ESTROGENS AND PROGESTINS
ESTROGENS AND PROGESTINS
•
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
THE MENSTRUAL CYCLE
Follicular
phase—first
half of the
cycle (days
1–14)
Follicular
phase—first
half of the
cycle (days
1–14)
Luteal phase
—second
half of the
cycle
Luteal phase
—second
half of the
cycle
Full cycle
typically
takes 28
days
Full cycle
typically
takes 28
days
THE MENSTRUAL CYCLE
Coordinating ovarian and
uterine events
Uterine changes are brought
about under the influence of
estrogens and progesterone
Anterior pituitary hormones, follicle-
stimulating hormone (FSH), and
luteinizing hormone (LH) regulate the
menstrual cycle
ESTROGENS
Biosynthesis and elimination
•
Female
•
Ovary is the principal organ
•
Follicles, then corpus luteum
•
Placenta produces large amounts pregnancy
•
Major estrogen produced is estradiol
•
Male
•
Small amounts of testosterone converted into estradiol and estrone by the
testes
•
Peripheral tissues
ESTROGENS
•
Effects on primary and secondary sex characteristics
•
Reproductive tract and secondary sex characteristics
•
Physiologic processes related to reproduction
•
(1) ductal growth in the breast
•
(2) thickening and cornification of the vaginal epithelium (3) proliferation of the
uterine epithelium
•
(4) copious secretion of thickened mucus from endocervical glands
ESTROGENS
•
Metabolic actions
•
Positive effect on bone mass
•
Favorable effects on cholesterol levels
•
Blood coagulation
•
Adverse effects
•
Endometrial hyperplasia and carcinoma
•
Promotes growth of existing breast cancer
•
Ovarian cancer
•
Cardiovascular events
•
Nausea
•
Adverse effects from use during pregnancy
ESTROGENS
•
Therapeutic uses
•
Hormone therapy after menopause
•
Female hypogonadism
•
Acne
•
Routes of administration
•
Oral
•
Transdermal
•
Intravaginal
•
Parenteral
ESTROGEN
(ETHINYL ESTRADIOL, ESTRONE, AND ESTRIOL)
Increases thickness of
endometrium proliferation
before ovulation
•
Use estrogen alone with
hysterectomy
*Estrogen does not cause
breast
cancer—it only promotes
the
growth of a cancer that already
exists, and then only if the cancer
is estrogen receptor–positive.
•
Benefit
•
Cardio protective
•
Decrease LDL, increase HDL
•
Lower risk of MI in premenopausal
•
Decrease in menopausal symptoms
•
Stimulate clotting
•
Block bone resorption; promote mineral
deposition
•
Help control acne
•
Manage hot flashes and other menopausal sx
•
Disadvantage
•
Increased risk of seizures
•
Can inhibit lactation
•
Substrate of CYP 3A4
•
Increased risk of
VTE (esp with smoking)
•
ADR:
Nausea,
changes in menstrual flow,
breast tenderness, headache, edema
•
In men – feminization
of genitalia and
impotence
Copyright © 2015 Wolters Kluwer • All Rights Reserved
CHAPTER 26
•
Figure 26.3
