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Pharm exam 4 > Estrogen and Progestins > Flashcards

Estrogen and Progestins Flashcards

1
Q

what progestin is progesterone derived? (others are 19-nor cmds)

A

medroxyprogesterone acetate (MPA)

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2
Q

what are the estrogen drugs

A

conjugated equine estrogens

diethylstilbestrol

estradiol

ethinyl estradiol

mestranol

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3
Q

what cells are required for estradiol synthesis

A

theca and granulosa

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4
Q

when does positive feedback from estrogen and progesterone occur? (otherwise its negative feedback)

A

mid-ovarian cycle (day 14) - induces ovulation

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5
Q

what phase is estrogen first synthesized? when is this phase?

A

follicular phase

  • first 1/2 (days 1-13)
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6
Q

what induces ovulation

A

LH and FSH spike (day 14)

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7
Q

what phase is estrogen and progesterone synthesized

A

Luteal phase

2nd half (15-28 day)

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8
Q

what promotes proliferation of endometrial cells

A

estrogen

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9
Q

what promotes differentiation of the endometrium and supports implantation and decreases uterine contractions

A

progesterone

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10
Q

when does estrogen peak

A

day 11-13 –> causes LH surge

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11
Q

when does progesterone peak

A

luteal phase

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12
Q

natural water-soluble estrogen sulfate

A

conjugated equine estrogens

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13
Q

synthetic steroid estrogens

chemically modified estradiol

A

ethinyl estradiol

mestranol

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14
Q

1st synthetic non steroidal estrogen

A

DES

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15
Q

how can estrogen be used for hypogonadism

A

promotes development of ovaries, fallopian tubes, uterus, vagina, breasts

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16
Q

how can estrogen be used as a hormone replacement therapy

A

Target HPG axis and endometrium

Metabolic effects:
-bone: antiresorptive

Development:
- ovaries, fallopian tubes, uterus, vagina, breast

*decrease bone resorption/vasomotor sx/urogenital atrophy

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17
Q

what are risk of using hormone replacement therapy

A

Coronary heart disease

Stroke

PE

invasive breast cancer

decreases: colorectal cancer, hip fractures

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18
Q

how can estrogen be used to prevent contraception

A

Negative feedback pressure on HPG axis - suppression of LH/FSH surge

  • inhibit ovulation
19
Q

How can estrogen be used for acne tx

A
  • may suppress steroidogenesis
  • increase SHBG production by liver and decrease free testosterone concentrations
  • Liver: increase plasma proteins
20
Q

Adverse effects of estrogen are related to what physiological effects?

A
  1. breast tenderness
  2. endometrial hyperplasia
  3. increased blood coagulation
  • endometrial proliferation
  • blood: increase expression of coag factros, decreases AT
  • development: breast
21
Q

other SE of estrogen

A
  • Nausea
  • cholestasis
  • migraine (sign of altered blood coag)
  • cancer (endometrial and breast)
  • bloating (loss of intravascular fluid)
22
Q

HRT combination therapy has an increase risk of what cancer

A

invasive break canser (likely due to progestin not estrogen)

23
Q

HRT estrogen monotherapy has increase risk of what cancer (only do if someone had a hysterectomy or early on during hypogonadism)

A

endometrial

24
Q

contraceptive therapy has a reduced risk for what cancers

A

ovarian and endometrial cancer

25
Q

Progestin that is commonly combined with estrogen for HRT

used as a long acting contraceptive

A

medroxyprogesterone (MPA)

26
Q

combinational or progestine only hormone cnotraception

19-nortestosterone derivative

A

norgesterel

norethindrone

27
Q

how can progesterone be used as a contraceptive agent (alone or in combo)

A

negative feedback on HPG axis (steoidgenesis and ovulation)

increase cervical mucous viscosity

28
Q

How can progestins be used as HRT

A

***decrease risk of endometrial hyperplasia cuased by estrogens

29
Q

How can progestins be used for dysmenorrhea

A

UTerus smooth muscle:

  • decrease uterine contractions
  • decrease prostaglandin production
  • decrease endometrial mass
30
Q

how can progestins be used for endometriosis

A
  • decrease endometrial proliferation by regulating ER expression

and stimulating differentiation of endometrial cells.

31
Q

SE of progestin related to key physiological effects

A
  1. breakthrough bleeding
  2. impaired glucose tolerance
    - increase fasting glucose levels
  3. change in lipid metabolism
    - Lipids: increase LDL, increase fat deposition
32
Q

other important SE related to 19-nortestosterone effects

A
  1. acne

2. hirsutism

33
Q

how does estrogen effect lipids

A

decrease LDL

increase HDL

increase TG

34
Q

MOA of BC

A
  1. inhibit ovulation
  2. inhibit follicle develoment
  3. disrupt normal endometrial growth and development
  4. change viscosity of cervical mucus
35
Q

what type of oral use and parenteral use does progesterone only BC have

A

oral: monophasic, emergency
parenteral: injectable, implantable

36
Q

what type of oral use and parenteral use does combined BC have

A

Oral: monophase, multiphasic, extended, emergency

parenteral: transdermal, injectable

37
Q

what is postcoital BC

A

emergency

38
Q

what percent of expected pregnancies were prevented when taken within 72 hours of intercourse

A

50%

39
Q

when are you most loikely to get pregnant

A

1-2 days before ovulation (30%)

40
Q

Contraindications for estrogen containing contraceptives

A
  1. known or suspect breast cancer or cancer of female reproctive tract (reduce risk of ovarian and endometrial cancer)
  2. Thromboembolitic disorders
  3. Liver disease
  4. history of CV disease
  5. Smokers 35 y/o or older
41
Q

what drug interactions do estrogen containing BC have?

A
  1. HIV agents, anticonvulsants and St. John’s wort induce hromone metabolism
  2. antibiotics lower contraceptive effectiveness
42
Q

what is the most effective BC

A

Implanon = 0.05

combo oral contraception

43
Q

describe the difference in T1/2 of estradiol and estradiol ethinyl

A

Estradiol ethinyl = longer

decreases 1st pass effect

Pharm exam 4 (15 decks)

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