Raloxifene Hydrochloride

Indications

Raloxifene Hydrochloride is used for: Post-menopausal osteoporosis, Malignant gastrointestinal stromal tumours, Prevention & risk reduction of invasive breast cancer

Adult Dose

Oral Prophylaxis of postmenopausal osteoporosis; Osteoporosis in postmenopausal women Adult: 60 mg once daily. Breast Cancer Prevention; risk reduction of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer 60 mg PO qDay for 5 years Hepatic impairment: Contraindicated.

Child Dose

Renal Dose

Renal impairment: Severe: Contraindicated.

Administration

May be taken with or without food.

Contra Indications

Active or history of venous thromboembolic events including DVT, pulmonary embolism, retinal vein thrombosis. Unexplained uterine bleeding. Patients w/ signs/symptoms of endometrial cancer. Hepatic (including cholestasis) and severe renal impairment. Pregnancy, women who may become pregnant, and lactation.

Precautions

Women w/ risk factors for venous thromboembolism including CHF or active malignancy, risk factors for stroke (e.g. TIA, AF), history of oestrogen-induced hypertriglyceridaemia. Moderate renal impairment. Monitoring Parameters Monitor serum triglyceride concentration. Lactation: Excretion in milk unknown; contraindicated

Pregnancy-Lactation

Pregnancy Category: X Lactation: Excretion in milk unknown; contraindicated

Interactions

Cholestyramine reduces the absorption of raloxifene. Raloxifene with warfarin may reduce the prothrombin response and time. Caution when used in hghly protein-bound drugs such as diazepam, lidocaine and diazoxide.

Adverse Effects

Side effects of Raloxifene Hydrochloride : >10% Hot flashes (8-29%), Flu syndrome (14-15%), Cramps/muscle spasm (6-12%), Arthralgia (11-16%), Infection (11%) 1-10% Insomnia (6%), Vomiting (5%), Sinusitis (10%), Venous thromboembolism (1-2% ), Bronchitis (10%), Pharyngitis (8%), Breast pain (4%), Gastroenteritis (<3%), Diaphoresis (3%) Frequency Not Defined Deep vein thrombosis, Cerebrovascular accident, Thrombosis of retinal vein (rare), Pulmonary embolism, Decreased fibrinogen

Mechanism of Action

Raloxifene is a selective oestrogen receptor modulator that has both selective agonist or antagonist activities on oestrogen receptors. It acts as an agonist on bone by preventing bone loss and partially on cholesterol metabolism by decreasing total and LDL cholesterol levels but antagonises oestrogen effects leading to development of breast and uterine cancer.