Ifenprodil for prolonged spinal blockades of motor function and nociception in rats

Background The aim of the study was to compare the proposed spinal anesthetic effect of ifenprodil, an alpha receptor antagonist, with that of the long-acting local anesthetic bupivacaine. Methods After intrathecally injecting the rats with five different doses of each drug, the dose-response curves of ifenprodil and bupivacaine were constructed to obtain the 50% effective dose (ED₅₀). The spinal blockades of motor function and nociception of ifenprodil were compared with that of bupivacaine. Results We showed that either ifenprodil or bupivacaine produced spinal blockades of motor function and nociception dose-dependently. On the ED₅₀ basis, the potency of ifenprodil (0.42(0.38-0.46) μmol; 0.40(0.36-0.44) μmol) was equal (p > 0.05) to that of bupivacaine (0.38(0.36-0.40) μmol; 0.35(0.32-0.38) μmol) in motor function and nociception, respectively. At the equianesthetic doses (ED₂₅, ED₅₀, and ED₇₅), duration produced by ifenprodil was greater than that produced by bupivacaine in motor function and nociception (p < 0.05 for the differences). Furthermore, both ifenprodil and bupivacaine showed longer duration of sensory blockade than that of motor blockade (p < 0.05 for the differences). Conclusions The resulting data demonstrated that ifenprodil produces a dose-dependent local anesthetic effect in spinal anesthesia. Ifenprodil shows a more sensory-selective duration of action over motor block, whereas the duration of anesthesia is significantly longer with ifenprodil than with bupivacaine.