Description
Estrapause (Estradiol Valerate) 2 mg Tablets
Estrapause 2 mg is listed here as an oral estradiol valerate tablet. Estradiol valerate is an oestrogen medicine used in hormone replacement therapy to relieve symptoms caused by oestrogen deficiency after the menopause.
Active Ingredient and Medicine Class
The verified active ingredient is estradiol valerate. It belongs to the class of natural and semisynthetic oestrogens. After oral administration, estradiol valerate is converted in the body to estradiol, the main active oestrogen hormone.
Established Medical Uses
Oral estradiol valerate is used for established hormone replacement therapy indications in peri- and postmenopausal women, mainly for relief of oestrogen deficiency symptoms. It is also used in some authorised products for prevention of postmenopausal bone loss or osteoporosis in women at high fracture risk when other suitable medicines are not appropriate.
Authorised use varies by country and product, so the official product information should always be checked for the exact indications of a specific brand.
How It Works
Estradiol valerate is a prodrug of estradiol. Once absorbed, it is broken down to release estradiol, which then binds to oestrogen receptors in target tissues. This helps replace the reduced oestrogen levels that occur after menopause and can improve vasomotor and urogenital symptoms. Oestrogen also helps slow postmenopausal bone loss.
Important Safety Information
Oral oestrogen therapy is not suitable for everyone. Important contraindications include current, past or suspected breast cancer, other oestrogen-dependent tumours, unexplained vaginal bleeding, untreated endometrial hyperplasia, previous or current venous thromboembolism, active or recent arterial thromboembolic disease, severe liver disease, hypersensitivity to the medicine, and porphyria.
Special caution is needed in women with risk factors for thrombosis, liver disease, hypertriglyceridaemia, fluid retention, migraine, endometriosis, fibroids, or a history of chloasma. If the uterus is present, a progestogen is generally required with systemic oestrogen to reduce the risk of endometrial stimulation.
Clinically significant interactions may occur with medicines that induce liver enzymes, such as rifampicin, carbamazepine, phenytoin, phenobarbital, primidone, nevirapine, efavirenz and St John’s wort, which may reduce oestrogen exposure. CYP3A4 inhibitors, including certain azole antifungals, macrolides, verapamil, diltiazem and grapefruit juice, may increase oestrogen levels. Oestrogens may also affect lamotrigine and some antiviral regimens.
Possible Side Effects
Reported side effects of oral oestrogen therapy include nausea, vomiting, abdominal discomfort, bloating, headache, dizziness, migraine, mood changes, breast tenderness or enlargement, vaginal bleeding or spotting, changes in bleeding pattern, fluid retention, weight change and skin reactions such as rash or chloasma.
More serious adverse effects can include venous thromboembolism, stroke, myocardial infarction, gallbladder disease, cholestasis and, with longer-term use, increased risk of breast or endometrial cancer depending on the treatment regimen and duration.
Scientific Evidence
Clinical reviews of menopausal hormone therapy consistently support systemic oestrogen as an effective treatment for menopausal symptoms, especially vasomotor complaints. Reviews also note that oral and transdermal preparations differ in pharmacokinetic behaviour and risk profile, with route of administration influencing hepatic first-pass effects.
Evidence syntheses further emphasise that benefit-risk balance depends on age, time since menopause, dose, treatment duration and whether oestrogen is used alone or with a progestogen. Oral oestrogen can relieve symptoms and help prevent bone loss, but it is not recommended for cardiovascular prevention.
Medical Information Notice
This page is an educational summary based on sources available at the time of review. It does not replace the official patient leaflet, local prescribing information or assessment by a qualified healthcare professional.
Medical Sources
- Medicines.org.uk (emc), Bayer plc. Progynova 2 mg Tablets SmPC. Official prescribing information for oral estradiol valerate 2 mg tablets, including indications, contraindications, interactions and adverse effects. View official SmPC
- Abbie Laing et al. Oestrogen-based therapies for menopausal symptoms. Best Practice & Research Clinical Endocrinology & Metabolism, 2024. View scientific article
- Gina Lundberg et al. Menopausal Hormone Therapy: a Comprehensive Review. Current Atherosclerosis Reports, 2020. View scientific article
