toremifene

Contraindicated in:

Hypersensitivity;
History of thromboembolic disease;
Congenital or acquired QT prolongation, hypokalemia, or hypomagnesemia;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Bone metastases (↑ risk of hypercalcemia);
HF;
Hepatic impairment;
Pre-existing endometrial hyperplasia (avoid long-term treatment).

Adv. Reactions/Side Effects ⬆ ⬇

CV: angina, arrhythmias, edema, HF, MI, QT interval prolongation, thrombophlebitis, TORSADES DE POINTES

Derm: sweating

EENT: blurred vision, cataracts, corneal keratopathy, dry eyes, glaucoma

Endo: hot flashes

F and E: hypercalcemia

GI: nausea, HEPATOTOXICITY, vomiting

GU: vaginal discharge, ENDOMETRIAL CANCER, endometrial hyperplasia/hypertrophy, uterine polyps, vaginal bleeding

Hemat: anemia

Neuro: depression, dizziness, headache, lethargy

Resp: PULMONARY EMBOLISM

Misc: tumor flare

Interactions ⬆ ⬇

Drug-drug:

QT interval prolonging drugs may ↑ risk of torsades de pointes; avoid concurrent use.
Strong CYP3A4 inhibitors, including ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, nelfinavir, ritonavir, and voriconazole, may ↑ levels and risk of toxicity; avoid concurrent use.
Strong CYP3A4 inducers, including dexamethasone, phenytoin, carbamazepine, rifampin, rifabutin, and phenobarbital, may ↓ levels and effectiveness.
Concurrent use of agents that urinary excretion of calcium (thiazide, diuretics) may ↑ risk of hypercalcemia.
May ↑ effects of warfarin and phenytoin.

Drug-Natural Products:

St. John's wort may ↓ levels and effectiveness.

Availability ⬆ ⬇

(Generic available)

Tablets: 60 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 60 mg once daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Exerts antiestrogenic effects by competing for estrogen-binding sites found in breast cancers.

Therapeutic effects:

Regression of breast cancer.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: antiestrogens

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration.

Distribution: Widely distributed to tissues.

Protein Binding: 99.5%.

Metabolism/Excretion: Extensively metabolized; undergoes enterohepatic circulation.

Half-Life: 5 days.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	3 hr	4–6 wk‡

‡Steady-state plasma concentrations occur after 4–6 wk.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient to take as directed. If a dose is missed, take as soon as remembered. If close to the time for the next dose, skip the missed dose and go back to scheduled time. Do not take two doses at the same time or extra doses.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Advise patient to report bone pain to health care professional promptly. Pain may be severe. Inform patient this may be an indication of the drug’s effectiveness and will resolve over time. Analgesics should be ordered to control pain.
Advise patient that medication may cause hot flashes. Notify health care professional if these become bothersome.
Instruct patient to notify health care professional promptly if pain or swelling of legs, shortness of breath, weakness, sleepiness, confusion, nausea, vomiting, dizziness, headache, loss of appetite, or blurred vision occurs. Patient should also report menstrual irregularities, vaginal bleeding, or pelvic pain or pressure.
May cause vaginal bleeding. Advise patient of importance of baseline and annual gynecological exams during therapy and to notify health care professional if vaginal bleeding, changes in vaginal discharge, or pelvic pain or pressure occur.
Advise patient to avoid grapefruit and grapefruit juice.
Rep: May cause fetal harm. May also induce ovulation. Advise patient to use a nonhormonal method of contraception during therapy and for 1 mo after the course of therapy and to avoid breastfeeding during therapy.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇