PHARMACOKINETICS OF THE ACTIVE METABOLITE (MDL-74,156) OF DOLASETRON MESYLATE - AFTER ORAL OR INTRAVENOUS ADMINISTRATION TO ANESTHETIZED CHILDREN

Background: Dolasetron mesylate is a selective 5-HT3 receptor antagoni st under investigation as an antiemetic in children. Published studies indicate that its antiemetic activity results from the active metabol ite (MDL 74,156), which is produced within 10 minutes of administratio n of dolasetron mesylate, Methods: The pharmacokinetics of MDL 74, 156 and the safety and tolerability of dolasetron mesylate were studied a fter a single oral or intravenous dose of 1.2 mg . kg(-1) dolasetron m esylate to healthy children from 2 to 12 years of age, Oral dolasetron was administered to 12 children 1 to 2 hours before anesthesia, Intra venous dolasetron was administered to 18 children at induction of anes thesia, Serial blood samples were collected for 24 hours after dosing to measure the plasma concentration of MDL 74,156, Indexes of Liver an d kidney function were determined, and electrocardiograms and adverse events were recorded.