estradiol valerate: clinical use

Prescribing considerations

• Confirm that symptoms materially affect quality of life and review the individual benefit-risk balance.
• Establish uterine status and provide appropriate endometrial protection when the uterus is present.
• Assess personal and family history, including breast cancer, thromboembolism, cardiovascular disease, migraine and liver disease.
• Oral HRT increases venous-thromboembolism risk; consider route in people with relevant risk factors.
• The product contains lactose and sucrose and may be unsuitable in specified rare hereditary carbohydrate-intolerance disorders.
• It is not contraceptive.

Contraindications and cautions

• Known, previous or suspected breast cancer
• Known or suspected oestrogen-dependent malignancy
• Unexplained genital bleeding or untreated endometrial hyperplasia
• Current or previous venous thromboembolism or a known thrombophilic disorder
• Active or recent arterial thromboembolic disease, including angina or myocardial infarction
• Acute liver disease, or previous liver disease before liver tests have returned to normal
• Porphyria
• Hypersensitivity to estradiol valerate or an excipient

Monitoring

• Review symptom control, adverse effects and ongoing benefit-risk balance.
• Use history-directed breast and pelvic examination and maintain appropriate screening.
• Assess unexpected, persistent or heavy vaginal bleeding.
• Monitor relevant conditions that may recur or worsen, including hypertension, migraine, liver disease, diabetes, gallstones, epilepsy, asthma, endometriosis and fibroids.
• Stop and reassess for jaundice or deteriorating liver function, a significant blood-pressure rise, new migraine-type headache, pregnancy or a newly identified contraindication.
• Sex steroids can affect some liver, thyroid, adrenal, renal, lipid, glucose and coagulation test results.

Clinical pharmacology

Estradiol valerate is rapidly hydrolysed to estradiol and valeric acid after oral administration. Estradiol binds mainly to albumin and sex-hormone-binding globulin; extensive first-pass metabolism contributes to relatively low oral bioavailability.

Formulation and product differences

• The selected product is an oral, sugar-coated, oestrogen-only tablet containing lactose and sucrose.
• Oral oestrogen undergoes first-pass hepatic metabolism; its thromboembolic risk profile differs from transdermal estradiol.
• It does not contain a progestogen, so it does not by itself protect the endometrium when the womb is present.