See Available Brands of Raloxifene in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation

Raloxifene is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women. Raloxifene is manufactured by Eli Lilly and Company and is sold under the brand name Evista.

Pharmacodynamics

Pharmacokinetics

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 hours (elimination half-life).

Raloxifene Indications / Raloxifene Uses

Information Not Available

Raloxifene Adverse Reactions / Raloxifene Side Effects

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.

Precautions

Warnings
Venous thrombosis
Increased risk of DVT and pulmonary embolism have been reported. Women with active or past history of venous thrombosis should not take raloxifene.

Stroke
The risk of death due to stroke may be increased in postmenopausal women with documented coronary heart disease or at increased risk of major coronary events.

Monitor
Monitor triglyceride plasma levels in women with a history of marked hypertriglyceridemia in response to treatment with oral estrogen or estrogen plus progestin.

Overdosage
May cause leg cramps and dizziness.

Special Precautions

CHF or active malignancy; history of oestrogen-induced hypertriglyceridaemia; renal insufficiency.

Other 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.

Other Interactions

Information Not Available

Dosage

Oral
Prophylaxis of postmenopausal osteoporosis
Adult: 60 mg daily.

Food(before/after)

May be taken with or without food

List of Contraindications

Raloxifene and Pregnancy

Contraindicated in pregnancy

Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Raloxifene and Lactation

Contraindicated in lactation

Raloxifene and Children

Safety and efficacy not established

Raloxifene and Geriatic

No overall differences in safety and efficacy have been reported between patients older than 65 years of age and younger subjects.

Raloxifene and Other 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.

Storage

Oral
Store at 15-30°C

Lab interference

Information Not Available