Female reproduction- pharm

  1. oral contraceptives work by:
    • - suppressing ovulation- main mechanism
    • -thickening the cervical mucus, preventing sperm from getting through
    • - changing the lining of the uterus, making implantation of a fertilized egg less likely
    • -reducing sperm access to the fallopian tubes, where eggs are fertilized
  2. How are progestins primarily responsible for the contraceptive activity?
    • - Prevent the LH surge needed for release of  the ovum·        
    •                Prior to ovulation, there is a big LH surge. Progestins prevent that from happening
    • -Thicken cervical mucus, hindering sperm entry into the uterus
    • - Decrease tubal motility,  impeding sperm transit through fallopian tubes
    • -Thin the endometrium, reducing implantation probability
  3. How are estrogens primarily responsible for the cycle control?
    • -Stabilize the endometrium, minimizing irregular bleeding                
    • - Inhibit the release of FSH, preventing the development of the dominant follicle
    • -Potentiate progestin’s inhibition of the LH surge
  4. Estrogen MOA
    Block LH and FSH to inhibit ovulation
  5. LH
    produced by gonadotroph cells in the anterior pituitary gland. Acute rise of LH triggersovulation & dev of the corpus luteum
  6. Corpus luteum
    temporary endocrine structure in XX mammals that is involved in the production of relatively high levels of progesterone & moderate levels of estradiol and inhibin A
  7. FSH
    regulates dev, growth, pubertal maturation, & reproductive processes of the body. Acts synergistically in reproduction c/ LH.
  8. indication of hormone contraception:
    to prevent preg
  9. what are other benefits from hormone contraception?
    • -less acne
    • -less menstrual flow and cramping
    • -less iron deficiency anemia that results from heavy menses
    • -fewer premenstrual symptoms, as well as related headaches and depression
    • -May help peri-menopausal women to smooth the transition
  10. Most COCs contain estrogen in the form of:
    ethinyl estradiol
  11. maximum dose of ethinyl estradiol that most women should receive:
    35 mcg
  12. what are some circumstances when higher doses of estrogen are appropriate?
    if women had spotting and needed more cycle control, if enzyme induced
  13. least potent progestin
  14. most potent progestin:
    Desogestrel, levonorgestrel, & norgestrel
  15. least androgenic progestins:
    • Desogestrel & norgestimate
    • least likely to cause acne & hirtusim
  16. most androgenic profile:
    • Norgesterel
    • increased libido
  17. intermediate in terms of androgenic activity:
    Norethindrone & ethynodiol
  18. Has anti-androgenic properties:
    and similar to spironolactone
  19. What is imp to monitor in a pt on Drospirenone?
    Potassium, for hyperkalemia
  20. Components that make up COC:

    On exam!
    • -20–50 mcg ethinyl estradiol
    •         —newer formulations rarely contain >35 mcg
    • -0.1–1.5 mg progestin
  21. How are oral contraceptives available?
    • - As progestin only 
    • -As a combination of estrogen and progestin (Most preparations are a combination of an estrogen plus a progestin)
    • -And in many options:  a vaginal ring, a patch, IM, an IUD, a subdermal rod, and a large variety of oral choices
  22. Dose that you would start an ethinyl estradiol + an older progestin (levonorgestrel, norethindrone, etc) have good balance of safety & efficacy
    20 mcg

    Start c/ 10 mcg if you are worried about SE
  23. what do you do if pt has breakthrough bleeding (spotting)?
    common during 1st few cycles
    • Tweak the dose
    • Increase the estrogen if the XX is taking less than 30 mcg, or change progestin if she on 30 mcg or higher
  24. What are cautions for COC?
    • migraines c/ aura (consider progestin only)
    • smoker
  25. SE of too much estrogen:
    Nausea, breast tenderness, increased blood pressure, melisma (darkening of the skin), headache
  26. SE of too little estrogen
     Early or mid-cycle breakthrough bleeding, increased spotting, hypomenorrhea
  27. SE of too much progestin:
    Breast tenderness, headache, fatigue, changes in mood
  28. SE of too little progestin:
    Late breakthrough bleeding
  29. SE of too much androgen:
    Increased appetite, weight gain, acne, oily skin, hirsutism, increased LDL cholesterol, decreased HDL cholesterol
  30. Monophasic:
    • hormone levels remain constant
    • ortho-Novum
    • Demfun
    • Lo-ovral
    • ortho-cyclen
    • Loestrin
    • Alesse
    • Ortho-cept
  31. Biphasic:
    • Its a change of one hormone level of either estrogen or progestin
    • one will change and one stays the same
    • Ortho-Novum
  32. Triphasic
    • 3 diff doses of hormones changing q 5-10 days in 1st 3 weeks
    • Ortho-Novum
    • Ortho-Tricyclen
    • Ortho-Tricyclen lo
    • Tri-Norinyl
  33. Four-Phasic
    • 4 diff doses of hormones changing thru out 28 day cycle
    • Natazia
  34. the first OC to contain estradiol instead of ethinyl estradiol
  35. Drug reps will promote Natazia for:
    heavy menstrual bleeding
  36. Instead of the usual 7-day hormone free interval, Natazia has:
    • 4 estrogen-only tabs plus 2 inert tabs.
    • Idea behind it was decreased breakthrough bleeding.
    • But they don’t really know what causes this
  37. Many women start with an NSAID to reduce cramps and bleeding. Why?
    • Prostaglandin levels are higher in women who have heavy bleeding.
    • NSAIDs block the prostaglandins    
    • Go to a contraceptive if an NSAID isn't enough for bleeding. 
  38. what other OC’s can also be used for heavy bleeding?
    • Progestin only
    • Mirena (levonorgestrelIUD) 
  39. Natazia and other combo OCs reduce blood loss by about____ in women with heavy menstrual bleeding.
  40. (Estradiol valerate/dienogest)
Card Set
Female reproduction- pharm
Pharm; Female reproduction