estradiol vaginal

Action and Spectrum

Actions and Spectrum:  

Action: 

Restoring vaginal tissue: estradiol vaginal helps restore vaginal tissue that has become thin, dry, and irritated due to decreased estrogen levels.  

Reducing vaginal symptoms: can reduce vaginal itching, burning, and discomfort during sexual intercourse.  

Preventing urinary tract infections: estradiol vaginal can also help to prevent urinary tract infections by maintaining a healthy vaginal pH.  

Spectrum:  

Vaginal atrophy: estradiol vaginal is commonly used to treat vaginal atrophy,when the vaginal tissue becomes thin, dry, and irritated due to a decreased in estrogen levels.  

Menopause-related symptoms: Apart from alleviating symptoms associated with menopause like hot flashes, mood swings, and night sweats, it has the potential to effectively treat other related symptoms as well.  

Urinary tract infections: estradiol vaginal can help to prevent recurrent urinary tract infections by maintaining a healthy vaginal pH. 

Drug Interaction

Adverse Reaction

Frequency defined  

>10% 

Headache (5-16%)  

1-10% 

Vulvovaginal pruritus (8%) 

Diarrhea (5%) 

Vulvovaginal mycotic infection (5-8%) 

Back pain (7%) 

Abdominal pain (7%) 

Black Box Warning

Black Box Warning:  

The black box warning for estradiol vaginal cream relates to an increased risk of endometrial cancer, cardiovascular events, breast cancer, and dementia. Additionally, the use of estrogen-only therapy in women who have undergone hysterectomy is associated with an increased risk of stroke, blood clots, and cancer of the ovaries. Women who use estradiol vaginal cream should be monitored closely by their healthcare provider for any signs or symptoms of these conditions. 

Contraindication / Caution

Contraindication/Caution:   

Undiagnosed abnormal vaginal bleeding: estradiol vaginal is not recommended for use in women with undiagnosed abnormal vaginal bleeding, as this can indicate a more serious underlying condition.  

Known or suspected estrogen-dependent tumors: Women with known or suspected estrogen-dependent tumors, such as breast cancer, should not use estradiol vaginal as it may increase the risk of cancer growth.  

History of liver disease: estradiol vaginal can be processed by the liver, and women with active liver disease or a history of liver disease may have difficulty metabolizing the medication, leading to adverse effects.  

History of blood clots or stroke: The use of vaginal estradiol may heighten the probability of developing blood clots and experiencing a stroke. Hence, females who have a history of these ailments should refrain from using this medication.  

Hypersensitivity to estradiol or any of its components: Women who have a known hypersensitivity to estradiol or any of the ingredients in the medication should not use it, as this may cause an allergic reaction. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:

estradiol vaginal is available as a vaginal tablet or cream. The tablet form is inserted into the vagina using an applicator, while the cream is applied directly to the vaginal area. The medication is rapidly absorbed by the vaginal tissues and transported to the systemic circulation. 

Pharmacodynamics: 

The pharmacodynamics of estradiol vaginal involves the binding of the medication to estrogen receptors in various tissues, leading to the activation of cellular processes that help to maintain female reproductive health, urogenital health, and bone metabolism.  

MOA: estradiol vaginal works by binding to estrogen receptors in the vaginal tissue and promoting the growth and proliferation of vaginal epithelial cells. This leads to an increase in vaginal lubrication, blood flow, and the thickness of the vaginal lining.  

Pharmacokinetics: 

Absorption 

When administered vaginally, estradiol is absorbed into the bloodstream through the vaginal mucosa. The absorption rate is relatively slow and the maximum plasma concentration is achieved within 8 to 12 hours after administration. 

Distribution  

estradiol is distributed to target tissues, including the vaginal epithelium, uterus, and breast tissue. It binds to estrogen receptors in these tissues and exerts its pharmacological effects. 

Metabolism 

estradiol is metabolized in the liver and other tissues by the enzymes cytochrome P450 3A4 and 2C19. The main metabolites of estradiol are estrone, estriol, and several hydroxylated derivatives. 

Excretion and elimination 

The metabolites of estradiol are excreted in urine and feces. The elimination half-life of estradiol is approximately 13 hours, with 40-50% excreted in the urine and 25-30% excreted in the feces. 

Adminstartion

Administration:   

Before administering the estradiol vaginal medication, it’s important to clean your hands with soap and water.  

Also, ensure that the applicator is free of any particles by removing it from the package and checking its cleanliness.  

To prepare the medication, gently shake the container containing the estradiol vaginal cream.  

Squeeze the medication into the applicator until it is filled to the prescribed level.  

Insert the applicator into the vaginal canal gently and push down the plunger slowly to administer the medication. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: estradiol vaginal 

Why do we use estradiol vaginal?   

estradiol vaginal is a medication that is used to treat vaginal atrophy, a condition that occurs when there is a decrease in the levels of estrogen in a woman’s body, often due to menopause. 

The medication contains estradiol, which is a form of estrogen hormone that is produced by the ovaries. When applied vaginally, the medication can help to relieve symptoms such as vaginal dryness, itching, burning, and discomfort during sexual intercourse, which are commonly associated with vaginal atrophy.  

estradiol vaginal can also help to restore the thickness and elasticity of the vaginal tissues, and can reduce the risk of vaginal infections.