Triamterene, primarily metabolized in the liver by CYP1A2 and CYP3A4 enzymes, forms inactive hydroxylated metabolites (like hydroxytriamterene sulfate and p-hydroxytriamterene). Elimination occurs mainly via renal excretion (50-60%), with the remainder excreted fecally. The drug's short half-life of 2-4 hours allows for multiple daily dosing. UGT enzymes may also play a minor role in metabolism.