Pharmacology of Sex Hormones Flashcards

1
Q

What are the female gonadal hormones?

A

Estrogen and Progesterone

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2
Q

What is the flow of the Hypothalamic Pituitary Gonadal Axis?

A

Hypothalamus = GnRH –> Pituitary = LH and FS –> Ovary = Inc or Dec Estrogen and Progesterone

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3
Q

What are the forms of Estrogen?

A

Estradiol E2 = ovaries
Estrone E1 = postmenopause
Estriol E3 = pregnancy

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4
Q

What is Progesterone?

A

Precursor for estrogen, androgen, and andrenocortical hormones

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5
Q

What is the Follicular Phase?

A

Development of the follicle

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6
Q

What is the Luteal Phase?

A

After ovulation until menstruation or fertilization

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7
Q

Testosterone is the precursor to what?

A

Estrogens via Aromatase Conversion

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8
Q

Sex Hormones are bound to what to travel across membranes as lipids?

A

SHBG

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9
Q

Where are steroid binding receptors found?

A

Cytoplasm, CYTOPLASMIC not cell surface

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10
Q

What are the physiological roles of estrogens?

A
  1. Females sexual maturation
  2. Menstruation the building up of endometrium
  3. CV protection
  4. Increased blood clotting
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11
Q

What are the pharmacological uses for estrogens?

A
  1. Contraception
  2. Hypogonadism
  3. Hormone Replacement postmenopause
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12
Q

What are the adverse effects of estrogens/

A
  1. Uterine bleeding
  2. Cancer risks
  3. Nausea
  4. Breast tenderness
  5. Migraine/HA
  6. Gallbladder malfunction
  7. HTN
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13
Q

What produces progesterone?

A

Corpus Luteum
Embyro/Placenta

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14
Q

What produces estrogen?

A

Ovaries
Developing Follicle
Corpus Luteum

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15
Q

What are the physiological roles of progestin?

A
  1. Endometrial changes following ovulation (secretory)
  2. Stimulates lipoprotein lipase and favors dat deposition
  3. Increases basal insulin
  4. Increase sodium reabsorption
  5. Increases body temp
  6. Increases sensitivity to P(CO2)
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16
Q

What are the pharmacological uses of progestins?

A
  1. Hormone replacement postmenopause
  2. Contraception
  3. Delay premature labor
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17
Q

What are the adverse effects of progestins?

A
  1. Increase BP
  2. Lower HDL
  3. Edema due to sodium retention
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18
Q

What is the follicular phase?

A

Development of follicles in ovary

19
Q

What is ovulation?

A

LH Surge

20
Q

What is luteal phase?

A

Corpus luteum to pregnancy or menstruation

21
Q

What is menses?

A

Onset at drop in Progesterone

22
Q

What do Ovulation Predictor kits track?

A

Rise in LH
Can give up to 2 day warning

23
Q

What do Fertility Monitors track?

A

Rise in Estrogen and LH
Can give 2-4 days before LH peak

24
Q

What is essential for the maintenance of pregnancy?

A

Progesterone

25
Q

How long will the corpus luteum supplement progesterone?

A

10 weeks, corpus luteum is kept healthy by hCG
>10 wks placenta takes over

26
Q

What are the qualities of the progestin generations?

A

1st: Norethindrone Acetate
2nd: Norgestrel, Levongrestrel more androgen
3rd: Desogestrel, Norgestimate less androgen
4th: Drospirenone, Dienogest mineralocorticoid and low androgen

27
Q

What formulations are progestin only?

A

Norethindrone Acetate and Drospirenone

28
Q

What is the MOA for Combined Estrogen and Progestin?

A

INHIBIT OVULATION
Increase cervical mucus
Decrease endometrium lining
Decrease flow in fallopian tubes

29
Q

What is the MOA of Progestin Only?

A

May Inhibit Ovulation
Increase cervical mucus
Decrease endometrium
Decrease flow in fallopian

30
Q

What are the dose related A/E of Contraceptives?

A
  1. Cardiovascular (HTN, DVT, Stroke)
  2. Cancer
  3. Endo/Metabolic
  4. Migraines/HA
  5. Nausea
  6. Edema
  7. Weight Gain
31
Q

What are the endocrine and metabolic A/Es of contraceptives?

A

Fluid retention
Increase LDL and decrease HDL
Glucose
Acne or Hirsutism

32
Q

What are the Contraindications for Hormonal Contraceptives?

A
  1. Clotting history (estrogen only)
  2. Uncontrolled cholesterol/HTN
  3. Pregnancy
  4. Estrogen postive cancer
  5. Smokers
  6. Migraines
  7. Gallbladder
33
Q

What is the MOA of Emergency Contraception?

A

INHIBITS OVULATION

34
Q

What is Ulipristal Acetate (Ella) and its MOA?

A

EC, selective progesterone receptor modulator, partial agonist at PG receptors, weak antagonist at GC receptors

35
Q

What product is an Abortifacient and its MOA?

A

Mifepristone RU486
Progesterone receptor ANTAGONIST

36
Q

What do you use with Mifepristone RU486 to induce abortion?

A

Misoprostol, prostaglandin E1 analog

37
Q

What are there SERMS?

A

Tamoxifen
Raloxifene
Clomiphene

38
Q

What is the MOA of Tamoxifen?

A

Estrogen ANTAGONISST in breast, treats breast cancer

39
Q

What is the MOA of Raloxifene?

A

Estrogen AGONIST in bone, treats osteoporosis

40
Q

What is the MOA of Clomiphene?

A

Estrogen PARTIAL AGONIST, induces ovulation for infertility

41
Q

What SERMS are used for Menopause?

A

Ospemifene
Medroxyprogesterone
Estrogens

42
Q

Ospemifene is used for what?

A

AGONIST, for vaginal dryness

43
Q

Medroxyprogesterone is used for what?

A

Hyperplasia of endometrium

44
Q

Estrogens SERM is used for what?

A

Relieve VMS and Urogenital Atrophy