BACKGROUND Clonidine, an alpha 2-adrenoceptor agonist, has been shown to be effective as a preanesthetic medication in adults. The current study was designed to investigate the efficacy of two doses of oral clonidine as a premedicant preceding oral atropine in children. METHODS In a prospective, randomized, double-blind, controlled clinical trial, 105 children, aged 4-12 yr, undergoing elective ophthalmologic surgery received 0.4 mg/kg diazepam, 2 micrograms/kg clonidine, or 4 micrograms/kg clonidine orally. These agents mixed with apple juice were administered 105 min before the estimated time of induction of anesthesia, and were followed by treatment with 0.03 mg/kg oral atropine 60 min before anesthesia. A blinded observer noted the children's level of sedation, quality of separation from parents, and degree of acceptance of mask application during inhalation of nitrous oxide used for establishment of venous access. Anesthesia was induced with 5 mg/kg thiamylal, and tracheal intubation was facilitated with 0.2 mg/kg vecuronium. Hemodynamic changes after tracheal intubation were compared among the three groups. RESULTS Clonidine produced significant sedation, and the effect was dose related. Clonidine, 4 micrograms/kg, provided better quality of separation and acceptance of mask than the two other regimens. This dose of clonidine attenuated the increases in blood pressure and heart rate after tracheal intubation. No clinically significant perioperative hypotension or bradycardia was observed. CONCLUSIONS These data indicate that, even in pediatric surgery, the combination of 4 micrograms/kg and 0.03 mg/kg oral clonidine is an effective premedication. However, the safety and optimal dose of clonidine in this setting remain to be determined.