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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
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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
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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
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Estrogen MOA
Block LH and FSH to inhibit ovulation
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LH
produced by gonadotroph cells in the anterior pituitary gland. Acute rise of LH triggersovulation & dev of the corpus luteum
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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
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FSH
regulates dev, growth, pubertal maturation, & reproductive processes of the body. Acts synergistically in reproduction c/ LH.
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indication of hormone contraception:
to prevent preg
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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
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Most COCs contain estrogen in the form of:
ethinyl estradiol
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maximum dose of ethinyl estradiol that most women should receive:
35 mcg
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what are some circumstances when higher doses of estrogen are appropriate?
if women had spotting and needed more cycle control, if enzyme induced
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least potent progestin
Norethindrone
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most potent progestin:
Desogestrel, levonorgestrel, & norgestrel
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least androgenic progestins:
- Desogestrel & norgestimate
- least likely to cause acne & hirtusim
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most androgenic profile:
- Norgesterel
- increased libido
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intermediate in terms of androgenic activity:
Norethindrone & ethynodiol
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Has anti-androgenic properties:
and similar to spironolactone
Drospirenone
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What is imp to monitor in a pt on Drospirenone?
Potassium, for hyperkalemia
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Components that make up COC:
On exam!
- -20–50 mcg ethinyl estradiol
- —newer formulations rarely contain >35 mcg
- -0.1–1.5 mg progestin
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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
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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
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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
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What are cautions for COC?
- migraines c/ aura (consider progestin only)
- smoker
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SE of too much estrogen:
Nausea, breast tenderness, increased blood pressure, melisma (darkening of the skin), headache
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SE of too little estrogen
Early or mid-cycle breakthrough bleeding, increased spotting, hypomenorrhea
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SE of too much progestin:
Breast tenderness, headache, fatigue, changes in mood
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SE of too little progestin:
Late breakthrough bleeding
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SE of too much androgen:
Increased appetite, weight gain, acne, oily skin, hirsutism, increased LDL cholesterol, decreased HDL cholesterol
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Monophasic:
- hormone levels remain constant
- ortho-Novum
- Demfun
- Lo-ovral
- ortho-cyclen
- Loestrin
- Alesse
- Ortho-cept
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Biphasic:
- Its a change of one hormone level of either estrogen or progestin
- one will change and one stays the same
- Ortho-Novum
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Triphasic
- 3 diff doses of hormones changing q 5-10 days in 1st 3 weeks
- Ortho-Novum
- Ortho-Tricyclen
- Ortho-Tricyclen lo
- Tri-Norinyl
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Four-Phasic
- 4 diff doses of hormones changing thru out 28 day cycle
- Natazia
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the first OC to contain estradiol instead of ethinyl estradiol
Natazia
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Drug reps will promote Natazia for:
heavy menstrual bleeding
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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
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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.
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what other OC’s can also be used for heavy bleeding?
- Progestin only
- Mirena (levonorgestrelIUD)
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Natazia and other combo OCs reduce blood loss by about____ in women with heavy menstrual bleeding.
50%
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(Estradiol valerate/dienogest)
Natazia
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