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Purpose: There are no sufficient evidences for the sedative effect of gabapentin during anesthesia, especially intravenous sedation (IVS). The purpose of this study was to evaluate the sedative effect of gabapentin as preanesthetic medication during the IVS with propofol., Methods: 10 volunteer subjects joined this study. They underwent propofol IVS three times on separate days. On the first day, the IVS without gabapentin was performed as a control. On the second and the third day, gabapentin 200 mg and 400 mg were administered before the IVS, respectively. The target blood concentration (C T ) of propofol was gradually increased, and the bispectral index (BIS) value and Ramsay sedation score (RSS) were evaluated at each propofol C T . Postanesthetic complications and influences on vital signs were also evaluated., Results: Compared to the control group, the propofol C T s in the gabapentin 400 mg group significantly reduced at the BIS values of 60 and 70 (p = 0.031 and p = 0.043, respectively), and at RSS 3, 4, 5 and 6 (p = 0.040, p = 0.004, p = 0.001 and p = 0.004, respectively). There was no significant difference in propofol C T s between the control group and the gabapentin 200 mg group. There were no abnormality and no deterioration in circulation and respiration in all groups. There were no significant increases in complications with the administration of gabapentin., Conclusion: The oral administration of 400 mg dose of gabapentin reduced the propofol C T s for achieving an adequate sedation level on IVS.

Purpose: The sedative effects of pregabalin during perioperative period have not been sufficiently characterized. The aim of this study was to verify the sedative effects of premedication with pregabalin on intravenous sedation (IVS) using propofol and also to assess the influences of this agent on circulation, respiration, and postanesthetic complications., Methods: Ten healthy young volunteers underwent 1 h of IVS using propofol, three times per subject, on separate days (first time, no pregabalin; second time, pregabalin 100 mg; third time, pregabalin 200 mg). The target blood concentration (C T ) of propofol was increased in a stepwise fashion based on the bispectral index (BIS) value. Ramsay's sedation score (RSS) was determined at each propofol C T . Propofol C T was analyzed at each sedation level. Circulation and respiration during IVS and complications were also verified., Results: Propofol C T was reduced at BIS values of 60 and 70 in both premedicated groups (100 mg: p = 0.043 and 0.041; 200 mg: p = 0.004 and 0.016, respectively) and at a BIS value of 80 in the pregabalin 200 mg group (p < 0.001). Propofol C T was decreased at RSS 4-6 in the pregabalin 100 mg group (RSS 4: p = 0.047; RSS 5: p = 0.007; RSS 6: p = 0.014), and at RSS 3-6 in the pregabalin 200 mg group (RSS 3-5: p < 0.001; RSS 6: p = 0.002)., Conclusion: We conclude that oral premedication with pregabalin reduces the amount of propofol required to obtain an acceptable and adequate sedation level.

Purpose: Numerous reports suggest that intravenously administered (IV) anesthetics affect postsynaptic events in the central nervous system. However, there is little evidence about how general anesthetics influence the presynaptic processes. The level of presynaptic calcium (Ca(2+)) concentration ([Ca(2+)](pre)) regulates neurotransmitter release. In this study, we investigated the effects of anesthetic propofol IV and the barbiturate pentobarbital on neurotransmitter release by measuring [Ca(2+)](pre) in the presynaptic nerve terminals (boutons) on a dissociated single hippocampal rat neuron., Methods: Sprague-Dawley rats 10-14 days old were decapitated under pentobarbital anesthesia, and brain slices were prepared. The hippocampal CA1 area was touched with a fire-polished glass pipette, which vibrated horizontally, and neurons were dissociated, along with the attached presynaptic boutons. The presynaptic boutons were visualized under a confocal laser-scanning microscope after staining with FM1-43 dye, and [Ca(2+)](pre) was measured with acetoxymethyl ester of fluo-3 (fluo-3 AM)., Results: High potassium (K(+)) (15-90 mM) increased the [Ca(2+)](pre) in the Ca(2+)-containing solution in a concentration-dependent manner. Whereas propofol (10 μM) and pentobarbital (300 μM) suppressed the high K(+) (60 mM)-induced increase in [Ca(2+)](pre) in the boutons attached to the dendrite, they did not affect [Ca(2+)](pre) in the boutons attached to the soma or dendrite base. As a large majority of excitatory synapses are located on dendritic spines, these agents may affect Ca(2+) mobilization in the excitatory presynaptic boutons., Conclusions: Propofol and pentobarbital may affect neurotransmitter release from the excitatory presynaptic nerve terminals due to inhibition of increase in [Ca(2+)](pre).