
(Z)-2-[4-(1,2-diphenylbut-1-enyl)phenoxy]-N,N-dimethyl-ethanamine
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.
Aminoglutethimide, phenobarbital :Tamoxifen concentrations may be reduced.
Anastrozole :Plasma concentrations of anastrozole may be decreased. Do not coadminister.
Bromocriptine :Tamoxifen concentrations may be increased.
Cytotoxic agents :Increased risk of thromboembolic events.
Letrozole :Plasma concentrations may be decreased by tamoxifen, reducing the therapeutic effect.
Rifamycins (eg, rifampin) :Tamoxifen plasma levels may be reduced, decreasing the antiestrogenic effect.
Warfarin :Increased hypoprothrombinemic effect.



