Estradiol Val 20mg/ml Inj, 5ml
WARNING: Do not use this drug to prevent heart disease or dementia. A study of women taking an estrogen with a progestin showed a raised chance of heart attack, stroke, blood clot, breast cancer, and dementia. The chance of stroke, blood clot, and dementia was also raised when the estrogen was taken alone. Not all products and doses were studied. It is not known if the same effects may happen with this drug.The chance of endometrial cancer may be raised with the use of estrogen alone in patients with a uterus. Use of a progestin along with estrogen may lower the risk. Call your doctor right away if you have unexplained or long-lasting vaginal bleeding.Use this drug for the shortest time needed at the lowest useful dose. Your doctor will talk with you on a regular basis to see if you need to keep taking this drug. @ COMMON USES: It is used to prevent or lower the signs of the change of life (menopause).It is used to add estrogen to the body when the ovaries have been taken out or do not work the right way.Rarely, it is used to treat breast or prostate cancers.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Estrogen
Pharmacologic Class
Estrogen Receptor Agonist
Pregnancy Category
Category X
FDA Approved
Mar 1954
DEA Schedule
Not Controlled
Overview
What is this medicine?
Estradiol valerate injection is a form of estrogen, a female hormone. It's used to treat symptoms of menopause like hot flashes, to replace hormones when the body doesn't make enough (e.g., due to ovarian failure), and sometimes to treat certain types of prostate cancer in men. It's given as an injection into a muscle, usually every few weeks.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is administered via injection into a muscle. If you are self-administering the injection, your doctor or nurse will provide guidance on the proper technique.
Before using, inspect the solution for any signs of cloudiness, leakage, or particles. The solution should be colorless to faint yellow; do not use it if the color has changed.
Safe Disposal of Needles and Supplies
After use, dispose of needles in a designated needle/sharp disposal box. Never reuse needles or other items. When the disposal box is full, follow local regulations for proper disposal. If you have any questions or concerns, consult your doctor or pharmacist.
Storage and Disposal
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist for guidance on proper storage.
Missed Dose
If you miss a dose, contact your doctor to determine the best course of action.
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is administered via injection into a muscle. If you are self-administering the injection, your doctor or nurse will provide guidance on the proper technique.
Before using, inspect the solution for any signs of cloudiness, leakage, or particles. The solution should be colorless to faint yellow; do not use it if the color has changed.
Safe Disposal of Needles and Supplies
After use, dispose of needles in a designated needle/sharp disposal box. Never reuse needles or other items. When the disposal box is full, follow local regulations for proper disposal. If you have any questions or concerns, consult your doctor or pharmacist.
Storage and Disposal
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist for guidance on proper storage.
Missed Dose
If you miss a dose, contact your doctor to determine the best course of action.
Lifestyle & Tips
- Maintain regular physical activity and a healthy diet.
- Avoid smoking, as it increases the risk of blood clots and cardiovascular events.
- Limit alcohol intake.
- Discuss any new medications, supplements, or herbal products with your doctor.
- Attend all scheduled doctor appointments and monitoring tests.
Available Forms & Alternatives
Available Strengths:
- Estradiol 0.05mg Patch (once Wk)
- Estradiol 0.1mg Patch (once Wk)
- Estradiol 1mg Tablets
- Estradiol 2mg Tablets
- Estradiol 0.5mg Tablets
- Estradiol 0.025mg Patch (once Wk)
- Estradiol 0.075mg Patch (once Wk)
- Estradiol Tds 0.0375mg Patches 4s
- Estradiol Tds 0.06mg Patch 4s
- Estradiol 0.025mg Patch (twice Wk)
- Estradiol 0.075mg Patch (twice Wk)
- Estradiol 0.0375mg Patch (twice Wk)
- Estradiol 0.1mg Patch (twice Wk)
- Estradiol 0.05mg Patch (twice Wk)
- Estradiol 0.0375mg Patch (twice Wk
- Estradiol 10mcg Vaginal Tabs 8s
- Estradiol 10mcg Vaginal Tabs 18s
- Estradiol 0.01% Vag Cream 42.5gm
- Estradiol Val 20mg/ml Inj, 5ml
- Estradiol Valerate 40mg/ml Inj, 5ml
- Estradiol Valerate 40mg/ml Inj, 5ml
- Estradiol 0.5mg/day Top Gel Pk
- Estradiol 0.5mg/day Top Gel Pk
- Estradiol 1mg/day Top Gel Pk
- Estradiol 1mg/day Top Gel Pk
- Estradiol 0.75mg/day Top Gel Pk
- Estradiol 0.75mg/day Top Gel Pk
- Estradiol 0.25mg/day Top Gel Pk
- Estradiol 0.25mg/day Top Gel Pk
- Estradiol 1.25mg/day Top Gel Pk
- Estradiol 1.25mg/day Top Gel Pk
- Estradiol Valerate 10mg/ml Inj, 5ml
- Estradiol Val 20mg/ml Inj, 5ml
- Estradiol Valerate 10mg/ml Inj, 5ml
- Estradiol 1.25mg/day Top Gel Pk
- Estradiol 0.75mg/day Top Gel Pk
- Estradiol 1mg/day Top Gel Pk
- Estradiol 0.5mg/day Top Gel Pk
- Estradiol 0.25mg/day Top Gel Pk
- Estradiol 0.06% Gel 37.5gm(pumps)
- Estradiol 0.06% Gel 37.5gm(pumps)
Dosing & Administration
Adult Dosing
Standard Dose:
Varies significantly by indication. For moderate to severe vasomotor symptoms associated with menopause: 10 to 20 mg intramuscularly every four weeks. For hypoestrogenism due to hypogonadism, castration, or primary ovarian failure: 10 to 20 mg intramuscularly every four weeks. For palliative treatment of advanced prostate cancer: 30 mg or more intramuscularly once or twice weekly.
Dose Range:
10 - 30 mg
Condition-Specific Dosing:
vasomotor_symptoms_menopause:
10-20 mg IM every 4 weeks
hypoestrogenism:
10-20 mg IM every 4 weeks
prostate_cancer_palliative:
30 mg or more IM once or twice weekly
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (except for specific conditions like Turner syndrome, where dosing is individualized and typically lower)
Adolescent:
Not established (except for specific conditions like Turner syndrome or gender-affirming care, where dosing is individualized)
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, but use with caution.
Moderate:
No specific dose adjustment recommended, but use with caution.
Severe:
No specific dose adjustment recommended, but use with caution. Estrogens are primarily metabolized by the liver.
Dialysis:
Not specifically studied. Use with caution.
Hepatic Impairment:
Mild:
Use with caution. Estrogens are extensively metabolized by the liver.
Moderate:
Contraindicated in severe hepatic dysfunction. Use with extreme caution, if at all, in moderate impairment.
Severe:
Contraindicated.
Pharmacology
Mechanism of Action
Estradiol valerate is a prodrug of estradiol, the primary estrogen produced by the human ovary. It is hydrolyzed to estradiol, which then binds to and activates estrogen receptors (ERΞ± and ERΞ²) in target tissues. This binding leads to gene transcription and protein synthesis, mediating the physiological effects of estrogens, including effects on the reproductive system, bone density, cardiovascular system, and central nervous system. In prostate cancer, high doses of estrogen suppress luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release from the pituitary, leading to a reduction in testicular androgen production.
Pharmacokinetics
Absorption:
Bioavailability:
Not directly applicable for IM prodrug; estradiol is slowly released from the oil depot.
Tmax:
Estradiol peak concentrations typically occur within 3-7 days after IM injection of estradiol valerate.
FoodEffect:
Not applicable for intramuscular injection.
Distribution:
Vd:
Approximately 1 L/kg for estradiol.
ProteinBinding:
Approximately 98% bound to sex hormone-binding globulin (SHBG) and albumin.
CnssPenetration:
Yes (estradiol crosses the blood-brain barrier).
Elimination:
HalfLife:
Estradiol: Approximately 13-17 hours after IM injection of estradiol valerate (due to sustained release from depot).
Clearance:
Approximately 600-700 mL/min for estradiol.
ExcretionRoute:
Primarily renal (as glucuronide and sulfate conjugates), with some biliary excretion.
Unchanged:
Less than 1% (estradiol)
Pharmacodynamics
OnsetOfAction:
Clinical effects may be observed within days to weeks, depending on the indication.
PeakEffect:
Varies by indication and individual response.
DurationOfAction:
Approximately 3-4 weeks due to the sustained release from the intramuscular depot.
Confidence:
Medium
Safety & Warnings
BLACK BOX WARNING
Estrogens and progestins should not be used for the prevention of cardiovascular disease or dementia. 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 receiving daily oral conjugated equine estrogens (CEE) combined with medroxyprogesterone acetate (MPA) compared to placebo. The WHI study also reported an increased risk of stroke and deep vein thrombosis in postmenopausal women receiving daily oral CEE alone compared to placebo. The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older receiving daily oral CEE combined with MPA or CEE alone compared to placebo. Other doses of oral conjugated estrogens and other dosage forms of estrogens and progestins were not studied in the WHI and, in the absence of comparable data, these risks should be assumed to be similar. Estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin with or without fever, wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes.
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades, yellow skin or eyes, fever with chills, bloating, or severe upset stomach or vomiting.
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting.
Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight.
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight.
Eyesight changes or loss, bulging eyes, or changes in how contact lenses feel.
Breast lump, breast pain or soreness, or nipple discharge.
Vaginal itching or discharge.
Abnormal vaginal bleeding.
Depression or other mood changes.
Memory problems or loss.
Fever.
Difficulty urinating or changes in urine output.
Pain while urinating.
This medication may cause fluid retention or swelling in the body. Inform your doctor if you experience swelling, weight gain, or trouble breathing.
Blood Clots and High Calcium Levels
Seek medical attention immediately if you experience signs of a blood clot, such as:
Chest pain or pressure
Coughing up blood
Shortness of breath
Swelling, warmth, numbness, changes in color, or pain in a leg or arm
Trouble speaking or swallowing
High calcium levels have been reported in some people with cancer taking this medication. Contact your doctor right away if you experience signs of high calcium levels, such as:
Weakness
Confusion
Feeling tired
Headache
Upset stomach or vomiting
Constipation
Bone pain
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical attention:
Dizziness or headache
Hair loss
Upset stomach or vomiting
Constipation
Stomach pain or cramps
Bloating
Enlarged breasts
Tender breasts
Vaginal bleeding or spotting
Painful periods
Signs of a common cold
Nose or throat irritation
Weight gain or loss
Joint pain
Leg cramps
Changes in sex interest
Irritation at the site of administration
Reporting Side Effects
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin with or without fever, wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes.
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades, yellow skin or eyes, fever with chills, bloating, or severe upset stomach or vomiting.
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting.
Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight.
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight.
Eyesight changes or loss, bulging eyes, or changes in how contact lenses feel.
Breast lump, breast pain or soreness, or nipple discharge.
Vaginal itching or discharge.
Abnormal vaginal bleeding.
Depression or other mood changes.
Memory problems or loss.
Fever.
Difficulty urinating or changes in urine output.
Pain while urinating.
This medication may cause fluid retention or swelling in the body. Inform your doctor if you experience swelling, weight gain, or trouble breathing.
Blood Clots and High Calcium Levels
Seek medical attention immediately if you experience signs of a blood clot, such as:
Chest pain or pressure
Coughing up blood
Shortness of breath
Swelling, warmth, numbness, changes in color, or pain in a leg or arm
Trouble speaking or swallowing
High calcium levels have been reported in some people with cancer taking this medication. Contact your doctor right away if you experience signs of high calcium levels, such as:
Weakness
Confusion
Feeling tired
Headache
Upset stomach or vomiting
Constipation
Bone pain
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical attention:
Dizziness or headache
Hair loss
Upset stomach or vomiting
Constipation
Stomach pain or cramps
Bloating
Enlarged breasts
Tender breasts
Vaginal bleeding or spotting
Painful periods
Signs of a common cold
Nose or throat irritation
Weight gain or loss
Joint pain
Leg cramps
Changes in sex interest
Irritation at the site of administration
Reporting Side Effects
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Sudden severe headache or migraine
- Sudden vision changes (e.g., partial or complete loss of vision)
- Sudden numbness or weakness on one side of the body
- Slurred speech or difficulty speaking
- Sudden severe chest pain, shortness of breath, or coughing up blood
- Pain, swelling, or tenderness in one leg
- Yellowing of the skin or eyes (jaundice)
- New breast lump or changes in existing breast lumps
- Unusual vaginal bleeding (especially after menopause)
- Severe abdominal pain
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
A history of certain health conditions, such as:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are estrogen-dependent
Unexplained vaginal bleeding
Pregnancy or potential pregnancy. Note: This medication is contraindicated during pregnancy and should not be taken if you are pregnant.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Do not initiate, stop, or adjust the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
A history of certain health conditions, such as:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are estrogen-dependent
Unexplained vaginal bleeding
Pregnancy or potential pregnancy. Note: This medication is contraindicated during pregnancy and should not be taken if you are pregnant.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Do not initiate, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Your doctor may advise you to stop taking this drug before certain surgical procedures, and will provide guidance on when to resume taking it after the surgery or procedure.
If you anticipate being immobile for extended periods, such as during long trips, bedrest after surgery, or illness, consult with your doctor. Prolonged immobility may increase your risk of developing blood clots.
If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels while taking this medication.
As this medication can cause high blood pressure, it is essential to have your blood pressure checked regularly, as advised by your doctor. Additionally, your doctor will recommend regular blood tests and bone density checks to monitor your health.
Regular breast exams and gynecology check-ups are vital, and you should also perform breast self-exams as instructed by your doctor.
The risk of certain side effects, such as heart attack, stroke, breast cancer, ovarian cancer, and others, may vary depending on factors like the duration of estrogen use, whether it is taken with or without a progestin, and other individual factors. Discuss the benefits and risks of using this medication with your doctor.
Be aware that this medication can cause high triglyceride levels. If you have a history of high triglyceride levels, inform your doctor.
This medication may cause dark skin patches on your face, so it is essential to avoid sun exposure, sunlamps, and tanning beds. Use sunscreen and wear protective clothing and eyewear to minimize sun exposure.
As this medication may affect certain laboratory tests, inform all your healthcare providers and lab workers that you are taking this medication.
Smoking can increase the risk of heart disease, so it is recommended that you do not smoke. Consult with your doctor for guidance on quitting.
Limit your alcohol consumption while taking this medication. If you regularly drink grapefruit juice or eat grapefruit, discuss this with your doctor, as it may interact with the medication.
In some cases, this medication may affect growth in children and teenagers. If applicable, they may require regular growth checks, and you should consult with their doctor.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
If you are breastfeeding, inform your doctor, as they will need to discuss the potential risks to your baby.
If you anticipate being immobile for extended periods, such as during long trips, bedrest after surgery, or illness, consult with your doctor. Prolonged immobility may increase your risk of developing blood clots.
If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels while taking this medication.
As this medication can cause high blood pressure, it is essential to have your blood pressure checked regularly, as advised by your doctor. Additionally, your doctor will recommend regular blood tests and bone density checks to monitor your health.
Regular breast exams and gynecology check-ups are vital, and you should also perform breast self-exams as instructed by your doctor.
The risk of certain side effects, such as heart attack, stroke, breast cancer, ovarian cancer, and others, may vary depending on factors like the duration of estrogen use, whether it is taken with or without a progestin, and other individual factors. Discuss the benefits and risks of using this medication with your doctor.
Be aware that this medication can cause high triglyceride levels. If you have a history of high triglyceride levels, inform your doctor.
This medication may cause dark skin patches on your face, so it is essential to avoid sun exposure, sunlamps, and tanning beds. Use sunscreen and wear protective clothing and eyewear to minimize sun exposure.
As this medication may affect certain laboratory tests, inform all your healthcare providers and lab workers that you are taking this medication.
Smoking can increase the risk of heart disease, so it is recommended that you do not smoke. Consult with your doctor for guidance on quitting.
Limit your alcohol consumption while taking this medication. If you regularly drink grapefruit juice or eat grapefruit, discuss this with your doctor, as it may interact with the medication.
In some cases, this medication may affect growth in children and teenagers. If applicable, they may require regular growth checks, and you should consult with their doctor.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
If you are breastfeeding, inform your doctor, as they will need to discuss the potential risks to your baby.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Breast tenderness
- Abdominal pain
- Drowsiness/fatigue
- Withdrawal bleeding (in females)
What to Do:
There is no specific antidote. Treatment is symptomatic and supportive. In case of suspected overdose, contact a poison control center immediately (e.g., 1-800-222-1222 in the US) or seek emergency medical attention.
Drug Interactions
Contraindicated Interactions
- Aromatase inhibitors (e.g., anastrozole, letrozole) - for breast cancer treatment
- Fulvestrant - for breast cancer treatment
Major Interactions
- CYP3A4 inducers (e.g., carbamazepine, phenobarbital, phenytoin, rifampin, St. John's Wort) - may decrease estradiol levels
- CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, ketoconazole, ritonavir, grapefruit juice) - may increase estradiol levels
- Thyroid hormones (e.g., levothyroxine) - estrogens can increase thyroid-binding globulin, potentially increasing thyroid hormone requirements
- Corticosteroids (e.g., prednisone) - estrogens may decrease corticosteroid clearance, increasing their effects
- Anticoagulants (e.g., warfarin) - estrogens may alter anticoagulant effects, requiring INR monitoring
Moderate Interactions
- Fibrates (e.g., gemfibrozil) - may alter lipid profiles
- Hypoglycemic agents (e.g., insulin, oral antidiabetics) - estrogens may affect glucose tolerance
- Cyclosporine - estrogens may inhibit cyclosporine metabolism, increasing levels
- Theophylline - estrogens may inhibit theophylline metabolism, increasing levels
Minor Interactions
- Not specifically identified as minor, but general caution with drugs affecting liver metabolism.
Monitoring
Baseline Monitoring
Complete medical history and physical examination (including blood pressure, breast and pelvic examination)
Rationale: To identify contraindications, risk factors, and establish baseline health status.
Timing: Prior to initiation of therapy.
Lipid profile (total cholesterol, HDL, LDL, triglycerides)
Rationale: Estrogens can affect lipid metabolism and cardiovascular risk.
Timing: Prior to initiation.
Liver function tests (ALT, AST, bilirubin)
Rationale: Estrogens are metabolized by the liver; identify pre-existing hepatic impairment.
Timing: Prior to initiation.
Mammogram (for women)
Rationale: To screen for pre-existing breast abnormalities due to increased breast cancer risk with estrogen therapy.
Timing: Prior to initiation and as clinically indicated.
Bone mineral density (BMD) scan (if indicated)
Rationale: To assess baseline bone health, especially if used for osteoporosis prevention/treatment.
Timing: Prior to initiation.
Routine Monitoring
Blood pressure
Frequency: Annually or more frequently if clinically indicated.
Target: <130/80 mmHg
Action Threshold: Sustained elevation requiring intervention.
Breast examination (clinical)
Frequency: Annually.
Target: Normal findings
Action Threshold: New lumps, pain, or discharge.
Pelvic examination (for women with uterus)
Frequency: Annually.
Target: Normal findings
Action Threshold: Abnormal bleeding, pain, or masses.
Mammogram (for women)
Frequency: As per national screening guidelines (e.g., every 1-2 years).
Target: Normal findings
Action Threshold: Abnormal findings requiring further investigation.
Lipid profile
Frequency: Periodically, as clinically indicated.
Target: Individualized based on cardiovascular risk.
Action Threshold: Significant adverse changes.
Liver function tests
Frequency: Periodically, if clinically indicated or symptoms arise.
Target: Within normal limits
Action Threshold: Significant elevation.
Symptom Monitoring
- Unusual vaginal bleeding (especially postmenopausal)
- Breast lumps or pain
- Leg pain, swelling, or tenderness (signs of DVT)
- Sudden chest pain, shortness of breath, or coughing up blood (signs of PE)
- Sudden severe headache, vision changes, slurred speech, weakness/numbness (signs of stroke)
- Yellowing of skin or eyes (jaundice)
- Severe abdominal pain
- Mood changes, depression
- Fluid retention, swelling of ankles/feet
Special Patient Groups
Pregnancy
Contraindicated in pregnancy. Estrogens are not indicated for use in pregnancy. There is no evidence that estrogens are effective in preventing threatened or habitual abortion, and there is evidence that estrogen exposure in utero may cause harm to the fetus (e.g., feminization of male fetuses, vaginal adenosis in female fetuses).
Trimester-Specific Risks:
First Trimester:
Potential for feminization of male fetuses, vaginal adenosis in female fetuses.
Second Trimester:
Potential for feminization of male fetuses, vaginal adenosis in female fetuses.
Third Trimester:
Potential for feminization of male fetuses, vaginal adenosis in female fetuses.
Lactation
Use is generally not recommended during lactation. Estrogens are excreted in breast milk and have been shown to decrease the quantity and quality of breast milk. They may also affect the nursing infant.
Infant Risk:
L4 (Possibly hazardous). Potential for adverse effects on the infant (e.g., feminization, jaundice) and reduction in milk supply.
Pediatric Use
Safety and effectiveness have not been established in pediatric patients, except for specific conditions like Turner syndrome or gender-affirming hormone therapy, where use is off-label and individualized by specialists. Estrogen therapy in prepubertal girls can cause premature epiphyseal closure, resulting in short stature.
Geriatric Use
Use with caution. Women 65 years of age or older may be at increased risk of probable dementia with estrogen therapy, as shown in the WHIMS study. The lowest effective dose for the shortest duration should be used. Increased risk of cardiovascular events and breast cancer also applies.
Clinical Information
Clinical Pearls
- Estradiol valerate is a prodrug that provides sustained release of estradiol, making it suitable for less frequent dosing compared to oral or transdermal estradiol.
- Due to the Black Box Warning, it's crucial to discuss the risks (cardiovascular events, breast cancer, endometrial cancer, dementia) with patients before initiating therapy, especially for hormone replacement.
- For women with an intact uterus, a progestin must be co-administered to reduce the risk of endometrial hyperplasia and cancer, unless contraindicated.
- IM injections should be administered deeply into a large muscle (e.g., gluteal muscle) to ensure proper absorption and minimize local reactions.
- Patients should be advised to report any signs of blood clots (e.g., leg pain/swelling, chest pain, shortness of breath) or stroke (e.g., sudden severe headache, vision changes, weakness) immediately.
- Regular monitoring, including blood pressure, breast exams, pelvic exams, and mammograms, is essential during therapy.
Alternative Therapies
- Oral estrogens (e.g., estradiol, conjugated estrogens)
- Transdermal estrogens (e.g., patches, gels, sprays)
- Vaginal estrogens (for localized symptoms)
- Non-estrogen therapies for vasomotor symptoms (e.g., SSRIs/SNRIs, gabapentin, clonidine)
- Testosterone (for gender-affirming care in some contexts)
- GnRH agonists/antagonists (for prostate cancer)
Cost & Coverage
Average Cost:
Varies widely, typically $50 - $200+ per 5ml vial (20mg/ml)
Generic Available:
Yes
Insurance Coverage:
Tier 1-3 (often covered, but may require prior authorization for certain indications or higher tiers for brand names)
General Drug Facts
If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance.
To ensure safe use, do not share your medication with others, and never take someone else's medication. Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion.
Proper disposal of unused or expired medications is crucial. Do not flush medications down the toilet or pour them down the drain unless specifically instructed to do so by a healthcare professional or pharmacist. If you are unsure about the best method for disposing of medications, consult with your pharmacist, who can provide guidance on safe disposal practices. Additionally, you may want to inquire about drug take-back programs available in your area.
Some medications may come with an additional patient information leaflet. It is a good idea to check with your pharmacist to see if this applies to your prescription. If you have any questions or concerns about your medication, do not hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider for clarification and support.
In the event of a suspected overdose, it is critical to seek immediate medical attention. Call your local poison control center or visit the emergency room right away. When seeking help, be prepared to provide detailed information about the medication, including the amount taken, the time it was taken, and any other relevant details.
To ensure safe use, do not share your medication with others, and never take someone else's medication. Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion.
Proper disposal of unused or expired medications is crucial. Do not flush medications down the toilet or pour them down the drain unless specifically instructed to do so by a healthcare professional or pharmacist. If you are unsure about the best method for disposing of medications, consult with your pharmacist, who can provide guidance on safe disposal practices. Additionally, you may want to inquire about drug take-back programs available in your area.
Some medications may come with an additional patient information leaflet. It is a good idea to check with your pharmacist to see if this applies to your prescription. If you have any questions or concerns about your medication, do not hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider for clarification and support.
In the event of a suspected overdose, it is critical to seek immediate medical attention. Call your local poison control center or visit the emergency room right away. When seeking help, be prepared to provide detailed information about the medication, including the amount taken, the time it was taken, and any other relevant details.