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Estrogens and Progestins Flashcards

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1
Q

Where are estrogens synthesized?

A

Ovary, liver (from estriol), and peripheral tissue (from androgens)

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2
Q

Where are progestins synthesized?

A

Ovary, testis, adrenal from circulating cholesterol

Placenta during pregnancy

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3
Q

Where are androgens synthesized?

A 
Testis (95%)
Adrenal glands (5%)
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4
Q

What is the more estrogenic/active estrogen?

A

Estradiol 17B (E2)

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5
Q

What are the natural estrogens?

A

Estradiol 17B (E2)
Estrone (E1)
Estriol (E3)

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6
Q

What are the synthetic steroidal estrogens?

A

Ethinyl estradiol
Mestranol
Quinestrol

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7
Q

What are the synthetic non-steroidal estrogens?

A

Diethylstilbestrol (DES)
Chlorotrianisene
Methallenestril

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8
Q

Which cells synthesize and secrete LH and FSH?

A

Gonadotrophs

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9
Q

Action of LH and FSH in females

A

LH stimulates theca cells to synthesize androgen which is aromatized to estrone (E1) and estradiol (E2) in granulosa cells via FSH action

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10
Q

Action of LH and FSH in males

A

LH stimulates testicular Leydig cells to increase the synthesis of testosterone, which diffuses to neighboring sertoli cells

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11
Q

Which cells synthesize and secrete Inhibin A, Inhibin B, and Activin

A

Sertoli cells

Granulosa cells

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12
Q

What is the action of inhibin on the gonadotrophs?

A

inhibits the release of FSH

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13
Q

what is the action of activin on gonadotrophs?

A

stimulates FSH release

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14
Q

What is the enzyme that converts testosterone to estrogen?

A

aromatase

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15
Q

Reproductive actions of estrogen

A 
Growth, development, structural maintenance of primary and secondary female sex characteristics
Changes at puberty
Regulation of menstrual cycle
Growth of uterine endometrium
Secretion of thin cervical mucus
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16
Q

Metabolic actions of estrogen

A 
Increase HDL, decrease LDL
Increase cholesterol saturation of bile
Increase BP via renin
Promote thrombosis (clotting factors)
Decrease bone reabsorption
Increase liver protein synthesis
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17
Q

CNS actions of estrogen

A

Positive effects on mood

Positive effects on cognition and memory

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18
Q

Major clinical uses of estrogens

A

Oral contraceptives
HRT during menopause
HRT for delayed puberty or hypogonadism in women
Rx of perimenopause, dysmenorrhea, oligomenorrhea, delayed puberty
Rx of acne

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19
Q

Estrogen preparations

A 
Conjugated estrogens
Estradiol
Estradiol transdermal
Ethinyl estradiol (syn steroid)
Diethylstilnestrol (DES) (syn non-steroid)
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20
Q

Estrogen indictions

A

Vasomotor symptoms of menopause (flushing)
Vulvar and vaginal atrophy
Female hypoestrogenism secondary to hypogonadism castration or primary ovarian failure
Retard bone loss/ osteoporosis

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21
Q

Estrogen side effects

A 
Nausea and vomiting
Edema
Headache
Breast tenderness
Venous thrombosis
Breakthrough bleeding
Estrogen alone (w/o progesterone) causes endometrial hyperplasia and possible endometrial carcinoma
Increase adenocarcinoma of vagina (DES)
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22
Q

Estrogen contraindications

A 
Breast and endometrial cancers
Cerebral vascular coronary artery disease
Benign or malignant liver tumors
Severe hypertension
Pregnancy
Female smokers over 35
Thrombotic disorders
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23
Q

Selective Estrogen Receptor Modulators (SERMs)

A

Tamoxifen
Clomiphene
Raloxifene

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24
Q

Tamoxifen (SERMS) Indication

A

Prevention, palliative, adjuvant therapy for breast cancer (ER+)
pre or post menopausal

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25
Tamoxifen (SERMS) MOA
Estrogen receptor antagonist in the breast tissue, partial agonist in the endometrium and bone
26
Tamoxifen (SERMS) side effects
``` Malignant neoplasm of endometrium Cataract Pulmonary embolism Hot flashes Abnormal menstruation Vaginal discharge ```
27
Tamoxifen (SERMS) contraindication
Deep vein thrombosis or pulmonary embolism | Pregnancy
28
Tamoxifen and endometrial cancer
Tamoxifen is associated with 4-6 fold increase in incidence of endometrial cancer Administered for no more than 5 years to minimize risk
29
Clomiphene (SERMS) indication
Female infertility due to ovulatory disorder
30
Clomiphene (SERMS) MOA
Estrogen receptor antagonist in hypothalamus and pituitary gland, partial agonist in ovaries
31
Clomiphene (SERMS) Side effect
Thromboembolism Ovarian cysts and hypertrophy Flushing and vasomotor symptoms Abdominal discomfort
32
Clomiphene (SERMS) contraindications
``` Pregnancy Thyroid or adrenal dysfunction Liver disease Endometrial carcinoma Ovarian cysts Intracranial lesion ```
33
Benefit of Clomiphene over exogenous FSH
Clomiphene is rarely associated with the ovarian hyperstimulation syndrome
34
Raloxifene (SERMS) Indication
Osteoporosis prevention and treatment
35
Raloxifene (SERMS) MOA
Estrogen receptor agonist in the bone and estrogen receptor antagonist in uterus and breast
36
Raloxifene (SERMS) Side Effects
Retinal vascular occlusion Venous thromboembolism Hot flashes Leg cramps
37
Raloxifene (SERMS) Contraindication
Pregnancy | History or presence of venous thromboembolism
38
What is the effect of Raloxifene on invasive breast cancer?
Decreases the risk of invasive breast cancer is POSTmenopausal women with osteoporosis
39
Estrogen receptor antagonists
Fulvestrant
40
Fulvestrant indications
Rx of estrogen receptor+ metastatic breast cancer in POST menopausal women with disease progression following anti-estrogen therapy (ex. Tamoxifen)
41
Fulvestrant MOA
Competitively inhibits estrogen binding to receptor | Estrogen receptor antagonist
42
Fulvestrant Side Effects
``` Nausea Asthenia (lack of strength) Pain Vasodilation (hot flashes) Headache ```
43
Fulvestrant contraindication
Pregnancy
44
Does fulvestrant have any agonist activity?
NO
45
What is the action of aromatase?
converts testosterone to estrogen
46
Aromatase Inhibitors
Anastrozole Letrozole Exemestane Formestane
47
Aromatase Inhibitors Indications
Treatment and prevention of estrogen receptor positive breast cancer (early, locally advanced, or metastatic)
48
Anastrozole and Letrozole MOA
Competitive inhibitors of aromatase (reversible)
49
Exemestane and Formestane MOA
Irreversible inhibitors of aromatase
50
Aromatase Inhibitor side effects
``` OSTEOPOROTIC FRACTURES Thromboplebitis Hypercholesterolemia Profuse vaginal bleeding Peripheral edema Rash Nausea Arthralgia Bone pain Headache Depression Dyspnea ```
51
Aromatase inhibitors vs. SERMs for the treatment of breast cancer
Aromatase inhibitors may be more effective than SERMs
52
Physiological actions of progesterone
``` Regulation of menstrual cycle Induces secretory uterine endometrium (implantation) Thick, viscous cervical mucus Increases body temperature Maintain pregnancy Development of mammary gland ```
53
Clinical uses of progestins
Oral contraceptives HRT in menopause Dysmenorrhea, oligomenorrhea, endometriosis, PCOS
54
What are the three major types of oral contraceptives?
Progestin only Combination (estrogen + progesteron) Emergency
55
Progestin only contraceptives
Norgestrel Norethindrone Medroxyprogesterone acetate Etonogestrel
56
Progestin only contraceptives indication
Contraception
57
Progestin only contraceptives MOA
Alter frequency of GnRH pulsing and and decrease anterior pituitary gland responsiveness to GnRH Alter tubal peristalsis, endometrial receptivity, cervical mucus secretions
58
Progestin only contraceptives Side Effects
``` Irregular periods Breast tenderness Nausea Dizziness Headaches ```
59
Progestin only contraceptives Contraindications
Acute liver disease Benign or malignant liver tumors Known or suspected breast cancer Pregnancy
60
Route of administration of progestin only contraceptives
Medroxyprogesterone: given parenterally every 3 months Etonogestrel (implant): effective for 3 years Levonogestrel (oral): emergency contraception
61
Estrogen-Progestin Combinations
Estrogens: Ethinyl estradiol, mestranol Progestins: Norgestrel, Levonorhestrel, Norethindrone, Norethindrone acetate, Ethynodiol, Norgestimate, Gestodene, Desogestrel, Drospirenone Combo OC: EE+ norgestrel EE+ drospirenone
62
Estrogen-Progestin Combinations Indications
Contraception
63
Estrogen-Progestin Combinations MOA
Suppress GnRH, LH and FSH secretion and follicular development, inhibit ovulation Alter tubal peristalsis, endometrial receptivity and cervical mucus secretions
64
Estrogen-Progestin Combinations Side Effects
``` Arterial and venous thromboembolism Pulmonary embolism Cerebral thrombosis Gallbladder disease Hypertension Hepatic neoplasm Abnormal menstruation Breakthrough bleeding Breast tenderness Bloating Migraine Weight change ```
65
Estrogen-Progestin Combinations Contraindications
``` Breast cancer Endometrial cancer Estrogen dependent neoplasms Cerebral vascular or CAD Cholestatic jaundice Liver tumors Severe hypertension Prolonged immobilization Pregnancy Female smokers >35 Thrombotic disorders ```
66
Which progestins have the highest androgenic activity?
Norgestrel and levonorgestrel
67
Progesterone Receptor Antagonist
Mifepristone (RU-486)
68
Mifepristone (Progesterone Receptor Antagonist) Indication
Abortion (through day 49)
69
Mifepristone (Progesterone Receptor Antagonist) MOA
Inhibits progesterone binding to receptor
70
Mifepristone (Progesterone Receptor Antagonist) Side Effects
``` Prolonged bleeding Bacterial infections Sepsis N/V/D Cramps Headache ```
71
Mifepristone (Progesterone Receptor Antagonist) Contraindications
``` Chronic adrenal failure Ectopic pregnancy Hemorrhagic disorders Anticoagulation therapy IUD ```
72
Emergency (morning after) contraception indication
Medication to prevent unwanted pregnancy after unprotected intercourse
73
Emergency (morning after) contraception
Two doses of "minipill" | 0.75 mg of levonorgestrel (12 hrs)
74
Emergency (morning after) contraception MOA
Potent progestin, blocks the LH surge, disrupting normal ovulation, produces endometrial changes for implantation
75
Emergency (morning after) contraception timing
Take first dose within 72 hours of intercourse, 2nd dose 12 hours after 1st dose
76
Emergency (morning after) contraception side effects
N/V Headache Dizziness Mastalgia
77
Indications for HRT
Vasomotor instability Mood changes Urogenital atrophy Osteoporosis
78
HRT preparations
``` Conjugated equine estrogens Micronized estradiol Conjugated synthetic estrogens Transdermal estrogens Vaginal ring Medroxyprogesterone Micronized progesterone Combination products (E+P) ```
79
Effects of HRT
Relief from vasomotor symptoms, urogenital atrophy, recurrent urinary symptoms Relief from fatigue, depression Maintenance of bone density
80
HRT Side Effects
E: nausea, mastalgia (breast pain), headache, fluid retention P: weight gain, headache
81
Estrogen alone associated with ____ risk of endometrial carcinoma
5-8 x increase

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