Bioavailability and Disposition of Metoclopramide after Single‐ and Multiple‐Dose Administration in Diabetic Patients with Gastroparesis

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Abstract
The disposition of metoclopramide after acute and chronic administration was determined in four diabetic patients with gastroparesis who had a creatinine clearance of 70.8 ±10.7 mL/min (mean ± SD). Single, 10‐mg oral and intravenous doses were administered on days 1 and 2, respectively, followed by 10 mg orally every six hours for three weeks. A second, 10‐mg intravenous bolus dose was administered on the last morning of chronic therapy. Metoclopramide concentrations were determined by high performance liquid chromatography. The elimination half‐life, steady‐state volume of distribution, and total body clearance after the initial intravenous dose were 3.9 ± 1.2 hr, 2.7 ± 0.3 L/kg, and 0.57 ± 0.14 L/hr/kg, respectively. The initial bioavailability was 67.7 ± 12.6%. After three weeks of chronic therapy, no significant differences in total body clearance (0.72 ± 0.42 L/hr/kg) or bioavailability (77.5 ± 16.8%) were observed. Thus the pharmacokinetics and bioavailability of metoclopramide were not altered during chronic therapy in these diabetic patients.