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Pharm II final > Sex Hormones > Flashcards

Sex Hormones Flashcards

1
Q

Leuprolide class

A

long-acting gonadotropin-releasing hormone agonist

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2
Q

GnRH Agonist MOA

A

(GnRH agonists are Leuprolide & goserelin)
continuous administration of this long-acting GnRH agonist causes initial surge, then ultimate inhibition of gonadotropin release

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3
Q

GnRH agonists: Indications/Therapeutic effects

A
  1. reduces androgen production in prostate CA
  2. treats precocious puberty
  3. stops endogenous LH surge when stimulating with exogenous gonadotropins for ART
  4. tx endometriosis, polycystic ovarian dz and uterine leiomyomas (fibroids)
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4
Q

goserelin (Zoladex) class

A

GnRH Agonist

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5
Q

Leuprolide (Lupron) class

A

GnRH agonist

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6
Q

Cetrorelix class

A

GnRH Antagonist

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7
Q

Ganirelix class

A

GnRH Antagonist

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8
Q

GnRH antagonist MOA

A

suppresses LH at lower doses

& FSH at higher doses

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9
Q

GnRH antagonist indications/therapeutic effects (2)

A
  1. suppress endogenous & FSH for Assisted Reproductive Technologies (ART)-only takes 4-5 days (leuprolide takes 3 weeks)
  2. tx endometriosis & uterine fibroids
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10
Q

Side Effects of long-acting GnRH agonists and GnRH antagonists

A

WOMEN: menopausal sxs
hot flashes, amenorrhea
decreased bone density (osteoporosis w/ long term use)
MEN: testicular atrophy

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11
Q

Follicle Stimulating Hormone physiology (3), pharm preps

A
  1. stimulates development of ovarian follicles & estrogen synthesis
  2. stimulates spermatogenesis
  3. secretion is increased in post-menopausal women

multiple pharm preps are available

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12
Q

hMG class

A

human menopausal gonadotropin

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13
Q

Pergonal

A

human menopausal gonadotropin

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14
Q

Menotropins

A

human menopausal gonadotropin

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15
Q

Human menopausal gonadotropin: origin, contents, use

A

isolated from urine of post-menopausal women
contains both FSH & LH; isolated from urine of post-menopausal women
used for FSH properties only

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16
Q

Luteinizing Hormone (LH): when is it secreted, what does it do (females, males)

A

LH secreted just before ovulation, stimulates ovulation & luteinization of ruptured follicle
required for PROGESTERONE synthesis in corpus luteum
stimulates TESTOSTERONE production in testes

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17
Q

human Chorionic Gonadotropin (hCG):
use
MOA
pharmokinetics

A
  1. the typical LH agonist used, extracted from urine of pregnant women
  2. binds to LH receptor
  3. longer half-life than LH
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18
Q

Gonadotropin indications (3)

A
  1. pituitary or hypothalamic hypogonadism with infertility
  2. Induce spermatogenesis in hypogonadotropic hypogonadal men (hCG & hMG is given for up to 1 year, >50% men become fertile
  3. infertility in women w/functional ovaries who have not responded to other txs (hMG[FSH] then LH [hCG] are given in sequence)
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19
Q

hMG class

A

gonadotropin mixture

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20
Q

Menotropins class

A

gonadotropin mixture

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21
Q

Urofollitropin class

A

Follicle stimulating hormone (FSH)

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22
Q

Human chorionic gonadotropin class

A

luteinizing hormone

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23
Q

Adverse Effects of gonadotropins

A
  1. uncomplicated ovarian enlargement
  2. ovarian hyperstimulation syndrome (rapid accum. of fluid in peritoneal, pleural & pericardial cavities, hypovolemia, fever, shock)
  3. multiple births (~20%)
  4. Gynecomastia sometimes occurs in males
  5. HA, depression, edema, precocious puberty
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24
Q

Gonadotropin contraindications/precautions

A

sex steroid-dependent neoplasia

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25
Q

3 major natural estrogens

A
  1. Estradiol
  2. Estrone
  3. Estriol
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26
Q

production of estradiol: location, regulated by

A

ovary of non-pregnant, premenopausal women

regulated by LH & FSH and is cyclical

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27
Q

Estrogen production location in pregnant women

A

fetal-placental unit

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28
Q

Estrone and estriol locations of formation

A

liver, kidney, adipose tissue, skeletal muscle, brain and testes

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29
Q

Estrogens MOA

A

act on nuclear protein receptors, which interact w/DNA

increases mRNA synthesis and protein synthesis

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30
Q

Estrogen metabolism

A

estrogens are metabolized by the liver and undergo enterohepatic circulation

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31
Q

Naturally occurring estrogen oral activity

A

not orally active, so synthetic compounds have been developed for therapeutic use

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32
Q

Synthetic estrogens found only in:

A

combination oral contraceptives

are very potent estrogens

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33
Q

Ethinyl estradiol is a:

A

synthetic estrogen compound found in combination oral contraceptives

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34
Q

Mestranol

A

synthetic estrogen compound found in combination oral contraceptives

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35
Q

Conjugates estrogens indication

A

post-menopausal hormone replacement therapy, oral contraceptives, primary hypogonadism (given to estrogen-deficient patients age 11-13 to stimulate development of puberty and growth), decrease dysfxnal uterine bleeding in absence of organic pathology, suppress ovulation, tx androgen dependent CAs (i.e. prostate)

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36
Q

Conjugate estrogens pharmokinetics

A

metabolized by the liver, undergo enterohepatic circulation

vaginal, transdermal or injected forms sometimes used to avoid these affects

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37
Q

Major adverse effects of conjugate estrogens (3)

A
  1. migraine headaches
  2. thromboembolism
  3. accelerated blood clotting
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38
Q

2 major Conjugate estrogens contraindications/precautions

A
  1. estrogen dependent neoplasms

2. history of thromboembolic disorders

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39
Q

Tamoxifen MOA

A

selective estrogen receptor modulator (SERM)
AGONIST IN UTERUS & BONE (prevents bone loss)
ANTAGONIST IN BREAST

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40
Q

Tamoxifen Therapeutic Effects

A

Tx of estrogen-dependent breast CA
pos. prophylactic prevention of breast CA
prevents bone loss
DOES NOT RELIEVE HOT FLASHES

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41
Q

Tamoxifen Adverse Effects

A

Increased risk of uterine CA
may decrease HDL
hot flashes, N/V

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42
Q

Toremifene: class & effects

A

SERM (selective estrogen receptor modulator)

similar to Tamoxifen but increases HDL

43
Q

Raloxifene: class & MOA

A

SERM
ANTAGONIST IN BREAST & UTERUS
AGONIST IN BONE and liver

44
Q

Raloxifene indications

A

postemenopausal osteoporosis

lowers total and LDL cholesterol in post-menpause

45
Q

Adverse effects of Roloxifene

A

hot flashes, DVT, leg cramps

46
Q

Clomiphene indication

A

DOC for infertility in women w/intact HPG axis

stimulates secretion of LH & FSH (by inhibiting negative feedback)

47
Q

Clomiphene adverse effects

A 
Multiple pregnancies (5010%)
hot flashes, HA, constipation, allergic rxns & hair loss
enlarges ovaries
48
Q

Fulvestrant MOA

A

pure estrogen receptor antagonist

effective in some pts w/ tamoxifen-resistant tumors

49
Q

Fulvestrant AEs

A

hot flashes, GI sxs, HA, back pain, pharyngitis

50
Q

Aromatase inhibitors MOA, indications

A

inhibit estrogen synthesis, do not inhibit other steroid synthesis
used to tx breast CA in post-menopause

51
Q

Anastrozole class

A

nonsteroidal competitive inhibitor of aromatase (final step in estrogen synthesis)
DO NOT INHIBIT ADRENAL STEROID SYNTHESIS

52
Q

Letrozole class

A

nonsteroidal competitive inhibitor of aromatase (final step in estrogen synthesis)
DON’T INHIBIT ADRENAL STEROID SYNTHESIS

53
Q

Exemestane class

A

irreversible aromatase inhibitor

54
Q

Exemestane Indication

A

DOC: tx of breast CA in post-menopause

2nd line tx for advances breast CA whose dz progressed during tamoxifen therapy

55
Q

Exemestane adverse effects

A

Menopausal sxs, even in post-menopausal women

diarrhea, abd. pain, N/C, bone fractures, joint pain, hypercholesterolemia

56
Q

Exemestane contraindications

A

premenopausal women

if used, will need ovarian ablation first to make women post-menopausal

57
Q

Progesterone synthesis & secretion:

a. occurs where
b. is stimulated by

A

synth and secretion by CORPUS LUTEUM

stimulated by LH & later in pregnancy by hCG

58
Q

Progesterone MOA

A

acts on nuclear protein receptors, which interact w/DNA->inc. mRNA synthesis & protein synthesis

59
Q

Progesterone effects on (4) target tissues

A
  1. Uterus: converts endometrium to secretory state needed to maintain pregnancy. Suppresses uterine contractility, especially during pregnancy
  2. Endocervical glands: regulates composition of cervical mucus
  3. Breasts: lobuloalveolar development in pregnancy & puberty
  4. Thermogenic action increases body temp
60
Q

Why do we use semi-synthetic progestin compounds instead of naturally occurring progestins?

A

Natural-occurring progestins are not orally active

61
Q

Progesterone class

A

derivative of progestin nucleus

varying levels of androgenic activity

62
Q

Medroxyprogesterone class

A

derivative of progestin nucleus

varying levels of androgenic activity

63
Q

Megestrol acetate class

A

derivative of progestin nucleus

varying levels of androgenic activity

64
Q

Norethindrone class

A

19-nortestosterone

has progestin & androgenic activity

65
Q

Norgestrel class

A

19-nortestosterone

has progestin & androgenic activity

66
Q

Levonorgestrel class

A

19-nortestosterone
progestin & androgenic activity
(aka Plan B)

67
Q

Norgestimate

A

19-nortestosterone

progestin & androgenic activity

68
Q

19-nortestosterone Indications (3)

A
  1. Oral contraceptives
  2. prevention of endometrial hyperplasia in HRT
  3. dysmenorrhea, endometriosus, hirsutism & bleeding when estrogens are contraindicated
69
Q

progesterone derivative indications

A
  1. Oral contraceptives
  2. prevention of endometrial hyperplasia in HRT
  3. dysmenorrhea, endometriosus, hirsutism & bleeding when estrogens are contraindicated
70
Q

19-nortestosterone & progesterone derivative indications

A

possible increase in BP

high dose progestin therapy may reduce plasma HDL levels, esp the estranes

71
Q

Mifepristone MOA

A

blocks progestin binding to the PROGESTERONE receptor
(aka RU 486)
also ANTAGONIZES GLUCOCORTICOID RECEPTOR

72
Q

Mifepristone indications/therapeutic effects

A

pregnancy termination

prevent implantation if administered w/in 72 hours after intercourse

73
Q

Mifepristone adverse effects

A

GI-vomiting, diarrhea, abdominal or pelvic pain, vaginal bleeding

74
Q

Mifepristone contraindications

A

pregnancy or breastfeeding

ppl on glucocorticoids

75
Q

Danazol MOA

A

weak progestin androgen & glucocorticoid that suppresses ovarian fxn

76
Q

Danazol indication

A

endometriosis

77
Q

Danazole adverse effects

A

weight gain, edema, acne & oily skin, hirsutism, deepening voice, HA, flush libido changes, cramps
(C) but (U) fairly mild

78
Q

Danazole contraindications

A

liver dysfunction

pregnant of breast feeding (possibly teratogenic)

79
Q

Combination Oral Contraceptive contents

& the name of the exception

A

estrogen & progestin in various amounts

exception is Drospirenon/ethinyl estradiol

80
Q

Adverse effects of combination oral contraceptives

A

increased breakthrough bleeding esp. during 1st year

hard to tell if you are pregnant

81
Q

Yasmin composition and advantages

A

ethinyl estradiol & drospirenone (mineralcorticoid antagonist)
adv: less water retention-FDA approved for PMDD
very little androgenic properties

82
Q

Natazia MOA

A

uses estradiol valerate to produce E2 in vivo->bioidentical hormones (uses dienogest as progestin, weird 4 cycle regimen)

83
Q

NuvaRing, what is this thing?

A

a vaginal ring containing a 3-week supply of etonogesterel & ethinyl estradiol

84
Q

Progestin-only pills use

A

87-98% effective for birth control

used for adolescents & breast feeding

85
Q

Depo-Provera

A

3-month depot injection of medroxyprogesterone

progestin-only contraceptive

86
Q

Implanon

A

single silastic tube implanted in arm

>99% effective-3 years, progestin-only

87
Q

Mirena

A

Intrauterine contraceptive containing levonorgesterel

99.9% effective-up to 5 years

88
Q

Plan P

A

levonorgestrel-only pill
take w/in 72 hours of intercourse, earlier is better
available without a prescription 18yos & up

89
Q

Mifepristone

A

aka RU-486, Mifeprix

can be used to prevent implantation if administered w/in 72 hours after intercourse

90
Q

(C) adverse effects of combo oral contraceptives

A 
weight gain
nausea
edema
depression
breakthrough bleeding (progestin alone or too little estrogen)
---try different combos
91
Q

other adverse effect of combo oral contraceptives

A

cardio: clotting (esp >35yo smokers), mild HTN, migraine, MI/stroke
Cholestatic jaundice & gallbladder dz
teratogenesis
fertility (can be suppressed for 3+ mos)

92
Q

Combo Oral Contraceptive Benefits

A

effective contraception

dec. risk of ovarian & endometrial CA, ovarian cysts, benign breast dz, ectopic pregnancy, iron deficienct, RA, PMS

93
Q

ABSOLUTE contraindications of combo oral contraceptives

A 
thrombophlebitis
THROMBOEMOLIC PHENOMENA
cardiovascular dos
ESTROGEN-DEPENDENT NEOPLASMS
pregnancy
94
Q

RELATIVE contraindications of combo oral contraceptives

A

LIVER DISEASE, pre-epiphyseal closure, asthma, eczema, migraine, HTN, DM, optic neuritis, retrobular neuritis, seizure dos, >35yos smokers

95
Q

What decreases the effectiveness of oral contraceptives

A 
P450 inducers  (phenytoin, rifamipin, carbamazepine, etc.)
Antibiotics reduce effectiveness of (stop enterohepatic circulation
96
Q

Oral contraceptives decrease effectiveness of:

A

anticoagulants, anticonvulsants, TCAs, guanethidine, oral hypoglycemics

97
Q

Menopause endocrine changes

A

↓ovarian response to gonadotropins
↓ovarian steroids
↑gonadotropins

98
Q

Menopause sxs:

A

Vasomotor, GU, Ostoporosis Hrt Dz

99
Q

Advantages of HRT

A

menopausal symptoms
osteoporosis
heart disease

100
Q

HRT concerns

A

breast CA

strokes

101
Q

General guidelines for HRT

A

10 years after menopause=HRT is not so great

102
Q

Androgens physiological effects (3 categories)

A
  1. Virilizing (androgenic effects): spermatogenesis, sexual development
  2. Anabolic effects: ↑bone density, ↑AA incorporation into muscle, ↑RBC mass, antagonize catabolic effect of glucocorticoids
  3. Puberty: development of 2ndary sexual characteristics in males
103
Q

Androgen uses (4)

A
  1. Men: testicular deficiency
  2. Women: female hypopituitarism (estrogens & androgens)
  3. both sexes: hypoproteinemia of nephrosis
  4. negative nitrogen balance patients

Pharm II final (1 decks)

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