Raloxifene

Registered South African indications: 

• Osteoporosis

Contraindications

• Hypersensitivity to the active ingredient or to any of its excipients
• Pregnancy
• Breastfeeding
• Severe renal impairment
• Hepatic impairment
• Women of child-bearing potential
• Porphyria
• Active or past history of venous thromboembolism
• Unexplained uterine bleeding
• Suspected endometrial cancer

Cautions

• Mild to moderate renal impairment
• History of or risk factors for stroke
• Risk factors for venous thromboembolism
• Atrial fibrillation
• Transient ischaemic attack
• Oestrogen-induced hypertriglyceridaemia
• Breast cancer
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: tab

Prevention and treatment of osteoporosis
To reduce the risk of development of invasive breast cancer in post-menopausal women with osteoporosis 

• Oral (tab): 60mg, dly

 Calcium and vitamin D supplements are advised in women with a low dietary intake

Not established for use in children

Pregnancy

• Contraindicated
• Raloxifene hydrochloride is only for use in postmenopausal women 4
• Raloxifene hydrochloride must not be taken by women of childbearing potential
• Raloxifene is an oestrogen antagonist in uterine tissue and oestrogen is required to maintain pregnancy
• Raloxifene may cause foetal harm when administered to a pregnant woman. If this medicinal product is used mistakenly during pregnancy or if the patient becomes pregnant while taking it, the patient should be informed of the potential hazard to the foetus
• Reproduction studies have been performed in rats and rabbits. In rats, doses that were > 0.2 times the human dose based on BSA (HD) caused retarded foetal development and developmental abnormalities (wavy ribs and kidney cavitation)

Breastfeeding

• Contraindicated
• It is unknown whether raloxifene metabolites are excreted in human milk 4
• A risk to the newborn/infant cannot be excluded. Its clinical use, therefore, cannot be recommended in breastfeeding women
• Raloxifene hydrochloride may affect the development of the baby
• Raloxifene is an oestrogen antagonist in breast tissue. The manufacturer warned against the use of raloxifene during breastfeeding and it was labelled as contraindicated during breastfeeding

Renal Impairment

• Mild to moderate: Caution; no dose adjustment recommended
• Severe: Contraindicated

Hepatic Impairment

• Contraindicated

Elderly

• No dose adjustment recommended

Porphyria Information

• Probably porphyrinogenic (PRP)

Drugs in Sport

• Prohibited - At all times

Central Nervous System Disorders

• Headache
• Cerebrovascular accident
• Migraine

Cardiovascular Disorders

• Vasodilation
• Increased blood pressure
• Venous thromboembolic events
• Pulmonary embolism
• Retinal vein thrombosis
• Superficial vein thrombophlebitis
• Arterial thromboembolic reactions

Gastrointestinal Disorders

• Nausea and vomiting
• Abdominal pain
• Dyspepsia

Genitourinary Disorders

• Breast enlargement
• Breast tenderness

Musculoskeletal Disorders

• Leg cramps

Skin and Subcutaneous Tissue Disorders

• Rash
• Peripheral oedema

Immune, Blood and Lymphatic System Disorders

• Thrombocytopenia
• Flu syndrome

• Hormone replacement therapy
• Systemic oestrogens
• Cholestyramine
• Warfarin
• Ampicillin

• Mammogram
• Breast examination
• Bone mineral density

Specific cases may require: 

• Hepatic function
• Serum triglycerides
• Electrolytes
• Prothrombin time

Raloxifene is a selective oestrogen receptor modulator, that has selective agonist or antagonist activities on tissues responsive to oestrogen. It acts as an agonist on bone and partially on cholesterol metabolism, but not in the hypothalamus or in the uterine or breast tissues. Raloxifene's biological actions, like those of oestrogen, are mediated through high affinity binding to oestrogen receptors and regulation of gene expression. This binding results in differential expression of multiple oestrogen-regulated genes in different tissues.

Tablet 60mg

• Evista (Eli Lilly) originator