Hellkatz: Female Repro Drugs Flashcards
How do you tx women with hypothalamic anovulatory function?
Give both FSH and LH w/ daily injection
For superovulation in normal ovulatory women (FSH/LH on d 2-3 of menstrual cycle)
How do you treat women with endogenous estrogen activity and normal hypothalamic-pituitary-ovarian function?
use clomiphene citrate an estrogen antagonist which induces FSH secretion
What is urine derived human gonadotropins?
Menotropins
Urofolitropoin
What is given w/ hCG in sequence for ovulation in anovulatory women and for production of multiple follicles?
menotropins
What is given w/ hCG in sequence for induction of ovulation of patients w/ PCOD (w/ FSH/LH and failed Clomiphene citrate)?
Urofolitropoin
Estrogen antagonist in the hypothalamus that acts on SERM and BLOCKS ER signaling in the hypothalamus and anterior pituitary and stimulates the release of GnRH and Gonadotropins?
Clomiphene citrate
What is used as a fertility drug to induce multiple ovulations?
Clomiphene citrate
*multiple fetuses are possible
Hot flashes and ovarian hyperstimulation syndrome are SE of what drug?
Clomiphene citrate
What has LH like induction of ovulation?
hCG
often used following follicle stimulation by clomiphene or gonadotropins
What are common SE of drugs that stimulate/mimic gonadotropins?
Hyperstimulation
Mutiple Fetuses
Ovarian hyperstimulation syndrome (w/shift of vascular fluids to abdominal and thoracic cavities- usually mild symptoms, occasionally severe)
Leupolide
Synthetic GnRH agonist
Non-pulsatile administration of this drug suppresses FSH/LH after an initial transient rise
Leupolide
What drug is often paired with FSH/LH or Clomiphene to stimulate follicle production?
Leuopolide
What drug reduces sxs of uterine fibroids and controls hormone dependent prostate and breast cancers?
Leupolide
Competitive antagonist of GnRH> suppresses Gonadotropin release
GnRH Antagonists
Ganirelix
Cetrorelix
What drug is used to prevent LH surge while promoting folliculogenesis, is used in breast/prostate cancer to inhibit steroid production and is used in benign uterine diseases?
Ganirelix
Cetrorelix
What are the metabolic effects of estrogen?
Na and water retention
Increase in HDL, decrease in LDL (yay)
What drugs usually are used in combination w/ progestins and interfere w/ the LH surge and ovulation?
Oral contraceptives
What is used to treat dysmenorrhea (painful periods)?
Estrogen
What is the hormonal contraceptive estrogen?
Estradiol 17B ethinyl estradiol
-readily absorbed in tissues, but is limited in effectiveness by first pass metabolism
What reduces the metabolism of estrogen and makes it orally active?
addition at C-17
What increases the syntehsis of SHBG?
estrogens (estradiol is bound to SHBG when circulating)
What drug is an estrogen antagonist in the breast and vasculature and an agonist in the uterus, bone, and lipoproteins?
Tamoxifen
What drug is used for the treatment and prevention of estrogen positive breast cancer?
Tamoxifen
Nausea, vomiting, skin rashes
Hot flashes
Thromboembolic events
Endometrial cancer
Are all SE of…
Tamoxifen
Clomiphene Citrate
What is an estrogen antagonist in some tissues but an agonist in oithers?
Clomiphene citrate
This drug is used for ovulatory dysfunction in pts who are NOT pregnant, have normal liver function, and may have amenorrhea and PCOD.
Clomiphene citrate
What drugs is an agonist of bone and lipoproteins and an antagonist in the breast and uterus?
Raloxifen
DVT and leg cramps are SE of…
Raloxifen
What drug is an antagonist in the breast and is often used for breast cancer treatment?
Toremifene
Also an agonist in the uterus but has NO effect on the bone
What are the pros and cons of toremifene?
SE: hot flashes
Benefit: lowers LDL, increases HDL
What are the four SERMs?
Tamoxifen
Raloxifen
Clomiphene citrate
Toremifine
What drug is a PURE estrogen antagonist that blocks receptor binding and down regulates ERs in all tissues?
Fulverstrant
Drug used for ER positive breast cancer treatment that is an IM injection 1x/month
Fulverstrant
You have a pt who you’re going to start on an ER positive breast cancer treatments. What do you warn her are the SE?
Fulverstrant
GI disturbances, hot flashes, thromboembolism
Aromatase inhibitors:
Anostrazole vs exemestane?
anastrozole= nonsteroidal, reversible
Exemstane= steroidal, non reversible
A postmenopausal women comes to your office who is being treated for an ER + cancer, but can’t remember the name of the drug. She is experiencing severe hot flashes.
Aromatase inhibitors:
Anostrazole or exemestane
Stimulation of these receptors develops and maintains the secretory endometirum, promotes uterine relaxation during pregnancy and prepares the breast for lactation.
Progesterone acting on:
PR-A and PR-B
Progestin interaction w/ Cortisol binding globulin vs. SHBG?
Progesterone= CBG
19-nor progestin= SHBG
This natural hormone is synthesized in the corpus luteum during the second half of the menstrual cycle, and by the placenta during the 2nd and third trimester.
Progesterone C21 steroid
What are the three major categories of synthetic progestins?
Medroxyprogesterone actetate
estranes
gonanes
What are the advantages of oral contraceptives?
- Reliable contraception, easy to use
- Decrease risk of endometrial and ovarian cancer
- Decrease incidence of intrauterine and ectopic pregnancy
- Menses regulation
- Reduces acne
What contraceptive may increase the risk of breast cancer over time, and may cause depression, weight gain, nausea, HTN and DVT?
OCPs
Levonogestrel
Progesterone agonist used for EC
Mifepristone and Ulipristal acetate
Progesterone antagonist used for EC
What EC is also an abortefacient when used at high doses +/- prostaglandin and in early term (</=49d post coitus)
Mifepristone
What drug is used as EC in smaller doses (w/in 3-5 d) and to terminate early pregnancy in larger doses?
Selective progesterone receptor modulators
Commonly used EC that prevents ovulation, CANNOT terminate a pregnancy and may cause N and V.
Levonogestrel (plan B)
EC that has efficacy up to 5 d after intercourse
Ella
EC that causes N/V, abd pain and heavy vaginal bleeding
Mifepristone
