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Toremifene citrate
Toremifene citrate (Fareston)
Toremifine citrate
(TOR-em-ih-feen)
Pregnancy Category: D Fareston (Rx)

Classification: Antineoplastic, hormone

See Also: See also Antineoplastic Agents.

Action/Kinetics: Antiestrogen that binds to estrogen receptors and may cause estrogenic, antiestrogenic, or both effects, depending on duration of treatment, genders, and endpoint/target organ selected. Antitumor effect is likely due to antiestrogenic effect, i.e., competes for estrogen at receptor and blocks growth-stimulating effects of estrogen in tumor. Well absorbed from GI tract. Peak plasma levels: 3 hr. t1/2, distribution: About 4 hr. t1/2, elimination: About 5 days. Extensively metabolized in liver and mainly excreted in feces.

Uses: Metastatic breast cancer in postmenopausal women with positive estrogen-receptor (ER) or ER unknown tumors.

Contraindications: Use with history of thromboembolic disease or in pediatric clients.

Special Concerns: Hypercalcemia and tumor flare in some breast cancer clients with bone metastases during first weeks of treatment. Use with caution during lactation.

Side Effects: CV: Cardiac failure, MI, pulmonary embolism, CVA TIA. GI: Constipation, nausea. Hematologic: Leukopenia, thrombocytopenia. Dermatologic: Skin discoloration, dermatitis, alopecia, pruritus. Ophthalmic: Cataracts, dry eyes, abnormal visual fields, corneal keratopathy, glaucoma, reversible corneal opacity. CNS: Tremor, vertigo, depression. Miscellaneous: Dyspnea, paresis, anorexia, asthenia, jaundice, rigors, vaginal bleeding.

Laboratory Test Alterations: AST, alkaline phosphatase, bilirubin. Hypercalcemia.

Overdose Management: Symptoms: Vertigo, headache, dizziness. Possibly, hot flashes, vaginal bleeding, vertigo, dizziness, ataxia, nausea. Treatment: General supportive measures.

Drug Interactions: Carbamazepine / Toremifene blood levels R/T liver breakdown Clonazepam / Toremifene blood levels R/T liver breakdown Erythromycin / Inhibition of toremifene breakdown Ketoconazole / Inhibition of toremifene breakdown Macrolide antibiotics / Inhibition of toremifene breakdown Phenobarbital / Toremifene blood levels R/T liver breakdown Phenytoin / Toremifene blood levels R/T liver breakdown Warfarin / PT