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Pharmacology > Estrogens, Progestins, and Androgens > Flashcards

Estrogens, Progestins, and Androgens Flashcards

1
Q

Ovulation inducers (anti-estrogens) indication:

A
  • Women with anovulatory cycles (unable to release egg)

- Women with PCOS

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2
Q

Name 2 drugs that are ovulation inducers:

A

1) Clomiphene citrate (SERM)

2) Letrozole (aromatase inhibitor) - off label use

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3
Q

Clomiphene citrate MOA:

A

1) Competitively inhibits estrogen receptors in hypothalamus
2) Negative estrogen feedback inhibited
3) Increased GnRH secretion, which results in FSH and LH release
4) Ovarian follicles grow at next ovulation (agonist in ovaries, but antagonist in hypothalamus)

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4
Q

Letrozole MOA:

A

1) Blocks conversion of testosterone and androstenedione to E2 and E1
2) Decrease negative estrogenic feedback at pituitary
3) Increased FSH release

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5
Q

Name a gonadotropin release hormone agonist:

A

Leuprolide acetate (lupron depot)

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6
Q

Leuprolide acetate indication:

A

1) Endometriosis
2) Uterine fibroids
3) Advanced prostate cancer

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7
Q

Leuprolide acetate MOA:

A

1) Agonizes pituitary GnRH receptors, interrupting its pulsatile stimulation
2) FSH and LH release inhibited
3) Ovarian estrogen and testicular testosterone production reduced (via receptor desensitization)

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8
Q

Leuprolide acetate AE:1

A

1) Menopausal sx (eg: hot flashes) - management: ltx with low dose estrogen

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9
Q

Vaginal estrogen therapies indication:

A

Local treatment of urogenital atrophy due to low estrogen levels - quickly restores urogenital health within 3 months

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10
Q

If woman is still experiencing vaginal sx after vaginal estrogen tx, what other therapy can be initiated?

A

Low dose systemic hormone therapy can be used at the same time

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11
Q

Are progestogens necessary with low dose vaginal txs?

A

No. (Only needed if systemic hormone therapy is also being used)

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12
Q

Estrogen acts as agonist in which tissues?

A

Breast, endometrium, bone (strong agonist)

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13
Q

Tamoxifen (breast cancer tx) acts as an agonist in which tissues?

A

Endometrium, bone (weak agonist)

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14
Q

Tamoxifen acts an antagonist in which tissue?

A

Breast

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15
Q

Raloxifene (used in osteoporosis tx) acts as an agonist in which tissue?

A

Bone (fair agonist)

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16
Q

Raloxifine acts as an antagonist in which tissues?

A

Breast, endometrium

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17
Q

Name a selective progestin receptor modulator (sprm):

A

Ulipristal acetate

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18
Q

Ulipristal acetate indication:

A

Moderate to severe sx of uterine fibroids in women eligible for surgery

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19
Q

Ulipristal acetate MOA:

A

1) Prevents progesterone from binding to the progesterone receptor (directly affects endometrium and fibroids)
2) Inhibits cell division and induces apoptosis, thereby decreasing size of uterine fibroids –> decreased bleeding and pain

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20
Q

What benefit does ulipristal acetate have over leuprolide acetate?

A

Less vasomotor SEs

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21
Q

What is the role of LH in male reproductive physiology?

A

LH interacts with receptors in testes Leydig cells to enhance testosterone synthesis

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22
Q

What is the role of FSH in male reproductive physiology?

A

1) Act on receptors in testes stroll cells to regulate spermatogenesis
2) Enhances synthesis of aromatase enzyme (converts testosterone to E2) and androgen binding protein

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23
Q

The amount of LH and FSH released depends on what?

A

1) How often and how strong GnRH pulses occur

2) How responsive the pituitary is to GnRH

24
Q

Are most of the testosterone in plasma bound or unbound?

A

Bound (to SHBG and albumin)

25
Q

What is testosterone’s role in male reproductive physiology?

A

1) Development and maintenance of secondary sex characteristics
2) Sex organ maturation
3) Voice deepening
4) Facial and body hair
5) Increase in lean body mass and decrease in fat mass
6) Skeletal growth
7) Behaviour changes

26
Q

Where does dihydrotestosterone (testosterone metabolite) act?

A

External genitalia (has higher affinity for androgen receptors than testosterone)

27
Q

What is estrogen’s role in male reproductive physiology?

A

1) Bone integrity
2) Normal sexual function (libido and erectile function)
3) Decreased body fat

28
Q

What are 6 sx of androgen deficiency?

A

1) Low libido
2) Decreased morning erections
3) Small testes
4) Gynecomastia
5) Body hair loss
6) Low BMD

29
Q

Androgen therapy indication:

A

1) Male hypogonadism

2) Off label: hypoactive sexual desire disorder in women (at 1/10 doses used for males)**

30
Q

What is hypogonadism?

A

A decrease in sperm or testosterone production

31
Q

What is primary and secondary hypogonadism a result of?

A

Primary: Testes disease
Secondary: Pituitary or hypothalamus disease

32
Q

What are 3 androgen therapies?

A

1) Oral testosterone (Andriol) - poor BA
2) Testosterone IM INJ (Cypionate or Enanthate) - long acting
3) Testosterone transdermal gels (Testim or Androgel)

33
Q

Describe the effects each androgen therapy has on plasma testosterone levels:

A

Andriol: suboptimal levels
IM INJ: fluctuating levels (initial elevation, then decline to hypogonadal levels)
Transdermal gel: steady levels for ≥ 24 hours

34
Q

What is an AE with long-term use of testosterone IM INJ?

A

Hepatic adenomas (benign liver tumour)

35
Q

Name 2 5-alpha reductase inhibitors (5API) :

A

1) Finasteride

2) Dutasteride

36
Q

5API MOA:

A

5-alpha reductase inhibitor - blocks conversion of testosterone to dihydrotestosterone –> decrease size and growth of prostate (improves urinary flow rate and decreases urinary retention)

37
Q

5API indication:

A

Benign prostatic hypertrophy

38
Q

5API SEs:

A

Sexual dysfunction (decreased libido and erectile problems)

39
Q

Name 2 non-steroidal androgens:

A

1) Flutamide

2) Bicalutamide

40
Q

Non-steroidal androgens MOA:

A

Inhibits androgen uptake/androgen binding

41
Q

Non-steroidal androgens indication:

A

Metastatic prostate cancer

42
Q

Cyproterone acetate MOA:

A
  • Steroid with antiandrogenic, antigonadotropic, and progestin-like activity
  • Blocks dihydrotestosterone binding to prostatic cancer cells
  • Inhibits LH secretin –> Decreases testosterone production
43
Q

Anabolic steroids

A

Slides 47-48

44
Q

What is premature menopause?

A

12 months of amonnorhea before the age of 40. needs hormone tx until age of 51 to protect woman’s cardiovascular system, bones, and brain.

45
Q

What are 2 sx of menopause?

A

1) Vasomotor (hot flashes, night sweats)

2) Increased sensitivity to core body temp changes

46
Q

Why are symptomatic menopausal women more sensitive to core body temp changes?

A

Bc their thermoneutral zone is smaller (hypothesis of theromoregulatory dysfunctions: core body temp thresholds)

47
Q

When is systemic hormone tx for menopause most effective?

A

It most effective when started within 10 years of menopause onset and woman is ≤ 60 y/o

48
Q

Which estrogens are commonly used for menopause VMS?

A

1) 17-B estradiol

2) oral conjugated estrogens

49
Q

Which progestogens are commonly used for menopause VMS?

A

1) micronized progesterone

2) medroxyprogesterone acetate

50
Q

When is progestogens required for menopause VMS?

A

It is required with systemic estrogen tx if uterus is intact (to prevent hyperplasia and possible uterine cancer)

51
Q

What are 2 different regimens to follow for menopause systemic hormone therapy?

A

1) Continuous regimen: hormones are given ctsly (associated with unpredictable spotting possible for 6-9 months and amenorrhea)
2) Sequential regimen: estrogen is given ctsly, but progestogen is given in pulses for 10-12 days/month (associated with predictable spotting)

52
Q

What is the narrowing of the thermoneutral zone associated with?

A

Elevated sympathetic activation via alpha-2 adrenergic receptors

53
Q

What is the most effective tx of menopausal sx?

A

Exogenous estrogens (bc widens thermoneutral zone)

54
Q

For how long can a symptomatic menopausal woman use systemic hormone therapy?

A

Hormone therapy is safe to use at lowest effective dose for as long as sx persists

55
Q

Which therapy is preferred for symptomatic menopausal women ≥ 60 y/o?

A

Transdermal estrogen bc it is associated with reduced risk of VTE and stroke

Pharmacology (9 decks)

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