Delestrogen 10mg/ml Inj

Estradiol is the primary estrogen secreted by the human ovary. It binds to and activates estrogen receptors (ERα and ERβ) located in target tissues (e.g., female reproductive organs, breast, hypothalamus, pituitary, bone, liver, cardiovascular system). This binding leads to conformational changes in the receptor, allowing it to translocate to the nucleus, bind to estrogen response elements (EREs) on DNA, and regulate gene transcription, thereby mediating the physiological effects of estrogens.

Serious Side Effects: Seek Medical Help Immediately

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 right away:

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 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, inform your doctor.

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
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
Common cold symptoms
Nose or throat irritation
Weight gain or loss
Joint pain
Leg cramps
Changes in sex interest
Irritation at the injection site

This is not an exhaustive list of potential 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.

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. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.

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, it is crucial to closely monitor your blood sugar levels.

This medication may cause high blood pressure, so it is essential to have your blood pressure checked regularly, as advised by your doctor. You should also have your blood work and bone density checked as recommended 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 medication, so inform your doctor if you have a history of elevated triglyceride levels. This drug may also cause dark skin patches on your face, so it is essential to avoid sun exposure, sunlamps, and tanning beds, and use sunscreen and protective clothing and eyewear.

This medication may affect certain laboratory tests, so inform all your healthcare providers and lab personnel that you are taking this drug. Smoking can increase the risk of heart disease, so it is recommended that you do not smoke; discuss this with your doctor. Limit your alcohol consumption, and if you regularly drink grapefruit juice or eat grapefruit, consult with your doctor.

In some cases, this medication may affect growth in children and teenagers, so 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 with your doctor to discuss any potential risks to your baby.

• Aromatase inhibitors (e.g., anastrozole, letrozole, exemestane) - concurrent use would counteract the effect of the aromatase inhibitor.
• Fulvestrant (estrogen receptor antagonist) - concurrent use would counteract the effect of fulvestrant.

• CYP3A4 inducers (e.g., carbamazepine, phenobarbital, phenytoin, rifampin, St. John's Wort) - may decrease estrogen levels, reducing efficacy.
• CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, ketoconazole, ritonavir, grapefruit juice) - may increase estrogen levels, increasing risk of adverse effects.
• Thyroid hormones (e.g., levothyroxine) - estrogens can increase thyroid-binding globulin (TBG), potentially increasing thyroid hormone requirements.
• Corticosteroids (e.g., prednisone) - estrogens may decrease the clearance of corticosteroids, leading to increased corticosteroid effects/toxicity.

• Anticoagulants (e.g., warfarin) - estrogens may alter the effects of anticoagulants; monitor INR/PT.
• Hypoglycemic agents (e.g., insulin, oral antidiabetics) - estrogens may impair glucose tolerance, requiring adjustment of antidiabetic therapy.
• Cyclosporine - estrogens may inhibit cyclosporine metabolism, increasing its levels and toxicity.

• Not many clinically significant minor interactions reported for estradiol injection.

• Unusual vaginal bleeding or spotting
• Breast lumps or pain
• Persistent headache or migraine
• Sudden severe chest pain, shortness of breath, or coughing up blood (signs of pulmonary embolism)
• Sudden numbness or weakness on one side of the body, sudden severe headache, sudden vision changes (signs of stroke)
• Chest pain, discomfort, pressure, or pain radiating to arm/jaw (signs of MI)
• Swelling, pain, or tenderness in one leg (signs of deep vein thrombosis)
• Yellowing of skin or eyes (jaundice)
• Abdominal pain, especially right upper quadrant
• Mood changes, depression

Contraindicated during pregnancy. 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 congenital anomalies in the fetus.

Use is generally not recommended during lactation. Estrogens are excreted in human milk and have been shown to decrease the quantity and quality of breast milk. They may also affect the nursing infant.

Generally not indicated for routine pediatric use. Can be used for pubertal induction in girls with hypogonadism, but careful monitoring of bone age and growth is required. Safety and efficacy in children under 18 for other indications are not established.

Increased risk of stroke, deep vein thrombosis, pulmonary embolism, and probable dementia in women 65 years of age or older. Use the lowest effective dose for the shortest duration consistent with treatment goals. Careful risk-benefit assessment is crucial.

• Delestrogen (estradiol valerate) is a long-acting injectable estrogen, providing sustained estradiol levels for 3-4 weeks, which can improve adherence compared to daily oral or transdermal forms.
• Always assess for contraindications, especially history of VTE, stroke, MI, estrogen-dependent cancers, or undiagnosed abnormal genital bleeding, before initiating therapy.
• The lowest effective dose for the shortest duration should be used, especially for menopausal symptom management, to minimize risks.
• Counsel patients extensively on the Black Box Warnings regarding cardiovascular events, breast cancer, and dementia, and the importance of reporting any concerning symptoms immediately.
• Smoking is an absolute contraindication due to significantly increased thrombotic risk.
• Regular follow-up, including blood pressure checks, breast exams, and mammograms, is crucial during therapy.

• Selective Estrogen Receptor Modulators (SERMs) (e.g., ospemifene for dyspareunia, bazedoxifene/conjugated estrogens for vasomotor symptoms and osteoporosis)
• Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine)
• Lifestyle modifications (e.g., diet, exercise, stress reduction, layered clothing for hot flashes)

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 reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed otherwise, do not flush medications down the toilet or pour them down the drain. If you are unsure about the correct 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 medical attention. Be prepared to provide information about the medication taken, the amount, and the time it occurred, as this will aid in receiving appropriate treatment.