Estrogens
Estrogens
Estrogens mimic the physiologic effects of naturally occurring female sex hormones.
To serve and protect
Estrogens are used to correct estrogen-deficient states and, along with hormonal contraceptives, prevent pregnancy.
Natural and synthetic estrogen
Estrogens that treat endocrine system disorders include:
- natural products, such as conjugated estrogenic substances, estradiol, and estropipate
- synthetic estrogens, such as esterified estrogens, estradiol cypionate, estradiol valerate, and ethinyl estradiol.
Pharmacokinetics
Estrogens are well absorbed and distributed throughout the body. Metabolism occurs in the liver, and the metabolites are excreted primarily by the kidneys.
Pharmacodynamics
The exact mechanism of action of estrogen isn’t clearly understood, but it’s believed to increase synthesis of deoxyribonucleic acid, ribonucleic acid, and protein in estrogen-responsive tissues in the female breast, urinary tract, and genital organs.
Pharmacotherapeutics
Estrogens are prescribed:
- primarily for hormone replacement therapy in postmenopausal women to relieve symptoms caused by loss of ovarian function
- less commonly for hormonal replacement therapy in women with primary ovarian failure or female hypogonadism (reduced hormonal secretion by the ovaries), for prevention and treatment of osteoporosis in postmenopausal women, and in patients who have undergone surgical castration
- palliatively to treat advanced, inoperable breast cancer in postmenopausal women and prostate cancer in men.
Hormone replacement therapy and heart disease
Following a 5-year study, the Women’s Health Initiative reported increased risks of myocardial infarction, stroke, breast cancer, pulmonary emboli, and deep vein thrombosis in women being treated with conjugated equine estrogens and progesterone as compared to those taking a placebo.
The U.S. Preventive Services Task Force recommends against the use of estrogen and pro-gestin to prevent coronary heart disease in healthy women.
What to do?
Because the long-term safety of short-term therapy has yet to be determined, the Food and Drug Administration and American College of Obstetricians and Gynecologists recommend that women who choose to take hormone replacement therapy for menopausal symptoms use these drugs for the shortest duration possible and in the lowest possible dosages.
Adverse reactions to estrogens
Adverse reactions to estrogens include:
- hypertension
- thromboembolism (blood vessel blockage caused by a blood clot)
- thrombophlebitis (vein inflammation associated with clot formation).
Drug interactions
Relatively few drugs interact with estrogens:
- Estrogens may decrease the effects of anticoagulants, increasing the risk of blood clots.
- Antibiotics, barbiturates, carbamazepine, phenytoin, primidone, and rifampin reduce estrogen effectiveness.
- Estrogens interfere with the absorption of dietary folic acid, which may result in a folic acid deficiency.
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