Estradiol Valerate 40mg/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
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 is used to treat symptoms of menopause, such as hot flashes and vaginal dryness, to replace hormones in women whose bodies don't produce enough estrogen, and sometimes to treat certain types of prostate cancer in men. It is 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 accompanying information carefully. 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.
Important Administration Instructions
Do not use the medication if the solution appears cloudy, is leaking, or contains particles.
The solution should be colorless to faint yellow; do not use it if the color changes.
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 your doctor, nurse, or pharmacist for guidance on proper storage procedures.
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 accompanying information carefully. 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.
Important Administration Instructions
Do not use the medication if the solution appears cloudy, is leaking, or contains particles.
The solution should be colorless to faint yellow; do not use it if the color changes.
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 your doctor, nurse, or pharmacist for guidance on proper storage procedures.
Missed Dose
If you miss a dose, contact your doctor to determine the best course of action.
Lifestyle & Tips
- Do not smoke, as smoking significantly increases the risk of blood clots, heart attack, and stroke, especially when taking estrogens.
- Maintain a healthy diet and regular exercise to support cardiovascular health.
- Discuss any planned surgeries or prolonged immobility with your doctor, as these can increase the risk of blood clots.
- Report any unusual vaginal bleeding immediately.
- Perform regular breast self-exams and attend scheduled mammograms and gynecological exams.
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:
Dosage varies significantly by indication. For menopausal symptoms: 10-20 mg IM every 4 weeks. For hypogonadism: 10-20 mg IM every 4 weeks. For prostate cancer palliation: 30 mg or more IM every 1-2 weeks.
Dose Range:
10 - 40 mg
Condition-Specific Dosing:
menopausalSymptoms:
10-20 mg IM every 4 weeks
hypogonadism:
10-20 mg IM every 4 weeks
prostateCancerPalliation:
30 mg or more IM every 1-2 weeks
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (limited use for specific conditions like Turner syndrome or gender-affirming care, dosage highly individualized by specialist)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended
Moderate:
No specific adjustment recommended
Severe:
Use with caution; monitor for fluid retention
Dialysis:
Use with caution; monitor for fluid retention
Hepatic Impairment:
Mild:
Use with caution; monitor for adverse effects
Moderate:
Contraindicated
Severe:
Contraindicated
Pharmacology
Mechanism of Action
Estradiol valerate is an ester of estradiol, the primary estrogen secreted by the human ovary. It is a prodrug that is hydrolyzed to estradiol. Estradiol diffuses into target cells and binds to estrogen receptors (ERΞ± and ERΞ²) in the nucleus. The activated hormone-receptor complex then binds to estrogen response elements (EREs) on DNA, leading to gene transcription and protein synthesis. This mediates the physiological effects of estrogens, including development and maintenance of female reproductive system and secondary sex characteristics, and effects on bone, cardiovascular system, and CNS.
Pharmacokinetics
Absorption:
Bioavailability:
High (after IM injection, as it's a prodrug that releases estradiol)
Tmax:
Approximately 3-7 days (for estradiol after IM injection of estradiol valerate)
FoodEffect:
Not applicable (IM injection)
Distribution:
Vd:
Approximately 1 L/kg (for estradiol)
ProteinBinding:
Approximately 98% (primarily to sex hormone-binding globulin (SHBG) and albumin)
CnssPenetration:
Yes (estradiol crosses the blood-brain barrier)
Elimination:
HalfLife:
Approximately 5-18 days (for estradiol after IM injection of estradiol valerate, due to slow release from the ester)
Clearance:
High (for estradiol)
ExcretionRoute:
Renal (primarily as glucuronide and sulfate conjugates), Biliary (minor)
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Days (due to slow release from ester)
PeakEffect:
Approximately 3-7 days
DurationOfAction:
Approximately 2-4 weeks
Safety & Warnings
BLACK BOX WARNING
Estrogens, including estradiol valerate, increase the risk of endometrial cancer, cardiovascular disorders (stroke, deep vein thrombosis, pulmonary embolism, myocardial infarction), and probable dementia. The Women's Health Initiative (WHI) study found increased risks of stroke and DVT in postmenopausal women receiving estrogen-alone therapy. The WHI also found increased risks of MI, stroke, DVT, PE, and invasive breast cancer in postmenopausal women receiving estrogen plus progestin therapy. Estrogen-alone therapy should not be used for the prevention of cardiovascular disease or dementia. The WHI Memory Study (WHIMS) found an increased risk of probable dementia in postmenopausal women 65 years of age or older receiving estrogen-alone or estrogen plus progestin therapy.
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 notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, redness, swelling, blistering, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of liver problems: dark urine, fatigue, decreased appetite, stomach pain or upset, light-colored stools, vomiting, or yellow skin and eyes.
Signs of gallbladder problems: pain in the upper right abdomen, right shoulder, or between the shoulder blades, yellow skin and eyes, fever with chills, bloating, or severe stomach upset or vomiting.
Signs of pancreatitis (pancreas problems): severe stomach pain, severe back pain, or severe stomach upset or vomiting.
Signs of high blood pressure: severe headache or dizziness, fainting, or changes in vision.
Weakness on one side of the body, difficulty speaking or thinking, balance problems, drooping on one side of the face, or blurred vision.
Changes in vision or loss of vision, bulging eyes, or changes in how contact lenses feel.
Breast lump, breast pain or tenderness, 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 breathing difficulties.
Blood Clots and High Calcium Levels
Seek immediate medical attention if you experience signs of a blood clot, such as:
Chest pain or pressure
Coughing up blood
Shortness of breath
Swelling, warmth, numbness, color changes, or pain in a leg or arm
Difficulty speaking or swallowing
High calcium levels can occur in some people with cancer taking this medication. Contact your doctor right away if you experience:
Weakness
Confusion
Fatigue
Headache
Stomach upset or vomiting
Constipation
Bone pain
Other Side Effects
Most people do not experience significant side effects, but some may occur. If you are bothered by any of the following side effects or if they persist, contact your doctor:
Dizziness or headache
Hair loss
Stomach upset or vomiting
Constipation
Stomach pain or cramps
Bloating
Breast enlargement or tenderness
Vaginal bleeding or spotting
Painful periods
Common cold symptoms
Nose or throat irritation
Weight changes
Joint pain
Leg cramps
Changes in sex drive
* Irritation at the site of administration
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult 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 notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, redness, swelling, blistering, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of liver problems: dark urine, fatigue, decreased appetite, stomach pain or upset, light-colored stools, vomiting, or yellow skin and eyes.
Signs of gallbladder problems: pain in the upper right abdomen, right shoulder, or between the shoulder blades, yellow skin and eyes, fever with chills, bloating, or severe stomach upset or vomiting.
Signs of pancreatitis (pancreas problems): severe stomach pain, severe back pain, or severe stomach upset or vomiting.
Signs of high blood pressure: severe headache or dizziness, fainting, or changes in vision.
Weakness on one side of the body, difficulty speaking or thinking, balance problems, drooping on one side of the face, or blurred vision.
Changes in vision or loss of vision, bulging eyes, or changes in how contact lenses feel.
Breast lump, breast pain or tenderness, 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 breathing difficulties.
Blood Clots and High Calcium Levels
Seek immediate medical attention if you experience signs of a blood clot, such as:
Chest pain or pressure
Coughing up blood
Shortness of breath
Swelling, warmth, numbness, color changes, or pain in a leg or arm
Difficulty speaking or swallowing
High calcium levels can occur in some people with cancer taking this medication. Contact your doctor right away if you experience:
Weakness
Confusion
Fatigue
Headache
Stomach upset or vomiting
Constipation
Bone pain
Other Side Effects
Most people do not experience significant side effects, but some may occur. If you are bothered by any of the following side effects or if they persist, contact your doctor:
Dizziness or headache
Hair loss
Stomach upset or vomiting
Constipation
Stomach pain or cramps
Bloating
Breast enlargement or tenderness
Vaginal bleeding or spotting
Painful periods
Common cold symptoms
Nose or throat irritation
Weight changes
Joint pain
Leg cramps
Changes in sex drive
* Irritation at the site of administration
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult 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
- Chest pain or pressure, pain radiating to arm or jaw
- Shortness of breath
- Sudden pain, swelling, or redness in a leg (especially calf)
- Yellowing of skin or eyes (jaundice)
- Dark urine, light-colored stools
- Unusual vaginal bleeding or spotting
- Lump in the breast
- 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, such as foods or drugs. Be sure to describe the signs and symptoms you experienced.
A history of certain health conditions, including:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
Pregnancy or potential pregnancy. Note: This medication should not be taken during pregnancy.
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. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the signs and symptoms you experienced.
A history of certain health conditions, including:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
Pregnancy or potential pregnancy. Note: This medication should not be taken during pregnancy.
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. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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, discuss this with your doctor, as prolonged inactivity may increase your risk of developing blood clots. Additionally, if you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels.
Be aware that medications like this one can cause high blood pressure. Follow your doctor's instructions for regular blood pressure checks. You should also have your blood work and bone density checked as directed by your doctor.
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, and ovarian cancer, 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.
High triglyceride levels have been associated with this drug. 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, and to use sunscreen and protective clothing and eyewear.
This drug may interfere with certain laboratory tests, so be sure to inform all your healthcare providers and lab personnel that you are taking this medication. Smoking can increase the risk of heart disease, so it is recommended that you do not smoke. Limit your alcohol consumption, and if you regularly drink grapefruit juice or eat grapefruit, discuss this with your doctor.
In some cases, this medication may affect growth in children and teenagers, and they may require regular growth checks. If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
If you anticipate being immobile for extended periods, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor, as prolonged inactivity may increase your risk of developing blood clots. Additionally, if you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels.
Be aware that medications like this one can cause high blood pressure. Follow your doctor's instructions for regular blood pressure checks. You should also have your blood work and bone density checked as directed by your doctor.
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, and ovarian cancer, 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.
High triglyceride levels have been associated with this drug. 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, and to use sunscreen and protective clothing and eyewear.
This drug may interfere with certain laboratory tests, so be sure to inform all your healthcare providers and lab personnel that you are taking this medication. Smoking can increase the risk of heart disease, so it is recommended that you do not smoke. Limit your alcohol consumption, and if you regularly drink grapefruit juice or eat grapefruit, discuss this with your doctor.
In some cases, this medication may affect growth in children and teenagers, and they may require regular growth checks. If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. If you are breastfeeding, consult your doctor to discuss any 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. Contact a poison control center or emergency medical services immediately. Call 1-800-222-1222.
Drug Interactions
Contraindicated Interactions
- Aromatase inhibitors (e.g., Anastrozole, Letrozole) - concurrent use for breast cancer
- Tranexamic acid (increased risk of thrombosis)
Major Interactions
- CYP3A4 inducers (e.g., Carbamazepine, Phenobarbital, Phenytoin, Rifampin, St. John's Wort) - decreased estrogen levels
- CYP3A4 inhibitors (e.g., Ketoconazole, Itraconazole, Ritonavir, Clarithromycin) - increased estrogen levels
- Thyroid hormone replacement (e.g., Levothyroxine) - increased thyroid-binding globulin, requiring higher thyroid hormone dose
- Anticoagulants (e.g., Warfarin) - may alter anticoagulant effect (monitor INR)
- Corticosteroids (e.g., Prednisone) - may increase corticosteroid levels
Moderate Interactions
- Lamotrigine (decreased lamotrigine levels)
- Cyclosporine (increased cyclosporine levels)
- Theophylline (increased theophylline levels)
- Folic acid (may decrease folic acid levels)
- Bosentan (decreased estrogen levels)
Minor Interactions
- Ascorbic acid (may increase estrogen levels)
- Acetaminophen (may increase estrogen levels)
Monitoring
Baseline Monitoring
Complete Medical History and Physical Exam
Rationale: To identify contraindications, risk factors for VTE, stroke, breast cancer, endometrial cancer, and other estrogen-related adverse effects.
Timing: Prior to initiation of therapy
Blood Pressure
Rationale: Estrogens can cause an increase in blood pressure.
Timing: Prior to initiation of therapy
Lipid Panel
Rationale: Estrogens can affect lipid profiles.
Timing: Prior to initiation of therapy
Liver Function Tests (LFTs)
Rationale: Estrogens are metabolized by the liver; severe hepatic impairment is a contraindication.
Timing: Prior to initiation of therapy
Breast Exam and Mammography
Rationale: To screen for breast cancer, as estrogen therapy can increase risk.
Timing: Prior to initiation of therapy (and as clinically indicated)
Pelvic Exam and Pap Smear
Rationale: To screen for endometrial cancer and other gynecological conditions.
Timing: Prior to initiation of therapy (and as clinically indicated)
Routine Monitoring
Blood Pressure
Frequency: Annually or as clinically indicated
Target: <130/80 mmHg (general target)
Action Threshold: Sustained elevation requiring intervention
Breast Exam
Frequency: Annually
Target: Normal
Action Threshold: New lumps, pain, or discharge
Mammography
Frequency: As per national screening guidelines (e.g., every 1-2 years for women over 40-50)
Target: Normal
Action Threshold: Abnormal findings requiring further investigation
Pelvic Exam and Pap Smear
Frequency: Annually or as per national screening guidelines
Target: Normal
Action Threshold: Abnormal findings requiring further investigation
Lipid Panel
Frequency: Periodically, as clinically indicated
Target: Individualized
Action Threshold: Significant adverse changes
Liver Function Tests (LFTs)
Frequency: Periodically, if clinically indicated or with symptoms of hepatic dysfunction
Target: Normal
Action Threshold: Significant elevation
Symptom Monitoring
- Signs of venous thromboembolism (VTE) such as leg pain, swelling, redness, shortness of breath, chest pain
- Signs of stroke (e.g., sudden severe headache, weakness/numbness on one side of body, vision changes, speech difficulty)
- Signs of myocardial infarction (e.g., chest pain, discomfort, shortness of breath)
- Abnormal vaginal bleeding
- Breast lumps or changes
- Severe headache or migraine
- Vision changes
- Jaundice or signs of liver dysfunction
- Mood changes, depression
Special Patient Groups
Pregnancy
Contraindicated in pregnancy. Estrogen use during pregnancy is associated with an increased risk of birth defects, particularly genital abnormalities in female fetuses.
Trimester-Specific Risks:
First Trimester:
Increased risk of congenital anomalies, particularly feminization of male fetuses and virilization of female fetuses.
Second Trimester:
Not recommended; potential for adverse effects on fetal development.
Third Trimester:
Not recommended; potential for adverse effects on fetal development.
Lactation
Contraindicated during lactation. Estrogens are excreted in breast milk and can reduce the quantity and quality of breast milk. They may also have adverse effects on the nursing infant.
Infant Risk:
High (potential for adverse effects on infant, reduction in milk supply)
Pediatric Use
Generally not indicated for pediatric use, except in very specific circumstances under specialist supervision (e.g., Turner syndrome, gender-affirming care) where benefits outweigh risks. Safety and efficacy not established for most pediatric indications.
Geriatric Use
Use with caution in women 65 years of age or older due to increased risk of probable dementia (as per WHIMS study) and potentially increased risk of VTE and stroke. Lowest effective dose for shortest duration should be considered. Close monitoring for adverse effects is crucial.
Clinical Information
Clinical Pearls
- Estradiol valerate is a long-acting estrogen formulation, typically administered every 2-4 weeks, which can improve adherence compared to daily oral formulations.
- The 40mg/ml concentration is relatively high and often used for specific indications like prostate cancer palliation or certain gender-affirming hormone therapy protocols, rather than standard menopausal hormone therapy.
- Always review the patient's complete medical history, especially for a history of VTE, stroke, MI, breast cancer, or liver disease, before initiating therapy.
- Emphasize the importance of not smoking while on estrogen therapy due to significantly increased cardiovascular risks.
- Patients should be educated on the signs and symptoms of serious adverse events (e.g., blood clots, stroke, heart attack) and instructed to seek immediate medical attention if they occur.
- For menopausal symptoms, the lowest effective dose for the shortest duration consistent with treatment goals should be used.
Alternative Therapies
- Selective Estrogen Receptor Modulators (SERMs) (e.g., Raloxifene, Ospemifene)
- Non-hormonal therapies for menopausal symptoms (e.g., SSRIs/SNRIs, Gabapentin, Clonidine)
- GnRH agonists/antagonists (for prostate cancer)
- Antiandrogens (for prostate cancer)
Cost & Coverage
Average Cost:
Varies widely, typically $50 - $300+ per 5ml vial (40mg/ml)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (for generics), Tier 3 or 4 (for brands)
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 and effective use of your medication, please follow these guidelines:
- Do not share your prescription drugs with others, and never take someone else's medication.
- Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion.
- Properly dispose of unused or expired medications. Unless instructed otherwise, do not flush them down the toilet or pour them down the drain. If you are unsure about the best disposal method, consult your pharmacist for guidance. Many communities have drug take-back programs that provide a safe and environmentally friendly way to dispose of unwanted medications.
Some medications may come with an additional patient information leaflet. If you have questions or concerns about your medication, it is crucial to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. They can provide personalized guidance and support to ensure you use your medication safely and effectively.
In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide critical information, including the name of the medication taken, the amount, and the time it was taken, to facilitate prompt and appropriate treatment.
To ensure safe and effective use of your medication, please follow these guidelines:
- Do not share your prescription drugs with others, and never take someone else's medication.
- Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion.
- Properly dispose of unused or expired medications. Unless instructed otherwise, do not flush them down the toilet or pour them down the drain. If you are unsure about the best disposal method, consult your pharmacist for guidance. Many communities have drug take-back programs that provide a safe and environmentally friendly way to dispose of unwanted medications.
Some medications may come with an additional patient information leaflet. If you have questions or concerns about your medication, it is crucial to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. They can provide personalized guidance and support to ensure you use your medication safely and effectively.
In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide critical information, including the name of the medication taken, the amount, and the time it was taken, to facilitate prompt and appropriate treatment.