L 31-32 Sex Hormones and Gonadotropins Flashcards

1
Q

Describe the HPG axis

A

This is the gonadal axis

GnRH is pulsatile and a constant signal will actually silence the axis

Also notice that Estrogen can inhibit and stimulate depending on concentration

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2
Q

Where in the HPG axis do you treat for infertility and secondary sex characteristics?

A

Fertility: treat at the LH/FSH level

Secondary Sex: treat at the steroid level

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3
Q

Gonadorelin (GnRH, Factrel)

A

Short acting GnRH

Used to treat infertility

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4
Q

Leuprolide, Nafarelin (Synarel)

Goserelin (Zoladex)

A

Long-Acting GnRH analogues

Continuous administration suppresses LH and FSH after an initial stimulation of gonadotropin release

Used to shut down the HPG for infertility treatment, precocious puberty, prostate or breast cancer

Cause menopausal Sx and testicular atrophy

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5
Q

Citrorelix (Cetrotide)

Ganirelix

A

GnRH antagonists

Suppress LH at low doses and FSH at higher doses

Has no initial surge of gonadotropins like the long-acting agonists would have

Used for ART and endometriosis

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6
Q

Human menopausal gonadotropins (hMG)

Menotropins (Menopur)

A

Both FSH and LH but used as FSH

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7
Q

Urofollitropin

A

Just FSH

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8
Q

Follitropin alfa (Gonal F)

Follitropin beta (Follistim)

A

rFSH

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9
Q

Human Chorionic Gonadotropin (hCG)

A

Similar structure and binds to LH receptors

Longer half-life than LH

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10
Q

Choriogonadotropin alfa (Ovidrel)

A

rhCG

Same action as LH

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11
Q

Lutropin (Luveris)

A

recombinant LH

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12
Q

Effects of LH and FSH on men and women

A

Men: LH increases testosterone for up to one year, FSH then induces spermatogenesis (takes months)

Women: FSH (9-12 days) stimulates ovaries and estrogen, Single dose of LH given to induce ovulation

Opposite in order given between men and women

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13
Q

How is estrogen metabolized?

A

Metabolized in the liver and excreted in the bile

Enterohepatic circulation–important for contraceptive use

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14
Q

Estradiol

A

Naturally occuring estrogen and not orally active–used as a patch or a cream

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15
Q

Ethinyl estradiol

Mestranol

A

Synthetic oral contraceptives that are estrogens

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16
Q

Premarin

Cenest

Estratab

Menest

A

Conjugated estrogens used for hormone replacement therapy

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17
Q

Diethylstilbesterol

A

Nonsteroidal estrogen

Not used much anymore

18
Q

When are estrogen drugs used?

A

In primary hypogonadism of 11-13 year old girls to stimulate growth

Postmenopausal hormone replacement therapy

Oral contraception

Suppress ovulation

19
Q

Side effects of estrogen use

A

Migraines

Gallbladder disease

Thromboembolism, blood clotting

Uterine hyperplasia

Nausea and breast tenderness

20
Q

Tamoxifen (Novaldex)

A

SERM (selective estrogen receptor modulator)

Agonist in uterus and bone

Antagonist in breast

Does not relieve hot flashes

Used to treat and prevent estrogen dependent breast cancer–DOC in premenopausal women

21
Q

Toremefine (Fareston)

A

Similar to tamoxifen (SERM), but better at increasing HDL

22
Q

Raloxifene (Evista)

A

SERM

Antagonist in breast and uterus

Agonist in liver and bone

Used to prevent postmenopausal osteoporosis

Does not relieve hot flashes

23
Q

Clomiphene (Clomid)

A

SERM

Typical DOC for infertility with intact HPG axis

Antagonizes negative feedback in the hypothalamus from estrogen to stimulate the release of LH and FSH inducing ovulation

24
Q

Fulvestrant (Faslodex)

A

Full estrogen receptor antagonist

Causes menopausal Sx

25
Q

Anastrazole (Arimidex)

Letrozole (Femara)

Exemastane (Aromasin)

A

Aromatase inhibitors that block all production of estrogen

Exemastane is irreversible

DOC–for postmenopausal breast cancer, advanced breast cancer after tamoxifen failure in postmenopausal women

Will increase testosterone causing hursutism

Will cause menopausal Sx

26
Q

Progesterone

A

Promotes gestation, maintains pregnancy, suppresses contractility during pregnancy, increases body temp

Regulated by LH and produced by corpus luteum and placenta

27
Q

Medroxyprogesterone (Provera)

A

Progesterone derivative

28
Q

Megestrol (Megace)

A

Progesterone derivative

29
Q

Norethindrone (Aygestin)

A

Progestin

More androgenic

30
Q

Norgestrel (Ovrette)

A

Progestin

31
Q

Levonorgestrel (Plan B)

A

Progestin

32
Q

Desogestrel (Desogen)

A

Progestin

33
Q

Norgestimate

A

Progestin

34
Q

Mifepristone (RU 486, Mifeprex)

A

Anti-progestin

Progesterone receptor antagonist

Terminates pregnancy

Used to prevent implantation within 72 hours of intercourse

35
Q

Danazol (Danocrine)

A

Anti-progestin

Weak progestin and androgen

Suppresses ovarian function

Used to treat endometriosis!!!!

36
Q

Drospirenone/ethinyl estradiol (Yaz)

A

Combination oral contraceptive

Works by inhibiting ovulation, thickening cervical mucus, changing the endometrium decrease implantation

This has less water retention than other contraceptives and anti-androgenic properties

37
Q

Adverse effects of combination oral contraceptives

A

Weight gain

Nausea

Edema

Depression

Clotting causing CV problems made worse by smoking or over 35 yo

Migraine

Teratogenesis

Fertility can be suppressed for 3+ months

Protects against ovarian and endometrial cancer for up to 15 years after use

Do not use with thrombotic problems or estrogen-dependent neoplasms

38
Q

Oral contraceptive drug interactions

A

P450 inducers reduce effectiveness

Antibiotics reduce effectiveness

39
Q

Adverse effects of hormone replacement therapy

A

Endometrial cancer–progesterone to prevent

Breast cancer

Gallbladder disease

CV

40
Q

Ketoconazole (Nizoral)

Spironolactone (Aldactone)

A

Androgen synthesis inhibitors

41
Q

Flutamide (generic)

Bicalutamide (Casodex)

Nilutamide (Nilandron)

A

Androgen receptor antagonists

Used in prostate cancer with long-acting GnRH agonists to suppress the flare of gonadotropins with initiation of treatment

Can be used topically for baldness and hirsutism

42
Q

Finasteride (Propecia)

Dutasteride (Avodart)

A

5alpha-reductase inhibitors

Suppress male sex accesory organs without affecting libido

No DHT means affects the prostate and hair follicle the most

Treats BPH and male pattern baldness

Causes impotence

Teratogenic