It is an aromatase inhibitor indicated for: ? Adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer ? First-line treatment of postmenopausal women with hormone receptor-positive or hormone receptor unknown locally advanced or metastatic breast cancer . ? Treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. Patients with ER-negative disease and patients who did not respond to previous tamoxifen therapy rarely responded to it.
Tamoxifen is a praparation of Tamoxifen which is a non-steroidal, triphenylene based drug and displays a complex spectrum of oestrogen antagonist and oestrogen agonist like pharmacological effects in different tissues. In breast cancer patients, at the tumour level, Tamoxifen acts primarily as an antioestrogen, preventing oestrogen binding to the oestrogen receptor. Additionally Tamoxifen has been reported to lead to maintenance of bone mineral density in post-menopausal women.
One 1 mg tablet taken once daily
When Tamoxifen is used in combination with coumarin type anticoagulants, a significant increase in anticoagulant effect may occur. Where such co administration is initiated, careful monitoring of the patient is recommended. When Tamoxifen is used in combination with cytotoxic agents, there is an increased risk of thromboembolic events.
Women of premenopausal endocrine status, including pregnant women ? Patients with demonstrated hypersensitivity to or any excipient
hot flashes, asthenia, arthritis, pain, arthralgia, pharyngitis, hypertension, depression, nausea and vomiting, rash, osteoporosis, fractures, back pain, insomnia, headache, peripheral edema and lymphedema, regardless of causality
Pregnancy: Tamoxifen must not be administered during pregnancy. There have been a small number of reports of spontaneous abortions, birth defects and foetal deaths after women have taken Tamoxifen, although no causal relationship has been established. Reproductive toxicology studies in rats, rabbits and monkeys have shown no teratogenic potential. Women should be advised not to become pregnant whilst taking Tamoxifen and should use barrier or other nonhormonal contraceptive methods if sexually active. Premenopausal patients must be carefully examined before treatment to exclude pregnancy. Women should be informed of the potential risks to the foetus, if they want to become pregnant whilst taking Tamoxifen or within two months of cessation of therapy. Lactation: It is not known if Tamoxifen is excreted in human milk and therefore the drug is not recommended during lactation. The decision to discontinue Tamoxifen should take into account in case of the importance of the drug to the lactating mother.
Signs observed at the highest doses following studies to determine LD50 in animals were
respiratory difficulties and convulsions.
Acute overdosage in humans has not been reported. In a study of advanced metastatic cancer
patients which specifically determined the maximum tolerated dose of NOLVADEX in
evaluating the use of very high doses to reverse multidrug resistance, acute neurotoxicity
manifested by tremor, hyperreflexia, unsteady gait and dizziness were noted. These symptoms
occurred within 3-5 days of beginning NOLVADEX and cleared within 2-5 days after stopping
therapy. No permanent neurologic toxicity was noted. One patient experienced a seizure several
days after NOLVADEX was discontinued and neurotoxic symptoms had resolved. The causal
relationship of the seizure to NOLVADEX therapy is unknown. Doses given in these patients
were all greater than 400 mg/m2
loading dose, followed by maintenance doses of 150 mg/m2
of
NOLVADEX given twice a day.
In the same study, prolongation of the QT interval on the electrocardiogram was noted when
patients were given doses higher than 250 mg/m2
loading dose, followed by maintenance doses
of 80 mg/m2
of NOLVADEX given twice a day. For a woman with a body surface area of
1.5 m2
the minimal loading dose and maintenance doses given at which neurological symptoms
and QT changes occurred were at least 6 fold higher in respect to the maximum recommended
dose.
No specific treatment for overdosage is known; treatment must be symptomatic.
Store between 20-25° C. Protect from light.
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