The safety and efficacy of premedication with oral transmucosal fentanyl citrate (OTFC) was compared with that of an orally administered solution of meperidine, diazepam, and atropine and no premedication in 59 children about to undergo elective operations. The patients were randomly assigned to receive no premedication (n = 19); 0.25 ml/kg of the oral solution (containing meperidine, 1.5 mg/kg, diazepam, 0.2 mg/kg, and atropine, 0.02 mg/kg, n = 20); or OTFC (15-20 micrograms/kg, n = 20). Children had activity (sedation) and anxiety scores, vital signs (including systolic and diastolic arterial blood pressures and heart and respiratory rates) and pulse oximetry determined oxygen saturation measured before and at 10-min intervals after premedication until they were taken to the operating room. Quality of induction and recovery was evaluated using scoring schedules; recovery times were measured and side effects noted. OTFC was readily accepted and provided significant reductions in preoperative activity (sedation) and anxiety starting after 30 min. After OTFC, sedation and anxiolysis were significantly greater than in children having no premedication but similar to children having the oral solution for premedication. Vital signs and oxygen saturations remained unchanged preoperatively in all groups. Induction and recovery evaluations and recovery times were similar in the three groups, although children having OTFC had the lowest requirements for narcotics in the recovery room. OTFC caused an 80% incidence of mild preoperative facial pruritus and a higher overall incidence of postoperative vomiting (37%) than premedication with the oral solution (5%) or no premedication (18%).(ABSTRACT TRUNCATED AT 250 WORDS)