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Body fluid concentrations of penicillin following intramuscular injection of single doses of benzathine penicillin G and/or procaine penicillin G



Body fluid concentrations of penicillin following intramuscular injection of single doses of benzathine penicillin G and/or procaine penicillin G



Antibiotic Medicine & Clinical Therapy 6(4): 232-241



Clinical studies of serum concentrations and, in some instances, urine concentrations, have been made as indicated in the following: (1) a 1,200,000 unit dose of an aqueous suspension of benzathine penicillin G in 30 subjects; (2) a 1,20,00 unit dose of an aqueous suspension of benzathine penicillin G plus 5 mg of prednisolone in 20 subjects; (3) a 1,200,000 unit dose of procaine penicillin G in oil with aluminum monostearate in 10 subjects; and (4) 1,20,000 units each of procaine penicillin G and benzathine penicillin G in aqueous suspension in 20 subjects. All products containing benzathine penicillin G produced prolonged penicillemia. After the injection of 1,200,000 units of benzathine penicillin G either with or without prednisolone, the average duration of detectable penicillemia was about 26 days, and the average duration of penicilluria was in excess of 100 days. The amount of penicillin in the urine on any given day was several hundred times as great as that demonstrable in the serum. Probenecid, administered 59 days after penicillin could no longer be detected in the blood of 1 subject, apparently inhibited the renal excretion of penicillin (penicilluria was still present) and increased the very low concentration of penicillin in the blood to the point where it could again be detected. If penicillin can be detected in the urine when it can no longer be detected in the blood, the discrepancy is related more to the sensitivity of the assay method than to the actual absence of this drug from the blood. The concentration of penicillin in the blood at that time would be approximately one three-hundredth as much as in the urine. The effect of unsuspected penicillemia on concentrations obtained from supervening penicillin medication of the benzathine penicillin type appears to be an increase in duration of penicillemia and penicilluria. Procaine penicillin G, 1,200,000 units in oil, produced a penicillemia of relatively short duration averaging only 2.6 days. Penicilluria persisted only for an average of 14.5 days, indicating a relatively short period of undetectable penicillemia. A combination of 1,200,000 units each of procaine penicillin G and benzathine penicillin G produced relatively high blood concentrations during the first 8 days; however, from the 11th to the 29th day, average serum concentrations were slightly lower than those from 1.2 million units of benzathine penicillin G alone. The duration of detectable penicillemia also was somewhat shorter.

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Accession: 024259415

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PMID: 13637700


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