen receptor surfaces?
SERMs
Antagonists in breast, uterus, & CNS
Agonist in bone (bone sparing)
Unknown in liver
Raloxifeine - SERM
Antagonist in breast & CNS
Partial antagonist in uterus & liver
Agonist in bone
Tamoxifen - SERM
Largest “extra” structure of all anti-estrogens.
So large it degrades the protein
Fulvestrant - SERM
Compounds that can have estrogenic activity by binding the ER, but made in plants
Phytoestrogens
Give examples of phytoestrogens
Isoflavinoid: Soy beans, can relieve menopausal symptoms
Lignnas: High fiber foods
Coumestans: various beans. Alfalfa and clover sprouts are highest.
What are used as HRT?
Conjugated Estrogens (Premarin/Equine/Ethyinyl Estradiol)
Estradiols (Estrace and Estraderm)
Duavee
This addresses long-term issues of aging that result from loss of estrogen after menopause
HRT
Relief of menopausal symptoms is clear, but longer term benefits harder to prove
HRT
Oral Conjugated Estrogens
Premarin
Tablet/cream form of estrogen
Estrace
Dermal patch form of estrogen
Estraderm
HRT that combines SERM + E2 for those worried about endometrial cancer
Duavee
What’s the rule in dosing regarding HRT?
Use low does that works for a few years (CV benefit is greater in younger women closer to 5-7years post-menopause)
List the aromatase inhibitors
Anastorozole
Letrozole
Exemestane
In what population should aromatase inhibitors be used?
Only use in post menopausal women
MOA of aromatase inhibitors
Aromatase tissue is active in the breast, so we prevent androgens from turning into estrogens which cause growth of breast cancer
Describe the differences between the aromatase inhibitors
Anastorozole and Letrozole are competitive inhibitors (substrates) that bind to androgen.
Exemestane is a suicide substrate