Estradiol Uses

• Estradiol indications
• Uses of Estradiol in details
• Estradiol description
• Estradiol dosage
• Estradiol interactions
• Estradiol side effects
• Estradiol contraindications

What is Estradiol?

Estradiol is a form of estrogen, a female sex hormone that regulates many processes in the body.

Some Estradiol products placed directly into the vagina are used for "local" treatment of vaginal menopause symptoms (such as dryness, burning, and irritation). Other vaginal Estradiol products are used for treating vaginal menopause symptoms and symptoms that affect other parts of the body (such as hot flashes). This type of vaginal Estradiol has "systemic" effects, meaning that it can affect parts of the body other than where the medicine is directly applied.

This medication guide provides information about Estradiol for local treatment of vaginal symptoms of menopause (such as dryness, itching, irritation, and pain during sexual intercourse).

Estradiol (local) may also be used for purposes not listed in this medication guide.

Estradiol indications

Estradiol is a Hormone Replacement Therapy (HRT). It contains the female hormone Estradiol.

Estradiol is used in postmenopausal women, particularly in women who have had their womb removed (have had a hysterectomy) and therefore do not require combined oestrogen/progestagen therapy.

Estradiol is

Used for: Relief of symptoms occurring after menopause: During the menopause, the amount of oestrogen produced by a woman’s body drops. This can cause symptoms such as hot face, neck and chest (‘hot flushes’). Estradiol alleviates these symptoms after menopause. Estradiol should only be prescribed if the symptoms seriously hinder the patient’s daily life.

Prevention of osteoporosis (thinning of the bones), if the patient is at high risk of future fracture and if unable to take other medications for this purpose.

There is only limited experience of treating women older than 65 years.

How should I use Estradiol?

Use Estradiol emulsion as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• An extra patient leaflet is available with Estradiol emulsion. Talk to your pharmacist if you have questions about this information.
• If you are switching from oral estrogen to Estradiol emulsion, stop taking the oral estrogen and wait 1 week before using Estradiol emulsion. However, if symptoms return, you may start using Estradiol emulsion sooner.
• Wash your hands with soap and water both before and after using Estradiol emulsion.
• Sit in a comfortable sitting position and apply Estradiol emulsion to clean, dry skin of the leg. Cut or tear the pouch of medicine and empty the entire contents of the pouch onto the top of the thigh. Rub the medicine in well into the thigh and calf of the leg for 3 minutes until it is completely absorbed. Rub any medicine remaining on the hands onto the buttocks. If you are using two pouches of Estradiol emulsion, apply the second pouch of medicine to the opposite leg in the same way.
• Allow the medicine to dry completely before covering with clothing to avoid transfer to other people.
• Grapefruit and grapefruit juice may increase the risk of Estradiol emulsion's side effects. Talk to your doctor before including grapefruit or grapefruit juice in your diet while you are taking Estradiol emulsion.
• If you miss a dose of Estradiol emulsion, use it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not use 2 doses at once.

Ask your health care provider any questions you may have about how to use Estradiol emulsion.

Uses of Estradiol in details

This medication is a female hormone (estrogen). It is used by women to help reduce symptoms of menopause (such as hot flashes, vaginal dryness). These symptoms are caused by the body making less estrogen. If you are using this medication to treat symptoms only in and around the vagina, products applied directly inside the vagina should be considered before medications that are taken by mouth, absorbed through the skin, or injected. This medication may also be used by women who are not able to produce enough estrogen (for example, due to hypogonadism, primary ovarian failure) and by men to treat prostate cancer.

How to use Estradiol intramuscular

Read the Patient Information Leaflet if available from your pharmacist before you start using this medication and each time you get a refill. If you have any questions, ask your doctor or pharmacist.

This medication is injected into a muscle as directed by your doctor, usually every 4 weeks. For the treatment of prostate cancer, this medication is usually given every 1 to 2 weeks. The dosage is based on your medical condition and response to treatment.

If you are using this medication at home, learn all preparation and usage instructions from your health care professional. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. If stored at low temperatures, crystal may form in the liquid. To dissolve these crystals, simply warm the product to room temperature prior to use. Learn how to store and discard medical supplies safely.

Use this medication regularly to get the most benefit from it. To help you remember, mark your calendar with a reminder of when to receive your doses.

Tell your doctor if your condition does not improve or if it worsens.

Estradiol description

Generally refers to the 17-beta-isomer of Estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of Estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Various isomers can be synthesized.

Estradiol dosage

Generally, when estrogen is prescribed for a postmenopausal woman with a uterus, a progestin should also be considered to reduce the risk of endometrial cancer. A woman without a uterus does not need a progestin. In some cases, however, hysterectomized women with a history of endometriosis may need a progestin.

Use of estrogen-alone, or in combination with a progestin, should be with the lowest effective dose and for the shortest duration consistent with treatment goals and risks for the individual woman. Postmenopausal women should be re-evaluated periodically as clinically appropriate to determine if treatment is still necessary.

Treatment Of Moderate To Severe Vasomotor Symptoms Due To Menopause

Start therapy with 0.025 mg per day applied to the skin once weekly. Therapy should be started at the lowest effective dose and the shortest duration consistent with the treatment goals. Attempts to taper or discontinue the medication should be made at 3 to 6 month intervals.

Treatment Of Moderate To Severe Symptoms Of Vulvar And Vaginal Atrophy Due To Menopause

Start therapy with 0.025 mg per day applied to the skin once weekly. Therapy should be started at the lowest effective dose and the shortest duration consistent with the treatment goals. Attempts to taper or discontinue the medication should be made at 3 to 6 month intervals.

Treatment Of Hypoestrogenism Due To Hypogonadism, Castration, Or Primary Ovarian Failure

Start therapy with 0.025 mg per day applied to the skin once weekly. The dose should be adjusted as necessary to control symptoms. Clinical responses (relief of symptoms) at the lowest effective dose should be the guide for establishing administration of the Estradiol transdermal system, especially in women with an intact uterus.

Prevention Of Postmenopausal Osteoporosis

Start therapy with 0.025 mg per day applied to the skin once weekly.

Application Of The Estradiol Transdermal System

Site Selection

• The adhesive side of Estradiol should be placed on a clean, dry area of the lower abdomen or the upper quadrant of the buttock.
• Estradiol should not be applied to or near the breasts.
• The sites of application must be rotated, with an interval of at least 1-week allowed between applications to the same site.
• The area selected should not be oily, damaged, or irritated. The waistline should be avoided, since tight clothing may rub the transdermal system off.
• Application to areas where sitting would dislodge Estradiol should also be avoided.

Application

• Estradiol should be applied immediately after opening the pouch and removing the protective liner.
• Estradiol should be pressed firmly in place with the fingers for at least 10 seconds, making sure there is good contact, especially around the edges.
• If the system lifts, apply pressure to maintain adhesion.
• In the event that a system should fall off reapply it to a different location. If the system cannot be reapplied, a new system should be applied for the remainder of the 7-day dosing interval.
• Only one system should be worn at any one time during the 7-day dosing interval.
• Swimming, bathing, or using a sauna while using Estradiol has not been studied, and these activities may decrease the adhesion of the system and the delivery of Estradiol.

Removal Of The Estradiol Transdermal System

• Removal of Estradiol should be done carefully and slowly to avoid irritation of the skin.
• Should any adhesive remain on the skin after removal of the Estradiol system, allow the area to dry for 15 minutes. Then gently rubbing the area with an oil-based cream or lotion should remove the adhesive residue.
• Used patches still contain some active hormones. Each patch should be carefully folded in half so that it sticks to itself before throwing it away.

How supplied

Dosage Forms And Strengths

• Estradiol (Estradiol transdermal system), 0.025 mg per day—each 6.5 cm² system contains 2 mg of Estradiol
• Estradiol (Estradiol transdermal system), 0.0375 mg per day—each 9.375 cm² system contains 2.85 mg of Estradiol
• Estradiol (Estradiol transdermal system), 0.05 mg per day—each 12.5 cm² system contains 3.8 mg of Estradiol
• Estradiol (Estradiol transdermal system), 0.060 mg per day—each 15 cm² system contains 4.55 mg of Estradiol
• Estradiol (Estradiol transdermal system), 0.075 mg per day—each 18.75 cm² system contains 5.7 mg of Estradiol
• Estradiol (Estradiol transdermal system), 0.1 mg per day—each 25.0 cm² system contains 7.6 mg of Estradiol

Estradiol (Estradiol transdermal system), 0.025 mg per day — each 6.5 cm² system contains 2 mg of Estradiol USP Individual Carton of 4 systems NDC 50419-454-04

Estradiol (Estradiol transdermal system), 0.0375 mg per day — each 9.375 cm² system contains 2.85 mg of Estradiol USP Individual Carton of 4 systems NDC 50419-456-04

Estradiol (Estradiol transdermal system), 0.05 mg per day — each 12.5 cm² system contains 3.8 mg of Estradiol USP Individual Carton of 4 systems NDC 50419-451-04

Estradiol (Estradiol transdermal system), 0.06 mg per day — each 15 cm² system contains 4.55 mg of Estradiol USP Individual Carton of 4 systems NDC 50419-459-04

Estradiol (Estradiol transdermal system), 0.075 mg per day — each 18.75 cm² system contains 5.7 mg of Estradiol USP Individual Carton of 4 systems NDC 50419-453-04

Estradiol (Estradiol transdermal system), 0.1 mg per day — each 25 cm² system contains 7.6 mg of Estradiol USP Individual Carton of 4 systems NDC 50419-452-04

Storage And Handling

Store at 20°C to 25°C (66°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F). Do not store above 86°F (30°C).

Do not store unpouched. Apply immediately upon removal from the protective pouch.

Used transdermal systems still contain active hormone. To discard, fold the sticky side of the transdermal system together, place it in a sturdy child-proof container, and place this container in the trash. Used transdermal systems should not be flushed in the toilet.

Manufactured for: Bayer HealthCare Pharmaceuticals Inc. Whippany, NJ 07981. Manufactured by 3M Drug Delivery Systems, Northridge, CA 91324. Revised: Oct 2013

Estradiol interactions

See also:
What other drugs will affect Estradiol?

Some products that may interact with this drug include: "blood thinners" (such as warfarin), corticosteroids (such as prednisone), thyroid replacement medication.

Other medications can affect the removal of Estradiol cypionate from your body, which may affect how Estradiol cypionate works. Examples include azole antifungals (such as itraconazole), macrolide antibiotics (such as erythromycin), rifamycins (such as rifampin), St. John’s wort, drugs used to treat seizures (such as carbamazepine, phenytoin), among others.

This medication may interfere with certain laboratory tests (including blood clotting, thyroid function), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

Estradiol side effects

See also:
What are the possible side effects of Estradiol?

See WARNINGS and Boxed Warning regarding the potential adverse effects on the fetus, the induction of malignant neoplasms, gallbladder disease, cardiovascular disease, elevated blood pressure, and hypercalcemia.

Skin irritation: In controlled clinical studies with Estradiol (Estradiol transdermal), the most commonly reported adverse events were topical reactions of erythema and/or pruritus at the application site. In general these reactions caused patients little or no discomfort, and led to premature discontinuation of treatment in 0.9% (3/317) of patients in these trials. The rate of application site reactions, based on 8,135 applications of the 0.025, 0.05, and 0.1 Estradiol (Estradiol transdermal) systems in these trials was 6.1 per 100 applications (4.9, 5.4, 10.7 for the 3 Estradiol (Estradiol transdermal) doses respectively) compared to 6.2 in the placebo treated patients (2,014 applications).

In a placebo-controlled trial of Estradiol (Estradiol transdermal) 0.025, 0.05, and 0.1 conducted in 196 patients in the US, the adverse events reported by at least 5% of patients in 1 or more of the treatment groups are shown in Table 5.

Urogenital Adverse Events : In the US placebo-controlled study, 72 patients were included who had intact uteri. As expected, after 12-13 weeks of continuous unopposed therapy, findings of endometrial hyperplasia (diagnosed either by endometrial biopsy and/or ultrasonography) were increased with increasing doses of Estradiol (placebo: 0/18 patients; Estradiol (Estradiol transdermal) 0.025: 1/14 (7.1%); Estradiol (Estradiol transdermal) 0.05: 12/22 (54.5%); Estradiol (Estradiol transdermal) 0.1: 10/18 (55.6%). In the 86 patients who had not previously undergone a total hysterectomy, vaginal bleeding was also increased with increasing doses of Estradiol [placebo: 2/21 patients (9.5%); Estradiol (Estradiol transdermal) 0.025: 6/19 (31.6%); Estradiol (Estradiol transdermal) 0.05: 14/25 (56.0%); Estradiol (Estradiol transdermal) 0.1: 12/21 (57.1%)].

In 2 long-term studies involving a total of 488 patients treated for a mean duration of 618 days and up to 3.5 years, the nature and incidence of adverse events did not change with prolonged duration of treatment.

The following additional adverse reactions have been reported with estrogen therapy:

1. Genitourinary System. Changes in vaginal bleeding pattern and abnormal withdrawal bleeding or flow; breakthrough bleeding, spotting; increase in size of uterine leiomyomata; vaginal candidiasis; change in amount of cervical secretion.

2. Breasts. Tenderness, enlargement.

3. Gastrointestinal. Nausea, vomiting; abdominal cramps, bloating; cholestatic jaundice; gallbladder disease.

4. Skin. Chloasma or melasma that may persist when drug is discontinued; erythema multiforme; erythema nodosum; hemorrhagic eruption; loss of scalp hair; hirsutism.

5. Eyes. Steepening of corneal curvature: intolerance to contact lenses.

6. Central Nervous System. Headache, migraine, dizziness; mental depression; chorea.

7. Miscellaneous. Increase or decrease in weight; reduced carbohydrate tolerance; aggravation of porphyria; edema; changes in libido.

Estradiol contraindications

See also:
What is the most important information I should know about Estradiol?

Estradiol can harm an unborn baby or cause birth defects. Do not use if you are pregnant.

You should not use this medication if you have any of the following conditions: liver disease, a bleeding disorder, unusual vaginal bleeding, a history of breast or uterine cancer, or if you have ever had a heart attack, stroke, or a blood clot.

Estradiol may increase your risk of developing a condition that may lead to uterine cancer. Your doctor may prescribe a progestin while you are using Estradiol, to help lower this risk. Report any unusual vaginal bleeding right away.

Long-term use of Estradiol may increase your risk of breast cancer, heart attack, stroke, or blood clot. Talk with your doctor about your individual risks before using Estradiol transdermal long term.

Have regular physical exams and self-examine your breasts for lumps on a monthly basis while using Estradiol transdermal.

Estradiol transdermal should not be used to prevent heart disease, stroke, or dementia, because this medicine may actually increase your risk of developing these conditions.

Active ingredient matches for Estradiol:

Estradiol

References

1. DailyMed. "ESTRADIOL HEMIHYDRATE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
2. PubChem. "estradiol". https://pubchem.ncbi.nlm.nih.gov/com... (accessed September 17, 2018).
3. DrugBank. "estradiol". http://www.drugbank.ca/drugs/DB00783 (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology