Estradiol dosage, forms, and strengths

Estradiol is a natural estrogen sex hormone that is also an active ingredient in many prescription drugs, including oral contraceptives. Many generic and brand-name prescription drugs contain estrogen alone. These drugs either contain estradiol or conjugated estrogens. Estradiol alone is used as hormone replacement therapy, primarily in menopausal and postmenopausal women, to relieve menopausal symptoms, such as hot flashes, and prevent osteoporosis. It’s also used as an end-stage treatment for breast and prostate cancer. 

Estradiol forms and strengths

There are many ways to get an estradiol dose. Some dosage forms are used for multiple reasons. Some are more specialized in an effort to minimize side effects. 

• Tablets: 0.5 milligrams (mg), 1 mg, 2 mg

• Weekly patch: 0.025 mg/day, 0.0375 mg/day, 0.05 mg/day, 0.06 mg/day, 0.075 mg/day, 0.1 mg/day

• Biweekly patch: 0.025 mg/day, 0.0375 mg/day, 0.05 mg/day, 0.075 mg/day, 0.1 mg/day

• Vaginal cream: 0.01% (0.1 mg/gram)

• Vaginal gel: 0.25 mg, 0.5 mg, 0.75 mg, 1 mg, 1.25 mg (0.1% gel); 0.53 mg/0.87 g (0.06% gel)

• Vaginal insert: 4 micrograms (mcg), 10 mcg

• Vaginal ring: 7.5 mcg/day

• Vaginal ring (estradiol acetate): 0.05 mg/day, 0.1 mg/day

• Transdermal spray: 1.53 mg/spray

• Injections: 5 mg/mL (estradiol cypionate), 10 mg/mL, 20 mg/mL, 40 mg/mL (estradiol valerate)

Estradiol dosage for adults

Dosages will depend on the condition being treated and the response to therapy. Estradiol treatment has several dosing complications. Systemic estradiol—doses that enter the bloodstream—require a dosing schedule of 21 days on the drug and seven days off of it. Women with a uterus will have to take progesterone along with estradiol in order to reduce the risk of endometrial cancer. 

Estradiol dosage for vasomotor symptoms due to menopause

Estrogen replacement therapy provides relief from moderate to severe vasomotor symptoms of menopause, which are caused by issues with the brain’s regulation of the body’s internal systems. The most common vasomotor symptoms of menopause are flushes, chills, and night sweats.

• Standard estradiol dosage for menopausal vasomotor symptoms: 1–2 mg oral tablets once daily in 21-day cycles followed by a seven-day break

Other dosages

• 25–100 mcg/day transdermal patch 

• 0.25–1.25 grams of 0.1% estradiol gel per day

• Two pumps (0.87–1.74 grams) of 0.06% estradiol gel daily

• One to three sprays (1.53–4.59 mcg) of estradiol spray each morning

• 0.05–0.1 mg/day estradiol acetate vaginal ring (Femring)

• 10–20 mg estradiol valerate intramuscular injections every four weeks

• 1–5 mg estradiol cypionate intramuscular injections every 3–4 weeks

Estradiol dosage for vaginal symptoms of menopause

Reduced estrogen causes changes in vaginal and urogenital tissues, leading to vaginal dryness, thinning of the tissues, vaginal burning, urination problems, and recurrent urinary infections. When estradiol is prescribed to treat vasomotor symptoms, as well as vaginal problems caused by menopause, healthcare providers will use tablets, patches, gels, sprays, and injections. However, when estradiol is prescribed only to treat vaginal or urogenital symptoms, healthcare providers use topical estradiol medicines to minimize side effects.

• Standard estradiol dosage for treatment of isolated menopausal vaginal symptoms: 2–4 g of 0.01% vaginal cream applied once per day for 1–2 weeks, followed by 1–2 g applied once per day for 1–2 weeks, followed by a maintenance dose of 1 g applied one to three times per week

Other dosages

• One 10 mcg vaginal insert once per day for 2 weeks, followed by a maintenance dose of one 10 mcg vaginal insert twice weekly 

• One 7.5 mcg/day estradiol vaginal ring (Estring)

Estradiol dosage for vaginal pain during sex in postmenopausal women

Imvexxy is a low-dose estradiol vaginal insert that specifically treats moderate to severe vaginal pain during sexual intercourse. 

• Standard estradiol dosage for treatment of vaginal pain during sex in postmenopausal women: One 4 mcg or 10 mcg vaginal insert (Imvexxy) once per day for 2 weeks, followed by a maintenance dose of one 4 mcg or 10 mcg vaginal insert twice weekly 

Estradiol dosage for osteoporosis prevention in postmenopausal women

Osteoporosis is a gradual loss of bone density after menopause, which leaves women vulnerable to fractures. Healthcare providers usually prescribe oral tablets, but they will use estradiol patches in severe cases when tablets don’t work.

• Standard estradiol dosage for osteoporosis prophylaxis in postmenopausal women: 0.5–2 mg oral tablets once daily in 21-day cycles, followed by a seven-day break

Other dosages

• 25 mcg/day transdermal patch 

Estradiol dosage for estrogen deficiency in premenopausal women

Estrogen deficiency (hypoestrogenism) is most commonly the result of menopause. However, estrogen deficiency can happen before menopause due to several causes. Estrogen replacement therapy is the appropriate treatment when estrogen deficiency is due to reduced ovary activity (hypogonadism), ovary removal, or primary ovarian failure. 

• Standard estradiol dosage for estrogen deficiency in premenopausal women: 1–2 mg oral tablets once daily in 21-day cycles, followed by a seven-day break

Other dosages

• 25–100 mcg/day transdermal patch 

• 10–20 mg estradiol valerate intramuscular injections every four weeks

• 1.5–2 mg estradiol cypionate intramuscular injections every 3–4 weeks

Estradiol dosage for metastatic breast cancer

Estradiol is used as an add-on palliative treatment in people with later-stage breast cancer. The medication is intended to help improve the quality of life, but not cure the cancer. 

• Standard estradiol dosage for metastatic breast cancer: 10 mg oral tablets taken three times per day for at least three months

Estradiol dosage for inoperable prostate cancer

Estradiol is also used as an add-on palliative treatment in men with inoperable prostate cancer. 

• Standard estradiol dosage for inoperable prostate cancer: 1–2 mg oral tablets taken three times per day 

Other dosages

• 30 mg estradiol valerate intramuscular injections every one to two weeks

Estradiol dosage for children

The FDA has approved the use of estradiol in adolescent girls (12 years of age and older) with estrogen deficiency due to hypogonadism. Younger women with estrogen deficiency are at an increased risk of heart disease. Starting doses will be very low—about 1/10 the normal dose for adult women. Doses will be gradually increased over two years to approximate adult doses. About one to two years after the start of therapy or when breakthrough bleeding starts, the adolescent will be given progestin for at least one week per month along with the estradiol. For most adolescents with estrogen deficiency, estrogen replacement is a lifelong treatment.

• Starting estradiol dosage for hypoestrogenism in adolescents ages 12 years and older: 0.25 mg tablet once daily in 21-day cycles, followed by a seven-day break

Other dosages

• 14 mcg/day transdermal patch 

• 0.2 mg estradiol cypionate intramuscular injection every four weeks

• Standard estradiol dosage for hypoestrogenism in adolescents ages 12 years and older: 0.5–2 mg once daily in 21-day cycles, followed by a seven-day break

Other dosages

• 25–100 mcg/day transdermal patch applied twice-weekly

• 1.5–2 mg estradiol cypionate intramuscular injection every four weeks

Estradiol dosage restrictions

Estradiol does not require dosage restrictions or reductions in people with kidney dysfunction. 

Estradiol is too hazardous to take with certain medical conditions. Contraindications include:

• Hepatic impairment

• Any history of breast cancer or other estrogen-related tumors

• Pregnancy

• History of a deep vein thrombosis or pulmonary embolism

• Any recent history of blood clot (thromboembolic) disorders

• Undiagnosed vaginal bleeding

Although dosage reductions may not be needed, estradiol may cause problems in people with:

• High blood pressure

• High triglycerides and cholesterol

• Underactive thyroid (hypothyroidism)

• Low calcium

• Fluid retention

• A history of jaundice

• Endometriosis

• Diabetes

• Epilepsy

• Migraines

• Lupus

How to take estradiol tablets (Estrace)

Estradiol tablets are relatively straightforward to take. They can be taken with or without food.

• Take this medicine as instructed.

• Take estradiol tablets at the same time each day.

• Swallow the tablet whole. 

How to use estradiol patches (Vivelle-Dot, Climara)

Estradiol patches are a bit more complex than tablets. There are more steps involved, and the patch can peel off if care isn’t taken.

• Please read the enclosed instructions before using estradiol transdermal patches.

• Some patches need to be replaced twice per week, and others need to be replaced every seven days.

• To ensure continual dosing, mark the days the patch needs to be changed on a calendar or task management app.

• Do not take the patch out of its pouch until you are ready to apply it.

• Remove the protective backing from the patch.

• Apply the sticky side of the patch to the lower right or left abdomen or lower right or left back below the waistline. 

• Do not apply the patch to the breasts or to any skin that is irritated or hurt.

• Press the patch firmly to the skin for 10 seconds.

• Rub along the edge of the patch to make sure it’s firmly attached.

• Remember: water (bathing, swimming) may cause the patch to peel off.

• If a patch comes off, put it back on. If you can’t, apply a new patch and take it off when scheduled. 

How to take topical estradiol (Divigel, Evamist)

Topical estradiol is applied to the skin once daily, either as a gel or spray. Both are relatively straightforward, but there are details to master.

• Read the instructions.

• Wash and dry your hands before applying this medicine.

• Clean and dry the skin where the medicine will be applied. The skin must be undamaged without cuts, rashes, or irritation.

• Never apply topical estradiol to the face, breasts, or genital area.

Estradiol gel:

• The gel comes in single-dose packets. Use the entire contents of each packet when taking a dose.

• Squeeze the contents of the packets onto the skin of the upper thigh.

• Spread the gel over an area of five to seven inches.

• Make sure the gel completely dries before dressing.

• Throw away the packet after it is used.

• Immediately wash your hands with soap and water to remove any gel.

Estradiol spray:

• The spray comes in an applicator.

• To prime the applicator before the first use, leave the cover on it and press the pump button three times. Each applicator needs only one priming.

• Take doses in the morning.

• Estradiol spray is applied to the skin on the inside of the forearm, starting near the elbow.

• Put the plastic cone against the skin.

• Push the pump button.

• Do not rub the medicine into the skin.

• Do not give repeated doses on the same area of skin. If a second dose is required, move the cone down the forearm and apply it there. The same rule applies to a third dose.

• Put the cover back on when finished.

• Wait two minutes for the spray to dry before covering the skin. 

• Wait one hour before washing the area.

How to take vaginal estradiol (Estrace, Vagifem)

Vaginal estradiol can be taken as an insert (vaginal tablets) or applied as a cream. 

• Read the patient information and instructions for use included with this medicine.

• Apply or take doses at the same time each day.

Estradiol cream:

• This medicine is administered with a graduated applicator.

• After opening the tube, screw the applicator into the tube. 

• Squeeze the tube to fill the applicator to the correct dose.

• Unscrew the applicator and replace the cap on the tube.

• Lie back with knees drawn back.

• Insert the applicator deep into the vagina and press the plunger to the end.

• After application, wash the plunger with mild soap and water.

Estradiol inserts:

• Do not take this medicine by mouth.

• Remove the insert from the blister pack.

• Choose the most comfortable position to insert the vaginal tablet. 

• When ready, put the insert at least two inches into the vagina using a finger.

How to use estradiol vaginal rings (Estring)

Vaginal rings are an extended-release topical estradiol for vaginal symptoms of menopause. They last for 90 days, so they don’t require daily dosing. 

• Read the patient information and instructions for use included with this medicine.

• Estradiol vaginal rings are inserted by the patient.

• The ring must be placed in the upper vagina to work best.

• Estradiol vaginal rings are intended to stay in the vagina for 90 days.

• After 90 days, the ring should be removed. Another ring may be prescribed by a healthcare professional.

• To insert the ring, first wash and dry your hands.

• Remove the ring from the pouch.

• Choose a comfortable position to insert the ring.

• Press the sides of the ring together.

• Holding the folds of the vagina apart with one hand, place the tip of the ring into the vagina with the other hand.

• Push the ring up the vagina as far as you can with your finger.

• If it’s uncomfortable, push it farther up. 

• When done, wash your hands with soap and water.

Estradiol dosage FAQs

Estradiol vs. estradiol ER: What’s the difference in doses?

Estradiol comes in a few extended-release formats: biweekly patches, weekly patches, and 90-day vaginal rings. Doses are measured in the amount of estradiol released daily.

What happens if I miss a dose of estradiol?

Ask the prescribing healthcare provider or pharmacist what to do about a missed dose. Taking a missed dose will depend on the dosing form used.

How long can you take estradiol?

Estradiol is a potentially hazardous medication when taken for a long time. When taken alone, estrogen therapy increases the risk of endometrial hyperplasia and uterine cancer, as well as heart attack, stroke, cancer, and blood clot disorders, according to the Women’s Health Initiative (WHI). The FDA advises that estradiol should be taken at the lowest effective doses for a limited time.

Can you overdose on estradiol?

Oral estradiol overdoses have not been associated with serious problems. Common symptoms are nausea, vomiting, and vaginal bleeding. If too much estradiol is taken, call a poison control center or get immediate medical help.

Is it safe to take estradiol during pregnancy?

Estradiol induces abortion, so estradiol should never be taken during a pregnancy. Estradiol is used cautiously in women who are breastfeeding because it gets into human breast milk. Estradiol therapy also decreases the quality and quantity of breast milk.

Sources

• Depo-estradiol- estradiol cypionate injection, NIH National Library of Medicine (2022)

• Divigel- estradiol gel, NIH National Library of Medicine(2023)

• Elestrin- estradiol gel, metered, NIH National Library of Medicine (2023)

• Estrace, Prescriber’s Digital Reference

• Estradiol cream, NIH National Library of Medicine (2019)

• Estradiol- estradiol gel 0.01% gel, NIH National Library of Medicine (2023)

• Estradiol insert, NIH National Library of Medicine (2023)

• Estradiol patch, extended-release, NIH National Library of Medicine (2021)

• Estradiol tablet, NIH National Library of Medicine (2021)

• Estradiol transdermal system- estradiol patch, NIH National Library of Medicine (2023)

• Estradiol valerate injection, NIH National Library of Medicine (2022)

• Estring- estradiol ring, NIH National Library of Medicine (2023)

• Evamist- estradiol spray, NIH National Library of Medicine (2023)

• Femring- estradiol acetate ring, NIH National Library of Medicine (2023)

• Imvexxy- estradiol insert, NIH National Library of Medicine (2023)

• Vagifem- estradiol insert, NIH National Library of Medicine (2023)