Estradiol Valerate

Generic Details

Generic Name

Estradiol Valerate

Other Names

  • Estradiol valerate
  • EV

Drug Class

  • Estrogen hormone

Chemical Formula

C23H32O3

Molecular Weight

356.5 g/mol

Mechanism of Action

  • Estradiol valerate is a prodrug of 17β-estradiol, the major biologically active human estrogen. It is converted to estradiol in the body.

Indications

  • Hormone replacement therapy in menopausal women
  • Treatment of menopausal symptoms such as hot flashes, vaginal dryness, and osteoporosis

Common Dosage Forms

  • Tablet
  • Injection

Typical Dosage

  • Oral: 1-2 mg once daily
  • Injection: 10-20 mg every 2-4 weeks

Pediatric Dosage

  • Not recommended for use in children

Geriatric Dosage

  • Use with caution and at the lowest effective dose

Side Effects

  • Nausea
  • Headache
  • Breast tenderness
  • Irregular vaginal bleeding
  • Fluid retention

Contraindications

  • Pregnancy
  • Breastfeeding
  • Liver disease

Pregnancy Category

  • Category X - Contraindicated in pregnancy

Lactation Safety

  • Not recommended during breastfeeding

Drug Interactions

  • Warfarin
  • Corticosteroids
  • Anticonvulsants

Overdose Symptoms

  • Nausea
  • Vomiting
  • Breast tenderness

Antidote for Overdose

  • No specific antidote, treatment is supportive

Storage Conditions

  • Store at room temperature away from moisture and heat

Pharmacokinetics

  • Absorption: Well absorbed after oral administration
  • Distribution: Distributed widely in the body, mainly in fatty tissues
  • Metabolism: Metabolized in the liver to estradiol and other metabolites
  • Excretion: Excreted primarily in urine and feces

Precautions

  • Monitor for signs of thromboembolism
  • Regularly monitor liver function tests

Warnings

  • Increased risk of endometrial cancer in women with an intact uterus
  • Increased risk of breast cancer

Others

  • Estradiol valerate should only be used for the shortest duration at the lowest effective dose.