Other Brands/Names

Andalan, Angeliq, Cyclofem, Cycloprogynova, Diane, Estreva, Estrofem, Eva, Femoston, Mycrogynon, Oestrogel, Rosetin, Synfonia.

How it Works

Estradiol is a type of estrogen hormone, alongside estriol. This medication is a synthetic version of estrogen that is often prescribed to relieve menopausal symptoms caused by a drop in estrogen levels in the body.

By attaching to estrogen receptors, estradiol helps ease menopausal complaints such as sudden hot flushes, vaginal dryness, and discomfort during sexual activity. In addition, estradiol supports bone health and helps lower the risk of osteoporosis (fragile bones) that may occur when estrogen levels decrease during menopause.

Indications

Estradiol is recommended as hormone replacement therapy in the following situations:

• To manage symptoms related to menopause.

• To treat low estrogen levels caused by hypogonadism (when sex glands do not produce sufficient hormones) or primary ovarian failure (when the ovaries stop working before the age of 40).

• To help prevent osteoporosis in women after menopause.

• As part of treatment for certain cancers, such as specific cases of breast cancer and prostate cancer.

Contraindications

This drug should not be used by individuals with the following conditions:

• Hypersensitivity or allergy to estradiol.

• Past or current breast cancer (except when the cancer has already spread to other organs).

• Cardiovascular problems such as stroke, pulmonary embolism, or deep vein thrombosis.

• Endometrial cancer.

• Porphyria, a genetic disorder that causes a buildup of porphyrins in the body.

• Blood clotting disorders.

• Liver disease.

• Pregnancy or breastfeeding.

Side Effects

Possible side effects include:

• Abdominal discomfort

• Nausea

• Vomiting

• Bloating

• Breast tenderness

• Headaches

• Weight changes

Some serious side effects may also occur, such as:

• Sudden mood changes

• Breast lumps

• Abnormal vaginal bleeding

• Yellowing of the skin and eyes

• Severe abdominal pain

This drug can increase the risk of blood clots, particularly in individuals who remain inactive for long periods, such as those bedridden or in a wheelchair. Estradiol may also trigger skin darkening, especially on the face, a condition known as melasma.

Types

In Indonesia, estradiol is available in several forms, including:

• Film-coated tablets

• Injectable solution

• Gel

Dosage

Tablets

• For hormone replacement therapy in cases of menopause or hypogonadism:

  • 1–2 mg daily.

  • Women who have had a hysterectomy usually receive continuous treatment.

  • Women with an intact uterus may follow a cycle (3 weeks on treatment, followed by 1 week off).

• For palliative therapy in breast cancer that has spread:

  • 10 mg three times a day for 3 months.

  • This is intended only to relieve symptoms and improve quality of life, not to cure the cancer.

Gel

For menopausal symptoms or hormone replacement therapy: apply once daily as a thin layer on the left or right thigh.

Safety

Pregnancy: Category X

Estradiol should not be used during pregnancy because it may cause birth defects. The drug is also excreted in breast milk and is not recommended for breastfeeding mothers.

Drug Interactions

• The use of estradiol may raise the risk of stroke, blood clots, high blood pressure, and heart attacks, particularly in patients who smoke while on treatment.
• Estradiol may also lower folic acid absorption.
• Drug interactions that can increase estradiol levels (raising the risk of side effects) include:
  

  • The antibiotic clarithromycin

  • The antifungal fluconazole

  • The blood pressure drug diltiazem

• Medications that can reduce estradiol levels (making it less effective) include:
  

  • The tuberculosis drug rifampicin

  • The antifungal griseofulvin

  • The anticonvulsant phenobarbital

  • The antiretroviral efavirenz

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