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17 Cards in this Set
- Front
- Back
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Typical oral contraceptive
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- Combination of an estrogen and progestational agent
- Taken for 3 successive weeks - Omitted for 1 week |
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Available Estrogens
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- Ethinyl Estradiol and its 3-methyl ether Mestranol
- Mestranol is converted by the liver to ethinyl estradiol |
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Available Progestins
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19-nortestosterone derivatives (one is an aldosterone derivative)
- Medroxyprogesterone - Norethindrone - Levonorgestrel |
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Progestins MOA
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- Reduce free testosterone level in serum and inhibit activity of 5-alpha-reductase and conversion of testosterone to its active metabolites
- Progestins have good effect on androgen related conditions such as Acne |
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Define monophasic preparation
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- same concentration throughout the cycle
- 21 tablets of ethinylestradiol (estrogen) and levonorgestrel (progestin) followed by 7 tablets of placebo or any iron prep |
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Define biphasic preparation
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- Ethinyl estradiol and norethindrone combination
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Define triphasic preparation
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constant estrogen + increasing doses of progestin given over three successive 7 day periods followed by 7 days placebo
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Transdermal patch
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ethiny estradiol + norelgestromin (a progestin)
one patch applied each week for 3wks and week 4 is patch-free (bleeding) less effective in women weighing more than 90kg |
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Trandermal patch adverse effects
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total estrogen exposure with transdermal patch is greater than with estrogen oral contrac.
increased exposure to estrogen can increase the risk of thromboembolism |
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Vaginal ring
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ethinyl estradiol + etonogestrel
ring inserted into vagina and left in place for 3wks and wk 4 is ring-free (bleeding) may occasionally slip or be expelled accidentally |
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Progestin-only pills
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contain progestin only (usually norethindrone or norgestrel)
taken daily on a continuous schedule deliver low, continuous dosage of drug less effective than the combination pill and may produce irregular menstrual cycles more frequently than combination product may be used for pts who are breast-feeding, are intolerant to estrogen, or are smokers |
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Progestin implants
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contains etonogestrel
capsule placed subcutaneously in the upper arm and provides contraception for 3 years reversible; does not rely on pt. compliance so very reliable |
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Progestin intrauterine device
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levonorgestrel-releasing intrauterine system
contraception for up to 5 years suitable for women who already have at least one child and dont have a history of pelvic inflammatory disease or ectopic pregnancy |
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Postcoital contraception
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high dose progestin (ex: levonorgestrel)
or high dose estrogen (ethinyl estradiol) plus progestin (levonorgestrel) admin 72 hours of unprotected intercourse and again 12 hours after the first dose progestin-only emergency contraceptive better tolerated single dose of mifepristone also can be used |
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Mechanism of action of contraceptives
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Not completely understood
combination of estrogen and progestin administered over a 3wk period inhibits ovulation (estrogen = negative feedback on release of LH and FSH and progestin inhibits LH release and thickens the cervical mucus) |
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Adverse effects of contraceptives
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- major: breast fullness, depression, fluid retention, headache, nausea, vomiting
- cardiovascular: rare but most serious; thromboembolism, thrombophlebitis, HTN, increased risk for MI, cerebral/coronary thrombosis [these are common in women who smoke and are older than 35] - cancer: OCP decrease incidence of endometrial and ovarian cancer - metabolic: abnormal glucose tolerance; weight gain in those taking nortestosterone derivatives - serum lipids: estrogen causes increase in HDL and decrease in LDL; progestins negate these beneficial effects (norgestrel causes greatest inc. in LDL:HDL ratio; Therefore, estrogen-dominant preps are best for those with inc. serum cholesterol) |
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Contraindications
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Those with cerebrovascular and thromboembolic disease, estrogen-dependant neoplasms, liver disease, and pregnancy.
Combination OCP shouldnt be used in pts over the age of 35 who are heavy smokers |
