Clinical pharmacological studies of amoxycillin: effect of probenecid.

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Abstract
Healthy adult [human] volunteers (8) were given 3 g amoxicillin with or without 1 g probenecid. Significantly higher peak plasma levels of amoxicillin were recorded in the presence (34.96 .mu.g/ml) of prebenecid than in its absence (22.72 .mu.g/ml). When plasma levels were plotted against time the mean area under the curve was significantly greater for subjects given probenecid than for those given amoxicillin alone. Amoxicillin (3 g) plus probenecid (1 g) provides better bioavailability than amoxicillin (3 g) alone. The plasma levels obtained were several times higher than the minimum inhibitory concentrations (MIC) of most strains of gonococci. Plasma levels in excess of the MIC for most strains were maintained for 8 h with both regimens, but the higher levels in the presence of probenecid support the better clinical results previously reported with this regimen. [Probenecid was used with ampicillin and amoxicillin for single-dose therapy for gonorrhea].