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Estrace (Estradiol)

Last updated on November 22nd, 2021

Generic name: Estrace

Brand names: Climara; Estraderm; Menostar; Femtrace; Gynodiol

General Information

Estrogens can be found in nature in several forms. Estrogen is a female hormone which is necessary for many processes in organism. Sometimes in females the ovaries produce from 70 to 500 micrograms of estradiol a day. This is converted to estrone and to a lesser extent estriol. After menopause, estrone is the most active circulating estrogen. Estrogens cause growth sex organs in women and influence sex characteristics, including pubic and underarm hair and the shape of body contours and skeleton. Estrogens also increase secretions from the cervix and growth of the inner lining of the uterus (endometrium).

Estrogens increase HDL-cholesterol (“good” cholesterol) and reduce LDL-cholesterol (“bad” cholesterol) concentrations in the blood. Estradiol is a form of estrogen. Estradiol is recommended for treatment of the symptoms associated with menopause (vaginal dryness, hot flashes, etc.), reduction of the risk of heart attacks and strokes, prevention of bone fractures associated with osteoporosis, and for  dysfunctional (excessive and painful) uterine bleeding. Estradiol can be even prescribed as part of cancer treatment in females and men. It works by replacing natural estrogens in women who can no longer produce enough estrogen. It works for advanced prostate cancer by antagonizing male hormones. Your doctor may prescribe Estradiol for any other purposes not listed above.

What should you know before using Estrace (estradiol)?

You should not take Estrace if you have:

  • circulation problems, a history of stroke
  • any type of uterine, breast, or hormone-dependent cancer
  • abnormal vaginal bleeding that your doctor has not checked
  • blood-clotting disorder or bleeding

It is important to report to a doctor if you have:

  • kidney or liver disease
  • migraines
  • depression
  • asthma
  • triglycerides, high cholesterol
  • angina, high blood pressure or heart disease
  • seizure disorder, epilepsy
  • gallbladder disease
  • diabetes
  • if you have had your uterus removed (hysterectomy)

Check your doctor regularly and check your breasts for lumps every month during treatment with Estrace. Estrace increases your risk of developing endometrial hyperplasia. This a condition may lead to cancer of the uterus. Taking progestins while using Estrace may lower this risk. Long-term Estrace treatment may increase your risk of stroke. Consult your physician before using Estrace long-term. Your medical assistant should check your progress on a regular basis (every 3 to 6 months) to determine whether you should continue this treatment. FDA pregnancy category X. Estrogens are contraindicated during pregnancy due to an increased risk of fetal abnormalities. Do not take Estrogens if you are breast-feeding.


How should you use Estrace (estradiol)?

Use Estrace exactly as your doctor recommended. Never change the dosage. This remedy should be taken with a full glass of water. You may take Estrace with food or after a meal to reduce stomach upset.

What should be done if I missed the dose?

In case you forgot to take the dose, take it at your earliest opportunity. Never double your dose if it is almost time for your next dose. Take only one dose at once.


Taking any medicine in large doses can lead to serious consequences for your health. If you feel an overdose, contact your physician. In large doses, this remedy may cause the following conditions: vomiting, nausea, vaginal bleeding.

Which side effects can I perceive from this remedy?

As any medicine, Estrace (estradiol) can cause side effects. But most people use it without experiencing any side effects. Usually if side effects do occur, they do not require any treatment or are easily treated.

Common and less serious side effects:

  • loss of hair
  • irregular vaginal bleeding or spotting
  • fluid retention
  • high blood pressure
  • headaches
  • vomiting and nausea
  • breast tenderness
  • vaginal yeast infections
  • bloating or abdominal (stomach) cramps
  • high blood sugar (hyperglycemia)
  • enlargement of benign tumors of the uterus (uterine fibroids)

Here is the list of side effects which are rare but more serious:

  • heart attacks
  • dementia
  • strokes
  • allergic reactions
  • gallbladder disease
  • blood clots
  • breast cancer, uterine cancer or ovarian cancer

The list of side effects is not complete. Contact your doctor if you experience any of the side effects.


What other medications will affect Estrace (estradiol)?

Estrace (estradiol) can potentially interact with various other drugs. Some of the drugs that may lead to Estrace interactions include:

  •     Barbiturates, including, but not limited to: Pentobarbital (Nembutal®), Butalbital (Fioricet®, Fiorinal®), Secobarbital (Seconal®), Amobarbital (Amytal®), Phenobarbital (Luminal®)
  •     Certain antifungal medicines or antibiotics, such as: Clarithromycin (Biaxin®), elithromycin (Ketek®), etoconazole (Nizoral®), soniazid (Nydrazid®), Miconazole, rythromycin (Ery-Tab®), Itraconazole (Sporanox®)
  •     Certain seizure medications, such as: Oxcarbazepine (Trileptal®), Phenytoin (Dilantin®, Phenytek®), Carbamazepine (Carbatrol®, Epitol®, Equetro™, Tegretol®)
  •     Cyclosporine (Gengraf®, Neoral®, Sandimmune®)
  •     Grapefruit juice
  •     Hypothyroidism (underactive thyroid) medications, including: Liothyronine (Cytomel®), Levothyroxine (Levoxyl®, Synthroid®, Unithroid®), Liotrix (Thyrolar®), Thyroid (Armor® Thyroid, Nature-Throid®)
  •     Protease inhibitor HIV medications, such as: Ritonavir (Norvir®), Indinavir (Crixivan®), Nelfinavir (Viracept®), Fosamprenavir (Lexiva®), Atazanavir (Reyataz®), Amprenavir (Agenerase®)
  •     Rifamycin antibiotics, including rifapentine (Priftin®), rifampin (Rifadin®) and rifabutin (Mycobutin®)
  •     St. John’s wort (Hypericum perforatum)

This list of interactions may be not complete. Provide your medical practitioners entire list of medicines, herbs, dietary supplements or non-prescription drugs you take. Moreover tell them whether you drink alcohol, use illegal drugs or smoke. Particular items may interact with your drug.

What should be proper storage of Estrace (estradiol)?

Keep the remedy in a closed container at room temperature between 15° (59°F) and 30°C (86°F), away from heat, moisture, direct light, children and animals. Don’t freeze.

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