Estradiol - Transdermal

What Is Estradiol?

Estradiol is a transdermal delivery system (a patch) that is used to treat and prevent moderate to severe symptoms associated with menopause, such as hot flashes, vaginal itching or dryness, and osteoporosis (bone loss).

Transdermal patches adhere to the skin as a way to deliver a drug. They provide a specific dose of medication that is absorbed through the skin and into the bloodstream.

Estradiol belongs to the class of medicines called estrogen hormones that work by replacing estrogen normally produced by the body.

Brand-name variations of this drug exist, such as Climara, Menostar, Minivelle, Vivelle, and Vivelle Dot.

However, while estradiol is also used in the form of a topical gel, such as Divigel, this article will highlight its uses as a transdermal patch as a generic product.

What Is Estradiol Used For?

The FDA has estradiol in the form of a transdermal patch to treat:

• Moderate to severe vasomotor symptoms (hot flashes or night sweats) due to menopause 
• Moderate to severe symptoms of vulvar and vaginal atrophy (a decrease in organ size) due to menopause. When prescribing only for the treatment of vulvar and vaginal atrophy symptoms such as itching, dryness, or burning sensation, first consider the use of topical vaginal products.
• Treatment of hypoestrogenism (low estrogen levels) due to hypogonadism (a decreased production of sex hormones by gonads) or primary ovarian failure.
• Prevention of osteoporosis in females experiencing or experiencing menopause. Consider using non-estrogen medications first and, if required, use only in females at increased risk of osteoporosis. 
  

Menopause is associated with a variety of symptoms caused by estrogen deprivation. Hot flashes are one of the most common symptoms affecting approximately 80% of females. Also, some females may continue to have symptoms like vaginal dryness. Others notice changes in their sex drive or develop bladder control problems.

Estradiol containing estrogen with or without progestin (progestin is a form of progesterone, the hormone that plays a role in the menstrual cycle and pregnancy) is highly effective in reducing the frequency and intensity of menopausal symptoms.

How to Use Estradiol

Read the information leaflet carefully before using estradiol patches and every time you get a refill.

The following offers instructions to safely and effectively use estradiol:

Use the estradiol patch as your healthcare provider tells you to use it. It is for use on the skin only. Wash and dry the skin area where you are ready to apply the patch. Apply the patch on the lower abdomen, upper buttocks, or the outer part of the hip.

Take off the previous patch and use the new one twice a week or as prescribed. Don't overuse the estradiol patches. Apply the new patch to a different skin area. 

Don't apply the patch on the same application site within one week. Always use the patch on clear skin free of cuts, rashes, or other skin problems. Don't apply the estradiol patch on your breasts or other body parts other than specified on the label.

Avoid the removal of the patch while wearing clothes. Take the patch out of the pouch only when ready to apply it. After applying the patch, press it firmly to stick it well on the skin.

Finally, dispose of the old patch properly, and don't stop using it without asking your healthcare provider.

Storage

Store estradiol at room temperature between 68 F to 77 F in their pouches. Take the patch out of the pouch when ready to apply it.

Keep your medications tightly closed and out of the reach of children and pets, ideally locked in a cabinet or closet. Do not store your medication in the bathroom.

Avoid pouring unused and expired drugs down the drain or in the toilet. Ask your pharmacist or healthcare provider about the best ways to dispose of this medicine. Visit the FDA's website to know where and how to discard all unused and expired drugs.

You can also find disposal boxes in your area. Ask your pharmacist or healthcare provider if you have any questions about the best ways to dispose of your medications.

If you travel with estradiol, get familiar with your final destination's regulations. In general, be sure to make a copy of your estradiol prescription. Also, keep your medication in its original container from your pharmacy with your name on the label.

Ask your healthcare provider if you have any questions about traveling with your medicine.

What Are the Side Effects of Estradiol?

This is not a complete list of side effects, and others may occur. A healthcare provider can advise you on side effects. If you experience other effects, contact your pharmacist or a healthcare provider. You may report side effects to the FDA at fda.gov/medwatch or 800-FDA-1088.

Like other medications, estradiol can cause side effects. Tell your healthcare provider about any side effects you experience while taking this medication.

Common Side Effects

Common side effects associated with the use of estradiol patches include:

• Anxiety
• Back, neck, or muscle pain
• Breast pain or tenderness
• Changes in mood
• Change in libido (sexual desire)
• Constipation
• Darkening of skin on the face 
• Depression
• Difficulty wearing contact lenses
• Hair loss
• Headache
• Heartburn
• Joint pain
• Nausea and vomiting
• Painful menstrual periods
• Redness or irritation on the skin where the patch is applied
• Runny nose or congestion
• Swelling, redness, or itching of the vagina
• Unwanted hair growth
• Vaginal discharge
• Weight gain or loss

Call your healthcare provider if the symptoms do not go away or worsen.

Severe Side Effects

Estradiol has a black box warning. A black box warning is the strongest warning required by the FDA.

Estrogen-alone therapy increases the risks of endometrial cancer in people with a uterus.

Estrogen-alone or estrogen plus progestin therapy increases the risk of the following conditions in postmenopausal people:

• Stroke, deep vein thrombosis (DVT; a condition caused by a blood clot developing in a vein)
• Pulmonary embolism (PE; a blood clot in arteries of the lungs)
• Myocardial infarction (MI; heart attack)
• Invasive breast cancer
• Dementia

Additionally, estrogen plus progestin or estrogen-alone therapy should not be used to prevent heart disease and dementia.

Contact your healthcare provider right away if you develop any signs of a severe reaction. Call 911 if your symptoms feel life-threatening.

Serious side effects and their symptoms include:

• Hypersensitivity reaction (swelling of the eyes, face, lips, tongue, throat, hands, feet, difficulty breathing or swallowing)
• Increase the risk of developing cancer of the ovaries and gallbladder disease
• Liver problems
• Cardiovascular (heart and blood vessels) disorders
• Stroke
• Blood clots
• Endometrial Cancer (the most common cancer of the uterus)
• Dementia in females 65 and older
• Vision loss

Dosage: How Many Estradiol Patches Should I Use?

Modifications

The following modifications (changes) should be kept in mind when using estradiol:

Severe allergic reaction: Avoid using estradiol if you have a known allergy to it or its ingredients. Ask your pharmacist or healthcare provider for a complete list of the ingredients if you're unsure.

Pregnancy: Estradiol is not indicated for use in pregnant people as there has not been enough research completed to safely asses the chance for risk. Therefore, make your healthcare provider aware if you are or intend to become pregnant while taking estradiol.

Breastfeeding: Estrogen is present in human breast milk. We don't know enough about the safety of estradiol in human breast milk and nursing babies. The use of this product should be decided considering the clinical needs of medicine for the mother and the risk to a nursing baby.

Talk with your healthcare provider to weigh the benefits and risks of using estradiol while nursing and the different ways to feed your baby if you plan to breastfeed.

Adults over 65: Clinical studies haven't included a large enough number of people in this age group to see whether they respond differently from younger adults. Older adults with several medical conditions or taking several medications should use caution with estradiol. Older adults might also be more sensitive to the side effects.

Children: Clinical studies using estradiol have not been conducted on children. The safety and effectiveness of estradiol have not been established in children, including children with hypoestrogenism.

Administration modifications: For transdermal (under the skin) use only.

Missed Dose

If you accidentally forgot to apply your estradiol patch, apply it as soon as you remember. If it's already close to your next scheduled dose, skip the missed patch and apply the following patch at your next scheduled time. Don't try to double up to make up for the missed dose.

Try to find ways that work for you to help yourself remember to routinely keep your appointments and take your medication. If you miss applying the estradiol patches, it might be less effective at treating your condition.

Overdose: What Happens If I Use Too Many Patches of Estradiol?

If you wear estradiol patches for longer or more than advised by your healthcare provider, an overdose may occur.

Too much absorption of estrogen in your bloodstream may cause the following symptoms:

• Abdominal pain
• Breast tenderness
• Drowsiness and fatigue
• Nausea or vomiting
• Withdrawal (vaginal) bleeding

In case of an overdose, discontinue applying the patches and report to your healthcare provider. 

If you think you're experiencing an overdose or life-threatening symptoms, seek immediate medical attention.

Precautions

What Are Reasons I Shouldn’t Use Estradiol?

The use of estradiol patches is discouraged in people with the following conditions:

• Abnormal genital (vaginal) bleeding
• Breast cancer or a history of breast cancer
• Estrogen-dependent neoplasia (a type of breast tumor dependent on estrogen hormone for growth)
• Active DVT, PE, or a history of these conditions
• Active arterial thromboembolic disease (e.g., stroke and heart attack) or a history of these conditions 
• Known anaphylactic (severe allergic) reactions or angioedema (swelling under the skin that occurs when fluid leaks from blood vessels), or hypersensitivity with estradiol transdermal system
• A history of liver disease
• Protein C, protein S, antithrombin deficiency (blood clotting disorders causing abnormal blood clots), or other known thrombophilic disorders (blood clots in veins)
  

What Other Medications Interact With Estradiol?

Estradiol contains estrogens metabolized (transitioned into energy) partially by the cytochrome P450 3A4 (CYP3A4) enzyme.

As a result, the following drugs can cause a decrease in therapeutic effects, a change in bleeding profile, or an increase in side effects.

Inducers of CYP3A4 enzyme may reduce the plasma levels of estradiol:

• Tagretol (carbamazepine)
• Dexamethasone
• Phenobarbital
• Dilantin (phenytoin)
• Rifadin (rifampin)
• St. John's Wort preparations (hypericum perforatum)
  

Inhibitors of CYP3A4 enzyme may increase the plasma levels of estradiol:

• Biaxin XL (clarithromycin)
• Ery-tab (erythromycin)
• Sporanox (itraconazole)
• Ketoconazole
• Norvir (ritonavir)
• Grapefruit juice
  

This may not be a complete list of drugs that interact with estradiol. Therefore, always consult your healthcare provider about all the prescription, non-prescription, multivitamin or herbal products you take. 

What Medications Are Similar?

Estradiol patches are available under different brand names. Some of the common brand names approved by the FDA are:

• Climara
• Menostar
• Minivelle
• Vivelle
• Vivelle-Dot

Always use the brand name prescribed by your healthcare provider. If you want to use an alternative, ask your healthcare provider.

How Can I Stay Healthy While Using Estradiol?

Menopause is a natural process but can be very challenging for some people. They may develop symptoms, such as feelings of warmth in the face, neck, and chest, and hot flashes, which can be very challenging.

Estradiol patches are indicated to manage the symptoms and other problems associated with these conditions.

The following are the measures that should be considered while using this medicine:

Always follow the prescription and guidelines of your healthcare provider. Keep a regular schedule of applying and removing the patches to avoid missing the dose or having an overdose. Don't use this transdermal patch for any condition other than prescribed.

Keep close monitoring for signs such as new breast lumps, unusual vaginal bleeding, changes in vision or speech, shortness of breath, weakness, and fatigue. Call your healthcare provider if any of these symptoms develop. 

Tell your healthcare provider about your health problems, if any, before initiating the treatment with estradiol. Keep regular appointments with your healthcare provider, breast screening or X-rays, pelvic examination, and other lab tests to determine any adverse effects of the drug.

Mention all the prescription and non-prescription drugs and other products you take to your healthcare provider. Don't use estradiol if you are pregnant or breastfeeding.

Consider working on risk factors that increase the chances of adverse effects such as heart problems. Talk with a healthcare provider to help lower your blood sugar levels, achieve a healthy weight, reduce tobacco intake and adopt a healthy lifestyle.