Pharmacokinetics and bioavailability of the anti-emetic agent bromopride

✍ Scribed by R. R. Brodie; L. F. Chasseaud; A. Darragh; R. F. Lambe; L. Rooney; T. Taylor

• Publisher: John Wiley and Sons
• Year: 1986
• Tongue: English
• Weight: 378 KB
• Volume: 7
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bdd.2510070302

✦ Synopsis

The pharmacokinetics of bromopride, an anti-emetic agent chemically related to metoclopramide, has been investigated in normal human subjects. After intravenous bolus doses of lOmg, a one-compartment open model appeared adequate to describe the plasma drug concentration data. The systemic clearance of bromopride was 899 ml min-' f 22 per cent CV, the volume of distribution was 215 I rt 16 per cent CV, and the elimination half-life was 2.9 h f 21 per cent CV. Over a wide drug concentration range of up to 650ng ml-', bromopride was only 40 per cent bound to plasma proteins. The systemic availability of orally and intramuscularly administered solution doses of 20mg of bromopride was 54 per cent and 78 per cent, respectively. Formulation of bromopride as the solid material in capsules delayed absorption but did not affect the extent of drug bioavailability. The pharmacokinetics of bromopride appeared similar t o that of metoclopramide. No evidence for non-linear kinetics was found when bromopride was administered orally in the dose range 10-30mg: after single oral doses of 10, 20, and 30mg, peak mean plasma drug concentrations were 20ng ml-' f 32 per cent CV, 38 ng ml-f 16 per cent CV, and 64 ng ml-l k 23 per cent CV, respectively.