Conjugated estrogens
Estrogens
EstrogensPregnancy: avoid
Not used in pregnancy.
A mixture of estrogen sulfates (estrone, equilin and others) for menopausal symptoms; with medroxyprogesterone, the regimen of the Women's Health Initiative.
Quick facts
- Group
- Estrogens
- Target
- Estrogen receptors α and β, nuclear receptors
- Used for
- Hot flushes of menopause
- Key effects
- Breast pain or tenderness · Nausea · Weight changes
- Monitor
- Need for continued treatment · Blood pressure
- ATC
- G03CA57
No doses: the clinician sets them by the current guideline.
Mechanism of action
Conjugated estrogens are a mixture; the figure shows estradiol, a related estrogen that occupies the same site, in the ligand-binding domain of human estrogen receptor α.
Conjugated estrogens are mainly sulfate esters of estrone, equilin and other estrogens. Gut enzymes remove the sulfate so the estrogens can be absorbed. They act on estrogen receptors α and β like other estrogens: they relieve hot flushes and vaginal atrophy, slow bone loss and lower LH and FSH by negative feedback. They stimulate the endometrium, so a progestogen is added in women with a uterus.
- Gut enzymes remove the sulfate and the estrogens are absorbed
- They bind estrogen receptors in target tissues
- Hot flushes ease and vaginal epithelium and bone are preserved
- The endometrium is stimulated unless a progestogen is added
Indications
- Hot flushes of menopause Menopause and climacteric syndrome →
- Vaginal atrophy of menopause Genitourinary syndrome of menopause (atrophic vaginitis) →
- Prevention of postmenopausal osteoporosis when other drugs are unsuitable Osteoporosis →
- Hypoestrogenism in young women with ovarian failure or hypogonadism Primary ovarian insufficiency →
Adverse effects
Common
- Breast pain or tenderness
- Nausea, stomach upset
- Weight changes
- Leg cramps
- Vaginal discharge or bleeding
Contraindications
- Undiagnosed abnormal genital bleeding
- Breast cancer or other estrogen-dependent cancer
- Active or past venous or arterial thromboembolism
- Liver disease
Key interactions
- St John's wort and other CYP3A4 inducers
- Lower estrogen effect
- Grapefruit and other CYP3A4 inhibitors
- Higher estrogen levels
- Levothyroxine
- Estrogen raises thyroid-binding globulin; the thyroid dose may need to rise
What is monitored
- Need for continued treatment
- Blood pressure
- Breast examination and mammography
- Abnormal vaginal bleeding
- Signs of thrombosis
Administration and safety
- Oral tablets at the same time each day
- In women with a uterus, given with a progestogen on the schedule ordered
- Lowest effective dose for the shortest time; reviewed regularly
Pregnancy and breastfeeding
Not used in pregnancy.
Nursing care
- Teach the warning signs of clots and stroke
- Teach to report vaginal bleeding and breast lumps
- Ask about smoking and past clots
- Ask about thyroid medication
- Check that a progestogen is prescribed if the uterus is present
Pharmacokinetics
- Absorption
- Oral tablets; the sulfate is removed in the gut before absorption
- Metabolism
- In the liver, partly by CYP3A4, with enterohepatic recirculation
- Elimination
- As conjugated metabolites in urine
Test yourself
Think of the answer, then tap the question to see it.
Which combination was studied in the Women's Health Initiative estrogen-plus-progestin arm?
Conjugated estrogens with medroxyprogesterone acetate.
What did that combination increase compared with placebo?
Venous thromboembolism, stroke, heart attack and invasive breast cancer, and probable dementia in women aged 65 or older.
What are conjugated estrogens made of, and how are they absorbed?
Mainly sulfate esters of estrone, equilin and other estrogens; gut enzymes remove the sulfate so the estrogens can be absorbed.
Connections
← Back to the class: Estrogens
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Estrogen: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); DailyMed - MEDROXYPROGESTERONE ACETATE tablet (DailyMed (U.S. National Library of Medicine), 2026); DailyMed - ESTRADIOL AND NORETHINDRONE ACETATE tablet (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.
