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OCPs & HRT
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63
Pharmacology
Professional
05/01/2011

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Term
two major preparations of OCs
Definition
combination estrogen and progestin
continuous progestin only
Term
clinical uses of OCs
Definition
contraception
help maintain cycle regularity
decrease dysmenorrhea
decrease ectopic pregnancies
decrease risk of ovarian cancer
decrease fibroadenomas/fibrocystic breast
Term
mechanism of action for OCs
Definition
override normal ovarian steroid regulation of reproductive function

exert negative feedback on hypothalamus and pituitary

-reduce GnRH secretion
-reduce FSH secretion-->incomplete follicular development
-reduce LH secretion-->no ovulation without pre-ovulatory LH surge
Term
effects of OCs on the ovary
Definition
steroidogenesis (particularly progesterone) is suppressed
Term
effects of OCs on the uterus
Definition
progestagenic component interferes with endometrial structure and consistency of the cervical mucous
Term
Why is progesterone secretion from the ovary suppressed with OCs?
Definition
progesterone is primarily produced by the corpus luteum

no ovulation-->no corpus luteum-->diminished progesterone
Term
What is the most commonly used estrogen in OCs?
Definition
ethinyl estroadiol
(Ovral, Orthotricyclen)
Term
What type of estrogen is found in some OCs that is converted to ethinyl estradiol?
Definition
mestranol
(Orthonovum)
Term
norethindrone
Definition
commonly used progestin
Term
levonorgestrel
Definition
commonly used progestin
Term
norgestimate
Definition
commonly used progestin
Term
desogestrel
Definition
commonly used progestin
Term
Rank the order of commonly used progestins with regard to their progestagenic potency from highest to lowest.
Definition
desogestrel
norgestrel
norgestimate = norethindrone
Term
Rank the order of commonly used progestins with regard to their androgenicity from highest to lowest.
Definition
norgestrel
norgestimate
norethindrone
desogestrel
Term
Which commonly used progestin is associated with a higher risk of thromboembolism?
Definition
desogestrel
Term
drospirenone
Definition
commonly used progestin
Term
What is special about drospirenone?
Definition
very low androgenicity

has been reported to have anti-androgenic effects similar in efficacy to spironolactone
Term
ethinyl E2 + levonorgestrel
Definition
Seasonale

extended OC (84+7 day regimen)
Term
What are the terms monophasic, biphasic, and triphasic referring to?
Definition
how many doses of progestin
Term
Ovral-28
Definition
monophasic combo pill
Term
Nelova
Definition
biphasic combo pill
Term
Triphasil
Definition
triphasic combo pill
Term
OrthoTricyclen
Definition
triphasic combo pill
Term
Ovrette
Definition
daily progestin (norgestrel) pill
Term
Norplant
Definition
implantable progestin
Term
medroxyprogesterone acetate
Definition
DepoProvera
injectable progestin
Term
Progestin only is less/more consistent in inhibiting ovulation.
Definition
less
Term
When are progestin only OCs used?
Definition
women who are at risk for certain estrogen-dependent cancers

women who do not tolerate the estrogenic component of combos
Term
Progestin only OCs may be a better choice for women who are...
Definition
breast feeding (only 0.1% of administered progestin ends up in breast milk)
Term
OC drug interactions
Definition
-phenytoin
-rifampin
-antibiotics/antimicrobials

*lower efficacy of OCs*
Term
OC side effects associated with estrogen
Definition
-thromboembolism
-cardiovascular risk (esp. in smokers)
-hypertension

-nausea
-headache/worsening of migraine
-edema (bloating)
-breast tenderness or "fullness"
-cancer?
Term
Why is thromboembolism a side effect of OCs?
Definition
due to effect of estrogens on clotting factors
Term
Why is cardiovascular risk increased with the use of OCs?
Definition
may be related to the effect of estrogens on clotting as well as effects of grogestagens (particularly norethindrone) on HDL
Term
Why can hypertension occur when taking OCs?
Definition
related to increased levels of renin substrate and sodium retention
Term
OC side effects associated with progestin
Definition
-cardiovascular disease
-stroke
-increased appetite
-weight gain (may be more prevalent with angdrogenic progestins)
-fatigue
-depression
Term
Why can OCs cause depression?
Definition
may be related to the ratio of progesterone to estrogen
Term
Progestins can increase ______ in certain individuals.
Definition
blood pressure
Term
What effect might the more androgenic progestin have on HDL?
Definition
reduce HDL levels
Term
OC contraindications
Definition
pregnancy
hx of estrogen-dependent cancer
hx of breast cancer
thromboembolic disorder
liver disease
heavy smokers (esp. >35)
Term
Plan B
Definition
levonorgestrel

unlikely to work if fertilized egg has already implanted
Term
RU486 (mifepristone)
Definition
luteolytic effect

usually combined with prostaglandin (such as mioprostol, an analog of PGE1)
Term
diethylstilbestrol (DES)
Definition
post-coital contraceptive

may interfere with the "timing" of uterine maturation
Term
female hormone therapy uses
Definition
-menopausal symptoms
-reducing risk of osteoporosis
-primary hypogonadism
-hypopituitarism
Term
male hormone therapy uses
Definition
-andropause ("male menopause")
Term
treatment of menopause
Definition
replace with low dose estrogen and a progestin (esp. in women with intact uterus)
Term
Premarin
Definition
conjugated equine estrogen (CEE)
Term
Provera
Definition
medroxyprogesterone
used to treat menopause
Term
PremPro
Definition
CEE + MPA
used to treat menopause
Term
PremPhase
Definition
CEE + phasic replacement of progestin
Term
estradiol cypionate
Definition
estrogen conjugate given IM once a month
Term
Estraderm
Definition
estradiol patch
Term
When are progestins given for women undergoing hormone therapy?
Definition
last 10-14 days of each month to prevent possibility of estrogen-induced endometrial and uterine cancer
Term
HT benefits
Definition
-possibly reduces incidence of MI and stroke in women by 40-50%
-reduces hot flashes
-decreases loss of bone (inhibits osteoclasts)
Term
Why is compliance often poor with HT in women?
Definition
cyclical bleeding associated with sequential therapy

fear of cancer
Term
adverse effects associated with estrogen therapy
Definition
-post-menopausal uterine bleeding
-nausea
-breast tenderness
-hyperpigmentation
-increased frequency of migraines
-cancer (although some can be reduced with combined progestin/estrogen therapy)
Term
hormone therapy contraindications
Definition
-pregnancy
-hx of estrogen-dependent cancer
-hx of breast cancer
-thromboembolic disorder
-liver disease
-heavy smokers (CV risk)
Term
Why is the route of administration important?
Definition
oral--large first pass effect
transdermal--less first pass effect
local--fewer side effects, reduced first pass effect
Term
advantages of transdermal estradiol vs. oral CEE preparations
Definition
-reduced conversion of estradiol (E2) to estrone (E1)
-no effect on SHBG
-little to no thromboembolic risk
Term
What is one advantage that oral CEE preparations may have over transdermal preparations?
Definition
transdermal estradiol may not have the same benefits on serum lipid profiles as oral preparations

(but no negative effects of transdermal E2 on lipid profiles have been reported)
Term
androgen therapy uses
Definition
-hypogonadal men
-anabolic agent to reverse atrophy following trauma, surgery, or debilitating diseases
-anemia
-osteoporosis (usuall in conjuction with estrogens)
Term
adverse effects of androgen therapy
Definition
-masculinizing effects
-gynecomastia in males
-hirsutism
-acne
-hepatic dysfunction
-azoospermia
-abuse (athletes)
Term
androgen therapy contraindications
Definition
-pregnant women
-men with hx of prostate or breast cancer
Term
What does the WHI study suggest?
Definition
women over 65 should not take HT
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