Triptans are potent serotonin (5-HT) 1B/1D receptor agonists used to abort and treat migraine headaches. Although the triptans share pharmacodynamic characteristics at 5-HT(1B/1D) receptors, they differ pharmacokinetically. This column reviews how the triptans are metabolized. Generally, the triptans are metabolized by phase I monoamine oxidases (MAOs) and by various cytochrome p450 enzymes. However, each triptan has a unique metabolic profile, leading to significant differences in each triptan's potential for drug-drug interactions. These differences are detailed in this review.