Contraception Flashcards
(30 cards)
1
Q
Estrogens
A
- Female sex hormone
MOA
- Transcription factor
- Directly modifies messenger RNA synthesis
- Passively enters cell and binds estrogen receptors in the nucleus
- Receptors dimerize and bind DNA at estrogen responsive elements
- Influence gene transcription
Effects
- Reproductive: female sexual maturation, endometrial growth, breast tissue stimulation
- Hematologic: increased tendency for clotting (increases circulating levels of vit K dependent clotting factors)
- Skin/mucosa: increased pigmentation; increased skin collagen content and skin thickness; maintenance of skin moisture (increased acid mucopolysaccharides and hyaluronic acid)
- Metabolic: decreased bone reabsorption via antagonism of PTH and IL-6; increased HDL, decreased LDL, increased trigs
2
Q
Estrogen indications
A
- Contraception
- Menopausal HRT (moderate to severe vasomotor sx, vulvovaginal atrophy)
- Endometriosis treatment
- Dysfunctional uterine bleeding
- Osteoporosis prevention
3
Q
Estrogen CI
A
- Undx abnormal genital bleeding
- Known/suspected/hx of breast cancer (unless treated for metastatic dz)
- Active DVT, PE, or h/o them
- Active arterial thromboembolic dz (stroke, MI), or h/o
- Anaphylactic rxn or angioedema to estrogen tablets
- Liver dysfunction or dz
- Protein C, protein S, or antithrombin deficiency or other known thrombophilic disorders
- Pregnancy
4
Q
Progesterone
A
- Increased oral bioavailability
- High protein bound
- Metabolized by 3A4 (inhibited by ketoconazole)
- Warnings for increased risk of DVT, PE, CVA, AMI, dementia, invasive breast cancer
Indications
- Secondary amenorrhea
- DUB
- PMS
- HRT
- Cervical ripening
- Mastodynia
- Endometrial hyperplasia
- Infertility
- Anovulatory bleeding
5
Q
Progestins
A
- AKA progestogens
First generation (pregnanes)
- Steroids with similar activity to progesterone
- Megestrol acetate (Megace)
- Medroxyprogesterone acetate (Provera, Depo-Provera)
Second generation (estranes)
- Norethindrone (Aygestin)
- Ethynodiol
- Used in OC’s
- Also have androgenic effects
Third generation (Gonanes)
- Norgestrel, Levonorgestrel
- Desogestrel
- Norgestimate
- Dienogest
- Oral and injectable contraceptives
- Less androgenic activity than estranes
Nonsteroidal
- Drospirenone
- Derived from spironolactone
6
Q
Progestins MOA
A
- Directly modify RNA synthesis
- Enter cell and bind nuclear progesterone receptors
- Dimerize and bind DNA
- Influence gene transcription
7
Q
Progestins effects
A
Reproductive effects
- Feedback loop with FSH and LH
- Decline determines onset of menstruation
- Changes endocervical gland secretions from watery to viscous (reduces sperm entry into the uterus)
- Maintains pregnancy
- Increased body temperature with preovulatory surge
- Mild sedative
Metabolic effects
- Increased insulin secretion and peripheral insulin resistance
- Increased lipase activity
- Possible increased fat deposition
- Increased LDL, decreased HDL
8
Q
Progestins Indications
A
- Contraception
- Post-menopause HRT
- Dysfunctional uterine bleeding
- Pregnancy maintenance
9
Q
Progestins CI
A
- Risk for DVT or PE
- Severe migraine
- Unexplained vaginal bleed
- Breast cancer
- Active liver dz
- Theoretical increase of CV risk due to reduced HDL, increased LDL
10
Q
Progestins ADR
A
- Androgenic activity: acne, hirsutism, increased LDL, insulin resistance
- DVT: higher incidence with third generation progestins
- Vaginal bleeding
- DMPA: bone loss
11
Q
Oral contraceptives
A
Estrogen-progestin combination
Progestin only
Estrogens
- Ethiyl estradiol
- Mestranol
- Estradiol valerate
Progestins
- Medroxyprogesterone
- Norethindrone
- Levonorgestrel
- Ethynodiol acetate
- Desogestrol
- Drospirenone
- Norgestimate
- Dienogest
- 28 day packs
Monophasic
- Fixed amount estrogen-progestin each pill
- Take daily x 21 days
- Last 7 days placebo pills
Multiphasic
- Varying concentrations of estrogens taken at different times during the cycle
Extended cycle
- 84 active pills, 7 placebo pills
Estrogen dose varies from 10mcg to 50 mcg
- Low estrogen < 35 mcg per pill
12
Q
Estrogen MOA
A
- Cycle control
- Some contraceptive activity
- Stabilizes endometrium
- Minimizes irregular shedding
- Inhibits FSH release (prevents dominant follicle development)
- Protentiates LH surge inhibition
13
Q
Progestin MOA
A
- Primarily responsible for contraceptive effect
- Prevents LH surge (no ovum released)
- Thickens cervical mucus (impedes sperm entry into uterus)
- Decreases tubal motility (impedes sperm transit thru fallopian tube)
- Thin endometrium (reduces probability of implantation)
14
Q
Oral contraceptives CI
A
- h/o stroke, clot, thrombophlebitis, VTE, valvular heart dz
- DM with vascular involvement
- Migraine with aura
- Uncontrolled HTN (>160/110)
- Major surgery with prolonged immobilization
- Thrombogenic mutations
- Breast cancer
- Liver dz
- Age > 35 smoking more than half a pack/day
- Pregnant
- Breastfeeding < 6 wks postpartum
15
Q
OC drug interactions
A
- Used backup method if drug interaction decreases efficacy
- Rifampin reduces efficacy
- Phenobarb, carbamazepine and phenytoin potentially reduce OC efficacy (many seizure meds are teratogenic; IUD, DMPA and implants may be other options)
- abx controversial: tetracyclines and PCNs reduce ethinyl estradiol concentration; ampicillin may cause breakthrough bleeding
16
Q
OC ADR
A
- Breakthrough bleeding
- Estrogen: HA, breast tenderness, DVT/clot, N
- Progesterone androgenic effects: Acne, hirsutism
17
Q
OCP symptoms
A
Estrogen Excess
- N, breast tenderness, HA, cyclic wt gain (fluid retention)— fix: lower estrogen OCP, POP or IUD
- Dysmenorrhea, menorrhagia, uterine fibroid growth— fix: lower estrogen OCP, POP, IUD, extended cycle OCP, NSAIDs for dysmenorrhea
Estrogen Deficiency
- Vasomotor sx, nervousness, decreased libido, early cycle BTB— fix: higher estrogen OCP
- Amenorrhea— fix: check for pregnancy, higher estrogen OCP or continue current
Progestin excess
- Increased appetite, wt gain, bloating constipation, depression, fatigue, irritability— fix: lower progestin OCP
- Acne, oily skin, hirsutism— fix: lower progestin OCP, less androgenic progestin
Progestin deficiency
- Dysmenorrhea, menorrhagia— fix: higher progestin OCP, extended cycle OCP, POP or IUD, NSAIDs for dysmenorrhea
- Late cycle BTB— fix: higher progestin OCP
18
Q
OCP efficacy
A
- Up to 99.7% efficacy with perfect use
- 91% efficacy with typical use (missed doses, missed timing of doses)
- Late: <24 hrs since the dose should have been taken
- Missed: > 24 hrs since dose should have been taken
If one late/missed
- Take the late or missed pill ASAP
- Continue taking the remaining pills at the usual time (even if it means taking two pills on the same day)
- No additional contraceptive protection is needed
If >2 consecutive pills missed
- Take the most recent missed pill ASAP (any other missed pills should be discarded)
- Continue taking the remaining pills at the usual time (even if it means taking two pills on the same day
- Use back-up contraception (e.g. condoms) or avoid sex until pill have been taken for 7 consecutive days
- If pills were missed in the last week of hormonal pills (day 15-21 for 28 day pill packs): omit hormone free interval by finishing the pills in current pack and starting a new pack the next day; if unable, use backup contraception
- emergency contraception should be considered if pills were missed during the first week and unprotected sex occurred in the pervious 5 days
19
Q
Ortho Evra patch
A
- Norelgestromin 150 mcg and 35 mcg ethinyl estradiol daily: Controversy over clot risk (may be twice as high as OCs; higher E exposure)
- Apply new patch weekly x 3 weeks
- No patch week 4
- Don’t cut patch
- Less effective in pts > 90 kg
If the patch has been off or partially off
- For less than 1 day, try to reapply it. If patch does not adhere completely, apply new patch immediately
- No backup contraception needed and patch change day stays the same
> 1 day or if not sure for how long, may not be protected from pregnancy
- To reduce this risk, apply a new patch and start a new 4 week cycle with new patch change day
- Use NON-HORMONAL BACKUP CONTRACEPTION (condom) for the first week of new cycle
20
Q
Nuvaring
A
- Etonogestrel 120mcg and 15 mcg EE daily (doesn’t seem affected by bw)
- Insert vaginally: leave in place x3weeks–remove–insert new ring one week after removal
- Additional ADR: vaginal irritation/infection/secretion
21
Q
Progestin only pills
A
- AKA minipill
- Norethindrone 0.35mg
- No estrogen
- Start anytime in cycle: if started within first 5 days of cycle, no backup needed; if more than 5 days of cycle, backup method needed
- Use postpartum
- Ok with breastfeeding
- Must be timed carefully (daily doses need to be within 3 hrs or considered late)
22
Q
Depo-provera
A
- Medroxyprogesterone acetate injection
- Given within 5 days of cycle start
- Long-acting: prevents ovulation for 3 months
- Repeat dose q12wks
- Safest 30 days after delivery in breastfeeding women
- MC ADR: irregular menstrual bleeding
- Other ADR: breast tenderness, wt gain, depression
Decreased BMD (slows after 1-2 yrs of tx)
- Not associated with increased fracture risk or osteoporosis
- BMD returns to near baseline after drug stopped
- Make sure pts get adequate calcium/vit D
23
Q
Implants
A
- Etonogestrel
- Good efficacy if correctly implanted (may be less effective in obese women)
- Major ADR: irregular bleeding
- Other ADR: HA, vaginitis, wt gain, acne, breast/abd pain
- Reversible
- Doesn’t affect bones
24
Q
Choosing a contraceptive
A
- Women w/o other medical conditions (OC<35mcg EE and < 0.5 mg norethindrone)
- Adolescents, underwt women, women> 40, perimenopausal women
- overwt/obese women
- migraine, h/o clot, heart dz, CVA and SLE with vascular dz, smokers> 35 yo, postpartum and/or breastfeeding, estrogen dependent cancer
25
Backup methods
- Abstinence
- Condoms
- Spermicide
- Diaphragm
- Cervical cap
- Sponges
26
Emergency contraception
- Yuzpe method
- Levonorgesterol (plan B, next choice)
- Ulipristal (Ella)
- Mifepristone (Korlym)
- Cu-IUD
For best results, must use within 5 days of unprotected intercourse
27
Yuzpe method
- 8/100 decreased to 2/100 become pregnant due to unprotected intercourse in the 2nd or 3rd week of their cycle
- 100mg EE with 0.5 levonorgestrel
- One dose within 72 hrs of intercourse, one dose 12 hours after first dose
- ADR: N/V
28
Ulipristal acetate (Ella)
- Selective progesterone modulator
- Antagonist and partial agonist effects
- MOA: inhibition or delay of ovulation (inhibits folliculogenesis and reduces estradiol concentration in mid-follicular phase; delays follicular rupture by 5-9 days when given at time of LH peak)
- Take 1 tablet within 120 hrs of unprotected intercourse
- ADR: HA, N/abd pain, dysmenorrhea, fatigue, dizziness, acne
- Rx only
29
Levonorgestrel (Plan B, next choice)
- Morning after pill
- Primary MOA: inhibits or delays ovulation
- Secondary MOA: prevents fertilization (impairs sperm transport and corpus luteum fxn)
- May inhibit implantation
- Not effective if woman already pregnant (higher incidence of ectopic pregnancy)
- ADR: irregular menses, N/ abd pain, fatigue, HA, dizziness, breast tenderness
- Plan B 1 dose within 72 hrs of unprotected intercourse, then 1 dose 12 hrs later
- May work as long as 120 hrs after unprotected intercourse
- Available OTC
30
Mifepristone (Korlym)
- AKA RU-486, abortion pill
- MOA: progesterone and cortisol receptor antagonist (selective progesterone receptor antagonist at low doses; blocks glucocorticoid receptor at higher doses; no effects on estrogen receptors)
- P450 metabolism
- Indications: Control hyperglycemia secondary to hypercortisolism in cushing's syndrome who have failed or are not candidates for surgery
- Pregnancy category X
- Used alone or in combo with misoprostol to end early pregnancy (must be dosed up to 70 days after first day of last menstrual period)
- Blocks progesterone which prevents maintenance of uterine lining (lining breaks down, ending pregnancy)
- Must be given in provider office
- Misoprostol given up to 2 days later (used to empty uterus-- similar to early miscarriage; most women will abort within 4-5 hrs after taking misoprostol; cramps, heavy bleeding, dizziness, N/V/D/abd pain)
- Follow up within 2 weeks to confirm end of pregnancy
- Watch for sx of sepsis: N/V/D, weakness, w/ or w/o abd pain; fever may or may not be present; check CBC with diff
- pt may become pregnant again immediately
