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Raloxifene

Raloxifene, sold under the brand name Evista among others, is a medication which is used in the prevention and treatment of osteoporosis in postmenopausal women and to reduce the risk of breast cancer in postmenopausal women with osteoporosis or at high risk for breast cancer. More

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Description

Raloxifene, sold under the brand name Evista among others, is a medication which is used in the prevention and treatment of osteoporosis in postmenopausal women and to reduce the risk of breast cancer in postmenopausal women with osteoporosis or at high risk for breast cancer.

Generic Name

Raloxifene

Chemical names

RALOXIFENE HYDROCHLORIDE; 82640-04-8; Raloxifene Hcl; Evista; Keoxifene hydrochloride

Brand names

Bonmax, Bontact, Esserm, Estroact, Evomate, Fiona, Gynista, Osral, Ralista, Ralocium, Ralofen, Ralosto, Ralotab, Ralox, Raloxifene, Ruftuf, Strong Kit

IUPAC name

2-(4-hydroxyphenyl)-3-{4-[2-(piperidin-1-yl)ethoxy]benzoyl}-1-benzothiophen-6-ol

Pharmacokinetics

  • Oral absorption 60%
  • 95% protein binding
  • Hepatic metabolism

Actions

 It produces estrogen-like effects on bone and lipid metabolism, while antagonizing the effects of estrogen on breast and uterine tissue. It is a SERM (selective estrogen receptor modulator).

Dosage/Dosage form

60 mg daily oral.

Therapeutic uses

For the prevention and treatment of osteoporosis in post-menopausal women, as well as prevention and treatment of corticosteroid-induced bone loss. Also for the reduction in the incidence of invasive breast cancer in postmenopausal women with osteoporosis or have a high risk for developing breast cancer.

Adverse effects/Side effects

Hot flushes, leg cramps, sweating, sleep disorders, peripheral oedema, vag bleeding; flu-like symptoms, rashes, GI disturbances, hypertension, headache, sinusitis, arthralgia.

Interaction

  • Cholestyramine reduces the absorption of raloxifene.
  • Caution when used in hghly protein-bound drugs such as diazepam, lidocaine and diazoxide.
  • Warfarin may reduce the prothrombin response and time with raloxifene.

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

Store at 15-30°C

Information

Molecular weight

473.583

Molecular formula

C28H27NO4S

CAS number

84449-90-1

Precautions

  • Renal insufficiency.
  • History of oestrogen-induced hypertriglyceridaemia;
  • CHF or active malignancy;