Cisapride is a substituted piperidinyl benzamidel It is chemically rel
ated to metoclopramide but lacks the antidopaminergic properties of me
toclopramide that affect the central nervous system and cause extrapyr
amidal side effects. Cisapride is indicated for the symptomatic treatm
ent of patients with nocturnal heartburn due to gastroesophageal reflu
x disease. Based on extensive assessment of the drug's pharmacokinetic
profile, the currently approved initial oral dosing regimen for cisap
ride is 10 mg QID. However, the pharmacokinetics of cisapride after or
al 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 (BI
D dosing). The results indicate that 20-mg BID and 10-mg QID regimens
produce similar steady-state concentrations.