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Estradiol Valerate 10mg/ml Inj, 5ml

Manufacturer XIROMED Active Ingredient Estradiol Injection(es tra DYE ole) Pronunciation es-tra-DYE-ole VAL-er-ate
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.
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Drug Class
Estrogen; Hormone Replacement Therapy; Antineoplastic
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Pharmacologic Class
Estrogen receptor agonist
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Pregnancy Category
Category X
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FDA Approved
Jan 1970
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Estradiol Valerate Injection is a form of estrogen, a female hormone. It is given as an injection into a muscle to treat symptoms of menopause (like hot flashes and vaginal dryness), to replace estrogen in women whose bodies don't make enough, or to help manage certain types of prostate cancer in men. It works by replacing the estrogen your body is missing or by counteracting male hormones in prostate cancer.
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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 faintly yellow; do not use it if the color has changed.

Safe Disposal of Needles and Supplies

After using a needle, dispose of it 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.

Missed Dose

If you miss a dose, contact your doctor to determine the best course of action.
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Lifestyle & Tips

  • Avoid smoking, as it significantly increases the risk of blood clots, heart attack, and stroke, especially when taking estrogens.
  • Maintain a healthy diet and engage in regular physical activity to support cardiovascular health.
  • Discuss any new or worsening symptoms with your healthcare provider promptly.
  • Attend all scheduled follow-up appointments and screenings (e.g., mammograms, pelvic exams).
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: Varies significantly by indication. For menopausal symptoms: 10-20 mg IM every 4 weeks. For hypoestrogenism: 10-20 mg IM every 4 weeks. For palliative treatment of prostate cancer: 30 mg IM every 1-2 weeks.
Dose Range: 10 - 30 mg

Condition-Specific Dosing:

menopausalSymptoms: 10-20 mg IM every 4 weeks
hypoestrogenism: 10-20 mg IM every 4 weeks
palliativeProstateCancer: 30 mg IM every 1-2 weeks
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established (generally not indicated)
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment provided; use with caution.
Moderate: No specific dose adjustment provided; use with caution.
Severe: No specific dose adjustment provided; use with caution.
Dialysis: Considerations: Not well-studied; use with caution due to potential fluid retention and metabolic effects.

Hepatic Impairment:

Mild: Use with caution; monitor for adverse effects.
Moderate: Contraindicated in severe hepatic dysfunction; use with extreme caution in moderate impairment.
Severe: Contraindicated

Pharmacology

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Mechanism of Action

Estradiol valerate is a prodrug that is hydrolyzed to estradiol, the primary estrogen in humans. Estradiol binds to and activates estrogen receptors (ERΞ± and ERΞ²) in target tissues (e.g., reproductive organs, breast, bone, CNS, cardiovascular system). This binding leads to a conformational change in the receptor, allowing it to translocate to the nucleus, bind to estrogen response elements (EREs) on DNA, and regulate gene transcription, thereby mediating estrogenic effects.
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Pharmacokinetics

Absorption:

Bioavailability: Not directly applicable as it's an IM prodrug; provides sustained release of estradiol.
Tmax: Estradiol levels peak within 2-3 days after IM injection.
FoodEffect: Not applicable for 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 3-5 days (effective half-life after IM injection due to depot effect; estradiol's intrinsic half-life is much shorter, hours)
Clearance: High hepatic clearance
ExcretionRoute: Renal (primarily as glucuronide and sulfate conjugates)
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: Within days (for symptomatic relief)
PeakEffect: Within 2-3 days (peak estradiol levels)
DurationOfAction: Approximately 3-4 weeks (due to depot effect of the valerate ester)
Confidence: Medium

Safety & Warnings

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BLACK BOX WARNING

Estrogens and estrogen plus progestin therapies 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 estrogens plus medroxyprogesterone acetate. The WHI study also reported an increased risk of stroke and deep vein thrombosis in postmenopausal women receiving daily oral conjugated estrogens alone. The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older receiving conjugated estrogens plus medroxyprogesterone acetate and in those receiving conjugated estrogens alone. Estrogens increase the risk of endometrial cancer in postmenopausal women with an intact uterus. Appropriate diagnostic measures, including directed endometrial biopsy when indicated, should be performed to rule out malignancy in all cases of undiagnosed persistent or recurrent abnormal vaginal bleeding.
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Side Effects

Serious 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, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
 Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of gallbladder problems, such as:
+ Pain in the upper right belly area, right shoulder area, or between the shoulder blades
+ Yellow skin or eyes
+ Fever with chills
+ Bloating
+ Severe upset stomach or vomiting
 Signs of pancreatitis (pancreas problem), including:
+ Severe stomach pain
+ Severe back pain
+ Severe upset stomach or vomiting
Signs of high blood pressure, such as:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
 Weakness on one side of the body
Trouble speaking or thinking
 Changes in balance
Drooping on one side of the face
 Blurred eyesight
Eyesight changes or loss
 Bulging eyes
Changes in how contact lenses feel
 Breast lump, pain, or soreness
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, leading to swelling or weight gain. If you experience swelling, weight gain, or trouble breathing, contact your doctor.

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 can occur in some people with cancer taking this medication. If you experience signs of high calcium levels, such as:
 Weakness
Confusion
 Fatigue
Headache
 Upset stomach or vomiting
Constipation
 Bone pain

contact your doctor right away.

Other Side Effects

Most people do not experience serious side effects, but some may occur. If you experience any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:

Dizziness or headache
 Hair loss
Upset stomach or vomiting
 Constipation
Stomach pain or cramps
 Bloating
Enlarged or 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

This is not a comprehensive list of all 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.
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Seek Immediate Medical Attention If You Experience:

  • Sudden chest pain or heaviness, pain spreading to arm or jaw, shortness of breath (signs of heart attack)
  • Sudden severe headache, sudden numbness or weakness (especially on one side of the body), sudden trouble speaking or seeing, sudden dizziness or loss of balance (signs of stroke)
  • Pain, swelling, or warmth in the leg (signs of deep vein thrombosis)
  • Sudden shortness of breath, chest pain, coughing up blood (signs of pulmonary embolism)
  • New breast lump or changes in the breast
  • Any unusual or abnormal vaginal bleeding (especially if you have a uterus)
  • Yellowing of the skin or eyes (jaundice), dark urine, light-colored stools, severe stomach pain (signs of liver problems)
  • Changes in vision or contact lens intolerance
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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 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 problems 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.
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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 instruct you on when to resume taking it after the surgery or procedure.

If you anticipate being inactive 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, 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, 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.

High triglyceride levels have been associated with this medication. If you have a history of high triglyceride levels, inform your doctor. This drug may also 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 medication may affect certain laboratory tests, so be sure to inform all your healthcare providers and lab personnel that you are taking this drug. Avoid smoking, as it increases the risk of heart disease, and limit your alcohol consumption. If you regularly consume 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. Discuss this with your 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, consult your doctor to discuss any potential risks to your baby.
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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

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Contraindicated Interactions

  • Thromboembolic disorders (history of DVT, PE, stroke, MI)
  • Estrogen-dependent neoplasia (e.g., breast cancer, endometrial cancer)
  • Undiagnosed abnormal genital bleeding
  • Severe hepatic dysfunction or disease
  • Pregnancy
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Major Interactions

  • CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, St. John's Wort): May significantly decrease estrogen levels, reducing efficacy.
  • CYP3A4 inhibitors (e.g., ketoconazole, ritonavir, clarithromycin, grapefruit juice): May increase estrogen levels, potentially increasing adverse effects.
  • Warfarin: Estrogens may alter the anticoagulant effect of warfarin; close monitoring of INR is required.
  • Thyroid hormones (e.g., levothyroxine): Estrogens can increase thyroid-binding globulin (TBG), leading to increased bound thyroid hormone and potentially requiring an increased dose of thyroid hormone.
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Moderate Interactions

  • Corticosteroids (e.g., prednisone): Estrogens may decrease the clearance of corticosteroids, leading to increased corticosteroid effects.
  • Folic acid antagonists (e.g., methotrexate): Estrogens may interfere with folate metabolism.
  • Lamotrigine: Estrogens may decrease lamotrigine levels, potentially leading to loss of seizure control.
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Minor Interactions

  • Certain laboratory tests: Estrogens can affect coagulation factors, lipid profiles, and thyroid function tests.

Monitoring

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Baseline Monitoring

Complete medical history and physical examination

Rationale: To identify contraindications, risk factors, and establish baseline health status.

Timing: Prior to initiation of therapy

Blood pressure

Rationale: Estrogens can affect blood pressure.

Timing: Prior to initiation of therapy

Lipid profile (total cholesterol, HDL, LDL, triglycerides)

Rationale: Estrogens can affect lipid metabolism.

Timing: Prior to initiation of therapy

Liver function tests (ALT, AST, bilirubin)

Rationale: Estrogens are metabolized in the liver; contraindicated in severe hepatic dysfunction.

Timing: Prior to initiation of therapy

Breast examination and mammography

Rationale: To screen for breast cancer, a known risk with estrogen therapy.

Timing: Prior to initiation of therapy, as per age-appropriate screening guidelines

Pelvic examination and Pap test

Rationale: To screen for gynecological conditions, including endometrial cancer (if uterus intact).

Timing: Prior to initiation of therapy, as per age-appropriate screening guidelines

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Routine Monitoring

Annual physical examination (including breast and pelvic exam)

Frequency: Annually

Target: Normal findings

Action Threshold: Any abnormal findings require further investigation.

Blood pressure

Frequency: Periodically (e.g., every 3-6 months or as clinically indicated)

Target: <130/80 mmHg (general target)

Action Threshold: Sustained elevation (e.g., >140/90 mmHg) requires evaluation and management.

Mammography

Frequency: As per national screening guidelines (e.g., annually or biennially for women over 40-50)

Target: No suspicious findings

Action Threshold: Suspicious findings require immediate follow-up.

Lipid profile

Frequency: Periodically (e.g., every 1-2 years or as clinically indicated)

Target: Individualized targets based on cardiovascular risk

Action Threshold: Significant adverse changes may warrant dose adjustment or discontinuation.

Liver function tests

Frequency: As clinically indicated (e.g., if symptoms of hepatic dysfunction arise)

Target: Within normal limits

Action Threshold: Significant elevation requires investigation and potential discontinuation.

Monitoring for abnormal vaginal bleeding (if uterus intact)

Frequency: Ongoing patient education and reporting

Target: Absence of abnormal bleeding

Action Threshold: Any new, persistent, or recurrent abnormal bleeding requires prompt evaluation to rule out endometrial pathology.

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Symptom Monitoring

  • Signs and symptoms of thromboembolic events (e.g., sudden chest pain, shortness of breath, sudden severe headache, sudden loss of vision, pain/swelling in leg)
  • Signs and symptoms of myocardial infarction (e.g., chest pain, discomfort in other areas of upper body, shortness of breath)
  • Signs and symptoms of stroke (e.g., sudden numbness or weakness, confusion, trouble speaking, sudden trouble seeing, sudden dizziness, severe headache)
  • New breast lumps or changes
  • Abnormal vaginal bleeding (spotting, prolonged bleeding, heavy bleeding)
  • Symptoms of liver dysfunction (e.g., jaundice, dark urine, light-colored stools, severe abdominal pain)
  • Severe headache or migraine
  • Changes in vision
  • Mood changes or depression

Special Patient Groups

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Pregnancy

Contraindicated. Estrogens are not indicated for use in pregnancy and there is no evidence of benefit from estrogen therapy during pregnancy. Exposure to estrogens during pregnancy has been associated with an increased risk of birth defects in the reproductive organs of female fetuses and other adverse outcomes.

Trimester-Specific Risks:

First Trimester: Potential for adverse effects on fetal development, particularly reproductive organs.
Second Trimester: Not indicated; continued exposure carries risks.
Third Trimester: Not indicated; continued exposure carries risks.
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Lactation

Contraindicated. Estrogens are excreted in human milk and can decrease the quantity and quality of breast milk. They may also cause adverse effects in the nursing infant (e.g., feminization).

Infant Risk: High risk (L5) due to potential for adverse effects on infant and reduction in milk supply.
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Pediatric Use

Not indicated for pediatric use. Safety and efficacy have not been established in pediatric patients. Use in children could lead to premature epiphyseal closure and other adverse effects on development.

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Geriatric Use

Use with caution. Women 65 years of age or older have an increased risk of probable dementia with estrogen therapy. The lowest effective dose for the shortest duration should be used. Increased risk of cardiovascular events (stroke, DVT, PE) and breast cancer has been observed in older postmenopausal women.

Clinical Information

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Clinical Pearls

  • Estradiol valerate injection is for intramuscular (IM) use only. Do not administer intravenously.
  • This medication is a long-acting estrogen formulation, providing sustained estradiol levels over several weeks.
  • For women with an intact uterus, a progestin should be co-administered to reduce the risk of endometrial hyperplasia and cancer, unless contraindicated.
  • Estrogens should be used at the lowest effective dose for the shortest duration consistent with treatment goals, especially for menopausal symptoms, due to associated risks.
  • Regular monitoring for signs of thromboembolic events, breast changes, and abnormal vaginal bleeding is crucial.
  • Not indicated for the prevention of cardiovascular disease, stroke, or dementia.
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Alternative Therapies

  • Selective Estrogen Receptor Modulators (SERMs) (e.g., tamoxifen, raloxifene - for specific indications like osteoporosis or breast cancer prevention)
  • Non-hormonal therapies for menopausal symptoms (e.g., SSRIs/SNRIs, gabapentin, clonidine)
  • Other antiandrogens or hormonal therapies for prostate cancer (e.g., GnRH agonists/antagonists, androgen receptor inhibitors)
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Cost & Coverage

Average Cost: Varies widely by pharmacy and insurance plan; typically ranges from $50 - $200+ per 5ml vial (10mg/ml)
Generic Available: Yes
Insurance Coverage: Often covered by most insurance plans, typically Tier 1 or Tier 2 for generic formulations.
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General Drug Facts

If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional, do not flush medications down the toilet or pour them down the drain. If you are unsure about the proper disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the quantity, and the time of ingestion.