raloxifene hydrochloride: clinical use

Prescribing considerations

• Confirm postmenopausal status and balance vertebral-fracture benefit against venous thromboembolism and cardiovascular risks.
• Assess previous VTE, stroke or transient ischaemic attack, atrial fibrillation and other major stroke risk factors.
• Interrupt treatment for illness or circumstances causing prolonged immobilisation; plan interruption before predictable immobilisation and restart only when fully mobile.
• Investigate any uterine bleeding during treatment, as bleeding is unexpected.
• Use for osteoporosis after breast-cancer treatment, including adjuvant therapy, has been completed.

Contraindications and cautions

• Hypersensitivity to raloxifene or an excipient
• Women of childbearing potential
• Active or previous venous thromboembolism, including deep-vein, pulmonary or retinal-vein thrombosis
• Hepatic impairment, including cholestasis
• Severe renal impairment
• Unexplained uterine bleeding
• Signs or symptoms of endometrial cancer

Monitoring

• Monitor anticoagulation when used with warfarin or another coumarin.
• Monitor triglycerides in patients with previous marked hypertriglyceridaemia caused by oral oestrogen.
• Closely monitor liver tests if bilirubin or liver enzymes become elevated.
• Arrange specialist investigation of uterine bleeding and reassess promptly if symptoms suggest thrombosis.

Clinical pharmacology

Raloxifene is a SERM with tissue-selective agonist and antagonist effects at oestrogen receptors. It reduces bone resorption through agonist activity in bone, undergoes extensive glucuronidation and enterohepatic recycling, and is highly protein bound.

Formulation and product differences

• The selected product is a white, elliptical film-coated tablet intended to be swallowed whole.
• It contains lactose monohydrate and is essentially sodium-free.
• Blisters should be kept in the outer carton to protect them from light and moisture; do not freeze.

Tablet

Route: Oral

Strengths: 60 mg