Raloxifene

Oral
Postmenopausal osteoporosis

Oral
Reduction of breast cancer incidence in women at high risk

Severe: Contraindicated.

Contraindicated.

May be taken with or without food.

Active or history of venous thromboembolic events (e.g. DVT, pulmonary embolism, retinal vein thrombosis); unexplained uterine bleeding; patients with signs and symptoms of endometrial cancer; cholestasis. Hepatic and severe renal impairment. Women of childbearing potential, pregnant and premenopausal women; lactation.

Patient with documented coronary heart disease; risk factors for major coronary events, stroke (e.g. history of stroke, TIA, atrial fibrillation, hypertension, smoking), or thromboembolism (e.g. active malignancy, CHF, superficial thrombophlebitis); history of breast cancer and oral-estrogen induced hypertriglyceridaemia (>5.6 mmol/L or >500 mg/dL). Patients on prolonged immobilisation (e.g. post-surgical recovery, prolonged bed rest). Not indicated to be used for primary or secondary prevention of CV disease, treatment of invasive breast cancer, and risk reduction in non-invasive breast cancer. Not indicated for use in men. The safety of concomitant use with systemic estrogen therapy has not been established; concurrent use is not recommended. Mild to moderate renal impairment.

Significant: Increased serum triglycerides (particularly in patients with history of estrogen-induced hypertriglyceridaemia); vaginal bleeding.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain, dyspepsia, flatulence.
General disorders and administration site conditions: Peripheral oedema.
Investigations: Increased blood pressure, weight gain.
Musculoskeletal and connective tissue disorders: Leg cramps, arthralgia, muscle spasms, myalgia, tendinopathy.
Nervous system disorders: Headache, migraine.
Psychiatric disorders: Depression, insomnia.
Renal and urinary disorders: UTI.
Reproductive system and breast disorders: Breast pain, enlargement, or tenderness; leukorrhoea, uterine or endometrium disease.
Respiratory, thoracic and mediastinal disorders: Flu syndrome, bronchitis, sinusitis, pharyngitis, pneumonia, laryngitis.
Skin and subcutaneous tissue disorders: Rash, sweating.
Vascular disorders: Hot flushes, superficial vein thrombophlebitis.
Potentially Fatal: Increased risk of venous thromboembolic events, including DVT, pulmonary embolism, and retinal vein thrombosis; stroke.

PO: Z (Animal studies showed embryo-foetal mortality and congenital abnormalities. Contraindicated.)

For postmenopausal osteoporosis treatment or prophylaxis: Ensure adequate Ca and vitamin D intake.

Monitor mammogram and breast exam prior to and regularly during treatment; lipid profile (in patients at risk for hypertriglyceridaemia). Assess for unexplained uterine bleeding or breast abnormalities and signs or symptoms of thromboembolism. For postmenopausal osteoporosis treatment or prophylaxis: Obtain serial BMD at baseline and every 1 to 3 years; serum Ca and 25-hydroxy vitamin D; annual height or weight measurement.

Reduced absorption and enterohepatic recycling with colestyramine or other anion exchange resins. May decrease the efficacy of warfarin or other coumarin derivatives; closely monitor prothrombin time. May reduce the absorption of levothyroxine.

Description:
Mechanism of Action: Raloxifene is a selective estrogen receptor modulator (SERM) that has selective agonistic or antagonistic effects on tissues responsive to estrogen. It acts as an estrogen agonist in the bone by decreasing bone resorption and turnover, increasing bone mineral density and reducing fracture incidence. Raloxifene exerts an antagonistic activity by inhibiting some estrogen effects in the breast and uterine tissues.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Bioavailability: Approx 2%.
Distribution: Widely distributed in the body. Volume of distribution: 2,348 L/kg. Plasma protein binding: 98-99%, mainly to albumin and α₁-acid glycoprotein.
Metabolism: Undergoes extensive first-pass metabolism in the liver to form glucuronide conjugates; undergoes enterohepatic recycling.
Excretion: Mainly via faeces; urine (<0.2% as unchanged drug, <6% as glucuronide conjugates). Elimination half-life: 27.7 hours (after a single dose); 32.5 hours (after multiple doses).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5035, Raloxifene. https://pubchem.ncbi.nlm.nih.gov/compound/Raloxifene. Accessed Jan. 25, 2024.

Store between 15-30°C. Protect from excessive heat, light and moisture. Follow applicable procedures for receiving, handling, administration, and disposal.

Agents Affecting Bone Metabolism

G03XC01 - raloxifene ; Belongs to the class of selective estrogen receptor modulators.

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