The reference site for Estradiol

Estradiol is a female sex hormone necessary for many processes in the body. Estradiol vaginal products release estrogen that is absorbed directly through the skin of the vaginal wall.

WHAT IS ESTRADIOL?

Estradiol is a female sex hormone necessary for many processes in the body. Estradiol vaginal products release estrogen that is absorbed directly through the skin of the vaginal wall.

This medication is also prescribed for symptomatic treatment of the usual symptoms associated with menopause (hot flushes, vaginal dryness, etc.), prevention of bone fractures associated with osteoporosis, reduction of the risk of heart attacks and strokes, and dysfunctional (excessive and painful) uterine bleeding.

The vaginal cream is prescribed for vaginal or vulvar atrophy associated with menopause.

 

Brand Name(s): Estrace; Climara; Estraderm; Gynodiol; Menostar
CAS nº: 50-28-2
(ess tra DYE ole)

Product Info

The sections below will provide you with more specific information and guidelines related to estradiol and its correct use. Please read them carefully.

FDA Information

Estradiol was approved by the FDA in 1975 for the treatment of moderate to severe vasomotor symptoms associated with menopause as well as for the prevention of osteoporosis.

Estradiol tablets, the generic equivalent of Bristol Myers Squibb’s Estrace®, has been approved for marketing. Barr Pharmaceuticals’ estradiol version will be available in 0.5, 1, and 2 mg strengths.

Why is this medication prescribed?

Estradiol is prescribed for symptomatic treatment of the usual symptoms associated with menopause (hot flushes, vaginal dryness, etc.), prevention of bone fractures associated with osteoporosis, reduction of the risk of heart attacks and strokes, and dysfunctional (excessive and painful) uterine bleeding. The vaginal cream is prescribed for vaginal or vulvar atrophy associated with menopause.

Estradiol enters cells freely and interacts with a cytoplasmic target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell.

Estradiol binds well to both estrogen receptors, ER&#945 and ER&#946, in contrast to certain other estrogens, notably medications that preferentially act on one of these receptors. These medications are called selective estrogen receptor modulators, or SERMs.

Other uses for this medicine

This medication may also be used to regulate your menstrual cycle.

However, it is strongly advised that you talk to your doctor about the possible risks of using this drug for your particular condition.

Dosage and using this medicine

Use estradiol exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

To use the estradiol vaginal ring:

Squeeze the sides of the ring together and insert it into the vagina as far as possible (into the upper 1/ 3 of the vagina). You should not be able to feel the ring once it is in position. If you can feel it, use a finger to push it further into the vagina. It is not possible for the ring to go too far in or become lost.

The ring should remain in place for 90 days. It should then be removed and replaced by a new ring, if prescribed by your doctor. If at any time the ring falls out, rinse it with warm water and reinsert it. If it slides down into the lower part of the vagina, use a finger to reinsert it.

The ring does not need to be removed during sexual intercourse. It should not be felt by either partner. If it is bothersome, it can be removed, rinsed with warm water, and reinserted following intercourse.

To remove the ring, loop a finger through the ring and gently pull it from the vagina.

To use the estradiol vaginal cream:

Using the marked applicator provided, measure the prescribed dose of cream.

Lie on your back with your knees drawn up, sit, or stand in a position that allows you comfortable access to the vaginal area. To deliver the medication, gently insert the applicator deep into your vagina and press the plunger downward to its original position.

Clean the applicator by pulling the plunger from the barrel. Wash it with mild soap and warm water.

Have yearly physical exams and examine your breasts for lumps on a monthly basis while using estradiol.

What special precautions should I follow?

BEFORE TAKING ESTRADIOL:

Tell your doctor if you have any of the following: high blood pressure, angina, or heart disease; high levels of cholesterol or triglycerides in your blood; liver disease; kidney disease; asthma; epilepsy; migraines; diabetes; depression; gallbladder disease; uterine fibroids; had a hysterectomy (uterus removed); a narrow, short, or prolapsed vagina; vaginal irritation; or a vaginal infection.

Do not use estradiol without first talking to your doctor if you have a circulation, bleeding, or blood-clotting disorder; undiagnosed, abnormal vaginal bleeding; or any type of breast, uterine, or hormone-dependent cancer. Using estradiol may be dangerous in some cases if you have any of the conditions listed above.

You may not be able to use estradiol, or you may require a dosage adjustment or special monitoring during treatment, if you have any of the conditions listed above.

Long-term treatment with estradiol may increase the risk of a stroke. Because of this risk, you should contact your doctor or healthcare provider to discuss your individual risks and benefits before taking estradiol during a long-term cycle. You should also talk to your doctor or healthcare provider on a regular basis (for example, every 3-6 months) about whether you should continue this treatment.

The Women’s Health Initiative (WHI) study reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50-79 years of age) during 5 years of treatment with oral conjugated estrogens combined with medroxyprogesterone acetate.

The WHIMS study found that postmenopausal women 65 years of age or older who were treated with oral conjugated estrogens plus medroxyprogesterone acetate had an increased risk of developing dementia. It is unknown whether this finding applies to younger postmenopausal women or to women using estrogen only therapy.

Estradiol is in the FDA pregnancy category X. This means that estradiol will cause birth defects in an unborn baby. Do not use estradiol if you are pregnant or are planning a pregnancy.

Estradiol may decrease milk flow and have other effects on milk composition. Do not use estradiol without first talking to your doctor if you are breast-feeding a baby.

What should I do if I forget a dose?

Insert the next dose of cream or ring as soon as you remember. Continue to follow your regular schedule. Do not use two doses simultaneously unless your doctor directs otherwise.

If at any time the ring falls out, rinse it with warm water and reinsert it. If it slides down into the lower part of the vagina, use a finger to reinsert it.

What side effects can this medication cause?

Common side effects from estradiol use include:

abdominal cramping or bloating
acne (usually less common after first 3 months and may improve if acne already exists)
breast pain
tenderness or swelling
dizziness
nausea
swelling of ankles and feet
unusual tiredness or weakness
vomiting

Tell your doctor if any of these symptoms are severe or do not go away:

decreased appetite, nausea, or vomiting
swollen breasts
acne or skin color changes
decreased sex drive
migraine headaches or dizziness
vaginal pain, dryness, or discomfort
water retention (swollen hands, feet, or ankles)
depression
changes in your menstrual cycle or break-through bleeding

If you experience any of the following symptoms, call your doctor immediately:

an allergic reaction (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives)
shortness or breath or pain in the chest
a painful, red, swollen leg
abnormal vaginal bleeding
pain, swelling, or tenderness in the abdomen
severe headache or vomiting, dizziness, faintness or changes in vision or speech
yellowing of the skin or eyes or
a lump in a breast

IMPORTANT NOTE: Estradiol increases the risk of developing a condition (endometrial hyperplasia) that may lead to cancer of the lining of the uterus. Taking progestins, another hormone drug, while using estradiol lowers the risk of developing this condition. Therefore, if your uterus has not been removed, your doctor may prescribe a progestin for you to take together while using estradiol. Visit your doctor regularly and report any unusual vaginal bleeding right away.

Treatment with estradiol long-term may increase the risk of a stroke. Because of this risk, you should contact your doctor or healthcare provider to discuss your individual risks and benefits before taking estradiol long-term. You should also talk to your doctor or healthcare provider on a regular basis (for example, every 3-6 months) about whether you should continue this treatment.

What storage conditions are needed for this medicine?

Keep the vaginal rings and cream in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).

Throw away any medication that is outdated or no longer needed. Should you have any concerns, please talk to your pharmacist about the proper disposal of your medication.

In case of an emergency/overdose

In the case of an overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.

Symptoms of overdose may include:

excessive vaginal bleeding (2-7 days following overdose)
fluid retention
breast tenderness
discoloration of urine
rash
nausea and vomiting
headache
drowsiness
mental changes

Product Images

PICTURES OF ESTRADIOL PILLS

Below you will find images and specific information on the principal types of estradiol that exist, including their respective brand name(s), strength, inscription codes and manufacturers.

The information below includes general information and guidelines for patients taking this medication and should never be used to substitute professional medical advice that can be provided by a qualified physician or family doctor.

Name: ESTRADIOL
Strength(s): 0.5 MG
Imprint: WATSON 528
Manufacturer: WATSON LABS.

Name: ESTRADIOL
Strength(s): 0.5 MG
Imprint: M | E3
Manufacturer: MYLAN

Name: ESTRADIOL
Strength(s): 0.5 MG
Imprint: b | 899 1/2
Manufacturer: BARR

Name: GYNODIOL®
Strength(s): 1 MG
Imprint: 1256
Manufacturer: NOVAVAX INC.

Name: ESTRADIOL
Strength(s): 1 MG
Imprint: b | 886 1
Manufacturer: BARR

Name: ESTRADIOL
Strength(s): 1 MG
Imprint: WATSON 487
Manufacturer: WATSON LABS.

Name: ESTRACE®
Strength(s): 1 MG
Imprint: MJ 755
Manufacturer: WC PROF PRODS.

Name: ESTRADIOL
Strength(s): 1 MG
Imprint: AP 026
Manufacturer: SANDOZ

Name: ESTRADIOL
Strength(s): 1 MG
Imprint: M | E4
Manufacturer: MYLAN

Name: GYNODIOL®
Strength(s): 1.5 MG
Imprint: 0158
Manufacturer: NOVAVAX INC.

Name: ESTRACE®
Strength(s): 2 MG
Imprint: MJ 756
Manufacturer: WARNER-CHILCOTT

Name: ESTRADIOL
Strength(s): 2 MG
Imprint: b | 887 2
Manufacturer: BARR

Name: ESTRADIOL
Strength(s): 2 MG
Imprint: AP 027
Manufacturer: SANDOZ

Name: ESTRADIOL
Strength(s): 2 MG
Imprint: WATSON 488
Manufacturer: WATSON LABS.

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