EXAM #5: ESTROGENS & PROGESTIN II Flashcards
What adverse effects are associated with progestins?
1) Breakthrough bleeding (endometrial vasculature)
2) Impaired glucose tolerance
3) Changes in lipid metabolism
- Elevated LDL
- Lowered HDL
What are the key adverse effects associated with 19-nortestosterone compounds?
1) Acne
2) Hirsutism
Thus, 19-nor effects of BC cause acne vs. estrogen which is protective against acne
What is birth control?
Combined estrogen-progestin or progestin only drugs
What can birth control drugs never be composed of?
Estrogen alone
What is the most common type of injectable BC?
Progestin alone i.e. depo-provera, which is given:
- Monthly
- or Quarterly
What are implantable BC methods composed of?
Progestin only
How long can an implantable BC stay implanted?
3 years
What is the composition of IUD BC?
Progestins only
How long can an IUD stay in?
5 years
How often are vaginal rings and transdermal BC placed?
Monthly
What is the general MOA of BC?
1) Suppress LH and FSH surge for ovulation
2) Alter cervical mucus
3) Alter endometrium
Give an example of a progestin only BC.
Nor-QD
What hormone is in “Depo-provera?”
Medroxyprogesterone
What is the major difference between normal contraceptive therapy and emergency contraception?
Higher doses for emergency contraception
How long after intercourse can one take Plan-B?
72 hours
*Note that this is the drug of choice for emergency contraception
What is the failure rate of oral contraception with typical use?
8%
What are the mild adverse effects associated with contraceptives?
- Nausea
- Mastalgia (breast tenderness)
- Breakthrough bleeding (Estrogen-mediated)
- Edema
- Headache
- Withdrawal bleed failure
- Serum protein changes
What are the moderate adverse effects of contraceptives?
- Breakthrough bleeding (Progestin-mediated)
- Weight gain
- Increased skin pigmentation
- Acne
- Hirsutism
- Vaginal infection
- Amenorrhea
What are the severe adverse effects of contraceptives?
- Thromboembolic disease
- MI
- CVA
- GI disorders i.e. cholestasis
- Depression
- ?Cancer
What are the benefits of contraceptives?
1) Reduced risk of ovarian and endometrial cancer
2) Reduction in dysmenorrhea/ endometriosis
3) Decreased incidence of ectopic pregnancy
4) Decreased benign breast disease
5) Increased Hb concentrations
6) Suppress acne and hirsutism
What are the contraindications to estrogen containing contraceptives?
1) Known/ suspected breast cancer
2) Thromboembolic disorder
3) Liver disease
4) Cardiovascular disease
5) Smoker 35 y/o+
What are the drugs that induce hormone metabolism?
1) HIV agents
2) Anti-convulsants
3) St. John’s wort
What effect do antibiotics have on contraceptives?
Decreased efficacy
What is the clinical indication for Clomiphene?
Fertility drug
What is the MOA of Clomiphene?
- PARTIAL AGONIST that blocks negative feedback on LH and FSH
- Increase liklihood of ovulation
What is a partial agonist?
Drug that produces a lower than maximal response compared to the agonist
What adverse effects are associated with Clomiphene?
1) Hot flashes
2) Multiple births
When in the menstrual cycle is Clomiphene given?
- Follicular phase for 5x days
- Removed prior to day 14 (ovulation)
What are SERMS?
Selective Estrogen Receptor Modulators
*Note that the same SERM can have different actions in different tissues i.e. agonist, partial agonist, antagonist
What is the function of SERMS in bone?
Suppress bone resorption (agonist)
*I.e. estrogen receptor agonism will reduce osteoporosis
What is the function of SERMS in the endometrium?
Proliferation (partial agonist)
This is an unintended adverse effect and can lead to development of endometrial hyperplasia and endometrial CA
What is the function of SERMS in pituitary and breast?
Antagonist, which will
- Hot flashes (pituitary)
- Inhibited proliferation in breast (anti-ER+ cancer)
List the two SERMS.
Tamoxifen
Raloxifene
What is the clinical indication for Tamoxifen?
ER+ Breast Cancer
What adverse effects are associated with Tamoxifen?
1) Hot flashes
2) Endometrial cancer
3) Nausea/vomiting
How does Raloxifene differ from Tamoxifen?
NO partial agonist effects on endometrium
What are the clinical indications for Raloxifene?
1) Breast cancer
2) Post-menopausal bone loss
What key adverse effect is associated with Raloxifene?
Hot flashes
What are the clinical indications for dananzol?
1) Endometriosis
2) Breast fibrocystic disease
What is the MOA of dananzol?
Decreased estrogen concentration in blood by displacing estrogen from serum proteins and increasing estrogen clearance
What adverse effects are associated with dananzol?
1) Hot flashes
2) Weight gain
3) Oily skin
4) Acne
5) Hirsutism
What is the MOA of anaztrozole and letrozole?
Aromatase inhibitors that prevent conversion of Testosterone to Estrogen
What are the indications for anaztrozole and letrozole?
ER+ breast cancer
What adverse effects are associated with anaztrozole and letrozole?
- GI disturbances
- Hot flashes
- Lethargy
List the anti-progesterone drugs.
Mifepristone
Ulipristal
What is the MOA of Mifepristone?
Progesterone receptor antagonist i.e. it will decrease the effects of progesterone
What is the clinical use of Mifepristone?
Abortifacient (less than 7 weeks/ first trimester)
Followed by misoprostol (synthetic prostaglandin, which further increases uterine contractions) 48 hours later
What is the clinical indication for Uliprastal?
Emergency contraception
What is the MOA of Uliprastal?
Partial progesterone agonist
What is the benefit of Uliprastal vs. Plan-B?
Can be used 5 days post-intercourse vs. 3 days for Plan-B
