Valestra
Generic Name
Estradiol Valerate
Manufacturer
Bayer
Country
Germany
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Price Details
Current market pricing information
| Variant | Unit Price | Strip Price |
|---|---|---|
| valestra 1 mg tablet | ৳ 10.00 | ৳ 100.00 |
| valestra 2 mg tablet | ৳ 19.00 | ৳ 190.00 |
Description
Overview of the medicine
Valestra (Estradiol Valerate) is an estrogen hormone used primarily for hormone replacement therapy (HRT) to alleviate menopausal symptoms like hot flashes and vaginal dryness. It is also used in the treatment of hypogonadism, osteoporosis prevention, and in certain cases of transgender hormone therapy.
Uses & Indications
Dosage
Adults
Typically 1-2 mg orally once daily. Dose should be individualized and adjusted based on individual response and indication. In HRT, it's often given cyclically or continuously combined with a progestin.
Elderly
No specific dose adjustment for elderly patients, but caution advised due to increased risk of adverse effects and comorbidities. Start with the lowest effective dose.
Renal_impairment
No specific dose adjustment required for mild to moderate renal impairment, but use with caution in severe cases due to potential for fluid retention and electrolyte imbalance.
How to Take
Take orally with or without food, usually at the same time each day. It is important to swallow the tablet whole with water.
Mechanism of Action
Estradiol valerate is an estrogen prodrug. After administration, it is rapidly hydrolyzed to 17β-estradiol, the primary and most potent human estrogen. Estradiol binds to estrogen receptors (ERα and ERβ) in target tissues, forming a complex that then translocates into the nucleus to regulate gene expression, leading to the characteristic estrogenic effects.
Pharmacokinetics
Onset
Effects typically observed within hours to days for menopausal symptoms, with sustained levels achieved over time.
Excretion
Primarily excreted in the urine as glucuronide and sulfate conjugates; some fecal excretion.
Half life
Estradiol has a relatively short half-life of 1-2 hours; however, Estradiol Valerate acts as a reservoir, providing sustained estradiol levels for approximately 12-24 hours after oral dose.
Absorption
Well absorbed from the gastrointestinal tract after oral administration. Hydrolyzed to estradiol during absorption and first-pass hepatic metabolism.
Metabolism
Undergoes extensive first-pass metabolism in the liver. Hydrolyzed to estradiol and valeric acid. Estradiol is further metabolized via hydroxylation and conjugation to estrone and estriol, and their glucuronide and sulfate conjugates.
Side Effects
Contraindications
- •Undiagnosed abnormal genital bleeding
- •Breast cancer or history of breast cancer
- •Estrogen-dependent neoplasia
- •Active deep vein thrombosis (DVT), pulmonary embolism (PE), or history of these conditions
- •Active arterial thromboembolic disease (e.g., stroke, myocardial infarction)
- •Liver dysfunction or disease
- •Known hypersensitivity to estradiol valerate or any component of the medication
- •Pregnancy and lactation
Drug Interactions
Warfarin
May alter the anticoagulant effects of warfarin, requiring monitoring of International Normalized Ratio (INR) and potential dose adjustment of warfarin.
Grapefruit Juice
May increase estradiol levels by inhibiting CYP3A4 metabolism, potentially increasing side effects.
Thyroid Hormones
Estrogen increases thyroid-binding globulin, which can increase the need for thyroid hormone replacement. Patients receiving thyroid hormone replacement should have their thyroid function monitored.
CYP3A4 Inhibitors (e.g., Ketoconazole, Erythromycin)
May increase estrogen levels, potentially leading to increased side effects such as nausea and breast tenderness.
CYP3A4 Inducers (e.g., Rifampicin, Carbamazepine, Phenytoin)
May decrease estrogen levels, reducing efficacy and potentially leading to return of symptoms or breakthrough bleeding.
Storage
Store below 30°C (86°F) in a dry place, away from direct sunlight and moisture. Do not freeze. Keep out of reach of children.
Overdose
Symptoms of overdose include nausea, vomiting, breast tenderness, abdominal pain, drowsiness/fatigue, and withdrawal bleeding in women. Overdose is generally not life-threatening. Treatment is symptomatic and supportive. There is no specific antidote.
Pregnancy & Lactation
Valestra is contraindicated in pregnancy due to potential harm to the fetus. If pregnancy occurs while taking this medication, it should be discontinued immediately. It is not recommended during lactation as it may decrease milk production and traces of estrogen may pass into breast milk, potentially affecting the infant.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
Typically 24 to 36 months from the manufacturing date, consult the product leaflet for specific details.
Availability
Pharmacies, hospitals
Approval Status
Approved by FDA/DGDA
Patent Status
Generic available
WHO Essential Medicine
YesAlternative Medicines in Bangladesh
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Global Brand Names
International brand names for this medicine
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