A battery of pain models can be used in clinical trials to investigate the efficacy and to establish the concentration‐effect relationship of novel analgesics. This study quantified the pharmacokinetics ( PK) of pregabalin after a single oral dose of 300 mg and the pharmacodynamics ( PD) on the pain tolerance threshold ( PTT) of the cold pressor, electrical stimulation, the pressure pain model, and on the pain detection threshold of a contact heat pain model. The PK were best described using a one‐compartment model with lag time, linear absorption, and linear elimination. The PTT of the cold pressor showed a negative linear decrease over time without pregabalin. A linear drug effect was identified on the PTT of the cold pressor test and an on/off effect for the electrical stimulation PTT. No PK/ PD relationship could be identified on the pressure pain and heat pain test. Citation: