Products
Raloxifene is commercially available in the form of film-coated tablets (Evista). It has been approved in many countries since 2000.
Structure and properties
Raloxifene (C28H27NO4S, Mr = 473.6 g/mol) is present in the drug as raloxifene hydrochloride, a benzothiophene and white to yellowish powder that is sparingly soluble in water.
Effects
Raloxifene (ATC G03XC01) is a SERM with selective agonistic and antagonistic effects on estrogen-sensitive tissues:
- Agonistic effects on bone and partially on cholesterol metabolism.
- Antagonistic effect on breast and uterine tissue.
Indications
For the prevention and treatment of osteoporosis in postmenopausal women. In the United States, it is additionally approved for the prevention of breast cancer.
Abuse
Raloxifene can be abused as a doping agent.
Dosage
According to the SmPC. Tablets are taken once daily, regardless of meals and at the same time of day.
Contraindications
- Hypersensitivity
- Childbearing women
- Current or previous venous thromboembolic events.
- Impaired liver function
- Cholestasis
- Severe renal insufficiency
- Unexplained uterine bleeding
- Endometrial cancer
Full precautions can be found in the drug label.
Interactions
Drug-drug interactions have been observed with vitamin K antagonists and cholestyramine. Other interactions are possible due to high protein binding.
Adverse effects
The most common possible adverse effects include flu-like symptoms, vasodilatation, flushing, gallstone disease, peripheral edema, calf cramps, liver and biliary disorders, and superficial phlebitis. Rarely, venous and arterial thromboembolic events are possible.
