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TAMOXIFEN CITRATE TABLETS

 

Tamoxifen citrate 

10 mg/tablet, 60 tablets/bottle


The citrate salt of an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM). Tamoxifen competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA. The result is a reduction in DNA synthesis and cellular response to estrogen. In addition, tamoxifen up-regulates the production of transforming growth factor B (TGFb), a factor that inhibits tumor cell growth, and down-regulates insulin-like growth factor 1 (IGF-1), a factor that stimulates breast cancer cell growth. Tamoxifen also down-regulates protein kinase C (PKC) expression in a dose-dependant manner, inhibiting signal transduction and producing an antiproliferative effect in tumors such as malignant glioma and other cancers that overexpress PKC.
Pharmacology
A nonsteroidal agent with antiestrogenic properties.
Pharmacokinetics
Absorption
Tamoxifen C max is 40 ng/mL (range, 35 to 45 ng/mL), T max is approximately 5 h after dosing, and steady state is achieved in about 4 wk.
Metabolism
Tamoxifen is extensively metabolized. The major metabolite is N-desmethyl tamoxifen. It is a substrate of CYP450 3A, 2C9, 2D6, and an inhibitor of P-glycoprotein.
Elimination
Tamoxifen t ½ is 5 to 7 days; 65% of a dose is excreted over a 2-wk period, with fecal excretion as the primary route of elimination.
Special Populations
Hepatic Function Impairment

The effects of reduced liver function have not been determined.
Indications and Usage
Adjuvant treatment of breast carcinoma in women; metastatic breast carcinoma in men and women; reduction in risk of breast cancer in high-risk women; lower risk of invasive breast cancer in women with ductal carcinoma in situ (DCIS).
Unlabeled Uses
Ovulation stimulation in specially selected anovulatory women desiring pregnancy; management and treatment of some types of mastalgia (eg, cyclical); malignant carcinoid tumor and carcinoid syndrome; migraine associated with menstruation; metastatic malignant melanoma; oligozoospermia; McCune-Albright syndrome in female pediatric patients (in combination with other agents); metastatic melanoma; desmoid tumors; symptomatic gynecomastia.
Contraindications
Hypersensitivity to drug; women who require concomitant coumarin-type anticoagulant therapy; women with a history of deep vein thrombosis or pulmonary embolus.
Dosage and Administration
Breast Cancer
Adults
PO 20 to 40 mg daily.
DCIS, Reduction in Breast Cancer Incidence in High-Risk Women
Adults
PO 20 mg daily for 5 yr.
General Advice
Divide dosages greater than 20 mg/day (morning and evening).
Storage/Stability
Do not store oral solution above 77 degree F. Do not refrigerate or freeze. To protect from light, store in original package. Use within 3 mo of opening. Store tablets at 68  to 77 degree F. Dispense in well-closed, light-resistant containers


 

2009-10-26 12:11:54

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