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Pharmacology > Sex steroids > Flashcards

Sex steroids Flashcards

1
Q

Estradiol has which pharmacokinetic properties

A

orally ineffective, slow release depot esters of estradiol

comes in topical preps

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2
Q

Therapeutic uses of Estradiol

A

used in HRT and hypogonadism

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3
Q

Conjugated estrogens, phamacokinetics

A

metabolized estrogen, can be given orally, IV, IM, vaginal

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4
Q

Therapeutic use of conjugated estrogens

A

HRT

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5
Q

What is the prototype synthetic estradiol analog

A

ethinyl estradiol

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6
Q

Pharmacokinetics of ethinyl estradiol

A

ethinyl group slows metabolism, increases potency and oral effectiveness

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7
Q

Side effects of estrogens

A

nausea, edema, breast tenderness, hyperpigmentation, migrane, cholestasis, insulin resistance, liver and gaul bladder disease. Thrombophlebitis, endrometrial cancer (reduced by progestin combos), feminization in men

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8
Q

Therapeutic uses of estrogens

A

oral contraceptives and HRT

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9
Q

Pharmacokinetics of progesterone

A

IM, creams, suppositories, IUD

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10
Q

Prototype of synthetic progesterones

A

medroxyprogesterone acetate

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11
Q

Use for progesterones

A

HRT, IM birth control

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12
Q

What are the synthetic progestin structurally related to testosterone

A

Norethindrone, and norgestimate (less androgen effects)

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13
Q

Therapeutic uses of progestins

A

alone or with estrogens as contraception or HRT
decrease endometrium proliferation
endometiral and breast cancer

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14
Q

Progestin related side effects

A

menstraul changes, nausea, bloating, breast tenderness, teratogenesis possibility

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15
Q

Androgen mediated side effects

A

acne, weight gain, masculinization, altered libido, decreased HDL increased LDL

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16
Q

What are the effect of long-term hormone replacement

A

bone health increase, but cardiovascular health decrease, increased endometrial cancer w/ estrogen alone, some improvement w/ both. E and P both increase breast cancer risk.

17
Q

HRT regimens

A

Oral conjugated estrogens and medroxyprogesterone is most common
cyclic estrogen plus progestin
continuous estrogen plus cyclic progestin
continuous estrogen and progestin
estrogen alone only if hysterectomy

18
Q

Agonist effect at estrogen receptors used for osteoperosis

A

Raloxifene

19
Q

Antagonist effect in breast cancer

A

Tamoxifen

20
Q

Tamoxifen agonist/antagonist actions on different tissues

A

antagonist- prevents breast cancer, menopausal side effects

agonist- increase uterine cancer risk, reduce osteoperosis, improve heart health

21
Q

Raloxifene agonist/antagonist actions on different tissues

A

antagonist- prevents breast and uterine cancer, causes menopausal side effects
agonist- decrease osteoperosis, increase thrombosis

22
Q

Most common ingredients of oral contraceptives

A

ethinyl estradiol and norethindrone or norgestimate

23
Q

Which progesterones have androgenic properties

A

norethindrone, levonorgestrel

24
Q

which progesterones have neither androgenic nor estrogenic properties

A

norgestimate

25
Q

Which progesterone has anti-androgenic effects

A

drospirenone

26
Q

which drugs are in the 3-week vaginal ring

A

etonogestrel and ethinyl estradiol

27
Q

Adverse effects of oral contraceptives due to estrogen component

A

nausea, irritability, headache, fluid retention, cyclic weight gain, breast enlargement and tenderness, menstrual changes, altered libido

28
Q

Adverse effects of oral contraceptives due to progestin

A

nausea, bloating, menstrual changes, depression, fatigue. Androgen properties can cause acne, hirsutism, increased libido, weight gain.

29
Q

Progestin used for IM contraception

A

Medroxyprogesterone

30
Q

Progestin used in “emergency” contraceptives

A

levonorgestrel

31
Q

Pharmacokinetics of testosterone

A

ineffective orally, limited parenteral effectiveness, rapidly metabolized. Topical preps becoming important for low T

32
Q

Testosterone ester pharmacokinetics

A

IM injection 2-3 times per week, some longer preps

33
Q

Adverse effects of testosterone

A

masculinization, feminization, testicular atrophy, prostatic enlargement, acne, hypertension, salt and water retention, liver disease, psychosis

Pharmacology (35 decks)

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