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

Pharm - Estrogens & Progesterone Flashcards

1
Q

What are the natural estrogens?

A

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

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2
Q

What are the 3 synthetic steroidal estrogens?

A

Ethinyl estradiol
Mestranol
Quinestrol

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3
Q

What are the 3 synthetic non-steroidal estrogens?

A

Diethylstilbestrol (DES)
Chlorotrianisene
Methallenestril

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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.

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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.

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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.

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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

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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.

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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
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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

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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.

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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

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13
Q

Indications for estrogen therapy

A

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

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14
Q

Side effects of estrogen therapy

A 
Venous thrombosis
Estrogen alone can cause endometrial hyperplasia, carcinoma
Breakthrough bleeding
Nausea/vomiting
Headache
Breast tenderness
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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
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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

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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

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18
Q

What are side effects of Tamoxifen?

A 
Malignant neoplasm of endometrium
Cataracts
Pulmonary embolism
Hot flash
Abnormal menstruation
Vaginal discharge
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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.

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20
Q

What are the contraindications for SERM treatment?

A 
Pregnancy
Thyroid or adrenal dysfunction
Liver disease
Endometrial carcinoma
Ovarian cysts
Organic intracranial lesion
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21
Q

What is an advantage of Clomiphene over exogenous FSH treatment?

A

Clomiphene is not associated with ovarian hyperstimulation syndrome

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22
Q

What is Raloxifene?

A

A SERM used for prevention and treatment of osteoporosis.

Agonist in bone and antagonist in uterus and breast

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23
Q

What are the side effects of Raloxifene?

A

Retinal vascular occlusion
Venous thromboembolism
Hot flashes
Leg cramps

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24
Q

What are the contraindications for Raloxifene treatment?

A

Pregnancy

History or presence of venous thromboembolism

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25
Q

What effect does Raloxifene have on breast cancer?

A

Raloxifene decreases the risk of invasive breast cancer in postmenopausal women with osteoporosis

26
Q

What is fulvestrant?

A

An estrogen receptor antagonist used for treatment of metastatic breast cancer in postmenopausal women with disease progression after estrogen therapy

27
Q

What are the side effects of fulvestrant?

A 
Nausea
Asthenia (lack of strength)
Pain
Vasodilation (hot flashes)
Headaches
28
Q

What are the aromatase inhibitors?

A

Anastrozole and Letrozole (reversible)

Eemestane and Formestane (irreversible)

29
Q

What are the aromatase inhibitors used for?

A

Treatment and prevention of breast cancer (early stage, locally advanced, and metastatic)

30
Q

What are the side effects of aromatase inhibitors?

A 
Symptoms associated with low estrogen including:
Osteoporotic fractures
Thromboplebitis
Hypercholesterolemia
Profuse vaginal bleeding
31
Q

Compare the effectivity of SERMs and aromatase inhibitors for treating breast cancer

A

Aromatase inhibitors have a better effect on estrogen levels and function and therefore may be more effective that SERMs for treating breast cancer

32
Q

What are the physiologic actions of progesterone?

A 
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
Q

What are the clinical uses of progestins?

A 
Oral contraceptives (alone or in combo with EE)
HRT in menopause
Treatment of dysmenorrhea, oligomenorrhea, endometriosis, and PCOS
34
Q

What are the 3 main categories of oral contraceptives?

A

Progestin-only
Combination oral contraceptives (COCs)
Emergency

35
Q

What are the Progestin only contraceptives?

A

Norgestrel
Norethindrone
Medroxyprogesterone acetate (injectable)
Etonogestrel (implant)

36
Q

What is the mechanism of action for progestin-only contraceptives?

A

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
Q

What are the side effects of progestin-only contraceptives?

A

Irregular periods, breast tenderness

Nausea, dizziness, headaches

38
Q

What are contraindications of treatment with progestin only contraceptives?

A

Acute liver disease
Liver tumors
Known or suspected breast cancer
Pregnancy

39
Q

What is the mechanism of action of combination oral contraceptives?

A

They mimmic negative feedback of E2 and progesterone in the luteal phase of the cycle to down-regulate gonadotropin secretion

40
Q

What are some examples of combination oral contraceptives?

A

Lo/Ovral 28: EE + norgestrel

Yasmin: EE + drospirenone

41
Q

What are some side effects of combination oral contraceptives?

A 
Thrombotic events
Abnormal menstruation, breakthrough bleeding, breast tenderness
Gall bladder disease
Hypertension
Weight gain
42
Q

What are the contraindications for contraindication oral contraceptives?

A

Breast cancer, endometrial cancer
Cerbrovascular or coronary artery disease, thrombotic disorders
Cholestatic jaundice of pregnancy, liver tumors
Smokers over 35 years of age

43
Q

Which progestins have the highest androgenic activity?

A

Norgestrel and levonorgestrel have the highest

Norethindrone has medium activity

44
Q

What is unique about drospirenone?

A

It is a synthetic progestin with anti-androgenic activity

45
Q

How is the risk of DVT minimized with COC treatment?

A

The lowest effective EE dose is used to reduce DVT risk

46
Q

What is the main reason that estrogen is not given alone as contraception?

A

Estrogen is always coadministered with progestin in order to avoid risk for endometrial cancer associated with estrogen activity

47
Q

What is Mifepristone?

A

Progesterone receptor antagonist used for abortion early in pregnancy

48
Q

What are the side effects of Mifepristone?

A

Prolonged bleeding time
Bacterial infections, sepsis
Nausea, vomiting, diarrhea, cramping
Headaches

49
Q

What are the contraindications for Mifepristone?

A

Chronic adrenal failure
Ectopic pregnancy
Hemorrhagic or coagulation disorders
Intrauterine device

50
Q

How does co-administration of misoprostol and mifepristone work?

A

Misoprostol is a prostaglandin analog that stimulates uterine contractions. Increases the efficacy of Mifepristone for abortions.

51
Q

What receptor does Mifepristone have cross-reactivity with?

A

At high levels, Mifepristone blocks glucocorticoid receptors in addition to progesterone receptors

52
Q

What is the minipill?

A

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
Q

What are the adverse effects of the minipill?

A

Nausea, vomiting
Headache, dizziness
Mastalgia

54
Q

What are the early consequences of estrogen deficiency?

A

Vasomotor
Insomnia
Fatigue
Mood changes

55
Q

What are the intermediate consequences of estrogen deficiency?

A

Urogenital atrophy
Urinary incontinence
Genital tract infection
Skin changes

56
Q

What are the long term consequences of estrogen deficiency?

A

Osteoporosis
CV disease
Cognitive effects

57
Q

What are some examples of Hormone replacement therapy preparations?

A

Estrogens
Progesterones
Combination products

58
Q

What are the effects of HRT?

A

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

59
Q

What are some adverse effects of HRT?

A

Estrogen can cause nausea, mastalgia, headache, fluid retention
Progestin can cause weight gain, headaches

60
Q

What risk is associated with long term HRT?

A

Breast cancer risk increased with long term HRT

MHD2/Pharm - Endocrine (7 decks)

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