Chapter 50: Estrogens And Progestins

Question 1

Estrogens and Progestins

Answer 1

Hormones with multiple actions
Promote female maturation
Help regulate ongoing activity of female reproductive organs
Estrogens affect bone mineralization and lipid metabolism
Principal endogenous estrogen is estradiol; principal progestational hormone is progesterone

Question 2

The menstrual cycle

Answer 2

Full cycle typically takes 28 days
Follicular phase: 1st half of the cycle (days 1-14)
Lu teal phase: 2nd half of the cycle

Coordinating ovarian and uterine events ->
Uterine changes are brought about under the influence of estrogens and progesterone ->
AP hormones, FSH, and LH regulate the menstrual cycle

Question 3

Estrogens -female production

Answer 3

Ovary is the principal organ
Follicles, then corpus luteum

Placenta produces large amounts during pregnancy
Major estrogen produced is estradiol

Question 4

Estrogens: effect on primary and secondary sex characteristics

Answer 4

Reproductive tract and secondary sex characteristics
Physiologic processes related to reproduction:
Ductal growth in the breast
Thickening and cornification of the vaginal epithelium
Proliferation of the uterine epithelium
Copious secretion of thickened mucus from endocervical glands

Question 5

Estrogens metabolic actions

Answer 5

Positive effect on bone mass
Favorable effects on cholesterol levels
Blood coagulation increased

Question 6

Estrogens ADR

Answer 6

Endometrial hyperplasia and carcinoma
Promotes growth of existing breast cancer
Ovarian cancer
Cardiovascular events
Nausea
Others: Gallbladder disease, jaundice, headache, and chloasma

Question 7

Estrogens therapeutic uses

Answer 7

Menopausal hormone
Female hypogonadism
Acne

Question 8

Estrogens routes

Answer 8

Oral
Transdermal
Intravaginal
Parenteral

Question 9

Phytoestrogens

Answer 9

plant base compound with weak estrogen if activity. Not s potent as estradiol but have the same risks and ADRs. If you’re going to use, get from whole food sources. 40-80 mg is typically dose

Question 10

Selective Estrogen Receptor Modulators (SERMs)

Answer 10

Activate in some tissues and block estrogen receptors selectively in others
Developed to provide benefits of estrogen while avoiding the drawbacks
Three available: tamoxifen, toremifene, and raloxifene
None of these offers all the benefits of estrogen and avoids all the drawbacks
Fbazedoxifone (duavee)

Question 11

Tamoxifen [Nolvadex]

Answer 11

blocks estrogen -> Breast cancer treatment: Inhibits cell growth in the breast, Produces hot flashes

activates estrogen -> Protects against osteoporosis
Risk for endometrial cancer and thromboembolism

Question 12

Raloxifene [Evista]

Answer 12

Does not activate estrogen in endometrium
Protects against breast cancer, osteoporosis
Promotes thromboembolism
Induces hot flashes

Question 13

Duavee (conjugated estrogens/bazedoxifene)

Answer 13

First drug to combine estrogen with an estrogen agonist/antagonist (bazedoxifene)
Bazedoxifene component reduces the risk of excessive growth of the uterine lining posed by the estrogen component
Contraindications are the same as for other products containing estrogen
Drug should be used for the shortest duration possible

Question 14

Progestins

Answer 14

Compounds that act like progesterone
Principal endogenous progestational hormone
Produced by ovaries and placenta

Question 15

Progestins ADR

Answer 15

Teratogenic effects
Gynecologic effects
Breast cancer
Depression
Breast tenderness
Bloating

Question 16

Progestins therapeutic uses

Answer 16

Postmenopausal hormone therapy
Dysfunctional uterine bleeding
Amenorrhea
Infertility
Prematurity prevention
Endometrial carcinoma and hyperplasia

Question 17

Menopausal Hormone Therapy Benefits

Answer 17

Relief of vasomotor symptoms
Management of urogenital atrophy
Prevention of osteoporosis and related fractures
Cardioprotection
Prevention of colorectal cancer
Positive effect on wound healing
Tooth retention
Glycemic control
Physiologic doses of estrogen (with or without progestin)
Taken to manage symptoms caused by loss of estrogen in menopause
Hot flashes, sleep disturbances, urogenital atrophy, bone loss, altered lipid metabolism
Use of hormone replacement therapy (HRT) has declined sharply

Question 18

Menopausal Hormone Therapy Risks

Answer 18

Cardiovascular events: Myocardial infarction, stroke, pulmonary embolism, and deep vein thrombosis
Endometrial cancer
Breast cancer
Ovarian cancer
Gallbladder disease
Dementia
Urinary incontinence

Question 19

Menopausal hormone use for approved indications

Answer 19

Treatment of moderate to severe vasomotor symptoms associated with menopause
Treatment of moderate to severe symptoms of vulvar and vaginal atrophy associated with menopause
Prevention of postmenopausal osteoporosis