Metoclopramide, a drug used for the relief of nausea and emesis, is currently under development as a radio‐ and chemosensitizing agent. Its usefulness in high doses, however, is limited by its central nervous system side effects. Neu‐metoclopramide (Neu Sensamide), a novel, concentrated, phosphate‐buffered, pH‐adjusted (pH = 6.5–7.0) formulation of metoclopramide, has been shown to have an improved side‐effect profile in animal studies. The present double‐blind, four‐way crossover study compared the central nervous system effects and pharmacokinetics of neu‐metoclopramide (intravenously and intramuscularly at 1.8 mg/kg) with intravenous metoclopramide and intramuscular placebo in 19 healthy male volunteers. Eight participants withdrew from the study, one because of noncompliance and seven because of adverse events. A total of 28 central nervous system events were observed with intravenous metoclopramide administration, whereas 16, 15, and 6 such events were attributed to intravenous neu‐metoclopramide, intramuscular neu‐metoclopramide, and placebo, respectively. Extra pyramidal effects occurred on 10 occasions: 7 after intravenous metoclopramide, 2 after intravenous neu‐metoclopramide, and 1 after intramuscular neu‐metoclopramide. No significant differences were observed in the pharmacokinetic profiles of the three formulations of metoclopramide. It may be speculated, therefore, that the molecular conformational changes inherent to neu‐metoclopramide result in a reduced side‐effect profile compared with conventional metoclopramide formulations.
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