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72 Cards in this Set
- Front
- Back
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What is the estrogen component used in combination oral contraceptives (COCs)?
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only the synthetic estrogen ethinyl estradiol (EE) is used
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MOA of estrogen in COCs
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-suppresses hypothalamic release of GnRH and subsequent pituitary release of FSH/LH
-inhibits ovulation in 95-98% of cycles -directly inhibits pituitary FSH release (preventing selection and emergence of dominant follicle) |
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what is the progestin component used in COCs?
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levonorgestrel (LNG)
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what are the four major properties of progestins?
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-progestational activity
-antiestrogenic activity -estrogenic activity -androgenic activity |
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what are the newer progestins that have lower estrogenic effects and that are less androgenic compared to LNG? (2)
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-desogestrel
-drospirenone |
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actions of progestational activity in COCs
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-inhibits ovulation
-hampers sperm transport -inhibits implantation -slows ovum transport -inhibits fertilization |
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How does progestational activity in COCs inhibit ovulation?
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disrupts the hypothalamic-pituitary-ovarian axis and decrease the mid-cycle LH/FSH surge
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How does progestational activity in COCs hamper sperm tansport?
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thickens cervical mucus
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How does progestational activity in COCs inhibit implantation?
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alters LH/FSH peaks; decreases progesterone production by corpus luteum
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contraceptive actions of progestin only mini-pills
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-hampers sperm transport
-inhibits implantation -slows ovum transport -inhibits fertilization (does not interfere with axis) |
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what is considered a low dose COC?
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</= 35 micrograms EE
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indications for low-dose COC
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-pts just starting COCs
-pts who need lower doses of estrogens due to ADR -pts approaching menopause to relieve Sx of declining estrogen levels |
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____________are best COCs for minimizing ADR of estrogen
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monophasic products containing 20 micrograms EE
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monophasic products containing 30 micrograms EE plus DSG advantage? disadvantage?
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-high progestin, low androgen minimizes androgenic effects
-may have increased risk of DVT over other progestins |
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monophasic products containing 30 micrograms EE plus drospirenone characteristics
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-antiandrogenic; no estrogenic or glucocorticoid actions; may cause weight gain
-progestin component drospirenone is a spironolactone analog with antimineralcorticoid activity; opposes the mineralcorticoid actions of EE |
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contraindications of the use of monophasic products containing 30 micrograms EE plus drospirenone
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-renal, adrenal, or hepatic insufficiency, or any condition predisposing to hyperkalemia
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spionolactone analog with antimineralcorticoid activity?
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drospirenone
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which progestin has some estrogenic activity?
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DSG
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Pt instructions for day 1 start of COC?
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-take 1st tablet on 1st day of menses
-backup method for 7 days preferred by clinicians, but not indicated |
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Is breast feeding affected by COC use?
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-studies do not show any effect of hormonal contraception on milk quality and quantity
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DI of COCs with antibacterials
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-antibacterial agents kill intestinal bacteria interrupting enterohepatic cycling of EE, allowing its fecal excretion and lowering its plasma levels
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what antibacterial agent has the highest clinical significant DI with COC?
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Rifampin
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what antibacterial agents are know to have moderately clinically significant DI with COCs? (4)
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ampicillin, amoxicillin, metronidazole,and tetracyclines
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what should be done when taking any of the highly or moderately significant antibacterial agents with a COC?
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use of a back-up method of contraception during course of antibacterial agent or until menses occur
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DI between COCs and inducing agents?
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-agents with the potential to induce hepatic enzymes can cause increased metabolic clearance of estrogens,and progestins
-results in decreased levels of both components and COC failure |
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anticonvulsants that are confirmed inducing agents (4)
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phenytoin, phenobarbital, topiramate, and carbamazepine
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antimicrobial that is an inducing agent
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rifampin
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antiviral that is an inducing agent
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nevirapine
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If use of inducing agents during COC is required, what should be done?
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temporary use of an alternative means of contraception
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Patients taking anticonvulsants (confirmed or suspect inducing agents) should ?
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-use alternative means of contraception permanently or increase estrogen content to 50 micrograms and monitor for BTB
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difference in MOA of progestin only minipills compared to COC
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--produces app. 25% of the amount of circulating progestin compared to a COC, which does not consistently suppress gonadotropin secretion; ovulation is not completely suppressed
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contraceptive effects of progestin only minipills
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-thickening of cervical mucus; impermeability to sperm
-endometrial involution; inhibits implantation |
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dosing of progestin only minipills
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-no placebo interval; all 28 tabs same
- must take at same time every day -3hrs late is considered a missed dose |
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___________is NOT as well prevented as intrauterine pregnancy with progestin only minipills
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-ectopic pregnancy
-incidence is still lower than with no contraception at all |
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advantages of progestin only minipills over COC
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-progestin content less than amts found in COC; reduces androgenic effects
-nl breast milk quantity and quality--preferred for BF pts -less likely to cause thromboembolic d/o associated with estrogen use |
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progestin only minipills should be considered for what pt populations?
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-smoker >35yrs old, FHx of CV dz, Hx of thromboembolic d/o, and women who cannot take estrogen safely
-mothers planning to breastfeed |
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disadvantages of progestin only minipills compared to COCs
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-higher failure rate (3%due to noncompliance)
-irregular cycles (40% ovulate normally, 20% switch back and forth between ovulatory and anovulatory cycles) -signs of progestin deficiency (high incidence of BTB resulting in noncompliance/ late-cycle spotting of BTB) |
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pt instructions for progestin only minipills
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-take at same time each day
-back up not needed on Day 1 start -if pill taken more than 3hrs late, use back-up method for 48 hrs |
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advantages of COCs that reduce the hormone-free intervals
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-minimize duration of withdrawal bleeding and menstrual related symptoms
-decreased risk of escape ovulation |
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COC that reduce the hormone free interval
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YAZ (20 mcg EE + drospirenone 3mg)
-also approved for PMDD -drospirenone helps reduce bloating, breast tenderness, and acne |
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current concepts regarding continuous use of COCs
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-endometrial proliferation limited during COC use and menses not required
-menses not required to prevent endometrial CA since cells shed during menses are from top layer, not the basal layer involved in neoplasia |
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benefits of continuous COC use
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-suppression of withdrawal bleeding may reduce dz states associated with hormonal fluctuations
-decrease anemia related to blood loss -relief of conditions exacerbated by menses -relief of Sx associated with menses |
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problems associated with continuous use of COC
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-increased exposure of ovarian hormones and known ADR
-absence of bleeding may cause concern over pregnancy -increased incidence of spotting and BTB inconvenient |
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Seasonique
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-extended cycle product
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Use of an extended cycle product with a lack of hormone-free interval may help ?
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menorrhagia,dysmenorrhea, menstrual migraine, and PMS
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Mechanism of postcoital use of levonorgestrel(LNG) within 72 hrs of unprotected sexual intercourse to prevent pregnancy
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-inhibition or delay of ovulation
-inhibition of fertilization -interferes with inplantation -NOT an abortifacient |
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postcoital use of_____________within 72hrs can be used as emergency contraception
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levonorgestrel (LNG)
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initiation of post-coital regimens for emergency contraception
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-most are initiated within 72hrs
-greater efficacy if started within12-24hrs after intercourse |
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1st generation ECs
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-high dose estrogens used in 5 day regimens
-not as effective at preventing ectopic pregnancies (same # as if no contraception) |
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major ADR of 1st generation ECs
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nausea
-an antiemetic given 1 hr prior to each dose helps prevent N/V |
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2nd generation of ECs
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-multiple tablets of one COC taken in two doses 12hrs apart
-contained estrogen and progestin |
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3rd generation ECs
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-specifically desigend for this use
-progestin only EC pill -2 doses of LNG 0.75mg 12hr apart -better tolerated(less N/V) and more effective |
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Plan B
-class -dosing -effectiveness |
-3rd generation EC
-Rx needed for age <17yrs -2 doses of 0.75mg LNG 12hrs apart -89%effective if used within 72hrs -95% effective if used within 24hrs |
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Plan B One-Step
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-one 1.5mg LNG tablet for OTC sale in women >17 and Rx for age <17
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what is ulipristal?
MOA? Cautions? |
-single dose EC indicated for use up to 120hr/5days after unprotected sex
-both progesterone agonist and antagonist properties -pregnancy category X (r/o pregnancy!!) -Rx required!!! |
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Depot medroxyprogesterone acetate (DMPA) products
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1. Depo-Provera
2. Depo-SubQ Provera |
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Depo-Provera administration
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-deep IM injection q 12wks
-contraceptive efficacy maintained for 12 wks +/- 2 wk grace period -initiate during day 1-5 of cycle or after ruling out pregnancy; otherwise use backup method 7 days |
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Depo-SubQ Provera administration
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-prefilled syringe formulation given SC q 3 mo
-initiate during day 1-5 of cycle or after ruling out pregnancy; otherwise use backup method 7 days |
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Depot medroxyprogesterone acetate (DMPA) MOA
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-progestin-only
-completely inhibits ovulation by suppressing LH surge -thickens cervical mucus -suppresses endometrial growth |
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Depot medroxyprogesterone acetate (DMPA) indications
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-estrogen-free contraception
-pts with sickle-cell dz -pts with epilepsy -breast-feeding pts |
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Depot medroxyprogesterone acetate (DMPA) effects in sickle cell pts
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-decreased frequency and intensity of crises
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Depot medroxyprogesterone acetate (DMPA) effects in pts with seizure d/o
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-30%decrease in seizure frequency in epileptic pts; high progestin levels raise the seizure threshold
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Depot medroxyprogesterone acetate (DMPA) effects on breast-feeding
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-does not interfere with prolactin binding; increased quantity and protein content of breast milk
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Advantages of Depot medroxyprogesterone acetate (DMPA)
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-can be used in pts who cannot tolerate estrogen side effects
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ADR of Depot medroxyprogesterone acetate (DMPA)
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-spotting, irregular bleeding due to insufficient estrogen to maintain endometrium
-amenorrhea due to unopposed antiestrogenic effects (no proleferation of endometrium) |
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Black Box Warning for Depot medroxyprogesterone acetate (DMPA)
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-bone loss: decreased bone density due to estrogen suppression
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Depot medroxyprogesterone acetate (DMPA) and the return of fertility after d/c
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-delayed about 10 mo after last injection in 50% of pts
-contraindicated in pts who wish to conceive promptly after d/c |
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levonorgestrel IUS (Mirena)
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-releases LNG @ 20mcg/d for 5yrs or until removed
-reduces menstrual bleeding/cramping -approved for tx of heavy bleeding and dysmenorrhea in pts who want IUD -return to ovulation is immediate upon removal of IUDs |
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NuvaRing
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-once monthly admin
-return to ovulation immediate with ovulation occurring within 1 mo after d/c |
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OrthoEvra Contraceptive Patch admin
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-worn continuously for 7 days and then replaced
-total 3 wk patch wear -start within 1st 24hrs of menstrual period (day 1 start) -no back up needed if 1st day start |
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OrthoEvra Contraceptive Patch efficacy compared with COC
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-efficacy equal, with better rate of consistent and correct use
-comparable incidences with BTB |
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FDA required warning on OrthoEvra Contraceptive Patch
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-average estrogen exposure is 60% higher than oral COCs due to absence of 1st pass effect with usage of patch
-although peak estrogen levels are actually 25% lower, exposure to higher continual levels occur with patch -may increase risk of VTE |
