Nolvadex (Tamoxifen Citrate)

Nolvadex Review

Nolvadex is used for treating breast cancer that has spread to other sites in the body.

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Nolvadex Drug Class and Mechanism

Tamoxifen competitively binds to estrogen receptors on tumors and other tissue targets, producing a nuclear complex that decreases DNA synthesis and inhibits estrogen effects. It is a nonsteroidal agent with potent antiestrogenic properties which compete with estrogen for binding sites in breast and other tissues. Tamoxifen causes cells to remain in the G0 and G1 phases of the cell cycle. Because it prevents (pre)cancerous cells from dividing but does not cause cell death, tamoxifen is cytostatic rather than cytocidal. Tamoxifen itself is a prodrug, having very little affinity for its target protein, the estrogen receptor. It must first be metabolized in the liver by the cytochrome P450 isoform CYP2D6 into the active metabolites 4-hydroxytamoxifen and des-N-methyl-4-hydroxytamoxifen (endoxifen). These active metabolites compete with estrogen in the body for binding to the estrogen receptor. In breast tissue, 4-hydroxytamoxifen acts as an estrogen receptor antagonist so that transcription of estrogen-responsive genes is inhibited.

Use Nolvadex as directed by your doctor. Nolvadex may be taken by mouth with or without food. Take Nolvadex with water or another nonalcoholic liquid. Swallow this medication whole. Do not break, crush, or chew before swallowing. Continue to take Nolvadex even if you feel well. Do not miss any doses. Taking Nolvadex at the same time each day will help you to remember to take it. Ask your health care provider any questions you may have about how to use Nolvadex.

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Nolvadex Side Effects

Tamoxifen is a selective estrogen receptor modulator. Even though it is an antagonist in breast tissue it acts as partial agonist on the endometrium and has been linked to endometrial cancer in some women. Therefore endometrial changes, including cancer, are among tamoxifen's side effects. The American Cancer Society lists tamoxifen as a known carcinogen, stating that it increases the risk of some types of uterine cancer while lowering the risk of breast cancer recurrence. The ACS states that its use should not be avoided in cases where the risk of breast cancer recurrence without the drug is higher than the risk of developing uterine cancer with the drug. For some women, tamoxifen can cause a rapid increase in triglyceride concentration in the blood. In addition there is an increased risk of thromboembolism especially during and immediately after major surgery or periods of immobility. Tamoxifen is also a cause of fatty liver, otherwise known as steatorrhoeic hepatosis or steatosis hepatis. A significant number of tamoxifen treated breast cancer patients experience a reduction of libido.

Nolvadex Pregnancy

NOLVADEX may cause fetal harm when administered to a pregnant woman. Women should be advised not to become pregnant while taking NOLVADEX or within 2 months of discontinuing NOLVADEX and should use barrier or nonhormonal contraceptive measures if sexually active. Tamoxifen does not cause infertility, even in the presence of menstrual irregularity. Effects on reproductive functions are expected from the antiestrogenic properties of the drug. In reproductive studies in rats at dose levels equal to or below the human dose, nonteratogenic developmental skeletal changes were seen and were found reversible. In addition, in fertility studies in rats and in teratology studies in rabbits using doses at or below those used in humans, a lower incidence of embryo implantation and a higher incidence of fetal death or retarded in utero growth were observed, with slower learning behavior in some rat pups when compared to historical controls. Several pregnant marmosets were dosed with 10 mg/kg/day (about 2-fold the daily maximum recommended human dose on a mg/m? basis) during organogenesis or in the last half of pregnancy.

Nolvadex Overdose

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/m? loading dose, followed by maintenance doses of 150 mg/m? of NOLVADEX given twice a day.

Nolvadex More Information

Nolvadex is to be used only by the patient for whom it is prescribed. Do not share it with other people. If your symptoms do not improve or if they become worse, check with your doctor.