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Repro / GU > SM_223b: Reproductive Pharmacology > Flashcards

SM_223b: Reproductive Pharmacology Flashcards

1
Q

Describe the reproductive axis

A

Reproductive axis

  • Reproductive hormones: GnRH, gonadotropins, estrogen, progesterone, testosterone
  • Therapeutic applications: reproductive hormones for therapy, drugs that impact reproductive axis
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2
Q

Describe agonists

A

Agonist

  1. Binds receptor
  2. Physiological conformational change
  3. Hormone-like physiologic response
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3
Q

Describe antagonists

A

Antagonist

  1. Binds receptor
  2. Non-physiological conformational change
  3. No physiologic response
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4
Q

Describe selective receptor modulators

A

Selective receptor modulators

  • Tissue-specific agonist or antagonist activity
  • Mechanisms: differential expression of receptor in target tissues, differential conformational shape with receptor binding, and differential expression of co-regulators in target tissues
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5
Q

Describe different conformational shapes in binding to the ER

A

Different conformational shapes in binding to the ER

  • ER + estradiol: gene transcription ON
  • ER + raloxifene: gene transcription OFF
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6
Q

SERMs activate ____ and ____

A

SERMs activate co-repressors and co-activators

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7
Q

Describe enzyme inhibitors

A

Enzyme inhibitors

  • Testosterone (biosynthetic pathways): estradiol is a potent estrogen, dihydrotestosterone is a potent androgen
  • 5-alpha reductase converts testosterone to dihydrotestosterone, hair follicles in male genitalia
  • Aromatase converts androgens to estrogens, in ovary / brain / bone / liver / fat
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8
Q

Prolactin ___ the reproductive axis

A

Prolactin inhibits the reproductive axis

  • Decreased GnRH pulses
  • Inhibits LH: no ovulation, inadequate corpus luteum
  • Adaptive: avoid pregnancy while lactating
  • Treatment goal: decrease prolactin levels
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9
Q

Describe symptoms of hyperprolactinemia

A

Hyperprolactinemia

  • Women: galactorrhea, menstrual irregularity, infertility
  • Men: galactorrhea, impotence, visual field abnormalities, headache, extraocular muscle weakness, anterior pituitary malfunction
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10
Q

Dopamine is an endogenous prolactin ___

A

Dopamine is an endogenous prolactin inhibitor

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11
Q

Dopamine agonists (bromocriptine, cabergoline) ___ and ___

A

Dopamine agonists (bromocriptine, cabergoline) decrease prolactin secretion and decrease the size of prolactinomas

  • Restore menstrual cycles and fertility
  • Cabergoline is specific D2 receptor agonist that is long acting and has fewer GI side effects
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12
Q

Polycystic ovary syndrome results from ___

A

Polycystic ovary syndrome results from excess androgen from the ovary

  • Follicles do not convert from androgenic to estrogenic milieu
  • Dominant follicle is not selected
  • No ovulation
  • Treatment goal: increase FSH to increase aromatase, decrease testosterone
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13
Q

Describe actions of clomiphene citrate

A

Clomiphene citrate

  • Increases endogenous estrogen
  • Anti-estrogen in brain, cervical mucus, endometrium
  • Leads to increased FSH due to perceived low estrogen, stimulates follicles (may be > 1), increases estrogen, causes ovulation
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14
Q

Describe actions of tamoxifen

A

Tamoxifen

  • Reduces incidence of breast cancer
  • Also induces ovulation
  • Biological action depends on cell type
  • Anti-estrogenic in breast, leads to hot flashes
  • Estrogenic: venous thrombosis, maintains bone density, vaginal mucosa, endometrium (increases risk of endometrial cancer)
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15
Q

Describe actions of aromatase inhibitor

A

Aromatase inhibitor

  • Blocks estrogen production: decreases negative feedback, leads to increased FSH -> follicle development
  • Adjuvant treatment for breast cancer
  • Short half-life and decreased anti-estrogenic effects (better endometrium) compared to clomiphene
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16
Q

Insulin ____ androgen production from theca cells, particularly in PCOS patients

A

Insulin increases androgen production from theca cells, particularly in PCOS patients

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17
Q

____ is best for ovulation induction in PCOS

A

Clomiphene plus metformin is best for ovulation induction in PCOS

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18
Q

Anovulation with PCOS has clinical consequences of ____, ____, and ____

A

Anovulation with PCOS has clinical consequences of

  • Endometrial cancer: due to continuous estrogen without periodic progesterone
  • Menstrual disturbances: 50% amenorrhea, 30% dysfunctional uterine bleeding
  • Infertility
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19
Q

Estrogen peaks in ____, while progesterone peaks in ____

A

Estrogen peaks in proliferative / follicular phase, while progesterone peaks in secretory / luteal phase

20
Q

Medroxyprogesterone acetate is a ___ used for ___ or ___

A

Medroxyprogesterone acetate is a progestin used for cycle control (5-10 day course) or contraception (Depo-Provera)

21
Q

Birth control pills consist of ___ or ___ and exert ___ feedback

A

Birth control pills consist of ethinyl estradiol (estrogen) or progestins and exert negative feedback

  • Decrease GnRH
  • Decrease LH and FSH
22
Q

Describe oral estrogens for contraception

A

Oral estrogens for contraception

  • Ethinyl group confers oral activity
  • Enovid 10
  • Ethinyl estradiol
  • Estradiol valerate
23
Q

Describe oral progestins for contraceptions

A

Oral progestins for contraceptions

  • 1st generation (derived from testosterone): norethindrone, norethindrone acetate, ethynodiol diacetate
  • 2nd generation (methyl group increased potency): norgestrel and levonorgestrel
  • 3rd generation (derived from levonorgestrel, less androgenic): norgestimate, desogestrel
  • Drospirenone: spironolactone activity, mild anti-androgen activity
  • Dienogest: strong anti-androgenic activity
24
Q

Combination OCPs consist of ___ and ___

A

Combination OCPs consist of ethinyl estradiol and progestin

  • Reduce ovarian androgen production
    • Decrease FSH and LH -> decrease ovarian steroidogenesis
    • Estrogen -> increase SHBG -> less free testosterone
  • Benefits: reduce acne and hirsutism, cycle control -> reduce risk of endometrial hyperplasia
25
Q

Menstrual bleeding is ____ and occurs ____

A

Menstrual bleeding is bleeding in response to ovulation and occurs 14 days later

  • In contrast, birth control pills cause hormone withdrawal bleeding
26
Q

Describe pharmacological effects of progestins in combination oral contraceptive pills

A

Pharmacological effects of progestins in combination oral contraceptive pills

  • Inhibit ovulation by suppressing HPO function
  • Diminish ovarian hormone production
  • Produce endometrial changes unfavorable for ovum implantation
  • Thicken cervical mucus to impede sperm transit
27
Q

Menopause is ____ and results in ____

A

Menopause is 1 year after final menses and results in ovarian failure

  • Ovarian failure may occur prematurely
28
Q

Menopause results in ____

A

Menopause results in estrogen deficiency

  • Tissue atrophy: breast, vagina, uterus
  • Osteoporosis: bone mineral density, life threatening
29
Q

Describe treatment for ovarian failure

A

Ovarian failure treatment

  • Hormone therapy: induce puberty if premature ovarian failure, relieve hypo-estrogenic symptoms (hot flashes, vaginal atrophy, maintain bone mineral density)
  • Fertility: oocyte donation is needed
30
Q

Estrogen alone can lead to ____

A

Estrogen alone can lead to endometrial cancer

31
Q

Raloxifene is a ___ used for ___ and ___

A

Raloxifene is a SERM used for osteoporosis or breast cancer

  • Biological action depends on cell type
  • Anti-estrogenic: breast, hot flashes, vaginal dryness
  • Neutral: endometrium
  • Estrogenic: venous thrombosis, maintain bone density
32
Q

Describe the ideal SERM

A

Ideal SERM

  • Anti-estrogen: decrease breast cancer, protect endometrium
  • Neutral: venous thrombosis
  • Estrogenic: no hot flashes, maintain bone mineral density, and vaginal mucosa
33
Q

Describe treatment for hypothalamic amenorrhea

A

Hypothalamic amenorrhea treatment

  • Fetility: oral medications usually do not work (trick brain into seeing low estrogen), injections with gonadotropins (FSH and LH) best
  • Hormone repalcement: relieve hypoestrogenic symptoms, maintain bone mineral density
34
Q
A
35
Q

Describe dominant follicle selection

A

Dominant follicle selection

  • Day 5-7: decreased FSH
  • Most follicles undergo atresia and 1 dominant follicle develops
36
Q

Describe ovarian follicles by ultrasound

A

Ovarian follicles by ultrasound

  • Normal ovary with 1 dominant follicle and other smaller follicles
  • Ovary with many follicles after treatment with gonadotropins
  • Gonadotropins in conjunction with IVF: more oocytes -> more embryos
37
Q

LH surge involves ____ feedback

A

LH surge involves positive estrogen feedback

  • Increased estrogen triggers LH surge
  • With IVF: many small follicles, high estradiol
  • For IVF: need pituitary suppression, prevent premature LH surge
38
Q

Describe GnRH regulation of LH and FSH

A

GnRH regulation of LH and FSH

  • Different pulses: amplitude, frequency
  • High frequency: favors LH-beta
  • Low frequency: favors FSH-beta
  • Continuous secretion: desensitization -> decreased FSH and LH
39
Q

Describe amino acid 6 and 10 positions in GnRH agonists

A

GnRH agonists

  • Amino acid 6 (D-substitution): increases metabolic stability
  • Amino acid 10 (ethylamide group): 10x increased affinity for receptors
40
Q

Desensitization is ___

A

Desensitization is decreased response with continuous stimulation

  • Uncoupling of receptor and signaling pathway
  • Downregulation of functional receptors: internalization of receptors (occurs with GnRH agonist)
41
Q

Describe GnRH agonists

A

GnRH agonists

  • Initial flare before suppression
  • May initially worsen symptoms
42
Q

____ is needed for oocyte maturation because it triggers ____ and ____

A

LH is needed for oocyte maturation because it triggers ovulation and final maturation (meiosis resumes, cumulus expands)

  • No LH commercially available so use GnRH agonist or hCG
43
Q

hCG is used in assisted reproduction instead of LH because ____

A

hCG is used in assisted reproduction instead of LH because binds same receptor with long half-life

  • hCG other uses are cryptorchidism, male hypogonadism
44
Q

5 alpha reductase inhibitors ____

A

5 alpha reductase inhibitors inhibit production of dihydrotestosterone (potent androgen)

  • Used for prostate cancer, BPH, male pattern baldness, and hirsutism
45
Q

Estrogen results in ____ of breast epithelial cells

A

Estrogen results in proliferation of breast epithelial cells

46
Q

Describe role of anti-estrogens in breast cancer

A

Role of anti-estrogens in breast cancer

  • Breast cancer prevention: SERMs (tamoxifen, raloxifene)
  • Breast cancer treatment: GnRH agonists (goserelin acetate), SERMs (tamoxifen, toremifene), aromatase inhibitors (anastrozole, letrozole)
47
Q

Describe drugs impacting the reproductive axis and therapeutic uses of reproductive hormones

A

Drugs impacting the reproductive axis and therapeutic uses of reproductive hormones

Repro / GU (46 decks)

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