Pharmacokinetics of bacmecillinam and pivmecillinam in volunteers.

The pharmacokinetics of bacmecillinam and pivmecillinam were studied in healthy fasting volunteers given tablets in a cross-over, randomized order. The mean (+/- SD) peak levels of plasma mecillinam were 1.43 +/- 0.34, 2.73 +/- 0.43, and 4.62 +/- 1.41 mg/l after bacmecillinam 100, 200, and 400 mg and 2.38 +/- 0.65 mg/l after pivmecillinam 400 mg. The corresponding areas under plasma Vs time curves (AUC) were 2.21 +/- 0.19, 3.99 +/- 0.63, and 7.74 +/- 1.38 mg . h. l-1 for bacmecillinam and 5.35 +/- 0.93 mg . h. l-1 for pivmecillinam. The elimination half-lives were 0.8-1.1 h for bacmecillinam and 0.7 h for pivmecillinam. The 12 h urinary recovery of unchanged mecillinam after the 400 mg doses was 41% for bacmecillinam and 30% for pivmecillinam. The 400 mg dose of bacmecillinam gave a significantly higher plasma peak (p less than 0.001), AUC (p less than 0.001) and urinary recovery (p less than 0.001) than did pivmecillinam 400 mg. The plasma peaks appeared earlier and the rate of absorption was higher after bacmecillinam than after pivmecillinam (p less than 0.05). In conclusion, bacmecillinam had a better bioavailability than pivmecillinam in the tablet formulations studied. The AUC increased linearly with increasing doses of bacmecillinam.