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Pharm Test 6 > Gonadal Steroids > Flashcards

Gonadal Steroids Flashcards

1
Q

Estrogens

A
  1. Estradiol, estrone, estriol: estradiol is the major one
  2. Act on nuclear protein receptors which interact w/DNA increasing mRNA/protein synthesis.
  3. Metabolized by liver and undergo enterohepatic circulation.
  4. Lots of effects, look at the handout.
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2
Q

Estradiol

A
  1. Endogenous estrogen, not orally active, patches/creams only.
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3
Q

Ethinyl estradiol, Mestranol

A

Only found in combination oral contraceptives, very potent

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4
Q

Conjugated estrogens

A

Used for Hormone replacement therapy. Conjugated equine estrogens, synthetic conjugated estrogens, esterified estorgens

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5
Q

Diethylstilbestrol

A
  1. Non-steroidal estrogen
  2. Primary hypogonadism, postmenopausal hormone replacement therapy, oral contraceptives, dec dysfunctional uterine bleeding, suppress ovulation in women w/intractable dysmenorrhea/excessive ovarian androgen secretion, tx of androgen dependent cancers.
  3. Metabolized in liver, enterohepatic circulation
  4. SE:
    - uterine hyperplasia in HRT,
    - Nausea,
    - breast tenderness, migraines, gallbladder disease
    - HTN
    - hyperpigmentation
    - accelerated blood clotting
    - SE are dose dependent.
  5. CI:
    - estrogen dependent neoplasms/breast cancer.
    - Undiagnosed genital bleeding,
    - uncontrolled HTN
    - liver disease
    - history of embolism
    - smoking, pregnancy
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6
Q

Tamoxifen

A
  1. Antiestrogen, DOC for premenopausal women w/estrogen dependent breast cancer.
  2. Selective estrogen receptor modulator (SERM). Agonist in uterus and bone (prevents bone loss), antagonist in breast.
  3. Tx of estrogen dependent breast cancer in premenopausal women.
    - May dec HDL.
    - Does not relieve hot flashes.
  4. Excreted by liver, oral, 2x/day
  5. Inc risk of uterine cancer, hot flashes/nausea/vomitting
  6. CI: thromboembolic disease, breast feeding.
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7
Q

Toremifene

A
  1. Antiestrogen

2. Increases HDL

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8
Q

Raloxifine

A
  1. Antiestrogen, SERM
  2. Antagonist in both breast and uterus (reduces likelihood of uterine cancer), agonist in bone and liver
  3. Useful in prevention of postmenopausal osteroporosis.
  4. SE: hot flashes, DVT, leg cramps
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9
Q

Clomiphene

A
  1. Antiestrogen, SERM
  2. Antagonist in hypothalamus, agonist elsewhere, DOC for infertility in women with an intact HPG axis
  3. Tx of infertility: used to stimulate secretion of LH and FSH
  4. 5 day course of tx, oral, 1x/day
  5. SE:
    - hot flashes/HA
    - constipation,
    - allergic rxns and hair loss may also occur
    - Multiple pregnancies
    - may enlarge ovaries, especially if they are enlarged prior to therapy.
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10
Q

Fulvestrant

A
  1. Pure estrogen receptor antagonist, effective in some pts with tamoxifen resistant tumors.
  2. SE: hot flashes, GI symptoms, HA, back pain, pharyngitis.
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11
Q

Anastrozole, Letrozole

A
  1. Nonsteroidal competitive inhibitors of aromatase (last step in estroen synthesis)
  2. DOC for breast cancer in post-menopausal women
  3. SE: menopausal symptoms
  4. CI: premenopausal women, pregnancy
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12
Q

Exemestane

A
  1. Steroid that is an irreversible aromatase inhibitor.
  2. Tx: DOC for breast cancer in postmenopausal women, 2nd line tx in postmenopausal women whose breast cancer progressed during tamoxifen therapy.
  3. SE:
    - menopausal symptoms
    - diarrhea, abdominal pain, N/V
    - bone fractures
    - joint pain
    - hypercholesterolemia
  4. CI: premenopausal women (can’t inhibt all the estrogen the ovary produces. Pregnancy: category X.
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13
Q

Progesterone

A
  1. Synthesis by corpus luteum, stimulated by LH
  2. Acts on nuclear protein receptors which interact w/DNA –> inc mRNA/protein synthesis.
  3. Physiological effects: lots, look ‘em up
  4. Natural protesterones not orally active, only synthetics. depending on structure varying levels of androgenic activity.
  5. Tx:
    - oral contraceptives
    - prevention of endometrial hyperplasia
    - dysmenorrhea, endometriosis, hirsutism, uterine bleeding disorders,
    - when estrogens are CI.
  6. SE: possible inc BP, reduction in HDL espec estranes, depression/drowsiness
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14
Q

Preganes

A
  1. Progestins: Progesterone, medroxyprogesterone, Megestrol acetate
  2. Derivatives of progestin nucleus,
    - antagonize the mineralcorticoid receptor
    - require IM injections (except megestrol acetate and medroxyprogesterone)
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15
Q

Estranes

A

Progestins: Norethindrone, Norethindrone acetate, dienogest. Derived from testosterone

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16
Q

Gonanes

A
  1. Have selective progestin activity. Desogestrel (no androgenic properties), Norgestimate, Norgestrel
17
Q

Mifepristone

A
  1. Antiprogestin, progesterone receptor antagonist
  2. Tx:
    - pregnancy termination
    - prevent implantation if w/in 72 hrs of intercourse
    - antagonizes glucocorticoid receptor
    - induction of labor at the end of the 3rd trimester following fetal death.
  3. SE: GI (V/D, abdominal/pelvic pain, vaginal bleeding)
  4. CI: pregnancy/breast feeding, pts on glucocorticoid therapy, anemia or anticoagulants.
18
Q

Danzol

A
  1. Weak progestin, androgen and glucocorticoid that suppresses ovarian function.
  2. Tx of endometriosis
  3. SE: wt gain, edema, acne/oily skin, hirsutism, deepening voice, HA, flush, libido changes and cramps. These are common but usually mild.
  4. CI: liver dysfunction, pregnancy/breast feeding
19
Q

Drospirenone/ethinyl estradiol

A
  1. Estrogen and a spironolactone derivative (mineralocorticoid antagonist) that has progesterone agonist effects.
  2. Has the ability to reduce water retention, thus it is the only combination pill that is FDA approved for reducing PMDD symptoms. Drospirenone has very low androgenic properties.
20
Q

progestin only birth control pills (Mini Pill)

A

MOA: prevent implantation
SE: break thru bleeding, weight gain, depression
- Less effective than the combination pill
- Used in breast feeding and in adolescents

Aside:
Long term tx with progestin: mirena, or implanon, will cause break thru bleeding initially followed by amenorrhea

Pharm Test 6 (12 decks)

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