Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

MHD2/Pharm - Endocrine > Pharm - Estrogens & Progesterone > Flashcards

Pharm - Estrogens & Progesterone Flashcards

(60 cards)

Start Studying
1
Q

What are the natural estrogens?

A

E2: estradiol, the most estrogenic
E1: estrone, less estrogenic
E3: estriol, low activity, metabolite of E2

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

What are the 3 synthetic steroidal estrogens?

A

Ethinyl estradiol
Mestranol
Quinestrol

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

What are the 3 synthetic non-steroidal estrogens?

A

Diethylstilbestrol (DES)
Chlorotrianisene
Methallenestril

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

What is the role of activin and inhibin?

A

Both are produced by sertoli and granulosa cells. Inhibins inhibit the release of FSH, activins stimulate the release of FSH.

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

How does estrogen production differ between the follicular and luteal phase of the menstrual cycle?

A

During the follicular phase, estrogen comes from ovarian follicles. During the luteal phase, estrogen comes from the corpus luteum. In both cases, aromatase produces estrogen from androgens.

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

Describe the mechanism of action of estrogen

A

Estrogen travels through blood bound to SHBG
It diffuses into cells and binds to its receptor in the cytoplasm
Estrogen-receptor complexes dimerize in the nucleus and bind to Estrogen receptor elements of DNA to promote or inhibit transcription of specific genes.

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

Reproductive functions of estrogen

A

Female sexual maturation, maintenance of sex characteristics
Neuroendocrine regulation of menstruation, endometrial growth during cycle
Secretion of thin cervical mucus

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

What is the difference in effect on cervical mucus between estrogen and progesterone?

A

Estrogen causes secretion of thin cervical mucus, which promotes migration of the ovum and the sperm. Progesterone makes the cervix secrete thick cervical mucus.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are the metabolic functions of estrogen?

A 
Increase HDL, decreases LDL 
Increase cholesterol saturation of bile
Increase BP via renin substrate
Promote thrombosis
Decrease bone reabsorption
Increased liver protein synthesis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What are the higher CNS functions of estrogen?

A

Positive effect on mood, cognition/memory (neurotrophic), and protective from ischemia and neurodegenerative disorders

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

What is the route of administration for estrogen?

A

Well absorbed orally and transdermally. There is significant first pass metabolism with oral administration.

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

Major clinical uses of estrogens

A

Oral contraceptives (Ethinyl estradiol)
Hormone replacement therapy for menopause, delayed puberty, hypogonadism
Treatment for menopause transition years
Treatment of acne

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

Indications for estrogen therapy

A

Vasomotor symptoms of menopause
Vulvar and vaginal atrophy
Female hypoestrogenism
Combinations to slow bone loss and osteoporosis

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

Side effects of estrogen therapy

A 
Venous thrombosis
Estrogen alone can cause endometrial hyperplasia, carcinoma
Breakthrough bleeding
Nausea/vomiting
Headache
Breast tenderness
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Contraindications for estrogen therapy

A 
Breast and endometrial cancers
Cerebral vascular coronary artery disease
Liver tumor disease
Severe hypertension
Pregnancy
Female smokers over 35 yo
Thrombotic disorders
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are SERMs?

A

Selective Estrogen Receptor Modulators

Act as antagonists in some tissues and agonists in other tissues due to estrogen receptor subtype selectivity

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

What is Tamoxifen?

A

A SERM used for prevention, palliation and adjuvant therapy for breast cancer.
Antagonist in breast tissue, and partial agonist in endometrium and bone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What are side effects of Tamoxifen?

A 
Malignant neoplasm of endometrium
Cataracts
Pulmonary embolism
Hot flash
Abnormal menstruation
Vaginal discharge
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What is Clomiphene?

A

A SERM used for female infertility due to ovulatory disorder
Antagonist in the hypothalamus and pituitary (blocks negative feedback) and partial agonist in the ovaries. Increases LH and FSH to stimulate ovulation.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What are the contraindications for SERM treatment?

A 
Pregnancy
Thyroid or adrenal dysfunction
Liver disease
Endometrial carcinoma
Ovarian cysts
Organic intracranial lesion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What is an advantage of Clomiphene over exogenous FSH treatment?

A

Clomiphene is not associated with ovarian hyperstimulation syndrome

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What is Raloxifene?

A

A SERM used for prevention and treatment of osteoporosis.

Agonist in bone and antagonist in uterus and breast

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

What are the side effects of Raloxifene?

A

Retinal vascular occlusion
Venous thromboembolism
Hot flashes
Leg cramps

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

What are the contraindications for Raloxifene treatment?

A

Pregnancy

History or presence of venous thromboembolism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
What effect does Raloxifene have on breast cancer?
Raloxifene decreases the risk of invasive breast cancer in postmenopausal women with osteoporosis
26
What is fulvestrant?
An estrogen receptor antagonist used for treatment of metastatic breast cancer in postmenopausal women with disease progression after estrogen therapy
27
What are the side effects of fulvestrant?
``` Nausea Asthenia (lack of strength) Pain Vasodilation (hot flashes) Headaches ```
28
What are the aromatase inhibitors?
Anastrozole and Letrozole (reversible) | Eemestane and Formestane (irreversible)
29
What are the aromatase inhibitors used for?
Treatment and prevention of breast cancer (early stage, locally advanced, and metastatic)
30
What are the side effects of aromatase inhibitors?
``` Symptoms associated with low estrogen including: Osteoporotic fractures Thromboplebitis Hypercholesterolemia Profuse vaginal bleeding ```
31
Compare the effectivity of SERMs and aromatase inhibitors for treating breast cancer
Aromatase inhibitors have a better effect on estrogen levels and function and therefore may be more effective that SERMs for treating breast cancer
32
What are the physiologic actions of progesterone?
``` Regulation of the menstrual cycle Induces secretory uterine endometrium Causes thick cervical mucus Increases body temperature Essential for maintainence of pregnancy and development of mammary glands ```
33
What are the clinical uses of progestins?
``` Oral contraceptives (alone or in combo with EE) HRT in menopause Treatment of dysmenorrhea, oligomenorrhea, endometriosis, and PCOS ```
34
What are the 3 main categories of oral contraceptives?
Progestin-only Combination oral contraceptives (COCs) Emergency
35
What are the Progestin only contraceptives?
Norgestrel Norethindrone Medroxyprogesterone acetate (injectable) Etonogestrel (implant)
36
What is the mechanism of action for progestin-only contraceptives?
Alters the frequency of GnRH pulsing and decreases the anterior pituitary responsiveness to GnRH Also interferes with tubal peristalsis, endometrial receptivity and mucus secretions
37
What are the side effects of progestin-only contraceptives?
Irregular periods, breast tenderness | Nausea, dizziness, headaches
38
What are contraindications of treatment with progestin only contraceptives?
Acute liver disease Liver tumors Known or suspected breast cancer Pregnancy
39
What is the mechanism of action of combination oral contraceptives?
They mimmic negative feedback of E2 and progesterone in the luteal phase of the cycle to down-regulate gonadotropin secretion
40
What are some examples of combination oral contraceptives?
Lo/Ovral 28: EE + norgestrel | Yasmin: EE + drospirenone
41
What are some side effects of combination oral contraceptives?
``` Thrombotic events Abnormal menstruation, breakthrough bleeding, breast tenderness Gall bladder disease Hypertension Weight gain ```
42
What are the contraindications for contraindication oral contraceptives?
Breast cancer, endometrial cancer Cerbrovascular or coronary artery disease, thrombotic disorders Cholestatic jaundice of pregnancy, liver tumors Smokers over 35 years of age
43
Which progestins have the highest androgenic activity?
Norgestrel and levonorgestrel have the highest | Norethindrone has medium activity
44
What is unique about drospirenone?
It is a synthetic progestin with anti-androgenic activity
45
How is the risk of DVT minimized with COC treatment?
The lowest effective EE dose is used to reduce DVT risk
46
What is the main reason that estrogen is not given alone as contraception?
Estrogen is always coadministered with progestin in order to avoid risk for endometrial cancer associated with estrogen activity
47
What is Mifepristone?
Progesterone receptor antagonist used for abortion early in pregnancy
48
What are the side effects of Mifepristone?
Prolonged bleeding time Bacterial infections, sepsis Nausea, vomiting, diarrhea, cramping Headaches
49
What are the contraindications for Mifepristone?
Chronic adrenal failure Ectopic pregnancy Hemorrhagic or coagulation disorders Intrauterine device
50
How does co-administration of misoprostol and mifepristone work?
Misoprostol is a prostaglandin analog that stimulates uterine contractions. Increases the efficacy of Mifepristone for abortions.
51
What receptor does Mifepristone have cross-reactivity with?
At high levels, Mifepristone blocks glucocorticoid receptors in addition to progesterone receptors
52
What is the minipill?
Emergency/Morning after contraception 2 doses of levonorgestrel (a potent progestin) separated by 12 hours, the first of which should be 72 hours after intercourse Prevents ovulation and impairs sperm transport and endometrial receptivity
53
What are the adverse effects of the minipill?
Nausea, vomiting Headache, dizziness Mastalgia
54
What are the early consequences of estrogen deficiency?
Vasomotor Insomnia Fatigue Mood changes
55
What are the intermediate consequences of estrogen deficiency?
Urogenital atrophy Urinary incontinence Genital tract infection Skin changes
56
What are the long term consequences of estrogen deficiency?
Osteoporosis CV disease Cognitive effects
57
What are some examples of Hormone replacement therapy preparations?
Estrogens Progesterones Combination products
58
What are the effects of HRT?
Relief from vasomotor symptoms, urogenital atrophy and recurrent urinary symptoms Relief from fatigue, depression Maintenance of bone mineral density
59
What are some adverse effects of HRT?
Estrogen can cause nausea, mastalgia, headache, fluid retention Progestin can cause weight gain, headaches
60
What risk is associated with long term HRT?
Breast cancer risk increased with long term HRT

MHD2/Pharm - Endocrine (7 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions