Acute Pharmacodynamics and Pharmacokinetics of Oral Amrinone

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Abstract
Amrinone was administered orally as a single 100‐mg dose to six male patients with moderate‐severe congestive heart failure to determine the acute pharmacodynamic effects and pharmacokinetics of the drug. Following right heart catherization and amrinone administration, measurements of hemodynamic parameters including cardiac index (CI), right atrial pressure (RA), pulmonary capillary wedge pressure (PCW), and serum amrinone concentrations (SAC) were made at hourly intervals for up to 8 hours. CI increased (29.0 per cent) significantly (P < 0.05) at 3 hours after dose. PCW declined quickly after dose and was significantly (P < 0.05) lower (–31.3 per cent) than control at 3 hours. RA declined gradually, and a significant (P < 0.05) reduction (–25.2 per cent) was achieved 5 hours after the dose. Amrinone was absorbed quickly (tmax = 1.4 hour), and the disappearance of amrinone from serum was log‐linear (t½ = 5.1 hours). The time courses of per cent change in CI and SAC were similar, and the correlation between the average per cent change in CI and average SAC was linear and significant (r = 0.80; P < 0.05).