Lecture 3 (part 2): Estrogens/Progestins Flashcards
Two types of estrogens
- Estradiol
2. Ethinyl Estradiol
What is the effect of the Ethinyl group in estrogens?
makes it resist to 1st pass effect and decr clearance
What is the ONLY form of estrogen that is active?
what converts Androstenedione –> Estrone and Testosterone –> 17 beta-estradiol
only active form = free estrogens
Aromatase (CYP19A1)
How does estrogen affect blood coagulation?
- which factors/products affected?
What one of the major risks a/w estrogens that relates to this?
- incr factors 2, 7, 9, 10 and plasminogen
- decr antithrombin
Risk of thromboembolism (stroke, MI)
What is a major risk a/w unopposed estrogen therapy? what is the result of this for how estrogen is used?
Incr risk of endometrial CA (post-menopausal women)
ESTROGEN IS NEVER USED ALONE
What is the site of estrogen production before ovulation? after ovulation?
before: follicle
after: corpus luteum
3 major forms of progestins?
- Natural progesterone in body
- Norethindrone
- Levonorgesterol
Why are E/P given together (what effect does Progestin have on the body)?
Progestin –> androgen effects (acne, hirsutism)
- estrogen mitigates these
What is the main effect of progesterone on body at PHYSIOLOGIC levels?
effect during pregnancy?
generates the endometrium
pregnancy: suppresses menstruation and uterine contractions
What are the 3 main effects of progesterone on body at PHARMACOLOGIC levels?
- cause endometrial regression (endometrium becomes atrophic, impairs implantation)
- creates THICK cervical mucus (decr sperm penetration)
- prevents ovulation (decr GnRH pulses)
3 major AE a/w progestin therapy?
- menstrual irreg/bleeding
- long term therapy –> delayed return of ovulation
- Incr risk of BCA when give w/estrogens in POSTmenopausal women
3 major CIs a/w progestin therapy?
- PMH of BCA
- Undx vaginal bleeding
- PMH of thromboembolic dz in last 6 mo
What is the benefit of the combo E/P in regards to dosing?
Addition of Progestin lowers the amt of Estrogen needed
