Contraceptives Flashcards
Estrogens: EE, CEE, 17B
use
Progestins: Synthetic N L N D E D
M
P
use
Ethinyl Estradiol, contraception
Conjugated equine estrogen, menopause
17B estradial (menopause)
Contraception Norethindrone Levonorgestrel Norgestimate Desogestrel Etonorgestrel Drosperinone
Medroxyprogesterone Acete (contraception and menopause)
Progesterone (menopause)
Therapeutic use of contras
Many ___ occur in women using contras
typically less than
Rates decline w age until
Hormonal contraception, HRT
unintended pregnancies
18yrs
40yrs
Combination oral contraceptives contain
POP (minipill) contain
Injections of P contain
Devices- nonsurgical contain
includes
Surgical implantation (P) includes
E/P (the pill)
Progestin only
Depot MPA
E/P
Contraceptive patches/rings
IUDs/implants
Ethinyl estradiol used for contraception bc it is
Steroidal estrogens
Endo Natural estrogen includes ____ for HRT
CEE includes ___ and ___ for HRT
Synthetic includes ___ for contraception
Nonsteroidal estrogens- D__ prevents miscarriage
Anti Estrogens- T___ for BC
C for infertility
Potentcy EE > __ > Natural estrogen
most potent
17B estradiol
Equilin sulfate, estrone sulfate
Ethinyl Estradiol
Diethylstilbestrol
Tamoxifen
Clomiphene
CEE
Synthetic progestins
N
L
D/N
D__ which is a __ deivative, anti-___/____
Chemically modified natural progestins include
Norethindrone
Levonorgestrel
Desogestrel/Norgestimate
Drospirenone- spironolactone, MC/androgen
MPA
___ is the universal precursor to other hormnes
E binds with ___ affinity to specific
P binds with high affinity to
P also binds to other hormone receptors such as ___, ___, ____ w weaker affinity
At pharm doses, some progestins can ____ at these receptors
PRs are dependent on exposure to
Progesterone
high, ER
PR
AR, ER, GR
elicit responses
E
Norethindrone (1st gen) can interact w
Levonorgestrel can interact w ___ receptors to a high degree (most potent)
Norgestimate/Desogestrel can interact w
ER, PR, AR
PR, AR
PR, AR
Ethinyl Estradiol and Syntehtic progestin can make
IUD contrains _____ and implant contains ____
The shot contains _____
Luteal phase- high conc of ___/___ NF on HP axis to suppress __/___
Hormone contraceptives thus inhibit ____
Drugs mimic ___ during the luteal phase to stop ___/___ surge
in the luteal phase, P ? E
Synthetic EE in
Synthetic P in
The pill, patch, ring
Levonorgesterel, etonorgestrel
MPA
E/P, FSH/LH
ovulation
hormonal enviro, FSH/LH
> micrograms
milligrams
Hormone contraceptives also thicken ___ and make the ___ unfavorable for implantation
Compliance is ___
Risk of pregnancy inc substantially for COCs when ____
for POPs when
OCP greatly inc the risk for
other RF for VTE are ___ mutation, __ and ___
look for ___, __pain, calf/thigh ___, ___
cervical mucosa, endometrial lining
very important
> 2 doses
> 3 hr delay
VTE
Factor 5 leiden, preg, postpartum
SOB, pleuritic, swelling/pain, orthopnea
Contraceptive effects/SE due to ____ of hormoenes
Estrogen can ___ clotting factors, ___ anticoag factors, ___ platelet count/aggregation
Inc __/___ and dec
Increases ___ retention
Inc ___
Stimulates ___
Progestin can also
metabolic effects
inc, dec, inc
TG/HDL, LDL
Na
SHBG
cell proliferation
inc HDL/Dec LDL, stim cell prolif
Estradiol has __ and ___ effects, w an acute __ effect
Endo 17B Estradiol/Prog
Chem modified natural E/P (CEE/MPA)
Synthetic E/P
Liver 1st pass, Oral admin, t1/2
Bioavailability diminished by
Drug admin ___ is first exposed to ___, resulting in metabolism before reaching __
Rapid, LT, VD
Yes, No (unless special), short
Less, Yes, longer
Less, Yes, longest
1st pass metabolism
orally, liver, raeching the body
Lipophilic estrogen is hydroxylated by ___ and conjugated to ____
E-glucuronide then excreted into ___ via ___
Some is ___, some enzymaticallly cleaved by ____
___ estrogen is
Enteroheptatic circ- orally admin estrogen can be ___ and have ___
Inc ___ responsible for some of the __ and ___ met effects of estrogen
CYP450, glucoronide
intestine, bile
excreted, intestinal bacteria
free, reabsorbed
recycled, prolonged effects
hepatic effects, beneficial/Adverse
Backup contraception needed until menses occur in pts taking R, T, P, C
Anticonvulsants induce
EE and some progestin met by
Meds that induce CYP3A4 may dec ___
Options for epilepsy pt
recommend contraceptive other than
may suggest higher dose ___
Rifampin, Tetracycline, Penicillins, Cephalosporins
liver enzymes CYP3A4
CYP3A4
contraceptive efficacy
COC
estrogen OCP
1st/2nd gen OCP placed pt at risk for
3rd gen (low dose pills)
blood clots, endometrial cancer
50ug
1.5mg
Multiphasic
mimic cycle
progestin
COC vary in the dose of __ and dose/potency of
EE doses
Doses < ___ are preffered
Lower doses may not be effective in
To minimize SE, make
Progestins potency
L > D > N > N
Doses can ___ or __ by phase of cylce (.05-1.5mg)
Can be __ or __
to minimize SE, switch to different ____ or different ___
EE, P
10, 20, 30, 35, 50ug
35ug
heavier women
dose adjustments
Levonorgestrel, desogestrel, norgestimate, norethindrone
remain, inc
monophasic, triphasic
progestin, phasic prep
Regimens \_\_ days active, \_\_ days placebo to induce \_\_\_ active, \_\_ placebo to minimize Extended cycle \_\_\_ continuously taken ie \_\_\_ days active, \_\_ placebo
Phasic prep
Triphasic- P progressively rises over ___ to __
Less exposure to ___
Minimizes ___
Monophasics- Constant dosage of ___
Preffered for woman w ___ (late cycle bleeding)
Preffered for pt experience ___ on the triphasic
21, 7, withdrawal bleeding
24, 4
active pills, 84, 7
21 days, mimic cycle
P
P related SE
E/P
P defic
mood swings
Extended/Continuous cycle regimens purpose
___ menstrual perod, to __ or __ entirely
Indicated for ___ or ___ (menorrhagia)
Concerns due to > cumulative exposure to __ w 21/7 regimen
No withdrawal bleeding can lead to ____
many women experience ___ after use
takes ___ to return to fertility after 1 yr use
shorten, dec freq/eliminate
painful periods, excess bleeding
estrogen
endometrial hyperplasia (endo ca)
inactive endometrium
3mnths
Newer OCP is COC w ___ as progestin
Drosperenone reduces ___
bc of its anti__/___ activity
reduces ___ and ___
___ level may inc
Caution w drugs that ___ such as NSAID, ACEI, ARB
Contraindicated in __ and ___ dz
inc risk for
Drospirenone
bloating, androgen/MC
Na and H2O
K
raise K
Kidney/adrenal
VTE
Nonoral contraceptives __ compliance and __ liver exposure
Bypassing oral means less effect on ___
Birth control patch has ___ delivery of E/P
Worn __ and then replaced
__ patch weeks, followed by ___
Less effective in
may inc risk for ___ due to higher EE than ___/__ (peak __ but more ___)
Vaginal ring delivers ___
Worn for ___
Followed by ___
inc, dec
clotting
transdermal delivery 7days 3, patch free week heavier women clot, Ring/COC lower, sustained
E/P
21 days
ring free week
to ensure OCP efficacy, take at ___
If 1 pill missed, take ___
2 pills missed in a row (wk 1 or 2)- take ___ on day remembered and __ next day
Backup necessary for ___
2 pills missed in a row wk3
Discard ___ and ___
or keep taking pill/day and skip __ and start new
or for Sunday starters (ex), take pill/day until ___ and then ___
Backup necessary for
2 pills next day
2 pills, 2 pills
1 wk
pack, start new
placebos
Sunday, start new
1wk
Tablet form POP uses N or N
Doses close to __ for efficacy
Take @ ___ and no ___
Most commonly used in ___
Norethindrone, Norgestrel
threshold
same time every day, pill free interval
lactating women
POP Depot formulations
More freq use than
Depo Provera for __ contraception
IM injection of
Nexplanon __ contraception
Subdermal tube of ___
Return to fertility w/in __
IUD ___ contraception
doses ___ daily
oral POPs
3m, MPA
3y
Etonorgestrel
months
5y
levonorgestrel
SE of POP Minipills have I, A A D
With Depo Provera
B- limit use to ___ (concern for __/__)
W
D
higher failure rate
Irregular bleeding, amenorrhea
Acne
Depression
Bone loss, <2yrs, adolescetns/YA
Weight gain in heavier women
Delayed return to fertility
OCP benefits
reduced risk of __ and __
Dec in ___ and ___ and ___
Greater ___
Lower blood loss during __
ovarian/endometrial cancer
fibrocytic dz, fibroadenomas, acute PID
cycle regulatiry
menses
