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Science 17 May 1946:
Vol. 103. no. 2681, pp. 618 - 620
DOI: 10.1126/science.103.2681.618
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Articles

The Low Therapeutic Activity of Penicillin K Relative to That of Penicillins F, G, and X, and Its Pharmacological Basis

HARRY EAGLE 1 and ARLYNE MUSSELMAN 1

1 The Johns Hopkins University and U. S. Public Health Service Venereal Disease Research Laboratory and Postgraduate Training Center, Baltimore, Maryland

One hour after the injection into rabbits or man of penicillins F, G, K, and X at 0.6 mg./kg., blood levels of K were one-fourth to one-eleventh of those observed with the other penicillins, and K persisted at demonstrable levels for relatively short periods.

In both rabbits and man the recovery of K in the urine averaged 30-35 per cent. This compares with an average recovery for F, G, and X of 74 per cent in rabbits and 91 per cent in man.

In the treatment of experimental pneumococcal infections in white mice, an impure preparation of K was one-sixth as active as G and one-eighth as active as X. In the treatment of experimental streptococcal infections in white mice, a pure preparation of K was one-eleventh as active as G, and one-thirtieth as active as X.

The above data suggest that penicillin K is inactivated in the body to a greater extent and more rapidly than either F, G, or X, resulting in a far lower therapeutic activity than would be anticipated from its bactericidal action in vitro. It seems clear that the amount of K in commercial penicillin should be minimized; and it would seem desirable to standardize impure mixtures of penicillins for therapeutic use by some method other than their bactericidal activity in vitro.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
CONTROVERSIAL POINTS IN PENICILLIN THERAPY OF OCULAR DISEASES.
L. VON SALLMANN (1948)
Arch Ophthalmol 39, 752-804
   Abstract »    PDF »
TREATMENT OF EARLY SYPHILIS WITH SODIUM PENICILLIN: A Preliminary Report with a Comparison of Results with 4,800,000 Units, Administered in Seven and a Half Days, with Smaller Dosages.
J. Q. BLACKWOOD, V. SCOTT, and E. G. CLARK (1948)
Arch Dermatol 57, 1028-1041
   Abstract »    PDF »
TREATMENT OF EARLY SYPHILIS WITH PENICILLIN.
T. H. STERNBERG and W. LEIFER (1947)
JAMA 133, 1-5
   Abstract »    PDF »
Inactivation of Penicillins G and K by Liver and Kidney.
J. TEPPERMAN, N. RAKIETEN, G. VALLEY, and E. W. LYON (1947)
Science 105, 18-19
   Abstract »    PDF »
SYPHILIS: A Review of the Recent Literature.
F. W. REYNOLDS and J. E. MOORE (1946)
Arch Intern Med 78, 733-769
   Abstract »    PDF »
The Differentiation of Penicillins G and K by an Assay Method in Vivo.
M. BUCK, A. C. FARR, and R. J. SCHNITZER (1946)
Science 104, 370-371
   PDF »


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