How does this medication work? What will it do for me?

Estrone vaginal cream belongs to the class of medications known as estrogen replacement therapy. Estrone vaginal cream is used to manage vaginal menopausal symptoms such as itching, burning, dryness in or around the vagina, and painful sexual intercourse.

Estrogen is a hormone that is produced by the ovaries. Once menopause is reached, the ovaries produce less estrogen and symptoms of menopause can occur. Estrone vaginal cream works by providing locally acting estrogen.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

Each gram of cream contains 0.1% w/w estrone. Nonmedicinal ingredients: arlacel 165, isopropyl myristate, methyl paraben, mineral oil, Peg 40 stearate, propyl paraben, sorbitan monostearate, stearic acid, and water.

How should I use this medication?

The dose of this medication is individualized to the person using the cream. The lowest dose that will treat the symptoms should be used.

The recommended adult dose of estrone vaginal cream ranges from 2 g to 4 g of cream daily. The cream is inserted into the vagina using the applicator provided. The cream is usually used on a regular cycle, with 3 weeks of use followed by 1 week off. Sometimes the cream is used continuously. Follow your doctor’s instructions. Treatment should be stopped as soon as possible because estrone vaginal cream is intended only for short-term use.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

To use the applicator, remove the cap of the tube of cream and screw the nozzle end of the applicator onto the tube. Squeeze the cream until it reaches the mark that indicates the dose prescribed by your doctor. Unscrew the applicator from the tube, place it into the opening of the vagina, and gently press the plunger to release the medication. Clean the applicator by pulling the plunger out from the barrel and washing it with mild soap and warm water.

Women who also take oral estrogen tablet may need to have the dose of their tablets adjusted when they start using the cream. Women who have not had their uterus removed should also take a progestin (such as medroxyprogesterone acetate). Talk with your doctor or pharmacist about which dosing schedule would work best for you if you are taking a progestin.

It is important to use this medication exactly as prescribed by your doctor.

If you miss a dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one.

If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Do not use estrone vaginal cream if you:

  • are allergic to estrone or any ingredients of the medication
  • are or may be pregnant
  • are breast-feeding
  • have a history of known or suspected estrogen-dependent tumours such as breast or uterine cancer
  • have abnormal liver test results caused by liver disease or liver problems
  • have endometrial hyperplasia (overgrowth of the lining of the uterus)
  • have or have had a history of blood clots (e.g., in the legs or lungs), heart attack, stroke, or heart disease
  • have any vision problems or other vision problems due to ophthalmic vascular disease (disease involving blood vessels of the eye)
  • have undiagnosed abnormal vaginal bleeding
  • have a history of migraine headaches with aura (classical migraine)

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • abdominal cramps, bloating
  • abdominal or back pain
  • breast tenderness
  • headache
  • migraine headaches
  • nausea or vomiting

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • breast changes (lumps, swelling, discharge)
  • changes in vaginal bleeding (spotting, breakthrough bleeding, prolonged or heavier bleeding, or complete stoppage of menstrual periods)
  • first migraine headache
  • increased blood pressure
  • signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
  • signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
  • stinging or redness in the genital area
  • unusual or unexpected uterine bleeding or spotting

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • sudden partial or complete loss of vision
  • symptoms of a blood clot in the leg (e.g., sharp pain in the foot or unexplained leg swelling, pain, redness, or tenderness)
  • symptoms of a blood clot in the lung (e.g., sharp pain in the chest, coughing blood, or sudden shortness of breath)
  • symptoms of a heart attack (e.g., sudden pain or discomfort in the chest, neck, jaw, shoulder, arms, or back; shortness of breath; nausea or vomiting; cool, clammy skin; anxiety or denial)
  • symptoms of a stroke (e.g., sudden weakness or numbness in the face, arm, or leg – even if the weakness is temporary; sudden trouble speaking; sudden confusion; sudden vision changes; sudden severe and unusual headache; or sudden dizziness or loss of balance)

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Note the following important information about estrogen replacement therapy: The Women's Health Initiative (WHI) study results indicated an increased risk of heart attack, stroke, breast cancer, blood clots in the lungs, and blood clots in the leg veins in postmenopausal women during 5 years of treatment with 0.625 mg conjugated equine estrogens and 2.5 mg medroxyprogesterone compared to women receiving sugar tablets. Other combinations of estrogen and progestins were not studied. However, until additional data are available, the risks should be assumed to be similar for other hormone replacement products. Therefore,

  • estrogen with or without progestins should be used at the lowest dose that relieves your menopausal symptoms for the shortest time period possible, as directed by your doctor.
  • estrogen with or without progestins should not be used to prevent heart disease, heart attacks, or strokes.

Blood clots: Estrogen with or without progestins is associated with an increased risk of blood clots in the lungs and legs. This risk also increases with age, a personal or family history of blood clots, smoking, and obesity. The risk of blood clots is also increased if you are immobilized for prolonged periods and with major surgery. If possible, this medication should be stopped 4 to 6 weeks before major surgery. Talk about the risk of blood clots with your doctor.

Breast cancer: Some studies have found an association between a modest increase in the risk of developing breast cancer and the use of hormone replacement therapy after menopause. Women who have a history of breast cancer should not use estrogens. If you have a family history of breast cancer, breast nodules, fibrocystic disease of the breast, or abnormal mammograms, you should be closely monitored by your doctor if you use estrogens. Women using estrogens should have regular breast examinations and should be taught how to do a breast self-examination. Your doctor may also recommend regular mammograms, depending on your age, risk factors, and previous mammogram results. This medication must not be applied to the breasts, as it may have harmful effects on the breast tissue. Discuss the benefits and risks with your doctor so that you can make an informed choice about using this medication.

Condoms, diaphragms, or cervical caps: Estrone vaginal cream contains mineral oil, which may weaken the latex rubber of condoms, diaphragms, and cervical caps. Therefore, they may not be effective in preventing pregnancy for women who use the cream.

Dementia: Women over age 65 receiving combined estrogen and progestin replacement therapy may be at increased risk of developing dementia (loss of memory and intellectual function). If you are over 65 years of age, your doctor should closely monitor you for loss of memory and intellectual function.

Diabetes: People with diabetes should monitor their blood glucose closely to detect any changes in blood glucose control that sometimes occurs with use of estrogens. If you have risk factors for diabetes, your doctor will monitor your blood glucose regularly while you are on this medication.

Endometrial cancer: Several studies suggest that estrogen replacement therapy increases the risk of cancer of the endometrium (uterus). Taking a progestin along with the estrogen reduces the risk to the same level as that of a woman not using estrogens. For this reason, all women who have not had their uterus removed should also take a progestin if they are using estrogens.

Fibroids: This medication may worsen fibroids, causing sudden enlargement, pain, or tenderness. If you notice these effects, contact your doctor.

Gallbladder: An increased risk of gallbladder disease has been reported by postmenopausal women who take oral estrogens. If you experience symptoms of a gallbladder attack, such as severe pain on the right side of the abdomen, nausea, vomiting, and fever, contact your doctor as soon as possible. If you have a history of gallbladder problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Heart disease and stroke: Studies indicate an increased risk of heart disease and stroke with estrogen (with or without progestins) for postmenopausal women. Get immediate medical attention if you experience symptoms of a heart attack (chest pain, tightness or pressure, sweating, nausea, feeling of impending doom) or stroke (sudden dizziness, headache, loss of speech, changes in vision, weakness or numbness in the arms and legs) while taking this medication.

High cholesterol or triglycerides: Estrogen may increase triglyceride (a type of fat found in the blood) levels, especially in those who already have high levels of triglycerides. If you have high levels of cholesterol or triglycerides, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. Your doctor may want to test your liver function (the liver makes cholesterol and triglycerides) regularly with blood tests while you are taking this medication.

Liver disease: Estrogens may reduce liver function and can cause liver failure. If you have liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. Your doctor may want to test your liver function regularly with blood tests while you are taking this medication.

If you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin, contact your doctor immediately.

Ovarian cancer: Several studies suggest that estrogen replacement therapy increases the risk of cancer of the ovaries, especially when taken for 5 years or longer. This may occur whether you are taking a progestin or not. If you are at an increased risk of developing ovarian cancer, discuss with your doctor how this medication may affect your risk, whether any special monitoring is needed, and whether this medication is appropriate for you.

Porphyria: Estrone vaginal cream may worsen symptoms of porphyria. If you have porphyria, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Seizures: Estrogens may cause an increase in the frequency of seizures for women who experience seizures or have a history of seizures. If you have a history of seizures, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Thyroid disease: Estrogens can affect how well the thyroid gland works. If you have thyroid disease such as hypothyroidism (low thyroid levels), discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Water retention: Estrogen may cause sodium (salt) and water retention, making symptoms worse for people with certain medical conditions such as epilepsy, asthma, and kidney or heart dysfunction. If you have any of these medical conditions, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Pregnancy: Estrogen should not be used during pregnancy. If you become pregnant while using this medication, contact your doctor immediately.

Breast-feeding: This medication passes into breast milk. If you are a breast-feeding mother and are using estrone vaginal cream, it may affect your baby. This medication is not recommended for breast-feeding mothers.

Children: The safety and effectiveness of this medication have not been established for children.

What other drugs could interact with this medication?

There may be an interaction between estrone vaginal cream and any of the following:

  • acetaminophen
  • acetylsalicylic acid (ASA)
  • anastrozole
  • ascorbic acid (vitamin C)
  • atorvastatin
  • barbiturates (e.g., phenobarbital)
  • bosentan
  • blood-pressure-lowering agents (e.g., propranolol, enalapril, diltiazem)
  • carbamazepine
  • celecoxib
  • corticosteroids (e.g., hydrocortisone, prednisolone, prednisone)
  • cyclosporine
  • cyproterone
  • dabrafenib
  • deferasirox
  • dehydroepiandosterone
  • dexamethasone
  • diabetes medications (e.g., chlorpropamide, glipizide, glyburide, insulin, metformin, nateglinide, rosiglitazone)
  • efavirenz
  • enzalutamide
  • etravirine
  • grapefruit juice
  • heparin
  • low molecular weight heparins (e.g., dalteparin, enoxaparin, tinzaparin)
  • mitotane
  • modafinil
  • morphine
  • phenylbutazone
  • phenytoin
  • primidone
  • rifabutin
  • rifampin
  • ropinirole
  • St. John's wort
  • somatropin
  • temazepam
  • teriflunomide
  • thalidomide
  • theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
  • thyroid medications (e.g., levothyroxine, liothyronine)
  • tocilizumab
  • warfarin

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.