Toremifene Citrate
A to Z Drug Facts
Toremifene Citrate |
(TORE-EM-ih-feen) |
Fareston |
Oral tablets |
60 mg |
Class: Antiestrogen hormone |
Actions A nonsteroidal antiestrogen that blocks the growth-stimulating effects of estrogen in the tumor. Absorption is not influenced by food. It binds extensively (> 99.5%) to serum proteins. It is extensively metabolized, principally by CYP3A4. Elimination half-life is » 5 days.
Indications Metastatic breast cancer in postmenopausal women.
Contraindications Standard considerations.
Breast Cancer
ADULTS: PO 60 mg once daily with or without food.
Anticonvulsants
May increase toremifene clearance by 2-fold.
CYP3A4
Toremifene may be altered by drugs that inhibit (eg, ketoconazole, itraconazole, macrolides) or induce (eg, phenobarbital, phenytoin, carbamazepine) this enzyme.
Thiazide diuretics
May cause hypercalcemia with agents that reduce renal excretion of calcium.
Warfarin
May increase the hypoprothrombinemic effect of warfarin.
Lab Test Interferences None well documented.
CARDIOVASCULAR: Edema; pulmonary embolism; thrombophlebitis; thrombosis; cerebrovascular accident; transient ischemic attack; cardiac failure; MI. CNS: Dizziness. ENDOCRINE: Hot flashes; sweating. GI: Nausea and vomiting; elevated LFTs. GU: Vaginal discharge; vaginal bleeding; endometrial thickening. METABOLIC: Hypercalcemia. MUSCULOSKELETAL: Bone and tumor pain at initiation of therapy; soft tissue lesions can temporarily increase in size. SPECIALSENSES: Cataracts; dry eyes; abnormal visual fields; corneal keratopathy; glaucoma; abnormal vision; diplopia.
Pregnancy: Category D. Lactation: Undetermined. Children: Safety and efficacy not established. Hypercalcemia and tumor flare: Drugs that decrease renal calcium excretion (eg, thiazide diuretics) may increase the risk of hypercalcemia in patients receiving toremifene. Hepatic dysfunction: Metabolized in the liver; dose reduction may be necessary in patients with liver disease. Thromboembolic disease: Caution in patients with thromboembolic diseases. Preexisting endometrial hyperplasia: Avoid long-term use.
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Copyright © 2003 Facts and Comparisons
David S. Tatro
A to Z Drug Facts