Classifications: antineoplastic; hormone, antiestrogen; Therapeutic: antineoplastic; antiestrogen
Pregnancy Category: D
60 mg tablets
Nonsteroidal antiestrogen chemical derivative of tamoxifen. Antitumor activity thought to be due to ability to compete with
estrogen for binding sites in the cancer cells.
Depresses growth in estrogen receptorpositive tumors in postmenopausal women.
Metastatic breast cancer in postmenopausal women who are estrogen receptor positive.
Hypersensitivity to toremifene; history of thromboembolic disease; pregnancy (category D); lactation.
Preexisting endometrial hyperplasia; bone metastases (may result in hypercalcemia); geriatric patients; leukopenia and thrombocytopenia;
liver disease; history of thrombolytic disease.
Route & Dosage
Adult: PO 60 mg q.d.
- Withhold drug and notify physician if severe hypercalcemia develops.
- Store at 15°30° C (59°86° F) in a tightly closed container and protect from light.
Adverse Effects (≥1%) Body as a Whole: Hot flashes, sweating,
Dizziness. GI: Nausea,
vomiting, abnormal liver function tests. Respiratory: Pulmonary embolism. Urogenital: Vaginal discharge,
vaginal bleeding. Special Senses:
Cataracts, dry eyes, corneal keratopathy.
InteractionsDrug: thiazide diuretics
increase risk of hypercalcemia; increased PT on warfarin; carbamazepine, phenobarbital, phenytoin
may increase toremifene metabolism
Rapidly absorbed from GI tract. Peak:
3 h. Distribution:
>99% protein bound; crosses placenta. Metabolism:
In liver by cytochrome P450 3A4. Elimination:
Primarily in feces. Half-Life:
Assessment & Drug Effects
- Lab tests: Periodically monitor CBC with differential, serum calcium, liver and kidney functions.
- Monitor patients carefully with bone metastases or those on drugs that decrease calcium excretion (e.g., thiazide diuretics)
for S&S of hypercalcemia (see Appendix F).
- Monitor PT and INR carefully when given concurrently with warfarin.
Patient & Family Education
- Report to physician promptly any of the following: Unexplained weakness or fatigue, musculoskeletal pain or calf pain and
tenderness, sudden chest pain, vaginal bleeding.
- Schedule periodic eye exams with long-term therapy.