Pharmacokinetics of Meptazinol in Man Following Repeated Intramuscular Administration

A study was performed in 6 healthy volunteers to determine whether 50 mg intramuscular doses of meptazinol repeated four hourly for 24 h would lead to accumulation of the drug. The first dose of meptazinol was rapidly absorbed with a subsequent mean (+/- SD) elimination half-life of 1.6 +/- 0.33 h. This value was unaffected by the administration of intermediate doses. There was no significant accumulation of the drug; 95% of the steady-state plasma concentration was achieved after a mean (+/- SD) of 1.9 +/- 0.39 and 99% after a mean (+/- SD) of 2.9 +/- 0.63 doses. These findings are consistent with the theoretical prediction for a rapidly absorbed drug with a plasma elimination half-life of 1.6 h. No clinically relevant changes were seen in pulse blood pressure, haematological or biochemical screens. Reported side effects were of a subjective and minor nature.