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Pharmacology > Sex hormones > Flashcards

Sex hormones Flashcards

1
Q

17 beta estradiol

A

Most important physiological estrogen
Pharm: eliminated by liver, poor oral availability, transdermal patches to avoid hepatic first pass
Uses: post-menopausal therapy

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2
Q

estrone sulfate, equiline sulfate

A

conjugated estrogens
Pharm: PO, absorbed lower GI tract
Uses: oral hormone replacement therapy in post menopausal women

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3
Q

estradiol valerate, estradiol cypionate

A

Esterified estrogens
Pharm: parenteral injections in oil, slower
Uses: prolonged systemic delivery of 17 beta estradiol to circulation 2-4 weeks that reduces hepatic effects of estrogens

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4
Q

ethinyl estradiol, mestranol

A

Synthetic steroidal estrogens
Pharm: PO, decreases hepatic first pass metabolism, long half life
Uses: combo with oral contraceptives

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5
Q

DES

A

Synthetic non-steroidal estrogen
Pharm: PO potent estrogen with prolonged effects

Uses: paliative treatment of metastatic prostate or breast cancer, relieves bone pain and improves quality of life

Side effect: CV toxicity due to high doses

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6
Q

medroxyprogesterone acetate

A

Progestin: support pregnancy in experimental animals, anti aldosterone effects, inhibit LH and FSH release
Pharm: DepoProvera given PO
Uses: hormone replacement regimens for post menopausal women

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7
Q

megestrol acetate

A

Progestin: support pregnancy in experimental animals, anti aldosterone effects, inhibit LH and FSH release
Uses: stimulate appetite and weight gain in patients with AIDS

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8
Q

norethindrone, levonorgestrel

A

Pharm: good PO availability, produce decidual change in endometrium, stronger inhibitors of LH and FSH
- weak androgen and antiestrogen effects

Uses: combo oral contraceptives, progestin alone, patches, emergency

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9
Q

Norethynodrel

A

Pharm: good PO availability, produce decidual change in endometrium, stronger inhibitors of LH and FSH
- estrogenic effects

Uses: combo oral contraceptives, progestin alone, patches, emergency

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10
Q

desogestrel, norgestimate

A

Pharm: good PO availability, produce decidual change in endometrium, stronger inhibitors of LH and FSH
- minimal androgenic or estrogenic effects

Uses: combo oral contraceptives, progestin alone, patches, emergency

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11
Q

dienogest

A

Pharm: good PO availability, produce decidual change in endometrium, stronger inhibitors of LH and FSH
- antiandrogenic

Uses: combo oral contraceptives, progestin alone, patches, emergency

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12
Q

drospirenone

A

spironolactone related progestin
Pharm: anti-mineralocorticoid similar to progesterone, no androgenic activity

Side effects: less water retention and breast tenderness

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13
Q

ulipristal acetate

A

Selective progesterone receptor modulator with agonist and antagonist effects
- used for emergency contraception

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14
Q

Testosterone (T)

A

Pharm: poor systemic bioavailability after oral dosing or subq or IM

Side effects: induce pubertal changes, no hepatotoxicity

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15
Q

testosterone ethanate, testosterone cypionate

A

Pharm: IM

Uses: induce pubertal changes in hypogonadal boys

Side effects: no hepatotoxicity

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16
Q

methyl testosterone, fluoxymesterone, oxandrolone

A

anabolic steroids - dose related hepatotoxicity

17
Q

danazol

A

Pharm: synthetic steroid derivative PO use
- mix of weak androgen, antiestrogen, progestin, glucocorticoid activity
Side effects: acne, cholestatic jaundice, liver tox, benign hepatic tumors, increased aggression

Uses: endometriosis, prevent hereditary angioneurotic edema in patients with complement C1 inhibitor deficiency

18
Q

Progestin only contraceptives

A

Used when estrogen is contraindicated

Side effects: weight gain, abnormal bleeding, delayed onset fertility, increases risk of osteoporosis

Uses: birth control, dysmenorrhea, endometriosis

Combo: dysmenorrhea, acne, hirsutism

19
Q

Levonorgestrel

A

Plan B
- used when begun within 72 hour of intercourse
Pharm: large doses of estrogen, estrogen and progestin

Side effects: nausea

20
Q

ella - ulpristal acetate

A

Selective progesterone receptor modulator

Uses: prevents ovulation and impairs implantation
- started within 120 hours of intercourse

Side effects: headache, nausea, dysmenorrhea

21
Q

medroxyprogesterone acetate with estrogen replacement therapy

A

Avoid risk of uterine cancer due to exposure to estrogen alone

Uses: menopause sx, decrease risk of osteoporosis
- no change in atherosclerosis, colon cancer, alzheimer’s disease

Side effects: increase risk of breast CA

22
Q

Estrogen premenopausal adverse effects

A

Side effects: nausea, breast tenderness, headache, altered skin pigmentation, increased risk of gall bladder disease, increased DVT, increased MI and stroke

23
Q

Estrogen postmenopausal adverse effects

A

VTE, DVT, uterine cancer unless progestin used as well

24
Q

flutamide, bicalutamide

A

Non steroidal antagonist of androgen receptor

Uses: prostate cancer therapy in combo with GnRH, prevents tumor flare due to rise in testosterone

Bicalutamide - potent, longer acting less hepatotoxicity

25
Q

spironolactone

A

weak androgen receptor antagonist
- reduces testis levels of steroid 17 alpha hydroxylase

Uses: hirsutism

26
Q

ketoconazole

A

Antifungal that can inhibit multiple steroidigenic enzymes to decrease androgen as well as corticosteroid synthesis

27
Q

finasteride

A

5 alpha reductase inhibitor

Uses: treatment of benign prostatic hypertrophy or male pattern baldness

28
Q

abiraterone

A

17 alpha hydroxylase that blocks androgen synthesis
Pharm: orally with glucocorticoid replacement

Uses: treatment of prostate CA after castration and doxetaxel therapy

29
Q

tamoxifen

A

selective estrogen receptor modulators

Uses: breast CA treatment and prevention, osteoporosis, infertility
- ER positive breast CA, prevention of breast CA in high risk patients

Side effects: estrogen effects to increase risk of venous thromboembolism, chronic use increases uterine cancer risk

30
Q

raloxifen

A

selective estrogen receptor modulators

Uses: osteoporosis,

Side effects: minimal estrogen agonist effects on uterus, less risk of uterine cancer with chronic use

31
Q

clomiphene

A

Selective estrogen receptor modulators

Uses: treatment of infertility

32
Q

anastrozole, letrozole, exemestane

A

Aromatase inhibitors

Pharm: inhibit CYP19, androgens to estrogens

Uses: breast cancer resistant to tamoxifen or aromatase inhibitors

Side effects: osteoporosis

33
Q

fluvestrant

A

pure estrogen receptor antagonist

uses: advanced breast cancer resistant to other therapies

side effects: increased risk of osteoporosis

34
Q

mifepristone

A

Progesterone receptor antagonist - used to induce first trimester abortions
- first 7 weeks of conception

Uses: stimulates uterine contractions to abort fetus

Side effects: nausea, vomiting, diarrhea, vaginal bleeding

Pharmacology (5 decks)

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