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Pharm II Test 3 > Estrogens & Progestins > Flashcards

Estrogens & Progestins Flashcards

1
Q

Conjugated Estrogen, Estradiol, Transdermal Estradiol, Ethinyl estradiol, Diethylstilbertrol/DES- Mech of Action

A

acts as estrogen

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2
Q

Conjugated Estrogen, Estradiol, Transdermal Estradiol, Ethinyl estradiol, Diethylstilbertrol/DES- Clinical Use

A

Vasomotor symptoms of menopause
vulvar and vaginal atrophy
female hypoestrogenism secondary to hypogonadism, castration, or primary ovarian failure
in combination to retard bone loss in osteoporosis

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3
Q

Conjugated Estrogen, Estradiol, Transdermal Estradiol, Ethinyl estradiol, Diethylstilbertrol/DES- Adverse Effects/Contraindications

A

Nausea, vomiting, edema, headache, breast tenderness, venous thrombosis, breakthrough bleeding

Estrogen alone causes endometrial hyperplasia and increases risk of carcinoma

Contraindicated in breast and endometrial cancer, cerebral vascular coronary artery disease, benign or malignant liver tumors, severe hypertension, pregnancy, smokers over 35, thrombotic disorders

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4
Q

Selective Estrogen Receptor Modulators- SERMS- Available Drugs

A

Tamoxifen
Clomiphene
Raloxifene

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5
Q

Estrogens- Available Drugs

A 
Conjugated estrogen
Estradiol
Transdermal estradiol
Ethinyl estradiol (steroidal synthetic)
Diethylstilbertrol/DES (non-steroidal synthetic)
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6
Q

Tamoxifen- Mech of Action

A

Estrogen receptor antagonist in breast tissue

Estrogen receptor partial agonist in endometrium and bone

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7
Q

Tamoxifen- Clinical Use

A

prevention, palliative, and adjuvant therapy for breast cancer

not given for any more than 5 years to reduce the chance of causing cancer

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8
Q

Tamoxifen- Adverse Effects/Contraindications

A 
malignant neoplasm of endometrium
cataracts
pulmonary embolism
hot flashes
abnormal menstruation
vaginal discharge

Contraindicated in hx of DVT or PE, pregnancy

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9
Q

Comiphene- Mech of Action

A

Estrogen receptor antagonist in hypothalamus and pituitary

Partial agonist in ovaries

Disinhibits GnRH, FSH, and LH release

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10
Q

Comiphene- Clinical Use

A

female infertility due to ovulatory disorder

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11
Q

Comiphene- Adverse Effects/Contraindications

A

Thromboembolism
ovarian cysts and hypertrophy
flushing and vasomotor symptoms
abdominal discomfort

Contraindicated in pregnancy, thyroid or adrenal dysfunction, liver disease, endometrial carcinoma, ovarian cysts organic intracranial lesion

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12
Q

Raloxifene- Mech of Action

A

Estrogen receptor agonist in bone

Antagonist in uterus and breast

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13
Q

Raloxifene- Clinical Use

A

prevention and treatment of osteoporosis

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14
Q

Raloxifene- Adverse Effects/Contraindications

A

retinal vascular occlusion
venous thromboembolism
hot flashes
leg cramps

Contraindicated in pregnancy and history of venous thromboembolism

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15
Q

Fulvestrant- Mech of Action

A

Complete estrogen receptor antagonist

NO agonist activity

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16
Q

Fulvestrant- Clinical Use

A

treatment of estrogen receptor positive metastatic breast cancer in post-menopausal women with disease progression following anti-estrogen therapy (Tamoxifen)

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17
Q

Fulvestrant- Adverse Effects/Contraindications

A 
nausea
asthenia
pain
vasodilation (hot flashes)
headache

Contraindicated in pregnancy

18
Q

Aromatase Inhibitors- Available Drugs

A

Anastrozole
Letrozole
Exemestane
Formestane

19
Q

Anastrozole, Letrozole- Mech of Action

A

competitive inhibitor of aromatase

prevent estrogen formation from androgens

20
Q

Aromatase Inhibitors- Clinical Use

A

treatment and prevention of estrogen receptor positive breast cancer (early stage, locally advanced, and metastatic)

may be more effective than SERMs

21
Q

Aromatase Inhibitors- Adverse Effects/Contraindications

A 
OSTEOPOROTIC FRACTURES
thrombophlebitis
hypercholesterolemia
profuse vaginal bleeding
peripheral edema
rash 
nausea
arthralgia
bone pain
headache 
depression
dyspnea

Contraindicated in hypersensitivity

22
Q

Exemestane, Formestane- Mech of Action

A

Irreversible inhibitors of aromatase

prevent estrogen formation from androgens

23
Q

Progestin Only Contraceptives- Available Drugs

A 
Norgestrel
Norethindrone
Medroxyprogesterone acetate (injectable)
Etonogestrel (implant)
Levonorgestrel
24
Q

Norgestrel, Norethindrone, Medroxyprogesterone acetate, Etonogestral- Mech of Action

A

alter frequency of GnRH pulsing and decrease anterior pituitary responsiveness to GnRH

alter tubal peristalsis, endometrial receptivity, and cervical mucus secretions

25
Q

Norgestrel, Norethindrone, Medroxyprogesterone acetate, Etonogestral- Clinical Use

A

contraception

26
Q

Norgestrel, Norethindrone, Medroxyprogesterone acetate, Etonogestral- Adverse Effects/Contraindications

A 
irregular periods
breast tenderness
nausea
dizziness
headaches

Contraindicated in acute liver disease, liver tumors, known or suspected breast cancer, pregnancy

27
Q

Levonorgestrel- Mech of Action

A

Block LH surge, disrupt normal ovulation, produce endometrial changes to prevent implantation

28
Q

Levonorgestrel- Absorption, Distribution

A

Two doses separated by 12 hrs

First dose w/i 72 hrs of intercourse

29
Q

Levonorgestrel- Clinical Use

A

Emergency Contraception

30
Q

Levonorgestrel- Adverse Effects/Contraindications

A 
Nausea
vomiting
headache
dizziness
mastalgia
31
Q

Combination Oral Contraceptives- Available Drugs

A

Estrogens:
Ethinyl estradiol
Mestranol

Progestins:
Norgestrel 
Levonorgestrel
Norethindrone
Norethindrone acetate
Ethynodiol
Norgestimate
Gestodene
Desogestrel
Drospirenone
32
Q

Combination Oral Contraceptives- Mech of Action

A

Suppress GnRH, LH, and FSH secretion and follicular development, thus inhibiting ovulation

Alter tubal peristalsis, endometrial receptivity, and cervical mucus secretions

33
Q

Combination Oral Contraceptives- Absorption, Distribution

A

PO
patches
vaginal rings

34
Q

Combination Oral Contraceptives- Clinical Use

A

contraception

35
Q

Combination Oral Contraceptives- Adverse Effects/Contraindications

A 
thromboembolism
PE
cerebral thrombosis
gallbladder menstruation
breakthrough bleeding
breast tenderness
bloating 
migraine
weight change

contraindicated in breast or endometrial cancer, cerebral vascular or coronary artery disease, jaundice, liver tumors, severe hypertension, prolonged immobilization, pregnancy, smokers over 35, thrombotic disorders

36
Q

Progesterone Receptor Antagonist- Available Drugs

A

Milfepristone (RU-486)

37
Q

Milfepristone (RU-486)- Mech of Action

A

inhibit progesterone binding to receptor

38
Q

Milfepristone (RU-486)- Clinical Use

A

abortion

administered w/ Misoprostol to stimulate uterine contractions

39
Q

Milfepristone (RU-486)- Adverse Effects/Contraindications

A 
prolonged bleeding time
bacterial infections
sepsis
nausea
vomiting
diarrhea
cramps
headache

contraindicated in adrenal failure, ectopic pregnancy, hemorrhagic disorders, anticoagulation therapy, inherited porphyrias, IUD, undiagnosed adnexal mass

40
Q

Hormone Replacement Therapy- Available Drugs

A 
conjugated equine estrogen
micronized estradiol
conjugated synthetic estrogens
transdermal estrogens
vaginal rings
medroxyprogesterone
micronized progesterone
combinations
41
Q

Hormone Replacement Therapy- Clinical Use

A

vasomotor instability
mood changes
urogenital atrophy
osteoporosis

42
Q

Hormone Replacement Therapy- Adverse Effects/Contraindications

A 
Estrogens:
nausea
mastalgia
headache
fluid retention
cancer (?)

Progestins:
weight gain
headache

contraindicated in breast or endometrial cancer, cerebral vascular or coronary artery disease, jaundice, liver tumors, severe hypertension, prolonged immobilization, pregnancy, smokers over 35, thrombotic disorders

Pharm II Test 3 (9 decks)

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