Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm > Estrogens and Progestins > Flashcards

Estrogens and Progestins Flashcards

1
Q

Where are estrogens synthesized?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Where are progestins synthesized?

A

Ovary, testis, adrenal from circulating cholesterol

Placenta during pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Where are androgens synthesized?

A 
Testis (95%)
Adrenal glands (5%)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is the more estrogenic/active estrogen?

A

Estradiol 17B (E2)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are the natural estrogens?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are the synthetic steroidal estrogens?

A

Ethinyl estradiol
Mestranol
Quinestrol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the synthetic non-steroidal estrogens?

A

Diethylstilbestrol (DES)
Chlorotrianisene
Methallenestril

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Which cells synthesize and secrete LH and FSH?

A

Gonadotrophs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

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

A

Sertoli cells

Granulosa cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is the action of inhibin on the gonadotrophs?

A

inhibits the release of FSH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

what is the action of activin on gonadotrophs?

A

stimulates FSH release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is the enzyme that converts testosterone to estrogen?

A

aromatase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

CNS actions of estrogen

A

Positive effects on mood

Positive effects on cognition and memory

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Estrogen preparations

A 
Conjugated estrogens
Estradiol
Estradiol transdermal
Ethinyl estradiol (syn steroid)
Diethylstilnestrol (DES) (syn non-steroid)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Selective Estrogen Receptor Modulators (SERMs)

A

Tamoxifen
Clomiphene
Raloxifene

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Tamoxifen (SERMS) Indication

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Tamoxifen (SERMS) MOA

A

Estrogen receptor antagonist in the breast tissue, partial agonist in the endometrium and bone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Tamoxifen (SERMS) side effects

A 
Malignant neoplasm of endometrium
Cataract
Pulmonary embolism
Hot flashes
Abnormal menstruation
Vaginal discharge
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Tamoxifen (SERMS) contraindication

A

Deep vein thrombosis or pulmonary embolism

Pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Tamoxifen and endometrial cancer

A

Tamoxifen is associated with 4-6 fold increase in incidence of endometrial cancer
Administered for no more than 5 years to minimize risk

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Clomiphene (SERMS) indication

A

Female infertility due to ovulatory disorder

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Clomiphene (SERMS) MOA

A

Estrogen receptor antagonist in hypothalamus and pituitary gland, partial agonist in ovaries

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Clomiphene (SERMS) Side effect

A

Thromboembolism
Ovarian cysts and hypertrophy
Flushing and vasomotor symptoms
Abdominal discomfort

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Clomiphene (SERMS) contraindications

A 
Pregnancy
Thyroid or adrenal dysfunction
Liver disease
Endometrial carcinoma
Ovarian cysts
Intracranial lesion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Benefit of Clomiphene over exogenous FSH

A

Clomiphene is rarely associated with the ovarian hyperstimulation syndrome

34
Q

Raloxifene (SERMS) Indication

A

Osteoporosis prevention and treatment

35
Q

Raloxifene (SERMS) MOA

A

Estrogen receptor agonist in the bone and estrogen receptor antagonist in uterus and breast

36
Q

Raloxifene (SERMS) Side Effects

A

Retinal vascular occlusion
Venous thromboembolism
Hot flashes
Leg cramps

37
Q

Raloxifene (SERMS) Contraindication

A

Pregnancy

History or presence of venous thromboembolism

38
Q

What is the effect of Raloxifene on invasive breast cancer?

A

Decreases the risk of invasive breast cancer is POSTmenopausal women with osteoporosis

39
Q

Estrogen receptor antagonists

A

Fulvestrant

40
Q

Fulvestrant indications

A

Rx of estrogen receptor+ metastatic breast cancer in POST menopausal women with disease progression following anti-estrogen therapy (ex. Tamoxifen)

41
Q

Fulvestrant MOA

A

Competitively inhibits estrogen binding to receptor

Estrogen receptor antagonist

42
Q

Fulvestrant Side Effects

A 
Nausea
Asthenia (lack of strength)
Pain
Vasodilation (hot flashes)
Headache
43
Q

Fulvestrant contraindication

A

Pregnancy

44
Q

Does fulvestrant have any agonist activity?

A

NO

45
Q

What is the action of aromatase?

A

converts testosterone to estrogen

46
Q

Aromatase Inhibitors

A

Anastrozole
Letrozole
Exemestane
Formestane

47
Q

Aromatase Inhibitors Indications

A

Treatment and prevention of estrogen receptor positive breast cancer (early, locally advanced, or metastatic)

48
Q

Anastrozole and Letrozole MOA

A

Competitive inhibitors of aromatase (reversible)

49
Q

Exemestane and Formestane MOA

A

Irreversible inhibitors of aromatase

50
Q

Aromatase Inhibitor side effects

A 
OSTEOPOROTIC FRACTURES
Thromboplebitis
Hypercholesterolemia
Profuse vaginal bleeding
Peripheral edema
Rash
Nausea
Arthralgia
Bone pain
Headache
Depression
Dyspnea
51
Q

Aromatase inhibitors vs. SERMs for the treatment of breast cancer

A

Aromatase inhibitors may be more effective than SERMs

52
Q

Physiological actions of progesterone

A 
Regulation of menstrual cycle
Induces secretory uterine endometrium (implantation)
Thick, viscous cervical mucus
Increases body temperature
Maintain pregnancy
Development of mammary gland
53
Q

Clinical uses of progestins

A

Oral contraceptives
HRT in menopause
Dysmenorrhea, oligomenorrhea, endometriosis, PCOS

54
Q

What are the three major types of oral contraceptives?

A

Progestin only
Combination (estrogen + progesteron)
Emergency

55
Q

Progestin only contraceptives

A

Norgestrel
Norethindrone
Medroxyprogesterone acetate
Etonogestrel

56
Q

Progestin only contraceptives indication

A

Contraception

57
Q

Progestin only contraceptives MOA

A

Alter frequency of GnRH pulsing and and decrease anterior pituitary gland responsiveness to GnRH
Alter tubal peristalsis, endometrial receptivity, cervical mucus secretions

58
Q

Progestin only contraceptives Side Effects

A 
Irregular periods
Breast tenderness
Nausea
Dizziness
Headaches
59
Q

Progestin only contraceptives Contraindications

A

Acute liver disease
Benign or malignant liver tumors
Known or suspected breast cancer
Pregnancy

60
Q

Route of administration of progestin only contraceptives

A

Medroxyprogesterone: given parenterally every 3 months

Etonogestrel (implant): effective for 3 years

Levonogestrel (oral): emergency contraception

61
Q

Estrogen-Progestin Combinations

A

Estrogens: Ethinyl estradiol, mestranol

Progestins: Norgestrel, Levonorhestrel, Norethindrone, Norethindrone acetate, Ethynodiol, Norgestimate, Gestodene, Desogestrel, Drospirenone

Combo OC:
EE+ norgestrel
EE+ drospirenone

62
Q

Estrogen-Progestin Combinations Indications

A

Contraception

63
Q

Estrogen-Progestin Combinations MOA

A

Suppress GnRH, LH and FSH secretion and follicular development, inhibit ovulation

Alter tubal peristalsis, endometrial receptivity and cervical mucus secretions

64
Q

Estrogen-Progestin Combinations Side Effects

A 
Arterial and venous thromboembolism
Pulmonary embolism
Cerebral thrombosis
Gallbladder disease
Hypertension
Hepatic neoplasm
Abnormal menstruation
Breakthrough bleeding
Breast tenderness
Bloating
Migraine
Weight change
65
Q

Estrogen-Progestin Combinations Contraindications

A 
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
Q

Which progestins have the highest androgenic activity?

A

Norgestrel and levonorgestrel

67
Q

Progesterone Receptor Antagonist

A

Mifepristone (RU-486)

68
Q

Mifepristone (Progesterone Receptor Antagonist) Indication

A

Abortion (through day 49)

69
Q

Mifepristone (Progesterone Receptor Antagonist) MOA

A

Inhibits progesterone binding to receptor

70
Q

Mifepristone (Progesterone Receptor Antagonist) Side Effects

A 
Prolonged bleeding
Bacterial infections
Sepsis
N/V/D
Cramps
Headache
71
Q

Mifepristone (Progesterone Receptor Antagonist) Contraindications

A 
Chronic adrenal failure
Ectopic pregnancy
Hemorrhagic disorders
Anticoagulation therapy
IUD
72
Q

Emergency (morning after) contraception indication

A

Medication to prevent unwanted pregnancy after unprotected intercourse

73
Q

Emergency (morning after) contraception

A

Two doses of “minipill”

0.75 mg of levonorgestrel (12 hrs)

74
Q

Emergency (morning after) contraception MOA

A

Potent progestin, blocks the LH surge, disrupting normal ovulation, produces endometrial changes for implantation

75
Q

Emergency (morning after) contraception timing

A

Take first dose within 72 hours of intercourse, 2nd dose 12 hours after 1st dose

76
Q

Emergency (morning after) contraception side effects

A

N/V
Headache
Dizziness
Mastalgia

77
Q

Indications for HRT

A

Vasomotor instability
Mood changes
Urogenital atrophy
Osteoporosis

78
Q

HRT preparations

A 
Conjugated equine estrogens
Micronized estradiol
Conjugated synthetic estrogens
Transdermal estrogens
Vaginal ring
Medroxyprogesterone
Micronized progesterone 
Combination products (E+P)
79
Q

Effects of HRT

A

Relief from vasomotor symptoms, urogenital atrophy, recurrent urinary symptoms
Relief from fatigue, depression
Maintenance of bone density

80
Q

HRT Side Effects

A

E: nausea, mastalgia (breast pain), headache, fluid retention
P: weight gain, headache

81
Q

Estrogen alone associated with ____ risk of endometrial carcinoma

A

5-8 x increase

Pharm (20 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions