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
Q

Mifepristone (Mifeprex): ADR

A

Risk of serious complications including bleeding and bacterial infections

ONLY available through restricted access program

26
Q

Progesterone: monitoring

A
  • Depression
  • Increased risk of seizures
  • In DM, monitor blood glucose
27
Q

Physiology of normal menstrual cycle

A

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
Q

Phases of menstrual cycle

  1. Follicular phase
  2. Ovulatory phase
  3. Luteal phase
  4. Menstrual
A

FSH stimulates several follicles to develop

Dominant follicle synthesizes enough estradiol to create negative feedback which decreases FSH levels

29
Q

Phases of menstrual cycle

  1. Follicular phase
  2. Ovulatory phase
  3. Luteal phase
  4. Menstrual
A

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
Q

Phases of menstrual cycle

  1. Follicular phase
  2. Ovulatory phase
  3. Luteal phase
  4. Menstrual
A

Progesterone prevents new follicle development as well as differentiation of endometrium

If there is no pregnancy, the corpus luteum degenerates –> menstrual bleeding

31
Q

Estrogen and progesterones: effect

A
  • Increases body temperature and insulin levels
  • May depress the CNS
32
Q

Mechanisms of pregnancy prevention: progestin

A
  • Primarily responsible for the contraceptive effect
  • Exhibit a negative effect in the hypothalamic-pituitary-ovarian axis
  • Cause atrophy of the endometrium, preventing implantation
33
Q

Noncontraceptive benefits

A
  • 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
Q

Injectable progestins: Depot medroxyprogesterone acetate (Depo-Provera)

A
  • 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
Q

Intrauterine progestin: patient education

A
  • 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
Q

Progestin implants

A

Provides contraception for up to 3 years

37
Q

Emergency contraception: patient education

A
  • Should be implemented asap (<72 hours) after unprotected intercourse
  • Methods include:
    • Combined OCs
    • Progestin only (Plan B and Next Choice)
    • Copper IUD