Week 11 - Progesterones Flashcards

1
Q

Role of progesterone in the body

A
  • Thins and stabilizes endometrium
  • Thickens cervical mucous
  • Relaxes smooth muscle of uterus
  • Thins vaginal mucosa
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2
Q

Progesterone: MOA

A
  • Thickening of cervical mucus to inhibit sperm migration
  • Suppresses ovulation
  • Lowers mid-cycle peak of FSH and LH
  • Slows egg movement through fallopian tube
  • Thins endometrium
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3
Q

Progestin-only therapy examples

A
  • Etonogestrel implant (Nexplanon)
  • Levonorgestrel-releasing intrauterine devices (IUDs; Mirena, Skyla)
  • Depot medroxyprogesterone (DMPA) injection (Depo-Provera)

Overall complication rates are LOW for all progestin-only methods

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4
Q

True/False: Progestin-only-pill doses are higher than doses in combined oral contraceptive (COCs)

A

False - doses are LOWER

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5
Q

Progestin-only-pills: norethindrone (Camila)

A

Administered continuously

Does not consistently suppress ovulation; approximately half of women ovulate

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6
Q

Progestin-only-pills: drospirenone (Slynd)

A

24 active and 4 inert tablets

Suppresses ovulation; antimineralcorticoid activity

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7
Q

Progesterone in contraception: cautions

A
  • If patient has acne, lower dose progesterone with less androgen effect
  • Overall effect of all COCs is anti-androgenic regardless of type of progestin
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8
Q

Names of progestin contraceptive pills with HIGH levels of activity

A
  • Norgestrel
  • Levonorgestrel
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9
Q

Progesterone in contraception: ADR

A
  • Irregular breakthrough bleeding
  • Breast tenderness
  • Galactorrhea
  • Nausea
  • Weight gain
  • Osteoporosis risk with 2+ year use
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10
Q

Progesterone in contraception: contraindications

A
  • Known or suspected pregnancy
  • Known or suspected breast cancer
  • Undiagnosed abnormal uterine bleeding
  • Benign or malignant liver tumors, cirrhosis, acute liver disease
  • Thromboembolic disease
  • Breast cancer
  • Depression
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11
Q

Combined oral contraceptives: drug interactions

A
  • Metabolism increased by any drug that increases liver microsomal enzyme activity
  • Efficacy diminished if concurrently taking a drug with this effect
  • Anticonvulsants
  • Gabapentin, levetiracetam, valproate, zonisamide DO NOT appear to reduce efficacy
  • Rifampin is the ONLY abx that reduces serum ethinyl estradiol and progestin levels
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12
Q

Progesterone in menopause: indications

A
  • Add progestin to MHT for women w/ uterus
    • Prevents uterine hyperplasia
  • NOT indicated in women who have undergone hysterectomy
  • NOT indicated in low-risk women on low dose vaginal estrogen
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13
Q

Progesterone in menopause: medroxyprogesterone acetate (MPA)

A
  • Prevents endometrial hyperplasia
  • Associated with increase risk of breast cancer, possibly coronary heart disease, and unfavorable effect on lipids
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14
Q

Progesterone in menopause: micronized progesterone

A
  • First line
  • Bioidentical, commonly prescribed
  • Protects endometrium
  • Minimal negative effect on lipids
  • No apparent increase to risk of breast cancer or coronary heart disease
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15
Q

Menopause hormone therapy (MHT)

  • Cyclic regimen
A
  • Natural progesterone (prometrium)
  • Days 1-14 of each calendar month
  • Given w/ continuous daily estrogen
  • Majority of women have monthly withdrawal bleeding
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16
Q

Menopause hormone therapy (MHT)

  • Continuous regimen
A
  • Estrogen and progestin are usually given as separate pills
  • Induces amenorrhea in most women
17
Q

Menopause hormone therapy (MHT)

  • Standard dose of estrogen
A
  • 17-beta estradiol 1mg oral
  • Transdermal estradiol 0.05mg
18
Q

Menopause hormone therapy (MHT)

  • Standard dose of progestin
A

Natural progesterone 100mg daily oral

19
Q

Combination estrogen-progestin products - oral options (progestins derived from testosterone)

A
  • Norethindrone
  • Norgestimate
  • Drospirenone (spironolactone derivative)
20
Q

Combination estrogen-progestin products - transdermal options (17-beta estradoil combined w/ progestin)

A
  • Norethindrone applied twice daily
  • Levonorgestrel applied once weekly
21
Q

What form of IUDs are not approved in the U.S. for endometrial protection in menopausal women on estrogen?

A

Levonorgestrel-releasing IUDs

  • Can be used off-label for women who cannot tolerate oral progestin
22
Q

Progesterone in menopause: ADR

A
  • Irregular bleeding
  • Bloating
  • Mood changes
23
Q

Progesterone antagonist: example

A

Mifepristone (Mifeprex, Korlym)

24
Q

Mifepristone (Mifeprex): indications

A
  • Termination of intrauterine pregnancy
  • Cushing syndrome
25
Mifepristone (Mifeprex): ADR
Risk of serious complications including bleeding and bacterial infections ONLY available through restricted access program
26
Progesterone: monitoring
* Depression * Increased risk of seizures * In DM, monitor blood glucose
27
Physiology of normal menstrual cycle
Menstrual cycle regulated by positive and negative feedback in hypothalamic-pituitary-ovarian axis GnRH from hypothalamus --\> FSH and LH from pituitary --\> secretion of estrogen and progesterone from ovary
28
Phases of menstrual cycle 1. **Follicular phase** 2. Ovulatory phase 3. Luteal phase 4. Menstrual
FSH stimulates several follicles to develop Dominant follicle synthesizes enough estradiol to create negative feedback which decreases FSH levels
29
Phases of menstrual cycle 1. Follicular phase 2. **Ovulatory phase** 3. Luteal phase 4. Menstrual
Estradiol levels peak and exert positive feedback to induce an **LH surge** --\> release of mature ovum Estrogen promotes proliferation of the endometrium and development of progesterone receptors in the endometrium
30
Phases of menstrual cycle 1. Follicular phase 2. Ovulatory phase 3. **Luteal phase** 4. Menstrual
Progesterone prevents new follicle development as well as differentiation of endometrium If there is no pregnancy, the corpus luteum degenerates --\> menstrual bleeding
31
Estrogen and **progesterones**: effect
* Increases body temperature and insulin levels * May depress the CNS
32
Mechanisms of pregnancy prevention: progestin
* Primarily responsible for the contraceptive effect * Exhibit a negative effect in the hypothalamic-pituitary-ovarian axis * Cause atrophy of the endometrium, preventing implantation
33
Noncontraceptive benefits
* Decreased dysmenorrhea, menstrual irregularities, menstrual blood loss * Lessening of acne and hirsutism * Fewer ovarian cysts * Reduced endometrial and ovarian cancer risk * Lower incidence of benign breast conditions such as fibrocystic changes and fibroadenoma * Reduced risk of hospitalization for gonorrheal PID * Suppression of endometriosis in women who do not currently desire pregnancy
34
Injectable progestins: Depot medroxyprogesterone acetate (Depo-Provera)
* Long acting * One injection is effective in suppressing ovulation for 12-13 weeks * Advantages * Once every 12 week dosing * Disadvantages * Spotting, followed by amenorrhea * **Black box warning**: decreased bone density with longer term use
35
Intrauterine progestin: patient education
* Can be left in place for 5 years * Small levels of systemic circulating hormone w/ minimal systemic side effects * Changes in menstrual bleeding, amenorrhea
36
Progestin implants
Provides contraception for up to 3 years
37
Emergency contraception: patient education
* Should be implemented asap (\<72 hours) after unprotected intercourse * Methods include: * Combined OCs * Progestin only (Plan B and Next Choice) * Copper IUD