Contraception and fertility drugs 1/4 Flashcards
Estrogen only , progestin only, or E + P: MOA as contraceptive, use
MOA: alters uterine and tubal mobitlity –> plan B (after boning) to interfere with implantation
Progestin only (p.o., i.m., IUD) MOA as contraceptive?
decrease in ovulation via decrease in LH/FSH
Increase cervical mucus viscosity
decrease tubal and uterine motility
ADEs of Progestin only
33% - intolerable nuisance complaints (bleeding)
Combination type contraceptive- an ethinylestradiol derivative + a 19-nortestosterone (low dose): MOA
Decreased LH/FSH release [dt -feedback]
Inhibits ovulation [dt Est effect]
Progestin assures prompt menses
mifepristone [RU-486]: MOA
Progesterone Receptor Antagonist, increased uterine mobility (inhibition of implantation)
How do you pick a contraceptive?
Choose the preparation with the lowest dose of estrogenic agent
The inhibition of ovulation (goal) and the cardiovascular side effects are both attributed to Which hormonal component of contraceptives?
the estrogenic component.
List the effects of estrogens on including liver function, clotting factors and thyroid hormone disposition
liver = increased LDL, decreasd HDL
clotting factors: increased
thyroid: increased TBG and total T4
What are the most important types of drug-srug interactions with progestin/estrogens
counteract Anticoagulants CYP450 inducer (microsomal enzyme inducer)
deficiency of progestin or estrogenic agents will cause what?
menstrual irregularities
Excess Estrogen leads to what?
Na and water retention (bloating)
PMS: Cervial mucorrhea, edema, nausea, bloating, breast tenderness, vascular headache, HTN
Excess Progestin leads to what (8)
androgenic effects of 19-nortestosterones: Acne, hirsutism, depression, fatigue, increased appetite, increaseed weight, vaginits, alopecia
What is the major ADE of the combo OCPs? why?
CVD dt increased clotting factors
What are the manifestations of increased risk of CVD with combo OCP use?
^MI, ^stroke, ^ thmbotic events
What increases risk of CVD ADE with combo OCPs? (5)
age (35-40), obesity, HTN, fHx, SMOKING!!!!
Absolute Contraindications to OCP use (5)
- HX of thmboembolic events
- impaired hepatic function/obstructive jaundice
- Estrogen-dependent neoplasia/breast CA/ genital bleeding
- pregnancy
- smoking >15 cigarettes/day
infertility tx for hyperPRLemia
bromocryptine
infertility dt anovulation in PCOS tx (2)
want to stimulate ovulation: cycling OCPs, clomiphene (
clomiphene MOA
estrogen receptor antagonist in hypothalamus–> increased release of LH/FSH (dt lack of inhibitory fb)–> ovulation
unfavorable cervical mucus (for fertility)
estrogen
infertility dt endometriosis tx
GnRH analogs (suppress LH/FSH)
infertility dt luteal phase dysfunction
progestin
anovulatory infertility dt Pituitary hypofunction: tx?
FSH/LH to stimulate the ovary directly
anovulatory infertility dt Feedback anomalies: tx?
Clomiphine- blocks negative feedback
