Hormones KC Flashcards
Indications for estrogen
- contraception
- menopausal hormone replacement
- endometriosis
- dysfunctional uterine bleeding
- urogenital atrophy
- infertility
- PCOS (w/ progesterone)
Estrogen CIs
- Liver disease
- hypercoagulable states
- cancer - breast, ovarian, uterine, endometrial
- Strong risk factors for atherosclerosis (HTN, DM, high cholesterol, strong FMHx of stroke, MI)
Estrogen MOA
helps modulate the pituitary secretion of gonadotropins, LH and FSH
Estrogen S/E
- migraines
- water retention, bloating
- weight gain
- stimulates reproductive organ tissues - vaginal bleeding/spotting, enlarge fibroids (pelvic cramping), breast tenderness
- gallbladder disease
- nausea
- thrombosis
- skin rashes
- increased triglycerides
special consideration for postmenopausal woman with uterus who is initiating estrogen therapy
must coadminister progesterone - interrupts proliferative process of endometrium and decreases risk of endometrial cancer
Indications for progestins
- contraception
- menopausal hormone therapy replacement
- decrease endometrial hyperplasia
- treatment for secondary amenorrhea
- emergency contraception (high dose)
- dysfunctional uterine bleeding
Progestin CI
- risks for DVT, PE
- unexplained vaginal bleeding
- breast cancer
- active liver disease
- conditions of concern for hypoestrogenic effects and reduced HDL (HTN, hx of ischemic heart disease, hx of stroke)
- diabetes >20 years or w/ neuropathy, retinopathy, nephropathy, or vascular disease
Progestin MOA
- inhibits pituitary gonadotropin release
- prevents follicular maturation
- transforms proliferative endometrium into secretory endometrium
- inhibits spontaneous uterine contractions
Generations of progestin agents and what they mean
first, second, third, fourth
based on degree of affinity for estrogen, androgen, and progesterone receptors
most androgenic progestin and what this means
Levonorgesterol
acne, hirsutism are most common side effects
Progestin S/E
- androgenic activity - acne, hirsutism, insulin resistance, increased LDL
- DVT
- vaginal bleeding/spotting
- weight gain
progestin good for women who complain about fluid retention or bloating with menstrual cycle
drospirenone
Routes of delivery for estrogen
- oral
- transdermal patch
- vaginal ring
- vaginal cream
routes of delivery for progestin
- oral
- IUD
- subcutaneous rods
- IM
routes of delivery for combination estrogen and progesterone
- oral
- transdermal patch
- vaginal ring
Schedule for PO progestin for birth control
don’t take week off, continuously take progesterone
benefits of IUDs
good for pts who cannot take estrogen but cannot tolerate or remember progesterone only pill
less side effects compared to PO
frequency of IM injections of progestin
every 3 months
benefits of transdermal patch
good for pts w/ GI issues because consistent levels compared to PO pill
how long does estrogen vaginal ring last?
90 days
benefits of estrogen vaginal ring
good for vaginal atrophy, urinary incontinence, symptoms related to menopause
how to use combination vaginal ring
for birth control only, left in for 3 weeks then take out 4th week
hormone options for contraception
- combination estrogen and progesterone
2. progesterone only
hormone options for hormone replacement therapy
- estrogen only (women w/o uterus)
- combination estrogen and progesterone (women w/ uterus)
- NOT progesterone alone
contraceptive options for combination estrogen and progesterone
- pill - monophasic, biphasic, triphasic
- nuvaring
- combipatch
contraceptive options for progesterone only
- depo provera injection
- IUD
- pill
- nexplanon, implanon
estrogen in contraception
ethinyl estradiol
types of progestin
- levonorgesterol
- norethindrone
- medroxyprogesterone
- norgestimate
- drospirenone
monophasic pill
same amount of ethinyl estradiol and progesterone for week 1, 2, 3 then take 4th week off
biphasic pill
same amount of ethinyl estradiol and progesterone for week 1, 2, 3 then 4th week has a little bit of estrogen
triphasic pill
same steady amount of ethinyl estradiol but levels of progesterone changes each week - tries to mimic body’s natural response
benefit of biphasic pills
prevent withdrawal - prevent headaches
benefit of triphasic pills
good for acne
typical dose of ethinyl estradiol you start someone at
10-25 mcg
Hormone contraception
- smoking (relatively if <35, definitely if >35)
- previous hx of DVT or PE
- familial factor V leiden
- 2 or more risk factors for cardiovascular disease (ie smoking, HTN, DM)
MOA hormone contraception
- suppress ovulation
- estrogen: suppression of production of FSH –> prevents follicle maturation
- progestin: prevent LH surge - changes endometrium making implantation less likely
- progestin makes lining inhospitable to implantation
- no thickening or uterine lining
- thickens cervical mucous
Hormone Contraception S/E
- breakthrough bleeding when OCP is started
- estrogen side effects
- progestin s/e - acne, hirsutism
what is extended cycle
continuous dosing, skipping placebo effect
monophasic pill
3 months of active pill, may have breakthrough bleeding so stop and have period then resume
specific s/e of extended cycle, progestin only, depo provera, morning after pill (hormone contraception)
extended cycle –> breakthrough bleeding, acne
progestin only –> breakthrough bleeding
depo provera –> decreased bone density (limit to 2 yrs)
morning after –> nausea
when OCPs are used properly, they prevent pregnancy ___% of the time
99
failure rate of OCPs
2-3%
Selective Estrogen Receptor Modulators examples
tamoxifen / Nalvadex
raloxifene / Evista
estrogen receptor antagonist example
Clomid / Clomiphene
SERM MOA
- estrogen agonist activity on bones and lipids
- estrogen antagonist effect on breast - block estrogen uptake in breast (tamoxifen)
- estrogen antagonist effect on breast and uterus (evista)
Indications for SERMs
- estrogen receptor positive breast cancer (tamoxifen)
- Prevention and treatment of osteoporosis in post menopausal women
- prevention of breast cancer in high risk women (raloxifene)
tamoxifen vs evista
tamoxifen does not block estrogen at uterus so can have stimulated endometrial growth and endometrial hyperplasia - requires endometrial screening
how long to give SERM
if low risk 5 years
if high risk 10 years
Clomid MOA
stimulates follicles to develop
SERMs CIs
pregnancy and lactation
history of thromboembolic events
SERMs S/E
- hot flashes
- nausea, vomiting
- menstrual irregularities
- endometrial effects (increased endometrial thickness, polyps, leiomyomas, cancer)
- thromboembolism
- stroke
Aromatase Inhibitors examples
anastrozole / arimidex
Letrozole / femara
Aromatase Inhibitors MOA
block the conversion of testosterone to estradiol and androstenedione into estrone (so no synthesis of estrogen)
Aromatase Inhibitors indications
- hormone-sensitive breast cancers in POST MENOPAUSAL WOMEN
- first-line therapy for metastatic breast cancer
- advanced therapy if treatment with tamoxifen fails and disease progression continues
Aromatase Inhibitors CIs
- pregnancy
- anastrozole not used in premenopausal women
- caution if renal insufficiency –> dose adjustment
Aromatase Inhibitors treatment timeframe
5 years if lower risk
Aromatase Inhibitors S/E
- reduced bone density and increased fractures
- hot flashes
- increased sweating
- nausea
- fatigue
- peripheral edema
- increased appetite
AIs vs. SERMs
estrogen metabolites reduced with AIs but not SERMS
SERMs will block exogenous estrogen but AIs won’t
oxytocin route of administration and half life
IV, SQ, 3 minutes
Oxytocin Indications
- induction of labor
- augmentation of labor
- prevention and treatment of postpartum bleeding
Oxytocin CIs
previous uterine rupture
anticipation of non-vaginal delivery
Oxytocin S/E
- hypotension with rapid administration (mom & baby)
- abnormally high uterine tone (uterine rupture)
- tachycardia
- premature ventricular contractions
