Estradiol (Transdermal)

Overview

Women who are in the postmenopausal stage of life may find effective relief from the symptoms associated with menopause through the use of estradiol. This medication is available by prescription and can be utilized as a patch, spray or gel. If you have uncomfortable hot flashes you may find that taking this medication can help to ease the discomfort.

This medication is also used to relieve symptoms such as vaginal burning, itching and dryness that can be caused by the decreased levels of estrogen that the body is producing. The estradiol can also be used to help prevent the osteoporosis that often comes with menopause. Estradiol can also be used in women who have not yet experienced menopause but whose bodies are not producing adequate levels of estrogen. In such cases, it is important that these women take effective birth control while using this hormone as it is not recommended for use in pregnant women. If you are taking estradiol and become pregnant, notify your doctor immediately.

Estradiol has been reported to cause anaphylaxis in some patients, which can be a life-threatening allergic reaction. It is important that any patients taking this medication familiarize themselves with the symptoms and signs of this reaction and seek emergency medical help should any of them occur.

If you are taking tranexamic acid your doctor may not want you to take both drugs concurrently. Prior to beginning your estradiol course of treatment be sure to inform your physician of all drugs that you are taking and for what ailments. They may alter the dosage of your estradiol or another medication in order to help minimize the occurrence of unwanted side effects that can happen when multiple drugs are taken at the same time.

Taking this drug may increase your risk of heart attack, stroke and blood clots. If you are at high risk for these conditions your doctor may not prescribe estradiol to you. These medications must be monitored, especially in women who are taking them over an extended period of time. If your doctor advises any diagnostic testing during your course of treatment with estradiol be sure to keep all appointments and undergo all recommended testing as directed. If you smoke, have high blood pressure, are overweight or have any of the conditions more fully explained below, you are at a higher risk for stroke, blood clots and heart attack while taking this medication. Be sure to inform your doctor of any changes to your overall health, any changes to the medications that you are taking for these conditions, or if you experience any negative effects while taking estradiol.

There can be an increased risk of certain cancers when taking this drug for an extended period of time. Your doctor will review your entire health profile and overall cancer risk prior to keeping you on this medication in order to decrease the likelihood of developing cancer. If you are instructed by your physician to undergo any testing or screening for cancer while you are taking this medication be sure to keep all appointments as directed.

In women who are over the age of 65 and are taking this medication, there can be an increased risk of developing dementia. If you experience any memory loss, loss of clarity, or confusion while taking this drug be sure to notify your physician right away.

Estradiol is available in these following delivery methods:

  • Cream or emulsion
  • Topical gels
  • Spray
  • An extended release patch

Conditions Treated

  • Symptoms of menopause
  • Low estrogen levels

Type Of Medicine

  • Endocrine-Metabolic Agent
  • Estrogen Replacement

Side Effects

There are other unwanted side effects that can occur when you are taking estradiol. In fact, some of these can potentially be a sign of a more serious problem. If you experience any of the symptoms below, it is important that you contact your doctor as you may require further medical attention. Notify your doctor as soon as possible if any of the following occur:

Unknown occurrence:

  • Abdominal or stomach cramps or pain
  • Vomiting
  • Anxiety
  • Unusually heavy or unexpected menstrual bleeding
  • Belching
  • Unpleasant breath odor
  • Bloating
  • Trouble walking
  • Breast tenderness, enlargement, pain or discharge
  • Trouble recognizing objects
  • Changes in skin color
  • Tightness in the chest
  • Chest pain or discomfort
  • Swelling of the abdominal or stomach area
  • Clay-colored stools
  • Sweating
  • Confusion
  • Sudden loss of consciousness
  • Convulsions
  • Sores, ulcers, or white spots in the mouth or on the lips
  • Darkening of the urine
  • Sore on the skin of the breast that does not heal
  • Difficulty with breathing
  • Sensitivity to the sun
  • Dimpling of the breast skin
  • Red, irritated eyes
  • Double vision
  • Puffiness or swelling of the eyelids or other areas of the face
  • Fast heartbeat
  • Poor insight and judgment
  • Fluid-filled skin blisters
  • Pains in the stomach, side torso or abdominal area
  • Headaches
  • Pain, redness, or swelling in the arm, foot or leg
  • Heartburn
  • Pain or discomfort in the arms, jaw, back or neck
  • Irregular heartbeat
  • Pain during sexual intercourse
  • Large, hive-like swelling on the face or other areas of the body
  • Itching of the vagina or genital area
  • Joint or muscle pain
  • Pain or feeling of pressure in the pelvis
  • Noisy breathing
  • Numbness and tingling in the mouth, fingertips or feet
  • Light-colored stools
  • A headache, severe and throbbing
  • Loss of bladder control
  • Indigestion
  • A migraine headache
  • Mood or mental changes
  • Full or bloated feeling or pressure in the stomach
  • Muscle spasm or jerking of all extremities
  • Inverted nipple
  • Loss of appetite
  • Pain in the ankles or knees
  • Muscle cramps in the hands, arms, feet, legs or face
  • Painful, red lumps under the skin, mostly on the legs
  • Lump in the breast or under the arm
  • Persistent crusting or scaling of the nipple
  • Nausea
  • Problems with memory or speech
  • Fever
  • Rash, hives, or itching
  • Fainting
  • Redness or swelling of the breast
  • Dizziness or lightheadedness
  • Skin thinness
  • Difficulty with swallowing
  • Sore throats
  • Diarrhea
  • Stomach discomfort, upset or pain
  • Coughing
  • Sudden shortness of breath or troubled breathing
  • Constipation
  • Swelling
  • Clear or bloody discharge from the nipple
  • Thick, white vaginal discharge
  • Chills
  • Tremor
  • Changes in vision
  • Trouble thinking and planning
  • Change in vaginal discharge
  • Unexpected or excess milk flow from the breasts
  • Blurred vision
  • Unusual tiredness or weakness
  • Blistering, peeling or loosening of the skin
  • Vaginal bleeding or spotting
  • Backaches
  • Vomiting of blood
  • Acid or sour stomach
  • Yellow eyes or skin

As your body adjusts to the estradiol and the increased amount of estrogen in the system, you may experience some side effects that will go away on their own. If you have any of the symptoms listed below, and they do not dissipate after a few days, or become worse, inform your doctor as there may be further medical attention that is necessary.

Less likely:

  • Muscle pain or stiffness
  • Back pain
  • Difficulty with moving
  • Stuffy or a runny nose
  • Muscle aches

Unknown occurrence:

  • Decreased interest in sexual intercourse
  • Redness of the skin
  • Hives or welts
  • Mental depression
  • Increased hair growth, especially on the face
  • Weight changes
  • Increased interest in sexual intercourse
  • Loss of scalp hair
  • Leg cramps
  • Loss of sexual ability, desire, drive, or performance
  • Mood disturbances
  • Irritability
  • Increase in sexual ability, desire, drive or performance
  • Patchy brown or dark brown discoloration of the skin
  • Twitching
  • Heavy bleeding

While this list aims to be comprehensive in nature, some patients may experience side effects that are not included in these lists. If you have any symptoms that become problematic, contact your prescribing physician for further advice.

Dosage

When taking estradiol it is important that you follow the dosing instructions that are provided by your physician. In order to avoid unwanted side effects do not take more than the prescribed amount or lengthen the course of therapy.

Estradiol is a topical medication that should not be ingested in any form or manner. Avoid contact with eyes, nasal membranes, breasts or vagina. Be sure to avoid application to any areas of the skin that are affected by burns, scrapes or cuts. If you happen to get estradiol in such areas be sure to thoroughly rinse with cool water. Be sure to wash the hands with soap and water following application in order to remove any excess medication.

When using the estradiol patch:

  • Prior to and following application be sure to thoroughly wash your hands with soapy water
  • Do not cut the pouch containing the patch, but instead tear it open
  • Remove the backing from the patch and apply to a hairless area on the upper region of the buttocks or the lower abdomen
  • Be sure to remove all lotions and powders prior to application
  • Hold the patch firmly in place for about 10 seconds
  • Avoid applying the patch to any skin folds
  • Do not apply the estradiol patch to the breast area
  • Avoid any irritated, oily, or otherwise harmed skin
  • Do not apply the patch that moves a lot or is disturbed by clothing as it may rub off
  • Keep the patch on for the recommended period of time and until it is time to place the new one
  • Alternate the location of where you place the patch, and do not put it in the same spot within the same week
  • Water will not affect the patch, and patients can bathe and shower regularly while wearing the patch
  • Be sure to throw the patch away where it cannot be accessible to pets or children
  • Do not attempt to flush the finished patch in the commode

Patients who are using the estradiol spray:

If your doctor has prescribed the estradiol spray, be aware that it comes in a pre-measured applicator that has the proper amount of spray to apply to the skin. The initial time that you use each applicator you will need to hold the applicator upright and pump at least 3 times prior to use. Once the applicator has been initially primed there is no need to repeat this step.

The best location to apply the spray is on the forearm. Find an area on the inside of the forearm in-between the wrist and elbow on skin that is not broken or irritated. It is best to avoid the area surrounding the vagina or applying it on or near the breasts. Be sure to allow at least one hour after applying the spray before showering; do not get dressed for a least a few minutes before you get dressed. With an increased dose, it is important to reapply the spray on a different area when applying the second or third application.

It is important that neither your children nor your pets lick or come in to close contact with the area where the estradiol spray is applied. If you are concerned that they have come into contact it is necessary to wash the affected area of the pet or child with soap and water.

Be sure to put the lid and protective cap back onto the application device. The maximum amount of sprays is 75 for each applicator. Patients are advised to wear sunscreen when taking this medication.

If you are using estradiol gel:

Estradiol in gel form is administered via a pump that is self-measuring. The first time that you use the pump you may need to press on the applicator a few times, but after the initial dose, this will not be necessary. The gel is meted out in one-pump increments which makes it easier to measure your dosage correctly.

As with the other methods of delivery, it is important that the estradiol is applied to clean and dry skin that is not broken, burnt or scratched. It is best to avoid the breast and vaginal areas with this gel. Once the gel has been applied wait a few minutes for the medicine to be absorbed before you dress. Apply the gel yourself and do not let anyone else come into contact with the area of your skin where it has been applied for at least one hour. It is recommended that sunscreen is used by patients that are using estradiol gel but that they wait about a half hour before applying to the area where the gel has been applied. This medication contains alcohol and is flammable; do not apply while smoking or near an open flame.

Each patient's medical requirements may differ, so it is important that you follow the specific instructions provided by your doctor. In addition to the amount of the drug that you should be taking, they will advise you on the frequency of doses or how much time to wait between each dose, and on the length of time, you should continue taking estradiol.

These guidelines are simply the typical amounts that patients are advised to take for each type of affliction; if your doctor has prescribed a different amount, it is important that you follow the instructions of their prescription.

In the treatment of hot flashes and other menopausal symptoms:

Transdermal gel dosage, depending on the exact type of medicine you will likely be prescribed one of the following amounts:

Apply 0.87 grams to the upper arm one time per day.
Apply 1.25 grams to the arm one time per day.

Transdermal patch dosage:

Place one patch containing 0.025 milligrams on the lower abdominal area or the upper buttocks one time per week.
Place one patch containing 0.0375 milligrams on the lower abdominal area or the upper buttocks two times per week every 3-4 days as directed by your physician.

Transdermal spray dosage:

A single spray one time per day, typically during the morning hours as directed by your physician.

When taken as prevention of postmenopausal osteoporosis:

Transdermal patch dosage:

Place one patch containing 0.025 milligrams on the lower abdominal area or the upper buttocks one time per week.
Place one patch containing 0.025 milligrams on the lower abdominal area or the upper buttocks two times per week every 3-4 days as directed by your physician.

Taken for the treatment of decreased levels of estrogen:

Transdermal patch dosage:

Place one patch containing 0.025 milligrams on the lower abdominal area or the upper buttocks one time per week.

If you forget to apply a patch at the scheduled time do not ever wear two to make up for the missed dosage as this can be dangerous. When you forget a dosage, it is best to apply the patch as soon as possible unless it is close to the next prescribed dosage time. If you have forgotten a dose and are unsure what to do, contact your doctor or pharmacist for further guidance.

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Do not apply the spray dosage in cases where more than 12 hours have elapsed after your most recent dose.

Major drug interactions:

There are certain drugs and medications that should not be taken concurrently due to the possibility of the combination causing negative effects. If you are taking tranexamic acid in the treatment of another ailment, your doctor may not opt to prescribe estradiol for your treatment of hot flashes and other symptoms related to menopause.

If you are prescribed both medications concurrently, be sure to inform your doctor of any significant side effects that you experience as you may need to have your dosage altered in one or both of the drugs, or an alternative medication may need to be found.

There are other drugs that are not recommended to be taken together but are often deemed the most effective drugs for the patient's particular situation. If you are taking both estradiol and one of the medications listed below, be sure to keep your doctor informed of any significant and unwanted side effects that you may experience:

  • Bupropion
  • Sugammadex
  • Ceritinib
  • Pitolisant
  • Tizanidine
  • Lixisenatide
  • Donepezil
  • Isotretinoin
  • Idelalisib
  • Dabrafenib
  • Lesinurad
  • Eliglustat
  • Lumacaftor
  • Darunavir
  • Pixantrone
  • Conivaptan
  • Theophylline
  • Carbamazepine

If you are currently using one of the drugs listed below and are prescribed estradiol, be aware that the combination of the two drugs may raise your chance of experiencing unwanted side effects.

  • Alprazolam
  • Troleandomycin
  • Aprepitant
  • Topiramate
  • Bacampicillin
  • Telaprevir
  • Bexarotene
  • St. John's Wort
  • Clarithromycin
  • Rufinamide
  • Cyclosporine
  • Ritonavir
  • Efavirenz
  • Rifampin
  • Primidone
  • Fosphenytoin
  • Phenytoin
  • Griseofulvin
  • Oxcarbazepine
  • Lamotrigine
  • Mycophenolic Acid
  • Licorice
  • Etravirine
  • Mycophenolate Mofetil
  • Modafinil
  • Nelfinavir
  • Levothyroxine
  • Phenobarbital
  • Ketoconazole
  • Prednisolone
  • Ginseng
  • Rifabutin
  • Fosaprepitant
  • Rifapentine
  • Fosamprenavir
  • Rosuvastatin
  • Delavirdine
  • Selegiline
  • Colesevelam
  • Tacrine
  • Bosentan
  • Tipranavir
  • Betamethasone
  • Troglitazone
  • Atazanavir
  • Voriconazole
  • Amprenavir
  • Warfarin

Be sure to inform your doctor of all of the medications that you are currently taking as well as those that you have recently stopped taking. This includes both prescription and non-prescription medications as well as all herbal remedies and any vitamin or mineral supplements. If you use tobacco or alcohol on a regular basis be sure to also inform your doctor of these habits before you start taking estradiol. If you have any concerns about the medications or supplements that you are taking and how they may interact with estradiol, discuss these concerns with your doctor or pharmacist rather than quitting your medication.

It is recommended that you curtail your use of caffeine or eliminate it altogether when taking estradiol. Your doctor or pharmacist can further guide you on this recommendation.

When patients have other medical conditions, the use of estradiol may not be as effective, or in some cases, may even be harmful. Be sure you discuss your comprehensive medical history with your doctor before taking estradiol, especially if you suffer from one of the following conditions:

  • Abnormal or unusual vaginal bleeding
  • Blood clots
  • Migraine headaches
  • Heart attack
  • Protein C or protein S deficiency
  • Hypocalcemia
  • Surgery and inactivity during post-op
  • Hypertension
  • Asthma
  • Hereditary angioedema
  • Diabetes
  • Gallbladder disease
  • Systemic lupus erythematosus (SLE)
  • Epilepsy
  • Jaundice during pregnancy or from using hormonal therapy
  • Heart disease
  • Edema
  • Hypercalcemia
  • Cancer
  • Hypertriglyceridemia
  • Tumors (estrogen-dependent)
  • Hypothyroidism
  • Stroke
  • Liver tumor
  • Endometriosis
  • Liver disease
  • Porphyria
  • Breast cancer

Warnings

Patients that are utilizing estradiol patches will likely need regular follow-up care as directed by their physician. They may order a series of diagnostic tests in order to monitor the efficacy of the medication along with the desire to check for any unwanted side effects. Your doctor may order a mammogram, breast exam or pelvic exam while you are taking the estradiol patches, gels or sprays. It is important that you keep all appointments and undergo all ordered tests while you are taking this medication.

As this medication is used in the treatment of post-menopausal women, it is unlikely that patients will become pregnant. If you do become pregnant while taking estradiol be sure to notify your doctor immediately.

Your doctor will review the risks of taking this medication with you, it has been reported to increase the likelihood of heart attack, stroke, and blood clots. The increased risk of these conditions may continue even after you have finished your estradiol course of treatment. Inform your doctor if you have any of the following conditions or lifestyle habits, as they can increase your risk for these serious ailments:

  • Tobacco use
  • Elevated blood pressure
  • High cholesterol
  • Use of tobacco products
  • Obesity
  • Overweight
  • Diabetes

The symptoms to look out for, especially if you have one of the above to consider, are:

  • Double vision
  • Unable to move extremities such as the arms and legs
  • Frozen facial muscles
  • Headaches
  • Confusion
  • Inability to speak properly

If you use estradiol over an extended period of time your likelihood of contracting certain cancers may increase. Your overall risk profile for endometrial cancer, uterine cancer, and breast cancer will need to be thoroughly reviewed prior to starting the estradiol course of treatment. If you have an increased likelihood of these cancers, your doctor will conduct regular screenings and exams to ensure that your treatment remains safe.

Women who have not undergone a hysterectomy may require a complementary treatment of progestin replacement.

Regardless of your past medical history, alert your doctor should you experience any unexpected vaginal bleeding while taking estradiol in any form. Use of this medication, especially in women over the age of 65 may increase the change of dementia. Inform your doctor of any changes in your level of clarity, or if you experience unusual memory loss.

Your doctor will also review the increased likelihood of gallbladder disease that can occur in patients that are taking estradiol.

During the time period that you are taking estradiol, your doctor may advise that you undergo an eye exam, if they recommend this course of action, be sure to keep all appointments. Inform your doctor of any changes to your vision that you experience while taking this medication.

Patients taking this medication have reported instances of an allergic reaction known as anaphylaxis. This is a serious condition that can be life-threatening in some instances and requires immediate emergency medical care. Seek emergency treatment right away if you are taking estradiol and experience:

  • Hoarseness
  • Excessive itching
  • Rash
  • Difficulty breathing
  • Difficulty with swallowing
  • Swelling of the hands or face
  • Mouth swelling

Do not allow children or pets to come into contact with this medication as it can have a detrimental effect on their health. If you notice any changes to their nipples, increased tenderness or swelling of the breasts in females, or enlarged breasts in males, it is best to seek medical or veterinarian attention. Be sure that your pets do not lick the area where you apply the medication as it can be absorbed into their system. Small pets, in particular, may be negatively affected by exposure to this drug.

While you are taking this medication it is best to avoid beverages such as grapefruit juice and supplements like St. John's Wort without first conferring with your doctor.

Advise your doctor of any changes that occur with the medications that you are taking or if you have any changes to your overall health and wellness.

Storage

Keep the estradiol patches in their unopened pouches until it is time to use them. Avoid exposure to direct light, moisture, extreme heat or cold. Be sure that the patches are kept at room temperature in a low-moisture environment. Do not freeze the patches.

Be sure to keep this and all medications away from children. Take care when discarding the patches, and ensure that they are placed in a receptacle that is not accessible to pets or children.

Summary

The transdermal estradiol treatment option has proven successful for many women looking to lessen the negative effects that often occur with menopause. This drug is also used in women who have not yet undergone menopause but do not produce enough estrogen, they may be prescribed this medication. If a woman who is not yet menopausal is taking this drug it is important that they utilize effective birth control while taking this medication and notify their doctor immediately if they do become pregnant.

Women who are taking this medication should familiarize themselves with the signs and symptoms of a potentially life-threatening allergic reaction known as anaphylaxis. This reaction requires immediate emergency medical treatment and the symptoms should not be ignored.

Estradiol has some contraindications with a number of medications and your doctor should be informed of all the medicines that you are taking prior to your starting the course of treatment. If you are taking tranexamic acid it is imperative that you work closely with your doctor to ensure that you do not suffer from any serious side effects. Patients are cautioned to not take both medications at the same time, but if your doctor believes that they are both the best treatment for your conditions they may alter your dosage for one or both of the drugs.

If you are taking this medication for a long period of time be sure to work with your doctor to manage the risk that can increase the longer you take estradiol. If you experience any significant side effects be sure to inform your doctor as this can be a sign of a more serious problem. This medication can also increase the risk of certain cancers, especially when taken for a long period of time. If you have a family history of cancer be sure that your doctor is thoroughly informed of this fact.

Estradiol can be an effective remedy for postmenopausal women who are suffering from hot flashes, vaginal issues such as dryness, and other symptoms caused by the decrease in the level of estrogen that their bodies are creating.