Raloxifene

Indications
Oral
Prophylaxis of postmenopausal osteoporosis
Adult: 60 mg daily.
Contraindications
Hypersensitivity; active or past history of venous thromboembolic events including DVT, pulmonary embolism and retinal vein thrombosis; hepatic and severe renal impairment. Pregnancy, lactation.
Warnings / Precautions
CHF or active malignancy; history of oestrogen-induced hypertriglyceridaemia; renal insufficiency.
Adverse Reactions
Hot flushes, leg cramps, sweating, sleep disorders, peripheral oedema, vag bleeding; flu-like symptoms, rashes, GI disturbances, hypertension, headache, sinusitis, arthralgia.
Potentially Fatal: Endometrial carcinoma and thromboembolic events.
Overdose Reactions
May cause leg cramps and dizziness.
Drug 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.
See Below for More raloxifene Drug Interactions
Mechanism of Actions
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.
Absorption: Well absorbed from the GI tract (oral).
Distribution: Protein-binding: Extensive to albumin and α1-acid glycoprotein.
Metabolism: Extensively hepatic; converted to glucuronide conjugates; undergoes enterohepatic recycling.
Excretion: Faeces; 27 hr (elimination half-life).
Administration
May be taken with or without food.
Storage Conditions
Oral: Store at 15-30°C.
ATC Classification
G03XC01 - raloxifene ; Belongs to the class of selective estrogen receptor modulators.
Storage
Oral: Store at 15-30°C.
Available As
  • Raloxifene 60 mg
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