Raloxifene Hydrochloride

Raloxifene is an estrogen agonist/antagonist indicated for:

• Treatment and prevention of osteoporosis in postmenopausal women
• Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis
• Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer

Important Limitations: Raloxifene is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer

Raloxifene is a selective estrogen receptor modulator (SERM). The biological actions of Raloxifene are largely mediated through binding to estrogen receptor. This binding results in activation of certain estrogenic pathways and blockade of others. Raloxifene reduces resorption of bone and decreases overall bone turnover. These effects on bone are manifested as reductions in the serum and urine levels of bone turnover markers. Clinical trials and data suggest that Raloxifene lacks estrogen like effects on the uterus and breast tissues. Raloxifene is rapidly absorbed after oral administration, metabolized in liver, and primarily excreted in faeces and rest in urine.

One tablet (60 mg) once daily orally. It can be taken without regard to meal. High fat meal increases the absorption of Raloxifene.

Co-administered with cholestyramin, ampicillin and amoxicillin may reduce the absorption of Raloxifene.

Hepatic & renal impairment. In active or past history of venous thromboembolic events, including deep vein thrombosis, pulmonary embolism and retinal vein thrombosis. Hypersensitivity to Raloxifene or any other constituents of the tablet.

Raloxifene is generally well tolerated. However, a few side effects like hot flushes, leg cramps, and influenza like symptoms, gastro-intestinal disturbances etc may be seen usually during first 6 months of treatment and were not different from placebo.

Pregnancy Category X: Raloxifene should not be used in women who are or may become pregnant.
Lactation: It is not known whether Raloxifene is excreted in breast milk. Lactating mother should not use Raloxifne.

Concurrent Estrogen Therapy: Concomitant use of Raloxifene with systemic estrogens is not recommended.

Lipid Metabolism: Concurrent use of Raloxifene and lipid-lowering agents has not been studied.

Incidents of overdose in humans have not been reported.

Inhibiting bone resorption.

Severe Renal Impairment: Contraindicated.
Hepatic Impairment: Contraindicated.