Formulary
Estradiol: Indications, Dosing, Side Effects and Interactions
Estradiol clinical drug profile including indications, dosing, side effects, cautions and interactions.
MedNext Academy | 6 min read
Estradiol: Indications, Dosing, Side Effects and Interactions
Estradiol clinical drug profile including indications, dosing, side effects, cautions and interactions.
Indications and dose
**Menopausal symptoms,Osteoporosis prophylaxis**
- **Adult** (By Transdermal Application): Apply 1 patch once weekly continuously, alternatively apply 1 patch once weekly for 3 weeks, followed by a 7-day patch-free interval (cyclical), to be used with cyclical progestogen for 12-14 days of each cycle in women with a uterus, initiate therapy with TS 50 patch, subsequently adjust according to response, women receiving TS 100 patches for menopausal symptoms may continue with this strength for osteoporosis prophylaxis.
**Menopausal symptoms**
- **Adult** (By Mouth): Initially 1 mg daily, to be started on day 1 of menstruation (or any time if cycles have ceased or are infrequent), increased if necessary to 2 mg daily, to be taken with a cyclical progestogen for 12-14 days of each cycle in women with a uterus.
**Osteoporosis prophylaxis**
- **Adult** (By Mouth): 2 mg daily, to be taken with a cyclical progestogen for 12-14 days of each cycle in women with a uterus.
**Menopausal symptoms not controlled with lower strength,Osteoporosis prophylaxis**
- **Adult** (By Mouth): 2 mg daily, started on day 1 of menstruation (or at any time if cycles have ceased or are infrequent), to be given with cyclical progestogen for 12-14 days of each cycle in women with a uterus.
Cautions
General cautions: Acute porphyrias ; diabetes (increased risk of heart disease); factors predisposing to thromboembolism; history of breast nodules-closely monitor breast status (risk of breast cancer); history of endometrial hyperplasia; history of fibrocystic disease-closely monitor breast status (risk of breast cancer); hypophyseal tumours; increased risk of gall-bladder disease; migraine (or migraine-like headaches); presence of antiphospholipid antibodies (increased risk of thrombotic events); prolonged exposure to unopposed oestrogens may increase risk of developing endometrial cancer; risk factors for oestrogen-dependent tumours (e.g. breast cancer in first-degree relative); symptoms of endometriosis may be exacerbated; uterine fibroids may increase in size Specific cautions: With vaginal use Review treatment at least annually to assess need for continued treatment Cautions, further information Risk of endometrial cancer The increased risk of endometrial cancer depends on the dose and duration of oestrogen-only HRT. In women with a uterus using systemic preparations, the addition of a progestogen cyclically (for at least 10 days per 28-day cycle) reduces the additional risk of endometrial cancer; this additional risk is eliminated if a progestogen is given continuously. However, this should be weighed against the increased risk of breast cancer. Risk of ovarian cancer Long-term use of combined HRT or oestrogen-only HRT is associated with a small increased risk of ovarian cancer. This excess risk disappears within a few years of stopping. Risk of venous thromboembolism Women using combined or oestrogen-only HRT are at an increased risk of deep vein thrombosis and of pulmonary embolism especially in the first year of use. In women who have predisposing factors (such as a personal or family history of deep vein thrombosis or pulmonary embolism, severe varicose veins, obesity, trauma, or prolonged bed-rest) it is prudent to review the need for HRT, as in some cases the risks of HRT may exceed the benefits. Travel involving prolonged immobility further increases the risk of deep vein thrombosis. Although the level of risk of thromboembolism associated with non-oral routes of administration of HRT has not been established, it may be lower for the transdermal route compared to the oral route; studies have found the risk associated with transdermal HRT to be no greater than the baseline population risk of thromboembolism. Risk of stroke Risk of stroke increases with age, therefore older women have a greater absolute risk of stroke. Combined HRT or oestrogen-only HRT increases the risk of stroke. Risk of coronary heart disease HRT does not prevent coronary heart disease and should not be prescribed for this purpose. There is an increased risk of coronary heart disease in women who start combined HRT more than 10 years after menopause. Although very little information is available on the risk of coronary heart disease in younger women who start HRT close to the menopause, studies suggest a lower relative risk compared with older women. Risk of breast cancer With systemic use: HRT use is associated with an increased risk of breast cancer-see Important safety information . Radiological detection of breast cancer can be made more difficult as mammographic density can increase with HRT use.
Contraindications
Active arterial thromboembolic disease (e.g. angina or myocardial infarction); history of breast cancer; history of venous thromboembolism; oestrogen-dependent cancer; recent arterial thromboembolic disease (e.g. angina or myocardial infarction); thrombophilic disorder; undiagnosed vaginal bleeding; untreated endometrial hyperplasia
Side effects
General side-effects: Common or very common Headaches; nausea; skin reactions Uncommon Hypertension Specific side-effects: Common or very common With oral use Asthenia; gastrointestinal discomfort; gastrointestinal disorders; haemorrhage; menstrual cycle irregularities; muscle complaints; pelvic pain; weight changes With transdermal use Abdominal pain; breast abnormalities; menstrual cycle irregularities; uterine disorders; vaginal discharge; weight changes With vaginal use Abdominal pain; vaginal haemorrhage; vulvovaginal disorders Uncommon With oral use Anxiety; back pain; breast abnormalities; cervical abnormalities; cystitis-like symptom; depression; dizziness; embolism and thrombosis; erythema nodosum; gallbladder disorder; oedema; palpitations; peripheral vascular disease; tumour growth; visual impairment; vulvovaginal candidiasis With transdermal use Asthenia; breast neoplasm benign; depression; flatulence; increased risk of infection; leiomyoma; mood swings; vertigo; vomiting With vaginal use Vulvovaginal fungal infection; weight increased Rare or very rare With oral use Angioedema; chorea; contact lens intolerance; haemolytic anaemia; hepatic disorders; hirsutism; malaise; sexual dysfunction; steepening of corneal curvature; vaginal discharge; vomiting With transdermal use Epilepsy exacerbated; galactorrhoea; glucose tolerance impaired; libido disorder With vaginal use Diarrhoea; endometrial hyperplasia; fluid retention; genital pruritus; increased risk of ischaemic stroke; insomnia; neoplasm malignant; neoplasms; vaginismus Frequency not known With oral use Carbohydrate metabolism change; cerebrovascular insufficiency; epilepsy exacerbated; hypertriglyceridaemia; increased risk of coronary artery disease; myocardial infarction; neoplasms; pancreatitis; systemic lupus erythematosus (SLE) With vaginal use Embolism and thrombosis Side-effects, further information Cyclical HRT (where a progestogen is taken for 12-14 days of each 28-day oestrogen treatment cycle) usually results in regular withdrawal bleeding towards the end of the progestogen. Continuous combined HRT commonly produces irregular breakthrough bleeding in the first 4-6 months of treatment. Bleeding beyond 6 months or after a spell of amenorrhoea requires further investigation to exclude serious gynaecological pathology.
Interactions
**Severe interactions:**
- Pharmacodynamic interactions During clinical trials with the HCV combination drug regimen ombitasvir/paritaprevir/ritonavir and dasabuvir with or without ribavirin, ALT elevations greater than 5...
- Estrogen-containing oral contraceptives have been shown to significantly decrease plasma concentrations of lamotrigine when co-administered due to induction of lamotrigine glucuronidation.
**Other interactions (5):**
- The metabolism of oestrogens (and progestogens) may be increased by concomitant use of substances known to induce drug-metabolising enzymes, specifically cytochrome P450 enzymes, such as...
- Ritonavir and nelfinavir, although known as strong inhibitors, by contrast exhibit inducing properties when used concomitantly with steroid hormones.
- Women using medicinal products containing oestrogens other than ethinylestradiol, such as estradiol, and ombitasvir/paritaprevir/ritonavir and dasabuvir with or without ribavirin had a rate of ALT...
- Although the potential interaction between estrogen-containing hormone replacement therapy and lamotrigine has not been studied, it is expected that a similar interaction exists, which may lead to a...
- Therefore, dose adjustment of lamotrigine may be necessary.
Pregnancy
Not known to be harmful.
Breast feeding
Avoid; adverse effects on lactation.
Hepatic impairment
Manufacturer advises caution; avoid in acute or active disease.
Medicinal forms
Tablet,Pessary,Gel,Patch,Spray
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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