Raloxifene


Full Generic Medicine Info
Dosage/Direction for Use

Oral
Prophylaxis of postmenopausal osteoporosis, Osteoporosis in postmenopausal women
Adult: 60 mg once daily.
Renal impairment: Severe: Contraindicated.
Hepatic impairment: Contraindicated.
Administration
May be taken with or without food.
Contraindications
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.
Special 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.
Adverse Reactions
Hot flushes, flu-like syndrome, leg cramps, peripheral oedema, sweating, arthralgia. Rarely, GI disturbances, rashes, thrombocytopenia, increased BP, headache including migraine, mild breast symptoms (e.g. tenderness, pain, enlargement).
Potentially Fatal: Venous thromboembolic events (including DVT, pulmonary embolism, retinal vein thrombosis), stroke.
Drug Interactions
Reduced absorption and enterohepatic recycling w/ colestyramine. May reduce efficacy of warfarin.
Action
Raloxifene is a selective oestrogen receptor modulator that has 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 not in the hypothalamus or in the breast or uterine tissues.
Onset: 8 wk.
Absorption: Absorbed from the GI tract. Bioavailability: Approx 2%.
Distribution: Extensively distributed in the body. Volume of distribution: 2,348 L/kg. Plasma protein binding: >95% (mainly to albumin and α1-acid glycoprotein).
Metabolism: Undergoes extensive first-pass hepatic metabolism to glucuronide conjugates; undergoes enterohepatic recycling.
Excretion: Mainly via faeces; urine (<0.2% as unchanged drug; <6% as glucuronide conjugates). Half-life: Approx 27 hr.
Storage
Oral: Store between 20-25°C.
CIMS Class
Agents Affecting Bone Metabolism
ATC Classification
G03XC01 - raloxifene ; Belongs to the class of selective estrogen receptor modulators.
Disclaimer: This information is independently developed by CIMS based on raloxifene from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 CIMS. All rights reserved. Powered by CIMSAsia.com
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