Pharmacokinetic profile of cisapride 20 mg after once- and twice-daily dosing.

Cisapride is a substituted piperidinyl benzamide. It is chemically related to metoclopramide but lacks the antidopaminergic properties of metoclopramide that affect the central nervous system and cause extrapyramidal side effects. Cisapride is indicated for the symptomatic treatment of patients with nocturnal heartburn due to gastroesophageal reflux disease. Based on extensive assessment of the drug's pharmacokinetic profile, the currently approved initial oral dosing regimen for cisapride is 10 mg QID. However, the pharmacokinetics of cisapride after oral administration of 20 mg BID have not been investigated. We present here findings from an open-label trial assessing the pharmacokinetics of cisapride 20-mg tablets after a single dose and at steady state (BID dosing). The results indicate that 20-mg BID and 10-mg QID regimens produce similar steady-state concentrations.