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tamoxifen_citrate: profile and news
Rodman & Renshaw 3rd Annual Global Healthcare Conference 2006 ... May 11, 2006 Cytogen Corporation to Present at the Rodman & Renshaw 3rd Annual ... May 9, 2006 Cytogen Reports First Quarter 2006 Financial Results May 8, 2006 Cytogen and Savient Finalize Exclusive Distribution Agreement for ... Apr 24, 2006 New licensing and development agreements. Apr 26, 2006 Cytogen Selling PSMA Joint Venture Share To Progenics Apr 24, 2006 Cytogen to distribute Soltamox in USA Apr 25, 2006 Other information Indication for the treatment of breast cancer Pharmacology Tamoxifen belongs to a class of drugs called selective estrogen receptor modulators (SERMs), which have both estrogenic and antiestrogenic effects. Tamoxifen has the same nucleus as diethylstilbestrol but possesses an additional side chain (trans isomer) which accounts for its antiestrogenic activity. Tamoxifen, chemically related to clomiphene., is used to in the therapy of metastatic breast cancer. Mechanism Of Action Tamoxifen binds to estrogen receptors (ER), inducing a conformational change in the receptor. This results in a blockage or change in the expression of estrogen dependent genes. The prolonged binding of tamoxifen to the nuclear chromatin of these results in reduced DNA polymerase activity, impaired thymidine utilization, blockade of estradiol uptake, and decreased estrogen response. It is likely that tamoxifen interacts with other coactivators or corepressors in the tissue and binds with different estrogen receptors, ER-alpha or ER-beta, producing both estrogenic and antiestrogenic effects. Drug Category Antineoplastic Agents; ATC:L02BA01 Brand Names/Synonyms ,Citrate; Apo-Tamox; CCRIS 3275; CTX; Citofen; Crisafeno; Diemon; Gen-Tamoxifen; HSDB 6782; Istubol; Kessar; Noltam; Nolvadex; Nolvadex-D; Nourytam; Novo-Tamoxifen; Oncomox; Pms-Tamoxifen; Retaxim; TRANS FORM OF TAMOXIFEN; Tamizam; Tamofen; Tamone; Tamoxasta; Tamoxen; Tamoxifen; Tamoxifen Citrate; Tamoxifen Drug Standard Solution; Tamoxifen and Its Salts; Tamoxifene [Inn-French]; Tamoxifeno [Inn-Spanish]; Tamoxifenum [Inn-Latin]; Trans-Tamoxifen; Valodex; Zemide Dosage Forms TABLET Absorption Not Available Interactions -->Interactions for Tamoxifen: When NOLVADEX is used in combination with coumarin-type anticoagulants, a significant increase in anticoagulant effect may occur. Where such coadministration exists, careful monitoring of the patientís prothrombin time is recommended. In the NSABP P-1 trial, women who required coumarin-type anticoagulants for any reason were ineligible for participation in the trial. There is an increased risk of thromboembolic events occurring when cytotoxic agents are used in combination with NOLVADEX. Tamoxifen reduced letrozole plasma concentrations by 37%. The effect of tamoxifen on metabolism and excretion of other antineoplastic drugs, such as cyclophosphamide and other drugs that require mixed function oxidases for activation, is not known. Tamoxifen and N-desmethyl tamoxifen plasma concentrations have been shown to be reduced when coadministered with rifampin or aminoglutethimide. Induction of CYP3A4-mediated metabolism is considered to be the mechanism by which these reductions occur; other CYP3A4 inducing agents have not been studied to confirm this effect. One patient receiving NOLVADEX with concomitant phenobarbital exhibited a steady state serum level of tamoxifen lower than that observed for other patients (ie, 26 ng/mL vs. mean value of 122 ng/mL). However, the clinical significance of this finding is not known. Rifampin induced the metabolism of tamoxifen and significantly reduced the plasma concentrations of tamoxifen in 10 patients. Aminoglutethimide reduces tamoxifen and N desmethyl tamoxifen plasma concentrations. Medroxyprogesterone reduces plasma concentrations of N-desmethyl, but not tamoxifen. Concomitant bromocriptine therapy has been shown to elevate serum tamoxifen and N-desmethyl tamoxifen. Drug/Laboratory Testing Interactions: During postmarketing surveillance, T4 elevations were reported for a few postmenopausal patients which may be explained by increases in thyroid-binding globulin. These elevations were not accompanied by clinical hyperthyroidism. Variations in the karyopyknotic index on vaginal smears and various degrees of estrogen effect on Pap smears have been infrequently seen in postmenopausal patients given NOLVADEX. In the postmarketing experience with NOLVADEX, infrequent cases of hyperlipidemias have been reported. Periodic monitoring of plasma triglycerides and cholesterol may be indicated in patients with pre-existing hyperlipidemias . |
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