Estradiol is a form of estrogen, a female sex hormone produced by the ovaries.
The drug is available under several trademarks, such as Estrace (oral tablets); EvaMist (spray); Vagifem (vaginal tablet); Estring, Femring (vaginal rings); Klimara, Alora (cream); and Divigel and Estrogel (gels).
Estradiol is used for treatment and prevention in women suffering from menopause. Estradiol gel is also used to treat vaginal dryness, itching and burning in women in menopause.
Estradiol is also usually combined with progestins in various doses of tablets that prevent pregnancy, preventing ovulation.
The drug can also be used to prevent osteoporosis, replace estrogen in women with ovarian failure or as part of a cancer treatment regimen.
Estradiol belongs to a class of drugs called estrogen hormones. It works by replacing the estrogen that usually produces the body.
Estradiol may increase the risk of developing endometrial cancer (cancer of the lining of the uterus). If you did not have a hysterectomy, you should take a progestin along with estradiol in order to reduce this risk.
However, before taking these two medicines together, talk with your doctor about your risk of health problems.
In one study, women who took estrogens (such as estradiol) through the mouth with a progestin had a higher risk of heart attacks, stroke, blood clots, breast cancer and dementia.
Women who use local estradiol alone or with a progestin may also have a higher risk of developing these conditions.
The use of topical estradiol may increase the risk of developing ovarian and gallbladder cancers. You should talk with your doctor about these risks.
Before taking estradiol, tell your doctor if you have or have ever had:
- Heart attack or stroke
- Heart disease
- Blood clots
- Any kind of cancer
- Abnormal vaginal bleeding
- High blood pressure
- High cholesterol
- Diseases of the gallbladder
- Thyroid disorder
- Epilepsy or other seizures
- Liver disease
- Breast hernia or abnormal mammogram results
- Uterine fibroids
- Yellowing of the skin or eyes (jaundice)
- Endometriosis (a condition in which the type of tissue that stretches the uterus grows in other areas of the body, usually in the stomach or pelvis)
- Low level of calcium in the blood
Also, tell your doctor if you smoke or drink tobacco products.
You should use the lowest dose of estradiol in the shortest time to control your symptoms.
Meet with your doctor every three to six months to determine if you should lower the dose or stop using this medication.
Tell your doctor if you are planning an operation with estradiol. Your doctor may recommend that you stop taking the medication to reduce the risk of blood clots.
Pregnancy and estradiol
Estradiol can harm an unborn baby or cause birth defects. You should not use this medicine during pregnancy.
Immediately notify your doctor if you are pregnant or can become pregnant while taking this medication.
Because estradiol can also penetrate into breast milk, talk with your doctor before breastfeeding while taking the drug.
Side effects of estradiol
Common side effects
You should tell your doctor if any of the following symptoms is serious or does not disappear:
- Chest pain
- Mood Changes or Depression
- Difficulty falling asleep
- Changes in sexual desire
- Stuffy nose, cough or flu symptoms
- Hair loss or unwanted hair growth
- Darkening of the face skin
- The complexity of wearing contact lenses
- Swelling, redness, burning, irritation or itching of the vagina
- Redness or irritation at the site of application
Estradiol and weight gain
Water retention, which increases your weight, is a common side effect.
Talk with your doctor about adjusting the dose of estradiol if weight gain becomes a problem.
Serious side effects
Immediately consult your doctor if you experience the following serious side effects:
- Sudden, severe headache
- Sudden, severe vomiting
- Problems with speech
- Dizziness or fainting
- Sudden, full or partial loss of vision
- Weakness or numbness in the hands or feet
- Chest pain
- Coughing up blood
- Sudden shortness of breath or shortness of breath
- Yellowing of the skin or eyes
- Loss of appetite
- Edema of the stomach
- Rash or blisters
- Movement that is difficult to control
- Swelling of the eyes, face, lips, tongue, throat, hands, feet, ankles or feet
- Difficulty swallowing
You must tell your doctor about all prescription, non-prescription, over-the-counter (over-the-counter), illegal or recreational drugs that you take, especially:
- Antifungal agents, such as itraconazole (sporanok) and ketoconazole (Nizoral)
- St. John’s Wort
- Carbamazepine (Carbatrol, Epitol, Equitro, Tegretol)
- Clarithromycin (Biaxin)
- Erythromycin (EES, erythrocin)
- Lovastatin (Alticor, Altoprev, Mevacor)
- Drugs for the treatment of diseases of the thyroid gland
- Rifampin (Rifadine, Rimatan, Rifamate)
- Ritonavir (Norvir, in Kaletra)
Estradiol and grapefruit
Grapefruit and its juice can interact with estradiol and cause unwanted side effects.
You should talk to your doctor before consuming grapefruit while taking estradiol.
Estradiol and other interactions
You should avoid exposure to the sun when taking estradiol, because the gel can make the skin more sensitive to sunlight.
Dosage of estradiol
Your dose of estradiol will depend on the condition that is being treated.
Estradiol tablets in doses of 0.5 mg (mg), 1 mg or 2 mg are usually taken daily.
Tablets can be taken more than once a day for certain conditions.
Gel and emulsions are applied to the skin at the same time every day.
The vaginal ring is inserted into the vagina and is worn for three months in a row.
The plaster should be glued on a dry, clean part of the body (but not on the chest). It can not be placed on irritated or damaged skin.
Overdose with estradiol
Symptoms of overdose include the following:
- Nausea or vomiting
- Severe vaginal bleeding
- Gentle breast
- Urine of strange color
If you suspect an overdose, you should immediately contact a toxicology center or an emergency room.
You can contact the Toxicology Center
The missed dose of estradiol
If you miss a dose of oral estradiol, take it as soon as you remember.
However, if it’s time to take the next dose, skip it and continue your regular schedule. Do not double the dose.
Do not use additional doses to fill in the missed ones.