Class of 2017 Pharm Review Flashcards
What is the drug used for estrogen replacement during menopause?
17-a-ethinylestradiol
What are the side effects of 17-a-ethinylestradiol?
Increased risk of MI, Stroke, endometrial carcinoma
What is norethindrone?
Progesterone equivalent
What are the side effects of norethindrone?
Increased risk of MI, stroke, breast cancer
What are the indications for estrogen or progesterone therapy?
hypogonadism, contraception, menospause
What is the DoC for menopausal syndrome treatment?
Ospemifene
What class of drug is Ospemifene and its MoA?
- SERM: partial agonist for bone and endometrium, partial antagonist for breast
- Promotes vaginal epithelial growth
What is the main concern of SERM use?
Endometrial hyperplasia and carcinoma
What SERM is used for infertility and polycystic ovarian syndrome?
Clomiphene Citrate
What is the MoA of clomiphene citrate?
Reduce estrogen hypothalamus negative feedback –> promote FSH and LH –> ovulation
What is the main side effect associated with Clomiphene Citrate?
Induced menopause due to estrogen block
What is the primary use of Letrozole?
Infertility
What is the MoA of letrozole?
Aromatase inhibitor: Blocks estrogen production –> FSH / LH stimulation –> ovulation
Drug for fat, infertile woman?
Metformin
What drugs (2) are used in a low to medium risk premenopausal, estrogen - receptor positive patient?
Tomoxifen or raloxifene
What drugs are used in a low to medium risk postmenopausal, estrogen - receptor positive breast cancer patient?
Tamoxifen, raloxifene, or letrozole (aromatase inhibitor)
What treatment (Rx) is used in a estrogen negative breast cancer patient?
Chemo
What is the limitation of SERMs?
5 year limit, will convert to breast agonist after this
What drugs will SERMs interact with?
SSRIs (CYP2D6 conversion)
What are three aromatase inhibitors?
Letrozole, anastrozole, exemestane
What is the MoA of aromatase inhibitors?
prevent estrogen production from androgens
What are the first line and second line drugs (classification) used in estrogen receptor positive breast cancer in post menopausal women?
SERM and Aromatase inhibitors, respectively
What are the benefits of aromatase inhibitors, when compared to SERMs?
No risk of endometrial cancer
No risk of thromboembolic
Effective after 5 years
What is the MoA and indication for Fulvestrant?
Estrogen receptor antagonist
Breast cancer resistant to tamoxifen
What are the GnRH agonists?
Leuprolide, Goserelin, Abarelix
What must be given with GnRH agonists, for how long, and why?
Estrogen antagonist, for two weeks, to prevent the effects of the initial FHS and LH flare
What biotech drugs can be given for HER2/erbB-2 positive breast cancers?
Trastuzumab, Pertuzumab, and Lapatinib (if Trast unresponsive)
What is the most effective contraceptive?
IUD
What is the MoA of IUDs?
Cu coating causes sterile inflammation and PMNs kill sperm
What is the major adverse effect of estrogen / progesterone OCPs?
Thromboembolism
What are the two (one unique) major risks associated with intravaginal contraceptives?
Cervical displasia (unique), thromboembolism
What is the emergency contraceptive?
Levonorgestrel
What is the MoA of levonorgestrel and its limitation?
Progesterone analog prevents ovulation
Must be taken within 3 days of coitus
What are the categories of medications, as they relate to pregnancy, and the categorical meanings?
A: No Risk, human studies performed
B: Animal studies show no risk, but no human trials. Animal studies show risk, but human ones don’t.
C: Animal studies show increased risk, but no human trials. Or no studies conducted.
D: Proven risk, but may be outweighed by benefits
X: Proven risk, benefit
