tamoxifen citrate


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tamoxifen citrate

Apo-Tamox, Gen-Tamoxifen, Nolvadex, Nolvadex-D, Novo-Tamoxifen, PMS-Tamoxifen, Soltamox, Tamofen

Pharmacologic class: Nonsteroidal antiestrogen

Therapeutic class: Antineoplastic

Pregnancy risk category D

FDA Box Warning

For women with ductal carcinoma in situ or high risk of breast cancer, serious and life-threatening events associated with drug use in riskreduction setting include stroke, pulmonary embolism, and uterine cancer. Some of these events were fatal. Discuss potential benefits versus potential risks of these events with these patients. In women already diagnosed with breast cancer, drug's benefits outweigh risks.

Action

Competes with estrogen receptors in tumor cells for binding to target tissues (such as breast); reduces DNA synthesis and estrogen response

Availability

Oral solution: 10 mg/5 ml

Tablets: 10 mg, 20 mg

Tablets (enteric-coated): 20 mg

Indications and dosages

Adjunctive treatment of breast cancer

Adults: 20 to 40 mg P.O. daily for 5 years. Daily dosages of 20 mg may be taken as a single dose; daily dosages above 20 mg should be divided and taken b.i.d. (morning and evening).

To reduce breast cancer incidence in high-risk women; treatment of ductal carcinoma in situ

Adults: 20 mg P.O. daily for 5 years

Off-label uses

• Mastalgia

• Ovulation stimulation

Contraindications

• Hypersensitivity to drug

• Concurrent warfarin use

• Women with a history of deep-vein thrombosis or pulmonary embolism

• Pregnancy or breastfeeding

Precautions

Use cautiously in:

• decreased bone marrow reserve, leukopenia, thrombocytopenia, cataracts, hyperlipidemia

• females of childbearing age.

Administration

• Don't break or crush enteric-coated tablets.

• Know that drug is indicated for reducing breast cancer risk only in high-risk women, defined as those older than age 35 who have at least a 1.67% chance of developing breast cancer over 5 years.

Adverse reactions

CNS: confusion, depression, headache, weakness, fatigue, light-headedness

CV: chest pain, deep-vein thrombosis

EENT: blurred vision, ocular lesion, retinopathy, corneal opacity

GI: nausea, vomiting, abdominal cramps, anorexia

GU: vaginal bleeding, discharge, or dryness; irregular menses; amenorrhea; oligomenorrhea; ovarian cyst; pruritus vulvae; endometrial or uterine cancer

Hematologic: leukopenia, thrombocytopenia

Metabolic: hypercalcemia, fluid retention

Musculoskeletal: bone pain

Respiratory: cough, pulmonary embolism

Skin: skin changes, hair thinning or partial hair loss

Other: altered taste, weight loss, tumor flare, tumor pain, hot flashes, edema

Interactions

Drug-drug. Aminoglutethimide, estrogens: decreased tamoxifen effects

Antineoplastics: increased risk of thromboembolic events

Bromocriptine: increased tamoxifen blood level

Warfarin: increased anticoagulant effect

Drug-diagnostic tests. Aspartate aminotransferase, bilirubin, calcium, creatinine, hepatic enzymes: increased levels

Platelets, white blood cells: decreased counts

Patient monitoring

• Monitor lipid panel, calcium level, mammography results, and gynecologic exam results.

Watch for signs and symptoms of thromboembolic events, including cerebrovascular accident and pulmonary embolism.

• Monitor menstrual cycle pattern for changes that may signal endometrial or uterine cancer.

Patient teaching

• Tell patient to swallow enteric-coated tablets whole without breaking or crushing.

Instruct patient to immediately report leg or calf pain, swelling, or tenderness; unexpected shortness of breath; sudden chest pain; coughing up blood; new breast lumps; vaginal bleeding; menstrual irregularities; changes in vaginal discharge; pelvic pain or pressure; and vision changes.

• Inform patient that increase in bone or tumor pain usually means drug will be effective. Advise her to discuss pain management with prescriber.

• Stress importance of undergoing regular blood tests, mammograms, and gynecologic exams to identify early signs of serious adverse reactions.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

ta·mox·i·fen cit·rate

(tă-mok'sĭ-fen sit'rāt),
A synthetic nonsteroidal estrogen antagonist used in the prevention and treatment of breast cancer.

Tamoxifen belongs to a class of synthetic agents known as selective estrogen receptor modulators (SERMs). By competing with naturally occurring estrogen for binding sites on tissue cells, tamoxifen inhibits the stimulant effect of estrogen on breast cancers. Tumors that have been shown by biochemical assay to be rich in estrogen receptors are most likely to respond to treatment. Since 1985, tamoxifen has been used to delay or prevent relapse in patients who have undergone surgery or irradiation for breast cancer. The drug has been found effective in reducing the risk of cancer recurrence or disease progression in women with or without axillary node metastasis. In women with extensive disease, tamoxifen therapy has been as effective as oophorectomy in retarding progression. Clinical trials of tamoxifen as a preventive agent in women at high risk of breast cancer have yielded conflicting results; current opinion is against using tamoxifen in women at low or normal risk of breast cancer because of side effects. Genomic analysis of healthy women who developed breast cancer while taking tamoxifen showed that tamoxifen reduced breast cancer incidence in women with the BRCA2 mutation, but not in those with the BRCA1 mutation. Women taking tamoxifen are at increased risk of endometrial carcinoma, stroke, deep venous thrombosis, pulmonary embolism, and cataracts. The danger of these adverse consequences is greatest in women older than 50. Long-term use of the drug is associated with recurrent vaginal candidosis. It is contraindicated during pregnancy because of the risk of fetal harm.

tamoxifen citrate

(tă-mŏks′ĭ-fĕn)
An antiestrogenic drug used in treating and preventing breast cancer.
References in periodicals archive ?
(i) Drugs: Tamoxifen citrate, which is sold under the trade name 'Nolvadex', was purchased locally.
In the group of animals treated with 3-MC and nano-formulation of tamoxifen citrate together, the mean xanthine oxidase activity is found to be lowest as 12.03 [+ or -] 0.81 on 15th day of treatment.
When compared with the combination group of 3-methylcholanthrene and tablet formulation of tamoxifen citrate, the xanthine oxidase activity is much elevated (p > 0.05).
Barr enters the picture because, as the result of a 1993 patent challenge, it has a nonexclusive supply and distribution agreement for tamoxifen citrate, which it sells as a generic product.
"Our direct and vigorous intervention in this case ensures that Barr's interests, and those of the millions of women who benefit from the generic tamoxifen citrate that we market, will be adequately represented," says Barr chairman, president and chief executive officer Bruce Downey.
According to DARA BioSciences Inc, Soltamox is the first and only FDA-approved oral liquid formulation of tamoxifen citrate, a first-line therapy for the prevention and treatment of breast cancer.
Last spring a study by the National Cancer Institute concluded that women taking Nolvadex (known generically as tamoxifen citrate) showed a reduced incidence of developing invasive breast cancer on average by 44%.
Downey, in announcing results of the company's second quarter of fiscal 1998 (ended December 31), points to continued success by the company, with sales of products it distributes growing 26%, primarily as a result of increases in volume of tamoxifen citrate, the breast cancer treatment distributed by Barr.
The deal has been signed for Gelclair, an FDA-approved bioadherent oral rinse gel to treat the aching symptoms of oral mucositis (OM), as well as Soltamox (tamoxifen citrate) oral liquid solution, to be available to RainTree's Nationwide Oncology Membership.
In March Barr won a two-year court battle with the maker of the only branded version of tamoxifen citrate to produce a generic version of the breast cancer treatment.
generic distributor to handle a generic version of tamoxifen citrate. The drug will continue to be manufactured by its creator, who, in return for letting Barr distribute the generic version, will retain its patent on the drug into the next century.
Barr has already gained approval to distribute tamoxifen citrate, the generic equivalent of ICT's Nolvadcx, a treatment for breast cancer.