Estrogen and Progestin Inhibitors Flashcards
What are different routes of admin of Birth control (“type”)
Oral pill Injectable Implantable Intrauterine Device Transdermal Vaginal Ring
Why can you never give Estrogen alone?
Endometrial effects?***
What hormones are given with different routes?
Oral pill- E+P or P Injectable- E+P or P Implantable- P Intrauterine Device- P or Copper Transdermal -E+P Vaginal Ring- E+P
What is the MOA of Hormonal Birrth Control
Supress LH and FSH surge
Alter Cervical mucous
Alter Endometrium
In general envt. less favorable for implantation
What is the most common dosing strategy in Oral birth ontrol pills?
21 active tablets
7 inert tablets
What can be done to decrease Side effects from Hormonal birth control?
Alter dosing strategy to more closely mirror their natural cycle.
What is the most common form of injectable BC?
Medroxyprogesterone (Depo-provera)
What is the strategy for Plan B Emergency Birth control?
Within 72 hrs post sexual intercourse (unfavorable envt for ovulation)
What hormone is used for Plan B Emergency Birth control?
Levonorgestrel
What defines “perfect use” of Emergency contraception?
Take drug at same time each day with the same meal, not missing any doses, etc.
What are the adverse effects of Hormonal Contraceptives?
Mild
Mod
Severe
Mild: Nausea, Breast Pain, Edema, BT bleeding(estrogen), Withdrawl bleed failure, serum protein changes
Mod: BT bleeding(progestin) Weight Gain Inc Skin pigmentation Acne Hirsuitism Vaginal infections Amenorrhea
Severe: Thromboembolus MI Cholestasis Depression Cancer Cerebrovascular Disease
When would you not prescribe hormonal BC?
Cancer(use progestin only pill) Thromboembolic Disorders Liver disease History of CVD Smokers older than 35yo
What are the Drug interactions with Contraceptives?
HIV agents, anticonvulsants, and St. Johns wort inc. hormone metabolism
Antibiotics lower contraceptive effectiveness.
What is the MOA of Clomiphene?
A partial agonist of estrogen. blocks estrogen negative feedback.
What are the AA of Clomiphene?
Multiple Births
HOT FLASHES
Ovary enlargement
Blurred vision
Wy does a partial agonist decrease action on Estrogen?
Net action is less bc it displaces a stronger agonist.
When is clomiphene given?
Follicular phase. Increase in LH and FSH
Remove the drug before the Luteal phase
What is the MOA of the SERMS?
They act differentlydepending on the tissue they are in
What are the actions of SERMS in different tissues? BONE ENDOMETRIUM PITUITARY BREAST
BONE: supress resorption
ENDOMETRIUM: proliferation
PITUITARY: hot flashes
BREAST: inhibit proliferation
What are the actions of Tamoxifen?
Antagonist: breast/ H-P-G axis
Partial agonist endometrium
What are the AA of Tamoxifen?
Endometrial Cancer, Hot flashes, N/V
What are the actions of Raloxifen?
Antagonist: breast/ H-P-G axis
Partial agonist endometrium (less)
Same as tamoxifen with less of an effect on endometrium.
Hot flashes are worse though
What is the MOA of Danazol?
Inhibit gonadal function
What is the use of Danazol?
Endometriosis, Breast fibrocystic disease
What are the AA of Danazol?
Weight Gain, Edema, oily skin, acne,hirsuitism, HOT FLASHES
What are teh types of Anti Progesterones?
Abortifacents
Emergency contraceptives
What is an example of an abortifacent?
Mifeprestone (used first as anti-rogesterone)
Used in combo with misoPROSTol-uterine contractions
What is the MOA ofUlipristal?
Partial Agonist of Progesterone.
What is the MOA of Anti progesterones?
Inhibit progesterone Receptors
Uterine Contractions
Lining of uterus is Shed
Opens cervix
