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Pharmacotherapeutics for the Advanced Practice Nurse > Estrogens and Progestins/Oral Contraceptives > Flashcards

Estrogens and Progestins/Oral Contraceptives Flashcards

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1
Q

Where are normal/endogenous progestins produced?

A

ovaries

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2
Q

What is the endogenous form of estrogen?

A

estradiol

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3
Q

What is the endogenous form of progestin?

A

progesterone

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4
Q

When is the follicular phase and what happens?

A

first half; 1-14 days
Ovaries: Ovarian follicles ripen, one mature one ruptures causing ovulation. Estrogens are secreted by maturing ovarian follicles causing endometrium changes
Uterus: endometrium prepares for nidation (implantation) by increasing in thickness and vascularity
FSH acts on developing ovarian follicles and helps them mature to produce estrogen

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5
Q

When is the ovulation phase and what happens?

A

Mid cycle

LH levels rise causing dominant folic to swell, burst, and release ovum

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6
Q

When is the luteal phase and what happens?

A

Second half; 15-28ish days
Ovaries: ruptured follicle evolves into corpus luteum where estrogen and progesterone are produced
Uterus: after ovulation the uterus continues its preparation by increasing secretory activity
If fertilization/implantation does not occur, the corpus luteum atrophies and the thickened endometrium breaks down causing menstruation

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7
Q

Therapeutic use of exogenous estrogens for non-contraceptive use(5):

A

1) menopausal hormone therapy: most common. usually accompanied with use of progestin.
2) female hypoginadadism: d/t ovarian failure, hypopituitarism, bilateral oophorectomy, turner syndrome (to promote breast development, mature reproductive organs, develop pubic hair, estrogen secretion)
3) acne: oral contraceptives
4) cancer: management of advanced prostate and some metastatic breast cancers
5) gender affirmation therapy for transgender women

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8
Q

Adverse effects of exogenous estrogen therapy:

A
  • potential for endometrial hyperplasia/cancer, breast cancer, blood clots
  • gallbladder dz, jaundice, HA/migraine
  • fluid retention
  • cholasma (patchy brown facial discoloration)
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9
Q

contraindications of exogenous estrogen therapy:

A
  • hx of DVT, PE, stroke, MI
  • pregnant
  • vaginal bleeding with unknown cause
  • hx of liver dz, estrogen-dependent tumors, breast cancer, usually
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10
Q

interactions of exogenous estrogen therapy:

A
  • CYP34A/CYP1A2 inducers can lower estrogen levels. Inhibitors raise levels.
  • May decrease effectiveness of anti-diabetic drugs and thyroid preparations
  • can interacts with coags
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11
Q

preparations for exogenous estrogen therapy:

A

esterified form: plant based

synthetic conjugated: urine of pregnant horses

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12
Q

route of administration for exogenous estrogen therapy:

A

oral: estradiol available alone or in combo
transdermal: emulsions, spray, gels, patches
intravaginal: inserts, creams, vaginal rings
parenteral: IV/IM. IV rarely used, mostly for emergency control of heavy uterine bleeding

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13
Q

advantages of transdermal compared to oral for exogenous estrogen therapy:

A

transdermal total dose is greatly reduced because liver is bypassed, less N/V, blood levels of estrogen fluctuate less, lower risk for DVT, PE, CVA

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14
Q

patient education for for exogenous estrogen therapy:

A

transdermal patch: apply to C/D/I skin by pressing in place for 10sec. If it falls off, put it back on or replace. Remove old and replace with new 1-2x/week according to directions. Rotate site so not used more than 1x/week
transdermal emulsion: apply each morning to indicated location
transdermal gel: apply after showering to location indicated
transdermal spray: 1,2,or 3 sprays daily. Let dry for 2mins b4 dressing/30mins b4 washing
intravaginal cream: apply high in vagina at bedtime using applicator
intravaginal ring: insert as deeply as possible, leave in place for 3 most, remove and replace
intravaginal insert: 1 daily for 2 weeks, following by 1 2x/week after. Place as deeply as possible with applicator

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15
Q

prescribing considerations for for exogenous estrogen therapy:

A
  • baseline data (HR, BP, weight, pregnancy test, TSH, lipid panel, screen for breast cancer and CVD)
  • monitor BP and weight, triglycerides, TSH if patient on thyroid replacement as well. routine breast/pelvic exams. -endometrial biopsy for bleeding that continues for 6 mos
  • high risk patients= do not prescribe: abnormal vaginal bleeding, estrogen-dependint cancer, hx of DVT/PE/CVA/MI, abnormal LFTs, pregnancy
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16
Q

SERMs purpose

A

created to receive benefits of estrogen while avoiding drawbacks

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17
Q

Tamoxifen purpose:

A

can inhibit cell growth in the breast, used to prevent and treat breast cancer
also protects against osteoporosis and favorable effect on lipids

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18
Q

Tamoxifen SE:

A

produces hot flashes, increases risk for endometrial cancer and blood clots

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19
Q

Raloxifene differences from Tamoxifen:

A

does not activate ERs in endometrium so no increased risk for uterine cancer
approved only for prevention and treatment of osteoporosis and prevent of breast cancer in high-risk women

20
Q

Duavee purpose:

A

reduces risk for excessive growth of uterine lining
prevents vasomotor symptoms and osteoporosis in postmenopausal women WITH a uterus
contraindications are same as exogenous estrogen

21
Q

Progestin MOA:

A
  • receptors are found in cell nucleus
  • must diffuse across the cell membrane, migrate to the nucleus and bind with a progesterone receptor (PR)
  • PR complex binds with a progesterone regulatory element on a target gene
  • PR-A: inhibitory actions
  • PR-B: stimulatory actions
22
Q

Therapeutic uses for progestin:

A
  • menopausal HT (or hormone replacement therapy)
  • dysfunctional uterine bleeding
  • amenorrhea
  • endometrial hyperplasia and carcinoma: can suppress hyperplasia, preventing cancer
  • supporting early pregnancy and preterm birth
23
Q

Adverse effects of progestin:

A
  • 20% of patients experience breast tenderness, HA, and discomfort, arthralgia, depression
  • when used for BC: spotting, breakthrough bleeding, irregular menses
  • in combo with estrogen: increased risk for breast cancer in postmenopausal women
24
Q

Routes of administration of progestin:

A
  • oral
  • IM
  • SQ
  • Vaginal insert
  • Transdermal
25
Q

Prescribing considerations of progestin:

A

same for estrogen

26
Q

Menopausal hormone therapy, drugs used:

A

Estrogen alone (ET) or estrogen plus progestin (EPT)

  • progestin present to combat negative effects of estrogen
  • do not use progestin in women with hysterectomy
27
Q

3 primary medical benefits for Menopausal hormone therapy:

A

1) suppression of vasomotor symptoms
2) prevention of urogenital atrophy
3) prevention of osteoporosis/fracture

28
Q

Pregnant women considerations for estrogen and progestin:

A

estrogens contraindicated during pregnancy

high dose therapy of progestins during first 4 months of pregnancy assoc. with increased incidence of birth defects

29
Q

Breast-feeding considerations for estrogen and progestin:

A

estrogens can affect infant development and may decrease quality of milk produced
progestins contribute to neonatal jaundice

30
Q

Flibanserin- indications and adverse effects

A
  • for women with low libido not assoc. with medical/mental health problem, relationship issues, med side effects
  • d/c if no improvement within 8 weeks
  • serious risks: CNS depression, hypotension w/ or w/out syncope
  • only available through REMS
31
Q

Bremelanotide- indications and adverse effects

A

-activates melanocortin receptors; MOA for improving sexual desire is unknown
-SubQ injection 45 mins b4 sexual activity. One dose in 24hrs max, no more than 8/month.
SE: N/V, HA, transient rise in BP 12hrs after taking, uncommonly has caused darkening of gums and portions of skin

32
Q

Most effective vs least effective forms of BC:

A

most effective: nexplanon, IUD, sterlization

least effective: barriers, periodic abstinence, spermicides withdrawal

33
Q

combination BC MOA:

A

estrogen inhibits follicular maturation while progestin acts in hypothalamus and pituitary to suppress LH surge which would normally cause ovulation. Also thickens cervical mucus to create a barrier to the penetration of sperm and alteration of endometrium making it less hospitable

34
Q

Women of higher weight have less effectiveness with combination oral BC- true or false

A

True

35
Q

Absolute contraindications vs relative contraindications of combination oral BC:

A 
ABSOLUTE:
-blood clots
-CVA
-coronary occlusion
-abnormal liver fxn
-breast cancer
-undiagnosed bleeding
-suspected/known pregnancy
-smokers older than 35
RELATIVE:
-HTN
-DM
-cholestatic jaundice of pregnancy 
-gallbladder dz
-uterine leiomyoma 
-epilepsy
-migraines
36
Q

For women that experience acne and hirtuism switch to:

A

drospirenone or dienogest

37
Q

For women that have DM switch to:

A

desogestrel or norgestimate

38
Q

Drugs whose effects can be reduced by OC:

A

decrease benefits of warfarin and hypoglycemic agents, increases levels of clotting factors and increases BG `

39
Q

Drugs whose effects are increased by OC:

A

theophylline, tricyclic anti-depressants, diazepam, chlordiazepoxide and can lead to toxic levels of these in the system

40
Q

What do you do if one or more pills are missed in the first week of OC?

A

take pill ASAP and continue with pack, use another form BC for 7 days

41
Q

What do you do if one of pills missed in 2-3week of OC:

A

take one pill ASAP and continue with active pills, skip placebo pills and go straight to new pack

42
Q

What do you do if three of pills missed in 2-3week of OC:

A

follow instructions for 1 pill missed and used another form of contraceptive for 7 days

43
Q

Dienogest and drospirenone:

A

greater risk for thrombosis. low risk for acne and hirtuism. risk for hyperkalemia

44
Q

Progestin only OC:

A
  • know as “mini pills” and do not cause thromboembolic events
  • less effective and need to be taken at the same time every day
  • use backup contractive if not taken same time every day and 7 days after starting
45
Q

Interactions with nexplanon:

A

Barbiturates, phenytoin, rifampin, carbamazepine, topiratame, HIV protease inhibitors, St. John’s wart- all reduce efficacy

46
Q

Considered good option for breastfeeding:

A

nexplanon after 21 days postpartum

47
Q

Contraindications of mifepristone with misoprostol:

A

ectopic pregnancy, hemorrhagic disorders, use of anticoagulants, adrenal insufficiency, long-term glucocorticoid therapy

Pharmacotherapeutics for the Advanced Practice Nurse (12 decks)

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