drospirenone + estradiol hemihydrate: clinical use

Prescribing considerations

• Confirm symptoms adversely affect quality of life and periodically review the individual benefit–risk balance.
• Assess cancer, thromboembolic, cardiovascular, migraine, liver, renal and unexplained-bleeding history.
• Consider route-specific risk factors because oral HRT increases venous-thromboembolism and stroke risk compared with transdermal oestrogen.
• Review planned major surgery or prolonged immobilisation in advance.
• The tablet contains lactose and is unsuitable for specified rare hereditary disorders of galactose handling.

Contraindications and cautions

• Undiagnosed genital bleeding or untreated endometrial hyperplasia
• Known, previous or suspected breast cancer, or known or suspected oestrogen-dependent malignancy
• Current or previous venous thromboembolism, known thrombophilia, or active or recent arterial thromboembolic disease
• Acute liver disease or unresolved abnormal liver function following liver disease
• Severe renal insufficiency or acute renal failure
• Porphyria or hypersensitivity to an ingredient

Monitoring

• Review symptom response, adverse effects and benefit–risk balance periodically.
• Investigate persistent, heavy or newly recurring vaginal bleeding.
• Support routine breast screening and assess reported breast changes.
• Monitor blood pressure and liver function where clinically indicated.
• Selectively check serum potassium in renal impairment with high-normal baseline potassium, especially with potassium-raising medicines.

Clinical pharmacology

Estradiol replaces endogenous oestrogen and undergoes extensive first-pass metabolism after oral absorption. Drospirenone is an albumin-bound synthetic progestogen with antimineralocorticoid activity and is extensively metabolised, including through CYP3A4.

Formulation and product differences

• The fixed oral combination does not allow its hormonal components to be adjusted independently.
• Food does not materially alter absorption.
• It contains lactose and requires no special storage conditions.

Tablet

Route: Oral

Strengths: 1 mg + 2 mg