Generic
Raloxifene Hydrochloride
3 brands available in the market
At a glance
Raloxifene Hydrochloride is a selective estrogen receptor modulator (SERM) used for prevention and treatment of osteoporosis in postmenopausal women. It prevents bone loss, strengthens bones, and lowers the risk of fractures.
Description
Raloxifene is a selective estrogen receptor modulator with selective agonist or antagonist activities on estrogen receptors. It acts as an agonist on bone (preventing bone loss) and partially on cholesterol metabolism (decreasing total and LDL cholesterol), but antagonizes estrogen effects leading to development of breast and uterine cancer.
Indications
- Prophylaxis of postmenopausal osteoporosis
- Osteoporosis in postmenopausal women
- Risk reduction of invasive breast cancer in high-risk postmenopausal women
Therapeutic class
Hormone Therapy (SERM)
Pharmacological class
Selective Estrogen Receptor Modulator (SERM)
Pharmacology
Raloxifene is a SERM with selective agonist and antagonist activities on estrogen receptors. It exerts estrogen-like effects on bone to prevent bone loss and reduces cholesterol, but acts as an antagonist in breast and uterine tissues, reducing cancer risk.
Mechanism of action
Prevents bone loss by exerting estrogen-like effects on bone.
Dosage
Adult Dose (Oral):
- Osteoporosis prophylaxis/treatment: 60 mg once daily
- Breast cancer prevention (high risk): 60 mg once daily for 5 years
- Severe hepatic/renal impairment: Contraindicated
Administration
- May be taken with or without food; take at a fixed time
- Swallow tablet whole; do not chew, crush, or break
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Hot flashes
- Leg cramps
- Peripheral edema
- Flu-like symptoms
- Joint pain
- Sweating
Precautions & warnings
- Does not usually affect driving ability
- Inform doctor if you have cancer, heart failure, kidney disease, high triglycerides, or liver disease
- Inform doctor if on estrogen therapy
- Discontinue if lumps in breast, signs of stroke, chest pain, sudden cough, leg pain/swelling occur
- Avoid prolonged sitting
- Inform doctor if vaginal bleeding occurs
Contraindications
- Active or history of venous thromboembolic events (DVT, pulmonary embolism, retinal vein thrombosis)
- Unexplained uterine bleeding
- Signs/symptoms of endometrial cancer
- Hepatic (including cholestasis) and severe renal impairment
- Pregnancy and lactation
Drug interactions
- Cholestyramine: Reduces raloxifene absorption
- Warfarin: Reduces prothrombin response and time
- Highly protein-bound drugs (diazepam, lidocaine, diazoxide): Caution
Food interactions
Caution is advised when consuming alcohol with Raloxifene Hydrochloride.
Use in pregnancy
Use in Pregnancy: Highly unsafe during pregnancy; significant harmful effects to the developing baby; do not use.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unsafe during breastfeeding; may cause toxicity to the baby; do not use.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
No dose adjustment required for elderly patients.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose adjustment may be needed; not recommended in severe kidney disease; consult your doctor.
Hepatic Impairment: Probably unsafe in liver disease and should be avoided; contraindicated; consult your doctor.
Overdose effects
No overdose information available; consult your doctor if taken in excess.
Storage conditions
Store in a cool and dry place; keep out of reach of children.
Chemical structure
Raloxifene Hydrochloride