Chapter 64: Estrogens Progestins

Estrogens (estradiol, estriol, and estrone) and progesterone have multiple actions; name them

• • They promote female maturation and help regulate the ongoing activity of female reproductive organs.

• • Affect bone mineralization and lipid metabolism.

• *Principal endogenous estrogen is estradiol; principal progestational hormone is progesterone

Where is estrogen and progresterone produced

• Both estrogen and progesterone are produced by the ovaries.

• During pregnancy, large amounts are produced by the placenta.

• Small amounts are produced in peripheral tissues.

Anterior pituitary hormones and their functions

follicle-stimulating hormone (FSH) and  luteinizing hormone (LH)

• Play central roles in regulating the menstrual cycle.

• Precisely timed alterations in the secretion of these hormones are responsible for coordinating the structural and secretory changes that occur throughout the menstrual cycle.

Physiologic processes related to reproduction caused by estrogens

• • 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

Metabolic actions of estrogens

• • Positive effect on bone mass

• • Favorable effects on cholesterol levels

• • Blood coagulation

adverse effects of estrogens

• • Endometrial hyperplasia and carcinoma

• • Promotes growth of existing breast cancer

• • Ovarian cancer

• • Cardiovascular events

• • Nausea

• • Others: Gallbladder disease, jaundice, headache, and chloasma

therapeutic uses for estrogens

•  Menopausal hormone

• . Female hypogonadism

• . Acne

routes of administration for estrogens

• Oral

• · Transdermal

• . Intravaginal

• · Parenteral

Selective Estrogen Receptor Modulators (SERMs) MOA

 Activate estrogen in some tissues and block estrogen receptors selectively in others

None offers all the benefits of estrogen and avoids all the drawback

Selective Estrogen Receptor Modulators (SERMs) indications

Developed to provide benefits of estrogen while avoiding the drawbacks

Examples of Selective Estrogen Receptor Modulators (SERMs)

• Four available:

Tamoxifen

Toremifene

Raloxifene

Bazedoxifene

Tamoxifen [Nolvadex] MOA/ indication

• Activates estrogen

• Breast cancer treatment: Inhibits cell growth in the breast

• Protects against osteoporosis

Tamoxifen [Nolvadex] adverse effects

• Produces hot flashes —educate patient

• Risk for endometrial cancer and thromboembolism

Raloxifene [Evista] MOA/ indication

• Does not activate estrogen

• Protects against breast cancer, osteoporosis

• Promotes thromboembolism

Raloxifene [Evista] adverse effects

hot flashes

Duavee (conjugated estrogens/bazedoxifene) MOA

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

Duavee (conjugated estrogens/bazedoxifene) nursing considerations

Contraindications are the same as for other products containing estrogen

• Drug should be used for the shortest duration possible

Phytoestrogens (Isoflavones, lignins, coumestans) MOA

Plant-based compounds with weak estrogen activity

Phytoestrogens (Isoflavones, lignins, coumestans) indication

Used as a 'natural' way to manage symptoms associated with menopause

Phytoestrogens (Isoflavones, lignins, coumestans) patient education

Women are encouraged to obtain these from whole food sources to prevent overdosage

Progestins MOA

• Compounds that act like progesterone

• • Principal endogenous progestational hormone

• • Produced by ovaries and placenta

Progestins indications

• Postmenopausal hormone therapy

• • Dysfunctional uterine bleeding

• • Amenorrhea

• • Infertility

• • Prematurity prevention

• • Endometrial carcinoma and hyperplasia

Progestins adverse effects

• Teratogenic effects

• • Gynecologic effects

• • Breast cancer

• • Depression

• • Breast tenderness

• • Bloating

Benefits of menopausal hormone therapy

• 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

benefit for giving 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