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PHAR 230 > M4 L2 Gonadosteroids > Flashcards

M4 L2 Gonadosteroids Flashcards

1
Q

what are the female sex hormones?

A
  1. estrogens: development of female sex characteristics
  2. progestins: control ovarian cycle + maintenance of pregnancy
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2
Q

what are the male sex hormones?

A

androgens: development of male sex characteristics

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3
Q

sex hormones are controlled by

A

hypothalamus and pituitary gland
through -‘ve feedback mechanism

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4
Q

how r sex hormones released

A

hypothalamus releases GnRH, and pituitary then releases LH and FSH which stim testosterone in testes, and estrogen/progesterone in ovaries

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5
Q

3 types of estrogen

A
  1. natural (endogenous)
    ex: estradiol, secreted by the ovaries
  2. semisynthetic
    ex: ethinylestradiol (inactive prodrug), estradiol valerate
  3. synthetic
    ex: mestranol, stilboestrol
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6
Q

how is estrogen absorbed through

A
  • GIT
  • Skin
  • Mucous membrane
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7
Q

how is estrogen transported

A

by binding too…
albumin, and sex steroid-binding globulin

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8
Q

estrogen half life

A

+/- 13 hrs

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9
Q

what is the metabolism and degradation of estrogen

A
  • liver
  • synthetic estrogens are less prone to degradation than natural
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10
Q

how is estrogen excreted

A

thru kidneys in urine

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11
Q

therapeutic indications of estrogen

A
  • contraception in females
  • replacement therapy due to estrogen deficiency
    (menopausal sympt, female hypogonadism)
  • transgender hormonal therapy
  • menstrual disorders
  • acne
  • prostatic cancer
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12
Q

what causes female hypogonadism

A

due to impaired ovarian function

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13
Q

types of female hypogonadism

A
  • pre-pubertal (delayed puberty)
  • post-pubertal (2ndary amenorrhea and infertility)
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14
Q

treatment of primary hypogonadism

A
  • begins at 11-13 yrs of age
  • aim to stim development of 2ndary sex characters and menstruation and stim optimal growth
  • small doses of estrogen on days 1-21 of each month (to mimic normal cycle
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15
Q

what is hyperestrogenemia

A
  • increased estrogen levels
  • in males this can cause feminization, and infertility
    in females this can cause endometrial carcinoma, and breast cancer
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16
Q

what are 4 antiestrogens

A
  • tamoxifen
  • clomiphene
  • letrozole
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17
Q

what is tamoxifen

A
  • estrogen receptor blocker
  • used to treat hormonally responsive breast cancer*
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18
Q

what is clomiphene

A
  • selective estrogen receptor modulator (SERM) -> this inhibits estrogen-mediated -‘ve feedback on hypothalamus and increases GnRH, FSH and LH levels
  • ovulation induction: used in treatment of infertility*
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19
Q

what is letrozole

A
  • aromatase enzyme inhibitor -> decrease estrogen synthesis

indications:
- hormonally responsive breast cancer (post-menopausal women)
- ovulation induction - treatment of infertility
- gynecomastia in men

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20
Q

Types of progestins

A
  1. natural
  2. synthetic (1st, 2nd, 3rd gen compounds
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21
Q

ex of natural progestins

A

progesterone
secreted by corpus luteum and placenta

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22
Q

ex of synthetic 1st generation compounds

A

medroxyprogesterone, norethindrone, norgestrel

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23
Q

ex of synthetic 2nd generation compounds

A

levonorgestrel

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24
Q

ex of synthetic 3rd generation compounds

A
  • desogestrel, gestodene, norgestimate
  • least androgenic effect
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25
Q

therapeutic indications of progestins

A
  • contraception in females
  • hormone replacement therapy
  • menstrual disorders
  • dysmenorrhea (painful menstruation)
  • endometriosis
  • endometrial carcinoma
26
Q

what is mifepristone

A
  • progesterone receptor blocker (antiprogestin)
  • indication: therapeutic abortion
27
Q

hormonal contraception options

A
  1. oral contraceptives
  2. injections and implants
  3. transdermal patch
28
Q

what are combined oral contraceptives

A
  • combo of estrogen and progestin
  • most popular
  • 2 types: monophasic (fixed dose), bi- or triphasic (variable dose)
29
Q

what is progestin mini pill oral contraceptives

A

low dose progestin

30
Q

monophasic OCC

A

estrogen: ethinyl estradiol 2 ug (days 1-21)
progestin: desogestrel 150 ug (days 1-21)

31
Q

triphasic OCC

A

estrogen: 20ug (like monophasic)
progestin: desogestrel increases by 25 each 7 days for 21 days from 100-150 ug

32
Q

minipill OCC

A

norgestril 75 ug (everyday

33
Q

what do estrogen-progestin combos do?

A
  • suppress ovulation, thicken cervical secretions, inhibit implantation
34
Q

what does low-dose progestin do

A
  • thicken cervical secretions
  • inhibit implantation
  • variable suppression of ovulation by effect on FSH/LH
35
Q

adverse effects of the combined OCC

A
  • salt and water retention (causes edema)
  • hypertension
  • vascular disorders (increases risk of clot formation)
  • migraine/headache
  • depression
  • post pill amenorrhea
36
Q

absolute contraindications of combined OCC

A
  • pregnancy
  • breast feeding
  • thromboembolic disease
  • breast/cervical/endometrial cancer
  • undiagnosed vaginal bleeding
37
Q

relative contraindications of combined OCC

A
  • hypertension
  • impaired liver function
  • migraine
38
Q

contraceptive injections

A

long acting progestins
- IM injections every 3 months
- ex: medroxyprogesterone (provera)

39
Q

contraceptive implants

A

long acting progestins
- SC insertion of small capsules
- effective for 3-5 yrs
- ex: levonorgestrel (norplant)

40
Q

what is hormone replacement therapy

A
  • estrogen replacement in postmenopausal women (low dose compared to contraceptives)
  • progestin can be added to reduce risk of endometrial carcinoma
41
Q

benefits of hormone replacement therapy

A
  • prevention of changes associated with menopause: osteoporosis, flushing, headaches, insomnia, genital tract atrophy, cardiovascular disease
42
Q

ex of natural androgens

A
  • testosterone
  • dihydrotestosterone (DHT)
  • dehydroepiandrosterone (DHEA)
  • androstenedione
43
Q

ex of synthetic androgens

A
  • methyltestosterone
  • ethylestrenol
  • stanozolol
44
Q

mech of action of androgens

A

regulate gene expression by activating a nuclear receptor

45
Q

effects of androgens

A
  • development of primary and secondary male sex characters
  • maturation of sperm
  • anabolic effect: some synthetic androgens have more anabolic than androgenic activity (ex: stanozolol)
46
Q

therapeutic indications of androgens

A
  • hormone replacement: male hypogonadism, hypopituitarism
  • anemia: androgens stim erythropoiesis
  • breast cancer: androgens may downgrade receptor expression
  • anabolic agents: compensate for protein loss, often abused by body builders and athletes
47
Q

male hypogonadism types

A

primary: testicular failure
secondary: hypothalamic-pituitary disease

48
Q

male hypogonadism treatment

A

aim:
- stim development of male secondary sex characters
- maintain muscle and bone mass
regimen:
- oral: TDS
- transdermal patch: every 24 hrs
- IM injection: every 2-3 weeks
- subdermal implants every 4-6 months

49
Q

hyperandrogenemia in females

A
  • virilization sympt: hirsutism, acne, amenorrhea, clitoral enlargement and deepening of voice
  • during preg: masculinization of external genitalia of infants
50
Q

hyperandrogenemia in prepubertal male children

A

precocious puberty

51
Q

what is an example of an androgen suppressor

A

leuprolide acetate

52
Q

what is the mech of action for androgen suppressors

A

there is an interruption of GnRH receptors which causes a decrease in FSH and LH, which leads to decrease in testosterone or estrogen to +/- 10% of basal levels

53
Q

what are androgen suppressors used to treat

A
  • prostatic carcinoma
  • endometriosis
  • breast cancer
54
Q

what is the administration of androgen suppressors

A

IM or SC injection every 1, 3, 4, or 6 months

55
Q

what is an example of androgen receptor inhibitors

A

cyproterone acetate

56
Q

mech of action for androgen receptor inhibitors

A
  • androgen receptor competitive antagonist
  • progestin action
57
Q

what are androgen receptor inhibitors used to treat

A
  • prostatic carcinoma
  • precocious puberty in boys
  • acne
  • hirsutism and virilization in women
58
Q

adverse effects of androgen receptor inhibitors

A

hepatotoxic

59
Q

administration of androgen receptor inhibitors

A

oral

60
Q

male oral contraceptive: gossypol

A
  • from seeds in cotton plant
  • inhibits sperm production
  • efficacy comparable to female OCC
  • adverse effects: irreversibility, hypokalemia

PHAR 230 (31 decks)

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